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Preprint ARTICLE | doi:10.20944/preprints202410.1929.v1

Anti-Migratory Activity of Brazilin Chemo-Diversification Products on Breast Cancer Cells

Alberto Hernández-Moreno, Dania A. Nava-Tapia, Miriam D. Zuñiga-Eulogio, Jorge Bello-Martínez, Monserrat Olea-Flores, Tadeo Hernández-Moreno, Mario Ordoñez, Ana E. Zacapala-Gómez, Miguel A. Mendoza-Catalán, Napoleón Navarro-Tito

Subject: Pharmacology And Toxicology, Medicine And Pharmacology Keywords: brazilin; semi-synthesis; chemo-diversification; cell migration; FAK activation

Online: 25 October 2024 (09:34:57 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202410.1902.v1

Evaluation of Short-Term Stability of Different Nitazenes in Dried Blood Spots by Liquid Chromatography-High Resolution Mass Spectrometry

Alessandro Vitrano, Alessandro Di Giorgi, Vincenzo Abbate, Giuseppe Basile, Nunzia La Maida, Simona Pichini, Annagiulia Di Trana

Subject: Pharmacology And Toxicology, Medicine And Pharmacology Keywords: nitazenes; stability study; LC-HRMS/MS; dried blood spots

Online: 24 October 2024 (11:30:30 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202410.1688.v1

Pharmacological Study of Amaranthus spinosus L. Root Extract on High-Fat Diet and Low-Dose Streptozocin-Induced Type 2 Diabetes Complications in Rats

Kokou Atchou, Povi Lawson-Evi, Kwashie Eklu-Gadegbeku

Subject: Pharmacology And Toxicology, Medicine And Pharmacology Keywords: Amaranthus spinosus; metabolic syndrome; type 2 diabetes; diabetes complications; retinopathy; renal fibrosis

Online: 24 October 2024 (10:01:52 CEST)

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Preprint COMMUNICATION | doi:10.20944/preprints202410.1638.v1

Impact of Extra-Corporeal Membrane Oxygenation (ECMO) on Serum Concentrations of Cefepime

Christopher J. Destache, Raul Isern, Dorothy Kenny, Rima El-Herte, Robert Plambeck, Catherine Palmer, Brent S Inouye, Maura Wong, Eldon Jeffrey North, Mari Roman Sotelo, Manasa Velagapudi

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: cefepime; ECMO; pharmacokinetics

Online: 21 October 2024 (16:26:47 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202410.0856.v1

Preclinical Pharmacokinetics studies of SPH5030, a Novel, Selective, Potent, and Irreversible HER2 Inhibitor

Xuelian Gong, Guangxin Xia

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: SPH5030; Selective and irreversible HER2 Inhibitor; Pharmacokinetic; Tissues distribution; drug-drug interaction

Online: 12 October 2024 (07:21:18 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202410.0529.v1

QSAR Regression Models for Predicting HMG-CoA Reductase Inhibition Based on MACCS Molecular Fingerprints and Virtual Screening of Natural Products

Robert Ancuceanu, Patriciu Constantin Popovici, Doina Drăgănescu, Ștefan Busnatu, Beatrice Elena Lascu, Mihaela Dinu

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: HMG-CoA reductase; QSAR; statins; nested cross-validation; virtual screening; Iris germanica; machine learning; feature selection; mlr3; MACCS fingerprints; molecular descriptors

Online: 8 October 2024 (11:16:56 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202410.0551.v1

Identifying Drugs That Target Glucokinase for Treating Primary Amoebic Encephalitis (PAM) &Amp; Diabetes

Jason Abraham, Neha Chauhan, Supriyo Ray

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Naegleria fowleri; Glucokinase; Hexokinase; type 2 diabetes; Levomefolic acid; Ziprasidone; Risperidone; Simeprevir; Indacaterol; Crizotinib; Mocetinostat

Online: 8 October 2024 (10:30:25 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202410.0401.v1

Effect of culture supernatant of Clostridium butyricum TO-A on human DNA repair factor-encoding gene promoters

Shunsuke Takaoka, Takuro Ishii, Yuriko Umihara, Ryuji Otani, Sota Akazawa, Takahiro Oda, Yoko Ogino, Yoichi Okino, Dian-Sheng Wang, Fumiaki Uchiumi

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Clostridium butyricum; culture supernatant; butyric acid; DNA repair; gene expression; RNAseq analysis

Online: 7 October 2024 (11:27:16 CEST)

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Preprint REVIEW | doi:10.20944/preprints202410.0325.v1

Quantitative Approach to Explore Regulatory T Cell Activity in Immuno-Oncology

Alejandro Serrano-Alcaide, Sara Zalba, Juan Jose Lasarte, Iñaki F. Troconiz, Natalia Riva, Maria J Garrido

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Treg cells; QSP model; Immunotherapy; Tumor growth dynamics; computational immune framework

Online: 4 October 2024 (13:03:32 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202410.0290.v1

Early-Stage IM Treatment with the Host-Derived Immunostimu-Lant CPDI-02 Increases Curative Protection of Healthy Outbred Mice Against Subcutaneous Infection with CA-MRSA USA300

Joseph Vetro

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: anti-microbial resistance; AMR; antibiotic resistance; ABR; drug-resistant bacteria; antibi-otic-resistant bacteria; multidrug resistance; MDR; host-directed therapy; EP67; complement peptide-derived immunostimulant; administration route; CPDI-02 toxicity; CPDI-02 dosing; IM dosing

Online: 4 October 2024 (08:12:03 CEST)

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Preprint REVIEW | doi:10.20944/preprints202410.0086.v1

Exploring the Next Generation of Metformin Derivatives and Their Biomedical Promise

Štěpán Žídek, Kateřina Štěpánková, Marian Lehocky

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: metformin; biguanide; metformin derivatives; structural modification; medicinal chemistry; diabetes mellitus

Online: 2 October 2024 (08:05:19 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202409.1977.v1

Pharmacokinetic Analysis of the Bioavailability of AQUATURM®, a Water-Soluble Curcumin Formulation in Comparison to a Conventional Curcumin Tablet, in Human Subjects

Gerald Muench

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: water-soluble curcumin; pharmacokinetics; plasma; curcuminoids; area under the curve; bioavailability

Online: 25 September 2024 (17:55:38 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202409.1651.v1

Neuropsychiatric Adverse Events with Monoclonal Antibodies Approved for Multiple Myeloma: An Analysis from the FDA Adverse Event Reporting System

Giuseppe Cicala, Giulia Russo, Vincenza Santoro, Tindara Franchina, Nicola Silvestris, Mariacarmela Santarpia, Edoardo Spina, Maria Antonietta Barbieri

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Neuropsychiatric Adverse Events; Multiple Myeloma; FAERS; Monoclonal Antibody; Pharmacovigilance

Online: 20 September 2024 (14:58:48 CEST)

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Background/Objectives: Monoclonal antibodies (mAbs) have revolutionized multiple myeloma (MM) treatment. However, post-marketing data on their neuropsychiatric safety is limited. This study aimed to evaluate neuropsychiatric adverse events (AEs) related to mAbs used for MM through a retrospective pharmacovigilance analysis using the Food and Drug Administration (FDA) Adverse Events Reporting System (FAERS) database. Methods: Individual case safety reports (ICSRs) from 2015 to 2023 with at least one neuropsy-chiatric AE and one of the MM-approved mAbs as the suspect drug (i.e., daratumumab, elo-tuzumab, isatuximab, belantamab mafodotin, teclistamab, elranatamab, and talquentamab) were analyzed using descriptive and disproportionality approaches. Results: Unknown signals of disproportionate reporting (SDR) included cerebral infarction for daratumumab (n = 45; reporting odds ratio (ROR) = 2.39, 95% confidence interval (CI) = 1.79-3.21; information component (IC) = 1.54, IC025-IC075 = 1.05-1.9), elotuzumab (25; 7.61, 5.13-11.28; 3.03, 2.37-3.51), and isatuximab (10; 2.56, 1.38-4.76; 1.67, 0.59-2.4); mental status changes for daratumumab (40; 2.66, 1.95-3.63; 1.67, 1.14-2.04) and belantamab mafodotin (10; 4.23, 2.28-7.88; 2.3, 1.22-3.03); altered state of consciousness for daratumumab (32; 1.97, 1.39-2.78; 1.32, 0.73-1.74) and belantamab mafodotin (6; 2.35, 1.05-5.23; 1.6, 0.19-2.52); Guil-lain-Barre syndrome (GBS) for daratumumab (23; 6.42, 4.26-9.69; 2.81, 2.11-3.3), isatuximab (8; 10.72, 5.35-21.48; 3.57, 2.35-4.37), and elotuzumab (3; 4.74, 1.53-14.7; 2.59, 0.52-3.8); and orthos-tatic intolerance for daratumumab (10; 12.54, 6.71-23.43; 3.75, 2.67-4.48) and elontuzumab (4; 28.31, 10.58-75.73; 5 , 3.24-6.08). Conclusions: Our analysis highlighted several previously unacknowledged SDRs for MM-approved mAbs. Given the complex and not entirely understood etiology of some neuropsy-chiatric AEs, including GBS, further investigations are necessary.

Preprint ARTICLE | doi:10.20944/preprints202312.1263.v2

A Method to Reverse Epimutations

Steven Olsen

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Homeostasis; HDEC; Hormesis; Epimutations; Susceptibility; Toxicogenomics

Online: 17 September 2024 (05:04:16 CEST)

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Preprint REVIEW | doi:10.20944/preprints202409.0899.v1

Exploring the Therapeutic Potential of N-Methyl-D-Aspartate Receptor Antagonists in Neuropathic Pain Management

Ciprian Pușcașu, Cornel Chiriță, Simona Negreș, Nicoleta Mirela Blebea

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: neuropathic pain; NMDA receptor antagonist; ketamine; memantine; methadone

Online: 11 September 2024 (15:02:14 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202408.2205.v1

In Silico and In Vivo Evaluation of Novel 2-Aminobenzothiazole Derivative Compounds as Antidiabetic Agents

Juan Andres Alvarado Salazar, Miguel Valdes, Alejandro Cruz, Brenda Moreno De Jesús, David Patiño González, Ivonne María Olivares-Corichi, Feliciano Tamay Cach, Jessica Elena Mendieta Wejebe

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: 2-aminobenzotiazol; isotioureas; guanidinas; diabetes tipo 2; actividad antidiabé; tica

Online: 30 August 2024 (09:38:35 CEST)

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Preprint REVIEW | doi:10.20944/preprints202408.1965.v1

AgNPs: An Adaptive Methodology in Malignant Growth Treatment, Disclosing Upgraded Radiotherapy and Beyond

BASIM ALMAYAHI

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Ag nanoparticles; growth cell; radiotherapy; in vitro; characterization

Online: 27 August 2024 (16:29:38 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202408.1870.v1

Evaluating the Efficacy of Delafloxacin and Combination Therapy Against Staphylococcus aureus Biofilms: Insights into Activity in Acidic Environments

Ana Paula de Andrade, Jaqueline Pilon de Meneses, Paula Hansen Suss, Gabriel Burato Ortis, Felipe Francisco Tuon

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Staphylococcus aureus; biofilm; delafloxacin; rifampicin

Online: 26 August 2024 (15:28:06 CEST)

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Background: Staphylococcus aureus is a major contributor to biofilm-associated infections, which complicate the treatment of chronic conditions like osteomyelitis and prosthetic infections. Bio-films, characterized by bacterial communities encased in a protective matrix, hinder the effec-tiveness of antimicrobial agents and contribute to persistent infections. Objective: This study aimed to evaluate the activity of delafloxacin, a novel fluoroquinolone, against biofilm-forming S. aureus strains, including methicillin-resistant (MRSA) and methicillin-sensitive (MSSA) isolates. Methods: Delafloxacin’s efficacy was compared with traditional antibiotics (vancomycin, line-zolid, doxycycline, sulfamethoxazole/trimethoprim, and rifampicin) using minimal inhibitory concentration (MIC) assays, including testing at different pH levels to simulate acidic biofilm conditions. Synergistic interactions between delafloxacin and other antimicrobials were assessed using the checkerboard method. Biofilm eradication was tested through minimal biofilm eradi-cation concentration (MBEC) assays, biomass quantification, and cell viability (MTT assay). Re-sults: The results showed that all isolates were susceptible to vancomycin and linezolid, with varying resistance to other antibiotics. Delafloxacin demonstrated potent activity, with MIC re-ductions observed in acidic conditions. Synergistic effects were minimal, with only a few isolates showing synergy with vancomycin and doxycycline. Biofilm eradication tests revealed limited success in eradicating biofilms at breakpoint concentrations. However, rifampicin in combination with delafloxacin significantly reduced biofilm biomass in some isolates. No significant changes in cell viability were noted across treatments. Conclusion: This study highlights delafloxacin's potential against biofilm-associated infections, particularly in acidic environments. Despite the challenges in biofilm eradication, delafloxacin combined with rifampicin shows promise for im-proved treatment strategies.

Preprint BRIEF REPORT | doi:10.20944/preprints202408.0746.v1

Short Cycle Therapy with Bictegravir/Emtricitabine/Tenofovir Alafenamide in a Small Cohort of Virally Suppressed People Living with HIV: A Long-Term Follow-Up

Massimiliano Lanzafame, Emanuela Lattuada, Andrea Delama, Giovanni Mori, Sandro Vento

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Antiretroviral treatment; short cycle therapy; HIV; virologically suppressed people; bictegravir

Online: 12 August 2024 (12:36:39 CEST)

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Preprint REVIEW | doi:10.20944/preprints202408.0522.v1

History and Toxinology of Palytoxins

Chad Roy, Harriet Hammond

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: palytoxin; ovatoxin; zoanthids; aerosol; inhalation; disease models

Online: 7 August 2024 (13:56:47 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.2610.v1

Comprehensive Analysis of Berberis aristata DC. Bark Extracts: In Vitro and In Silico Evaluation of Bioavailability and Safety

Giovanna Rigillo, Giorgio Cappellucci, Giulia Baini, Federica Vaccaro, Elisabetta Miraldi, Luca Pani, Fabio Tascedda, Renato Bruni, Marco Biagi

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: berberine; safety; bioavailability; cell viability; gene expression

Online: 1 August 2024 (05:19:58 CEST)

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Preprint REVIEW | doi:10.20944/preprints202407.2527.v1

Updated Risk Assessment of Cannabidiol in Foods based on Benchmark Dose-Response Modeling

Eva Wisotzki, Heike Franke, Constanze Sproll, Stephan G. Walch, Dirk W. Lachenmeier

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: cannabidiol; novel food; health-based guidance value; benchmark dose; risk assessment

Online: 31 July 2024 (09:50:10 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.2017.v1

Apigenin Induces Oxidative Stress in Triggering the Intrinsic Apoptotic Pathway in ELT3 Rat Uterine Leiomyoma Cells

Samak Sutjarit, Chanokchon Setthawongsin, Chainarong Sakulthaew, Nattakan Meekhanon, Kazuhiko Ochiai

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: apigenin; apoptosis; ELT3 cells; oxidative stress; reactive oxygen species

Online: 25 July 2024 (07:17:34 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.1944.v1

Real-World Evidence of the Effectiveness and Safety of Ciclopirox 8% HPCH Nail Lacquer Combined with Oral Antifungals for Onychomycosis Applying Artificial Intelligence to Electronic Health Records

Gaston Roustan, José Luis López Estébaranz, Pablo De La Cueva, Savana Research Group, Francesca Pajuelo, María Luisa Tamarit, Aida Valmaseda, Jordi Galván

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: onychomycosis; ciclopirox 8% HPCH; real-world data; machine learning; artificial intelligence; terbinafine; itraconazole; fluconazole

Online: 25 July 2024 (03:20:04 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.1888.v1

QCT-Based 3CL Protease Inhibitor: Tollovir

Dorit Arad

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Keywords: Coronavirus; 3CL protease; Drug target for Coronavirus; SARS-CoV

Online: 24 July 2024 (12:36:54 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.1818.v1

Cu2O Nanoparticles as Nanocarriers and Its Antibacterial Efficacy

M. I. Torres-Ramos, Ubaldo de Jesús Martín Camacho, Suresh Ghotekar, Jorge Alberto Sánchez-Burgos, Oscar Arturo González-Vargas, Momoune Fellah, Alejandro Pérez-Larios

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Cu2O nanoparticles; Sol-gel method; Drug delivery; Functionalization; Mesoporous materials.

Online: 24 July 2024 (07:02:17 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.1780.v1

Investigation of the Prevalence of Drug-Drug Interactions in the Cardiology Department

Jogaile Butauskaite, Austeja Zumbakyte, Lauryna Aukstikalne, Jolita Pancere, Skaiste Zukaitiene, Egle Karinauske

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: drug-drug interactions; drug safety; adverse drug reactions; polypharmacy

Online: 23 July 2024 (13:21:38 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.1002.v1

A Real-World Data Analysis of the Impact of Liposomal Amphotericin B on Renal Function Using Machine Learning in Critical Ill Patients

Ignasi Sacanella, Erika Esteve-Pitarch, Jessica Guevara-Chaux, Julen Berrueta, Alejandro García-Martínez, Josep Gómez, Cecilia Casarino, Florencia Alés, Laura Canadell, Ignacio Martin-Loeches, Santiago Grau, Francisco Javier Candel, María Bodí, Alejandro Rodríguez

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Liposomal amphotericin B; Acute Kidney Injury; Machine learning; Critical Care; Antifungal agents; Random Forest

Online: 15 July 2024 (15:52:44 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.0726.v1

Characterization of Antineoplastic Agents Inducing Taste and Smell Disorders Using the FAERS Database

Risa Hamazaki, Yoshihiro Uesawa

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: taste disorder; olfaction; chemotherapy; cancer

Online: 10 July 2024 (07:58:44 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.0679.v1

Pycnogenol-Assisted Alleviation of Titanium Dioxide Nanoparticle-Induced Lung Inflammation via Thioredoxin-Interacting Protein Downregulation

Je-Oh Lim, Woong-Il Kim, So-Won Pak, Se-Jin Lee, Changjong Moon, In-Sik Shin, Sung-Hwan Kim, Jong-Choon Kim

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Titanium dioxide nanoparticle; lung inflammation; pycnogenol; antioxidative effect; thioredoxin-interacting protein

Online: 9 July 2024 (08:20:44 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202407.0696.v1

Nuclear Receptors and Stress Response Pathways Associated with the Development of Oral Mucositis Induced by Antineoplastic Agents

Moena Kagaya, Yoshihiro Uesawa

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: oral mucositis; antineoplastic agent; molecular initiating event

Online: 9 July 2024 (06:51:59 CEST)

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Preprint CASE REPORT | doi:10.20944/preprints202406.1567.v1

Dipyrone-induced inappropriate antidiuretic hormone secretion: a case report

Jawad Hindy, Tova Rainis, Dana Greenberg

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Dipyrone; Metamizole; Hyponatremia; Hip fracture

Online: 24 June 2024 (12:37:44 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202406.1650.v1

Eugenol-Rich Essential Oils from Flower Buds and Leaves of Syzygium aromaticum Unveils Antifungal Activity against Candida and Cryptococcus Species

Evariste Josué Momo, François Nguimatsia, Laure Ateufouet Ngouango, Paul Keilah Lunga, Boniface Pone Kamdem, Pierre Michel Jazet Dongmo

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Syzygium aromaticum; Antifungal activity; GC-MS analysis, Essential oil, Volatile compounds

Online: 24 June 2024 (08:44:39 CEST)

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Plants from the Myrtaceae family are well known to contain considerable amounts of volatile compounds, ranging from oxygenated monoterpenes to hydrogenated sesquiterpenes, and others, which exhibit antimicrobial activity. One such plant includes Syzygium aromaticum that has been extensively used to treat a number of disorders, including bacterial and fungal infections. Thus, the scientific validation of the essential oil (EO) of Syzygium aromaticum vis-à-vis Candida and Cryptococcus species is valuable. To this end, the present study sought to investigate the antifungal activity of EO from S. aromaticum (clove) leaves and flower buds against Candida and Cryptococcus species. The antioxidant activity of S. aromaticum’s essential oils is also elucidated. The EO was extracted from fresh leaves and floral buds of S. aromaticum using a Clevenger-type apparatus. The as-prepared essential oils were further evaluated for antifungal activity against Candida and Cryptococcus species using a microdilution method. The phytochemical analysis of the EOs was assessed by gas chromatography/mass spectrometry (GC-MS). Antioxidant activities of the EOs were evaluated using standard methods. As a result, the GC-MS analysis revealed the presence of volatile compounds, such as eugenol (87.08%), β-caryophyllene (6.40%) and acetyleugenol (4.45%) as the major constituents of EO from the flower buds ; and eugenol (90.54%) and β-caryophyllene (24.65%) as the major components of the leaf’s EO. The eugenol-rich essential oils exhibited significant antifungal effects against Candida species (common MIC value: 200 ppm) and Cryptococcus neoformans (MIC value: 50 ppm), as well as antioxidant activity. Overall, essential oils of S. aromaticum demonstrated an-tioxidant and antifungal effects, thus validating the ethnopharmacological use of this plant in the treatment of fungal infections. However, antifungal mechanisms of action, in-depth toxicity and in vivo experiments, and pharmacokinetics are warranted to support the use of this plant in ethnomedicine.

Preprint ARTICLE | doi:10.20944/preprints202406.1288.v1

Antioxidant Activity and UHPLC-MS/MS Characterization of Polyphenol and Nicotine Content of Nicotiana glauca Leaf Extracts: A Comparative Study of Conventional and Deep Eutectic Solvent Extraction Methods

Reem Issa, Faisal Al-Akayleh, Lilian Alnsour, Tabarak Alsammaraie, Khaled W. Omari, Shady Helmi Awwad

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Nicotiana glauca; Chromatography; Mass Spectrometry; Antioxidants; deep eutectic solvents; sustainable extraction.

Online: 19 June 2024 (16:31:42 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202406.1291.v1

Exploring the Mechanism of Topical Application of Clematis Florida in the Treatment of Rheumatoid Arthritis through Network Pharmacology and Experimental Validation

Ting Lei, Chang Jiang, Li Zhao, Jizhou Zhang, Qing Xiao, Yanhong Chen, Jie Zhang, Chunquan Zhou, Gong Wang, Jing Han

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Clematis Florida; rheumatoid arthritis; network pharmacology; NF-κ B; MAPK

Online: 19 June 2024 (07:03:21 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202406.0844.v1

A Real-World Safety Profile in Neurological, Skin, and Sexual disorders of Antiepileptic Drugs Using Pharmacovigilance Database of the Korea Adverse Event Reporting System (KAERS)

DaJeong Kim, Sukhyang Lee

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Adverse event reporting system; Anti-epileptic drugs; Adverse reproductive outcome; Sodium channel blockers; Epilepsy; Pharmacovigilance

Online: 12 June 2024 (23:52:54 CEST)

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Preprint REVIEW | doi:10.20944/preprints202406.0822.v1

Colchicine—The Divine Medicine against COVID-19

Vanyo Mitev

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: COVID-19; colchicine doses; colchicine toxicity; cytokine storm; NLRP3 inflammasome

Online: 12 June 2024 (09:46:57 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202406.0258.v1

Comprehensive Analysis of Various Parkinson-Like Events and Induced Drugs

Mami Kikegawa, Hideko Sone, Yoshihiro Uesawa

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Parkinson-like events; Japanese Adverse Drug Event Report database; spontaneous reporting system; volcano plot; hierarchical clustering; principal component analysis

Online: 5 June 2024 (08:25:00 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202405.2057.v1

Re-Use of Caco-2 Monolayers for a Higher Throughput Assessment of Drug Permeability – Methodology and Validation for Passive Permeation

Cristiana L. Pires, Susana Rosa, Ana L. M. Batista de Carvalho, Lino Ferreira, Maria Paula M. Marques, Maria João Moreno

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Permeability assay; pharmacokinetics; Caco-2 monolayers; re-use; high throughput; passive diffusion; active transport

Online: 30 May 2024 (13:45:41 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202405.1968.v1

Pharmacokinetics and Tissue Distribution of Rosuvastatin in a Rat Model of Preeclampsia

Wanying Dai, Micheline Piquette-Miller

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: breast cancer resistance protein; preeclampsia; pharmacokinetic; pregnancy; transporters

Online: 29 May 2024 (11:56:56 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202405.1831.v1

Crude Extracts from Lippia adoensis (Hochst.) Inhibit the Growth of Plasmodium, Leishmania and Trypanosoma Parasites

Eugenie Aimée Madiesse Kemgne, Mariscal Brice Tchatat Tali, Darline Dize, Cyrille Armel Njanpa Ngansop, Boniface Pone Kamdem, Fabrice Fekam Boyom

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Lippia adoensis; Plasmodium falciparum; Leishmania donovani; Trypanosoma brucei; molecular networking; LC-MS analysis

Online: 28 May 2024 (11:28:34 CEST)

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Preprint REVIEW | doi:10.20944/preprints202405.1681.v1

Role of Oxidative Stress and Inflammation in Doxorubicin-Induced Cardiotoxicity: A Brief Account

Roberta Vitale, Stefania Marzocco, Ada Popolo

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: cardiotoxicity; doxorubicin; oxidative stress; inflammation

Online: 27 May 2024 (05:51:15 CEST)

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Preprint REVIEW | doi:10.20944/preprints202405.1549.v1

Marine Pharmacology in 2019‐2021: Marine Compounds with Antibacterial, Antidiabetic, Antifungal, Anti‐Inflammatory, Antiprotozoal, Antituberculosis and Antiviral Activities; Affecting the Immune and Nervous Systems, and Other Miscellaneous Mechanisms of Action

Alejandro M.S. Mayer, Veronica A. Mayer, Michelle Swanson-Mungerson, Marsha L. Pierce, Abimael D. Rodríguez, Fumiaki Nakamura, Orazio Taglialatela-Scafati

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: drug; marine; sea; pharmacology; pharmaceutical; review; toxicology; pipeline; preclinical; mechanism

Online: 23 May 2024 (12:40:49 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202405.1462.v1

Comprehensive Analysis of Kisspeptin Signaling: Effects on Cellular Dynamics in Cervical Cancer

Deisy Yurley Rodríguez-Sarmiento, Paola Rondón-Villarreal, Pedro Henrique Scarpelli-Pereira, Michel Bouvier

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: kisspeptin receptor; kisspeptin; cancer; cytotoxicity; signal transduction

Online: 23 May 2024 (02:55:45 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202405.1473.v1

Facile Access to Solifenacin Impurity K: One-Step Synthesis and an HPLC-MS Method for Its Determination

Raúl Xifra, Andreea L. Turcu

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: solifenacin succinate; impurity K; HPLC-MS analytical method

Online: 22 May 2024 (16:53:42 CEST)

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Preprint REVIEW | doi:10.20944/preprints202405.1367.v1

A Comprehensive Exploration of the Multifaceted Neuroprotective Role of Cannabinoids in Alzheimer's Disease Across a Decade of Research

Petros Tyrakis, Christina Agridi, Malamati Kourti

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Cannabinoids; Alzheimer’s disease; Cannabis sativa; CB1R; CB2R; Trpv-1; GPR-55

Online: 21 May 2024 (10:02:08 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202405.1092.v1

A Genomewide Association Study of Oxypurinol Concentrations in Patients Treated with Allopurinol

Maxime Meloche, Sylvie Provost, Grégoire Leclair, Essaïd Oussaïd, Isabelle St-Jean, Martin Jutras, Marie-Josée Gaulin, Louis-Philippe Lemieux Perreault, Diane Valois, Ian Mongrain, David Busseuil, Jean-Lucien Rouleau, Jean-Claude Tardif, Marie-Pierre Dubé, Simon de Denus

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: GWAS; pharmacogenomics; allopurinol; drug metabolism; biobank

Online: 16 May 2024 (13:43:56 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202405.0775.v1

Unveiling the Antitumor Mechanism of 7α-Acetoxy-6β-Hydroxyroyleanone from Plectranthus hadiensis in Glioblastoma

Mariana Magalhães, Eva María Domínguez-Martín, Joana Jorge, Ana Cristina Gonçalves, Francesca Massenzio, Renato Spigarelli, Teresa Ribeiro-Rodrigues, Steve Catarino, Henrique Girão, Barbara Monti, Enzo Spisni, Lino Ferreira, Paulo J. Oliveira, Thomas Efferth, Patrícia Rijo, Célia Cabral

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Glioblastoma; Plectranthus hadiensis Schweinf; Royleanone; Abietane diterpenes; Antitumor activity

Online: 13 May 2024 (08:23:46 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202405.0491.v1

Repurposing of Synthetic Acetaminophen Derivatives Containing Benzothiazole Scaffold as Alternative Therapy for Infectious Diarrhea Caused by Drug-Resistant Shigella Species

Boniface Pone Kamdem, Brice rostan Pinlap, Bijou-Lafortune Noumboue Kouamou, Aubin Youbi Kamche, Boris Arnaud Kuate, Joseph Tsemeugne, Orleans Ngomo, Pierre Mkounga, Fabrice Fekam Boyom

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Acetaminophen; Benzothiazoles; Azo dyes; Shigella flexneri; Anti-Shigella activity; Repositioning; Combination studies; Diarrhea.

Online: 8 May 2024 (11:33:24 CEST)

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Preprint REVIEW | doi:10.20944/preprints202405.0326.v1

3-Chymotrypsin-like Protease (3CLpro): Validation as a Molecular Target, Proposal of a Novel Catalytic Mechanism, and Inhibitors in Preclinical and Clinical Trials

Vitor Martins de Freitas Amorim, Eduardo Pereira Soares, Anielle Salviano de Almeida Ferrari, Davi Gabriel Salustiano Merighi, Robson Francisco de Souza, Cristiane Rodrigues Guzzo, Anacleto Silva de Souza

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: SARS-CoV-2; 3CLpro; Novel Mechanism of Catalysis; FDA-approved drugs; Triad

Online: 7 May 2024 (16:44:24 CEST)

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Preprint REVIEW | doi:10.20944/preprints202404.2000.v1

Resveratrol: A Review on the Biological Activity and Applications

Ludovic Everard Bejenaru, Andrei Biţă, Ionela Belu, Adina-Elena Segneanu, Antonia Radu, Andrei Dumitru, Maria Viorica Ciocîlteu, George Dan Mogoşanu, Cornelia Bejenaru

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: resveratrol; stilbenoids; grapes; wine; biological activity; applications

Online: 30 April 2024 (11:56:52 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202404.1954.v1

An Assessment of Semaglutide Safety Based on Real World Data: From Popularity to Spontaneous Reporting in EudraVigilance Database

Anca Butuca, Carmen Maximiliana Dobrea, Anca Maria Arseniu, Adina Frum, Adriana Aurelia Chis, Luca Liviu Rus, Steliana Ghibu, Anca Maria Juncan, Andrei Catalin Muntean, Antonina Evelina Lazăr, Felicia Gabriela Gligor, Claudiu Morgovan, Andreea Loredana Vonica-Tincu

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: semaglutide; obesity; weight loss; overdose; underdose; off-label use; EudraVigilance; GLP-1

Online: 30 April 2024 (10:14:22 CEST)

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Preprint REVIEW | doi:10.20944/preprints202404.1698.v1

Intravenous Lipid Emulsions in Anticonvulsants' Toxicity

Simeonka Dimitrova Dimitrova, Stela Toshkova Dragomanova, Gabriela Krasimirova Kehayova

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: intravenous lipid emulsion; acute intoxication; antiepileptics; antidote; Glasgow Coma Scale scores; QT interval

Online: 25 April 2024 (16:52:46 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202404.1660.v1

Antidiabetic Effect of Raru (Vatica perakensis) Bark Extract and Mocaf Activated Carbon in Streptozotocin-Induced Diabetic Rats

Gunawan Pasaribu, Novitri Hastuti, Saptadi Darmawan, Gustan Pari, Lisna Efiyanti, Totok Waluyo, Mody Lempang, Yelin Adalina

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: antidiabetic, extract, in-vivo, MAC, raru ; ;

Online: 25 April 2024 (10:17:29 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202404.1328.v1

Finding a Direct method for a Dynamic process: the DD (Direct and Dynamic) Cell-Tox method

Eneko Madorran, Lidija Kocbek Šaherl, Mateja Rakuša, Mihael Munda

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: cell viability; in vitro toxicology; dynamic direct cell death assay

Online: 22 April 2024 (08:36:16 CEST)

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Preprint REVIEW | doi:10.20944/preprints202404.0971.v1

The New Horizon of Antipsychotics beyond the Classic Dopaminergic Hypothesis—The Case of the Xanomeline-Trospium Combination: A Systematic Review

Octavian Vasiliu, Beatrice Budeanu, Mihai Stefan Catanescu

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: xanomeline; trospium; schizophrenia; Alzheimer’s disorder; psychoses; acetylcholine; muscarinic receptors; antipsychotics; dopaminergic hypothesis

Online: 15 April 2024 (14:36:30 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202404.0784.v1

Dramatic Suppression of Lipogenesis and No Increase in Beta- Oxidation Are the Main Effects of Bergamot Flavonoids on Gene Expression in Fatty Liver Disease

Maddalena Parafati, Daniele La Russa, Antonella Lascala, Francesco Crupi, Concetta Riillo, Bartosz Fotschki, Vincenzo Mollace, Elzbieta Janda

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: flavonoids; hepatic steatosis; lipogenesis; Citrus Bergamia; gene profiling

Online: 11 April 2024 (09:32:33 CEST)

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Preprint REVIEW | doi:10.20944/preprints202404.0659.v1

Gerontogen as the Toxicology of Aging

Rahma Rahma, Agian Jeffilano Barinda

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: aging; senescence; toxicology; gerontogen; senotherapy

Online: 10 April 2024 (03:17:10 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202404.0616.v1

Lysophosphatidic Acid Receptor 3 (LPA3): Signaling and Phosphorylation Sites

K. Helivier Solís, M. Teresa Romero-Ávila, Ruth Rincón-Heredia, J. Adolfo García-Sáinz

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Keywords: Lysophosphatidic acid: LPA; Lysophosphatidic acid receptor 3; LPA3; phosphorylation sites; signaling.

Online: 9 April 2024 (09:39:12 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202404.0592.v1

Alkaloid Profiling and Anti-Cholinesterase Potential of Three Different Genera of Amaryllidaceae Collected in Ecuador: Urceolina Rchb., Clinanthus Herb., and Stenomesson Herb

Luciana R. Tallini, Karen Acosta León, Raúl Chamorro, Edison H. Osorio, Jaume Bastida, Lou Jost, Nora H. Oleas

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Amaryllidoideae; alkaloids; Amazon lily; Alzheimer’ s disease; computational experiments

Online: 9 April 2024 (07:40:34 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202404.0541.v1

LPA3 Receptor Phosphorylation Sites: Roles in Signaling and Internalization

K. Helivier Solís, M. Teresa Romero-Ávila, Ruth Rincón-Heredia, J. Adolfo García-Sáinz

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Lysophosphatidic acid: LPA; Lysophosphatidic acid receptor 3; LPA3; phosphorylation sites; signaling

Online: 8 April 2024 (14:00:27 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202404.0523.v1

VIGI-4: Development of a Novel Pharmacovigilance Method Using ChatGPT

Eleftherios Teperikidis, Georgios Papazisis

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: pharmacovigilance; adverse drug reactions; ChatGPT; artificial intelligence; phase 4 studies; drug safety

Online: 8 April 2024 (11:16:12 CEST)

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Preprint ARTICLE | doi:10.20944/preprints202404.0503.v1

Formulation and Evaluation of Hydrophilic Matrix Tablets for Controlled Released Chlorzoxazone Delivery

Andreea Creteanu, Gabriela Lisa, Cornelia Vasile, Maria-Cristina Popescu, Daniela Pamfil, Claudiu N. Lungu, Gladiola Tantaru, Alina Diana Panaite

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: chlorzoxazone; collided; chitosan; matrix tablets; controlled release

Online: 8 April 2024 (07:15:31 CEST)

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The release of the active substance from the matrix modified-release tablets based on Kollidon®SR and chitosan depends on its solubility in the dissolution medium and on the composition of the matrix-forming polymers. The study is based on new oral matrix tablets based on Kollidon®SR and chitosan, formulated to optimize the low oral bioavailability of chlorzoxazone, a non-steroidal anti-inflammatory drug, a class II Biopharmaceutical Classification System. Nine types of chlorzoxazone matrix tablets were obtained using the direct compression method, and their combination at 1:1, 1:2, 1:3 chlorzoxazone/ excipients, 20%-40% (w/w) Kollidon®SR, 3-7% (w/w) chitosan and the auxiliary substances were formulated in constant concentrations. Pharmaco-technical characterization included the analysis of flowability and compressibility properties (flow time, friction coefficient, angle of repose, Hausner ratio, Carr Index), and of pharmaco-chemical characteristics (mass and dose uniformity, thickness, diameter, mechanical strength, Friability, degree of softening, in vitro release profile) of the tablets. Based on the initial evaluation of the pharmaco-technical analysis, pharmaco-chemical characteristics, and in vitro release profile, only three matrix tablet formulations (F1b, F2b, and F3b) were further tested. They were evaluated through Fourier-transform infrared spectrometry, X-ray Diffraction, thermogravimetry, differential scanning calorimetry, and in vitro dissolution tests. The three formulations were comparatively studied regarding the release kinetics of active substances using in vitro release testing. The results were analyzed by fitting into four representative mathematical models for the modified release oral formulations. In vitro kinetic study reveals a complex mechanism of release occurring in the first (0 - 2 hours) and second (2.0 hours – 36 hours) steps of drug release. Two factors have been calculated to assess the release profile of chlorzoxazone: f1 - the similarity factor and f2 - the factor difference. The results have shown that both Kollidon®SR and chitosan may be used as matrix-forming agents when combined with chlorzoxazone. In vitro dissolution tests revealed the F2b sample, data suggesting a faster drug release. The three formulations showed optimum pharmaco-technical properties and in vitro kinetic study, and they had tremendous potential to be used in oral pharmaceutical products for the controlled delivery of chlorzoxazone.

Preprint ARTICLE | doi:10.20944/preprints202404.0174.v1

Antioxidant and Cytotoxic Properties of Berberis vulgaris (L.) Stem Bark Dry Extract

Ionuț Mădălin Ivan, Octavian Tudorel Olaru, Violeta Popovici, Carmen Lidia Chițescu, Liliana Popescu, Emanuela Alice Luță, Elena Iuliana Ilie, Lorelei Irina Brașoveanu, Camelia Mia Hotnog, George Mihai Nițulescu, Rica Boscencu, Cerasela Elena Gîrd

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Berberis volgaris (L.) stem bark; dry hydro-ethanolic extract; phenolic secondary metabolites; berberine; antioxidant activity; cytotoxicity

Online: 2 April 2024 (10:27:54 CEST)

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Berberis vulgaris (L.) has remarkable ethnopharmacological properties and is widely used in traditional medicine. The present study investigates B. vulgaris stem bark (Berberidis cortex) by extraction with 50% ethanol. The main secondary metabolites were quantified, resulting in a polyphenols content of 17.6780 ± 3.9320 mg Eq Tannic acid / 100 g extract, phenolic acids amount of 3.3886 ± 0.3481 mg Eq Chlorogenic acid / 100 g extract and 78.95 µg/g berberine. The dried hydro-ethanolic extract (BVE) was thoroughly analyzed using Ultra-High Performance Liquid Chromatography coupled with High-Resolution Mass Spectrometry (UHPLC–HRMS/MS) and HPLC and 40 bioactive phenolic constituents were identified. Then, the antioxidant potential of BVE was evaluated using three methods; our results could explain the protective effects of Berberidis cortex EC50FRAP = 0.1398 mg/mL, IC50ABTS = 0.0442 mg/mL, IC50DPPH = 0.2610 mg/mL compared to ascorbic acid (IC50 = 0.0165 mg/mL). Next, the acute toxicity and teratogenicity of BVE and Berberine - Berberine sulfate hydrate (BS) - investigated on Daphnia sp reported significant BS toxicity after 24 h; BVE revealed considerable toxicity after 48 hours and induced embryonic developmental delays. Finally, the anticancer effects of BVE and BS were evaluated on different tumor cell lines after 24 and 48 hours of treatments. The MTS assay evidenced a dose- and time-dependent antiproliferative activity, higher on BS than BVE. The strongest diminution of tumor cell viability was recorded on breast (MDA-MB-231), colon (LoVo) cancer, and OSCC (PE/CA-PJ49) cell lines after 48 h of exposure (IC50 < 100 µg/mL). However, no cytotoxicity was reported on normal epithelial cells (HUVEC) and hepatocellular carcinoma (HT-29) cell lines. Extensive data analysis supports our results, showing a significant correlation between the BVE's concentration, phenolic compounds content, antioxidant activity, exposure time, and the viability rate of various normal cells and cancer cell lines.

Preprint ARTICLE | doi:10.20944/preprints202403.1853.v1

Evaluating the Antihyperalgesic Potential of Sildenafil-Metformin Combination and Its Impact on Biochemical Markers in Alloxan-Induced Diabetic Neuropathy in Rats

Ciprian Pușcașu, Cristina Elena Zbârcea, Anca Ungurianu, Emil Ștefănescu, Cornel Chiriță, Nicoleta Mirela Blebea, Simona Negreș

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: diabetic neuropathy; sildenafil; metformin; antihyperalgesic; IL-6; TNF-α

Online: 29 March 2024 (13:45:41 CET)

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Preprint ARTICLE | doi:10.20944/preprints202403.1299.v1

Changes on SOD and NF-kappaB Levels in Substantia Nigra and Intestine, by Oxidative Stress Effects in a Murine Model of Ozone Pollution

Selva Rivas-Arancibia, Erika Rodríguez-Martínez, Marlen Valdés-Fuentes, Alfredo Miranda-Martínez, Eduardo Hernández-Orozco, Citlali Reséndiz-Ramos

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: O3, oxidative stress, substantia nigra, intestine, 4HNE, NFκB, superoxide dismutase

Online: 21 March 2024 (10:47:10 CET)

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Preprint ARTICLE | doi:10.20944/preprints202403.0903.v1

Oleanolic Acid Acetate Alleviates Cisplatin-Induced Nephrotoxicity Via Inhibition of the Caspase and RIPK Pathways

Bori Lee, Yeon-Yong Kim, Seungwon Jeong, Seung Woong Lee, Seung-Jae Lee, Mun-Chual Rho, Sang-Hyun Kim, Soyoung Lee

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: acute kidney injury; oleanolic acid acetate; cisplatin; necroptosis; apoptosis

Online: 15 March 2024 (08:54:29 CET)

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Preprint REVIEW | doi:10.20944/preprints202403.0883.v1

Current Knowledge and Regulatory Framework on the Use of Hyaluronic Acid for Aesthetic Injectable Skin Rejuvenation Treatments

Jenny Allen, Kalliopi Dodou

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: dermal fillers; skin rejuvenation; collagen; hydrogel; hyaluronic acid; crosslinking; medical device; regulatory framework

Online: 15 March 2024 (08:54:03 CET)

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Preprint REVIEW | doi:10.20944/preprints202403.0713.v1

Manganese and Platinum Driven Oxidative and Nitrosative Stress in Oxaliplatin‐Associated CIPN with Special Reference to Ca4Mn(DPDP)5, MnDPDP and DPDP

Jan Olof Gustav Karlsson, Per Jynge

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Calmangafodipir; mangafodipir; manganese; platinum; MnSOD mimetics; oxaliplatin-associated CIPN; oxidative stress; nitrosative stress; chelation therapy

Online: 12 March 2024 (14:10:23 CET)

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Preprint REVIEW | doi:10.20944/preprints202403.0540.v1

Nano‐Delivery Systems for Curcumin

Jibira Yakubu, Amit V. Pandey

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Curcumin; curcuminoids; nanoparticles; nanomedicine; nano-encapsulation; nano-delivery.

Online: 8 March 2024 (16:40:22 CET)

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Preprint ARTICLE | doi:10.20944/preprints202403.0468.v1

Comparative Study of a Potent CNS-Permeable RARβ-Modulator, Ellorarxine, in Neuronal Cells In Vitro

Yunxi Zhang, Lilie Gailloud, Rosella Pinckney, Andrew Whiting, Paul Chazot

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Ellorarxine; DC645; NVG0645; retinoid; mitochondrial dysfunction; neuroinflammation; neurodegeneration; neuroprotective effects

Online: 8 March 2024 (04:32:14 CET)

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Preprint ARTICLE | doi:10.20944/preprints202402.1671.v1

Bioactive Properties of Venoms Isolated from Whiptail Stingrays and the Search for Molecular Mechanisms and Targets

Craig A. Doupnik, Carl A. Luer, Catherine J. Walsh, Jessica Restivo, Jacqueline Xinlan Brick

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: apoptosis; cell adhesion; cell growth; fibrosarcoma; galectin-like proteins; stingray; toxin; venom

Online: 29 February 2024 (11:41:25 CET)

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Preprint ARTICLE | doi:10.20944/preprints202402.1233.v1

The Combined Effects of Doxorubicin and a Novel Sulfonamide Derivative on Inducing Apoptosis in a Breast Cancer Cell Line (MCF-7)

Shabnam Pedarpour, Sevda Zarei, Zeinab Mahmoodi, Hossein Ghafouri

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Apoptosis; Breast cancer; Drug synergism; Doxorubicin; Sulfonamide

Online: 21 February 2024 (15:34:31 CET)

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Preprint ARTICLE | doi:10.20944/preprints202402.0808.v1

Association between Molecular Initiating Events (MIEs) in Drug-Induced Hiccups

Ryuichiro Hosoya, Reiko Ishii-Nozawa, Tomoko Terajima, Hajime Kagaya, Yoshihiro Uesawa

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: drug-induced hiccups; FAERS; nuclear receptor; stress response pathways

Online: 15 February 2024 (01:25:14 CET)

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Preprint REVIEW | doi:10.20944/preprints202402.0029.v1

Quercetin, A Flavonoid With Great Pharmacological Capacity

Eber Josue Carrillo-Martinez, Flor Yohana Flores-Hernández, Adriana María Salazar-Montes, Hector Fabián Nario-Chaidez, Luis Daniel Hernández-Ortega

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Quercetin; Antioxidant; Free radicals; Pharmacological properties; Nanoparticles

Online: 2 February 2024 (06:36:16 CET)

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Preprint ARTICLE | doi:10.20944/preprints202402.0015.v1

Green Synthesis of Cocos nucifera-Based Nanomaterials and Mechanistic Basis of Their Antimicrobial Action.

Zuriatou Yajeh Tanka, Naphtali Odogu Ankoro, Vincent Ngouana, Franklin Loïc Tchinda Taghu, Abongta Lum Mforbesi, Branly-nathalien Nguena-Dongue, Julius Nsami Ndi, Boniface Pone Kamdem, Paul Keilah Lunga, Fabrice Fekam Boyom

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Cocos nucifera; green synthesis; nanomaterials; activated carbon; antimicrobial activity; cytotoxicity; oxidative stress

Online: 1 February 2024 (08:34:18 CET)

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Caused by pathogenic microorganisms, such as bacteria, parasites, fungi, among others, infectious diseases can spread directly or from one individual to another. According to the World Health Organization, these diseases are known to cause high mortality rates, severe burdens of disability and serious worldwide aftermaths. The inappropriate use of antibiotics in humans are the main origins of the development of drug-resistant pathogens, which reduce the efficacy of these therapies, thus accentuating the need to search for effective antimicrobials. Medicinal plants have served as starting material for the preparation of a number of antimicrobial agents. To this end, the present study highlights the green synthesis of Cocos nucifera-based nanomaterials and evaluation of the mechanistic basis of their antimicrobial action. Accordingly, Cocos nucifera extract was used to reduce different concentrations (5, 10 and 20 mM) of silver nitrate solution to afford silver nanoparticles (AgNPs). These entities were further incorporated onto activated carbons (obtained by chemical activation using sulphuric acid as activation agent) to generate the nanocomposites. The antimicrobial activity of the as-prepared nanomaterials was evaluated using the broth microdilution method, while, the antioxidant activity was assessed through standard methods, such as 2,2-diphenyl-1-picrylhydrazyl (DPPH), and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays. Cytotoxicity of potent nanomaterials was assessed on Vero cells by spectrophotometric method. As a result, nanoparticles were successfully synthesized as evidenced by the color change of the solution from transparent to dark brown. Further characterization was carried out by UV-visible spectroscopy that showed an intense absorption spectrum at 433 nm. Fourier Transform Infrared Spectroscopy (FTIR) revealed the functional group moieties involved as a capping and reducing agent in the synthesis of AgNPs. The incubation of nanomaterials with selected bacterial and fungal strains led to significant inhibitory effects of these pathogens with minimum inhibitory concentrations ranging from 7.813 to 250 μg/ml. In antioxidant assays, the nanocomposites presented scavenging activities comparable to that of ascorbic acid. Cytotoxicity experiment revealed no toxic effects on the human mammalian cells Vero (range of selectivity indices: from >4 to >128). These results provide evidence of the implication of Cocos nucifera-based nanomaterials in targeting bacterial or fungal systems that mediate free-radical damage or by inhibiting the oxidative damage caused by selected bacteria and fungi, the most susceptible being Escherichia coli and Candida albicans, respectively.

Preprint ARTICLE | doi:10.20944/preprints202401.1398.v1

Susceptibility Patterns in Staphylococcus and Klebsiella Causing Nosocomial Infections upon Treatment with E-Anethole-Rich Essential oil from Clausena anisate

François Nguimatsia, Evariste Josué Momo, Paul Keilah Lunga, Virginia Lum Tamanji, Boniface Pone Kamdem, Pierre Michel Jazet Dongmo

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Nosocomial infections; Antibacterial activity; Drug resistance; Clausena anisata; GC-MS analysis; Essential oil

Online: 18 January 2024 (11:05:38 CET)

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High rates of resistance to antibiotics are associated with healthcare-related infections, thus appealing for the urgent need for effective antimicrobials against these maladies. The present study aims to determine the chemical composition of essential oil (EO) from Clausena anisata leaves, and evaluate their antibacterial activity against selected nosocomial bacteria. Fresh leaves of Clausena anisata were subjected to a steam distillation using a Clevenger apparatus to afford the essential oil. The phytochemical composition of this oil was analyzed using gas chromatography-mass spectrometry (GC-MS). The essential oil was further tested against selected nosocomial bacteria, including Staphylococcus and Klebsiella species, among others, using a microdilution method. As a result, 0.77% of essential oil was extracted from fresh leaves of Clausena anisata. The GC-MS analysis revealed that the as-prepared essential oil contain E-anethole (70.77%), methyl isoeugenol (13.85%), estragole (4.10%), γ-terpinene (3.33%), myrcene (2.82%) and sabinene (0.77%), with E-anethole being the major constituent. Meanwhile, twenty two compounds were identified in the EO of Clausena anisata leaves through gas chromatography. Upon antibacterial test against selected nosocomial pathogens, the E-anethole-rich essential oil exhibited minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values ranging from 3.91 to 125 µg/mL and 7.81 to 125 µg/mL, respectively, indicative of a bactericidal orientation of the plant’s essential oil (MIC/MBC ratio: 4). This novel contribution highlights the scientific validation of the use of Clausena anisata leaves in the traditional treatment of various infectious diseases. However, toxicity and pharmacokinetic studies, mechanistic basis of the antibacterial action, and in vivo antibacterial experiments of the E-anethole-rich essential oil of Clausena anisata should be investigated to successfully use this plant in the treatment of infectious diseases.

Preprint ARTICLE | doi:10.20944/preprints202401.1122.v1

Evaluation of In Vitro Synergistic Interactions of Tetracycline with Alkaloid-Related Compounds against Diarrheagenic Bacterial Pathogens

Hayford Osei-Owusu, Johana Rondevaldova, Marketa Houdkova, Tomas Kudera, Tersia Needham, Ladislav Kokoska

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: antimicrobial agents; combination therapy; diarrhoea; multidrug resistance; pathogens; synergistic effect

Online: 16 January 2024 (02:16:37 CET)

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Preprint ARTICLE | doi:10.20944/preprints202401.1072.v1

Partial mGlu5 Receptor NAM, M-5MPEP, Induces Rapid and Sustained Antidepressant-like Effects in the BDNF-dependent Mechanism and Enhances (R)-Ketamine Action in Mice

Agnieszka Pałucha-Poniewiera, Anna Rafało-Ulińska, Michał Santocki, Yana Babii, Katarzyna Kaczorowska

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: antidepressant; BDNF; mGlu5 receptor; M-5MPEP; RAAD; (R)-ketamine; TrkB receptor

Online: 15 January 2024 (08:30:44 CET)

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Preprint ARTICLE | doi:10.20944/preprints202401.0919.v1

Self-Completion Questionnaire on Sleep Evaluation in Patients Undergoing Oxaliplatin Therapy: An Observational Study

Maria Valentina Mussa, Sarah Allegra, Tiziana Armando, Silvana Storto, Beatrice Ghezzo, Giulia Soave, Giuliana Abbadessa, Francesco Chiara, Massimo Di Maio, Fiammetta Maria Dagnoni, Silvia De Francia

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: sleep-wake rhythm; alteration; oxaliplatin; cancer; health; life quality.

Online: 11 January 2024 (11:15:09 CET)

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Preprint REVIEW | doi:10.20944/preprints202401.0770.v1

Use of Metallic Nanoparticles Synthesized from Plant Extracts in the Wound Healing – a Review

Anaís Bezerra de Gusmão, Priscilla Barbosa Sales de Albuquerque, Ana Carolina de Carvalho Correia

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: green synthesis; metallic nanoparticles; nanotechnology; natural treatment; plant extracts; wound healing

Online: 10 January 2024 (09:46:27 CET)

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Preprint ARTICLE | doi:10.20944/preprints202401.0661.v1

Target-Based 6–5 Fused Ring Heterocyclic Scaffolds Display Broad Antiparasitic Potency In Vitro

Darline Dize, Mariscal Brice Tchatat Tali, Cyrille Armel Njanpa Ngansop, Rodrigue Keumoe, Eugenie Aimée Madiesse Kemgne, Lauve Rachel Tchokouaha Yamthe, Patrick Valere Tsouh Fokou, Boniface Pone Kamdem, Katsura Hata, Fabrice Fekam Boyom

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Protozoan diseases; Drug repurposing; Cytotoxicity; Dihydrofolate reductase inhibitors; Potassium (K+) channel blocker; ADME properties

Online: 9 January 2024 (10:30:36 CET)

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Preprint REVIEW | doi:10.20944/preprints202401.0324.v1

Effects of Pharmaceutical Substances with Obesogenic Activity on Male Reproductive Health

Caio Mascarenhas, Ana C. A. Sousa, Luís Rato

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Antidiabetics; Antihypertensives; Endocrine Disruptors; Male Fertility; Obesogens, Psychotropics

Online: 4 January 2024 (09:50:49 CET)

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Preprint ARTICLE | doi:10.20944/preprints202401.0319.v1

Anti-shigellosis Activity and Mechanisms of Action of Extracts from Diospyros gilletii Stem Bark.

Audrey Carrel Nguelo Talla, Eugénie Aimée Madiesse Kemgne, Vincent Ngouana, Bijou-Lafortune Noumboue Kouamou, Listone Monelle Nzeye Ngameni, Brice Rostan Pinlap, Yanick Kevin Dongmo Melogmo, Branly-Natalien Nguena-Dongue, Boniface Pone Kamdem, Paul Keilah Lunga, Fabrice Fekam Boyom

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Diospyros gilletii; Diarrhoea; Anti-shigellosis activity; Cytotoxicity; Mechanisms of action

Online: 4 January 2024 (07:27:34 CET)

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Shigellosis is a pathological condition that affects the digestive system to possibly cause diarrhoea. Shigella species, which are responsible for this disease, are highly contagious and spread through contaminated food and water. The increasing development of resistance by Shigella species necessitate the urgent need to search for new therapies against shigellosis causing diarrhoea. The scientific validation of medicinal plants, such as Diospyros gilletii, which is used for the traditional treatment of diarrhoeal conditions is worthwhile. The present study aims to investigate the antibacterial activity of extracts from D. gilletii against selected Shigella species. Extracts from D. gilletii stem bark were prepared by maceration using various solvents. An-tibacterial activity of D. gilletii extracts was evaluated on Shigella dysenteriae, S. flexneri, S. boydii, and S. sonnei using a microdilution method, whereas cytotoxicity test was performed on Vero and Raw cells using resazurin-based colorimetric assay. Bacterial membrane permeability studies were evaluated using pro-pidium iodide (PI) and 1-N-phenylnaphthylamine (NPN) uptake assays, whereas inhibition and eradica-tion tests on bacterial biofilms were carried out by spectrophotometry. As a result, methanol, ethanol and hydroethanol extracts of D. gilletii inhibited the growth of S. boydii, S. flexneri and S. sonnei with MIC values ranging from 125 to 500 µg/mL, without toxicity to Vero and Raw cells. Time kill kinetics revealed bacteri-cidal orientation at 2MIC and 4MIC, and bacteriostatic outcome at 1/2MIC. The mechanistic basis of anti-bacterial action revealed that D. gilletii extracts inhibited and eradicated Shigella biofilms, and promoted the accumulation of NPN and PI within the inner and outer membrane of bacteria to increase membrane per-meability, thereby causing membrane damage. This novel contribution toward the antibacterial and mech-anisms of action of D. gilletii extracts against Shigella species substantiate the use of this plant in the tradi-tional treatment of infectious diarrhoea.

Preprint ARTICLE | doi:10.20944/preprints202401.0211.v1

Tobacco Smoking as an EDC in Aging

Ho-Sun Lee, Hyun-Kyung Na, Seong-Sil Chang, Soo-Young Kim, Chang Seong Kim, Yoonjeong Song, Mihi Yang

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: tobacco smoking; biological monitoring; adolescent; genetic polymorphism; addiction; mtDNA alteration; aging

Online: 4 January 2024 (03:43:27 CET)

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Preprint REVIEW | doi:10.20944/preprints202312.2247.v1

Effects of Nonsteroid Anti-inflammatory Drugs on Pregnant Women and the Fetus: A Systematic Review of Literature

Natalia Guerrero, Nicolas Ayala, Natalia Duran, Angela Mayerly Cubides Munevar, Alejandro Botero Carvajal

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Nonsteroidal anti-inflammatory drugs; pregnancy; adverse effects; analgesics; self-medication

Online: 29 December 2023 (04:01:29 CET)

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Currently, the use of medications during pregnancy in Latin America is common; studies with Latin American samples find that nearly 90% of pregnant women use some medication at least once during pregnancy. Furthermore, approximately 21% of the respondents self-medicated. Worldwide, the prevalence of this disease is 32%. The most common medications are nonsteroidal anti-inflammatory drugs and analgesics. Many of these drugs are available over the counter without a prescription. For this reason, a systematic review of the literature on the adverse effects on the woman and the fetus was performed. Objective: To determine the adverse effects associated with the use of nonsteroidal anti-inflammatory drugs (NSAIDs) on pregnant women and fetuses during pregnancy. Methods: Systematic literature review. The following search strategy was used for the databases: Science Direct, PubMed, Scopus and Web of Science, through September 3, 2022. The population of pregnant women without previous comorbidities was defined. The intervention of interest was the use of NSAIDs during pregnancy. The outcomes of interest were adverse effects for the mother or fetus (weight of the newborn, congenital malformations present in the fetus, systemic effects in the pregnant woman during her gestation period). The types of studies included clinical trials, cohort studies and case‒control studies. Results: 1 study included 2,985 pregnant women without previous comorbidities. The use of aspirin more frequently during pregnancy stands out. The adverse effects on the fetus were preterm birth <37 weeks, low birth weight < 2500 g and increased admission to the neonatal intensive care unit. No adverse effects were found for the mother. Conclusions: There are not enough data indicating that the use of NSAIDs during pregnancy is safe. Some studies show that the use of NSAIDs during pregnancy could be related to problems in the development and growth of the fetus and health effects for the mother during pregnancy, so it is advisable to use these drugs under medical prescription and for the shortest possible time. in the gestation stage.

Preprint ARTICLE | doi:10.20944/preprints202312.1970.v1

Chitosan Nanoparticle Loaded with Quercetin and Valproic Acid: A Novel Approach for Enhancing Antioxidant Activity against Oxidative Stress in SH-SY5Y Cell Line

Fadime Canbolat, Neslihan Demir, Ozlem Tonguc Yayıntas, Melek Pehlivan, Aslı Eldem, Tulay Kilicaslan Ayna, Mehmet Senel

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: antioxidant effect; chitosan; nanoparticle; oxidative stress; quercetin; valproic acid

Online: 26 December 2023 (10:12:20 CET)

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Preprint ARTICLE | doi:10.20944/preprints202312.1709.v1

Harmaline and Human ClpP Activation for Pediatric Diffuse Intrinsic Pontine Glioma (DIPG) Treatment

Morena Miciaccia, Francesca Rizzo, Antonella Centonze, Gianfranco Cavallaro, Marialessandra Contino, Domenico Armenise, Olga Maria Baldelli, Roberta Solidoro, Savina Ferorelli, Pasquale Scarcia, Gennaro Agrimi, Veronica Zingales, Elisa Cimetta, Simone Ronsisvalle, Federica Maria Sipala, Paola Loguercio Polosa, Cosimo Gianluca Fortuna, Maria Grazia Perrone, Antonio Scilimati

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Harmaline; hClpP activation; DIPG; Molecular modeling

Online: 22 December 2023 (11:39:39 CET)

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Preprint ARTICLE | doi:10.20944/preprints202312.1263.v1

A Method to Reverse Epimutations

Steven Olsen

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Homeostasis; Hormesis; Epimutations; Toxicogenomics; Quantum biology

Online: 18 December 2023 (05:56:51 CET)

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Preprint COMMUNICATION | doi:10.20944/preprints202312.0894.v1

Assessing Antibiotic Safety: A Comparative Study of Four Promising Candidates Using pKCSM Database

IVAN VITO FERRARI

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Antibiotics,pkCSM, Max.tolerated dose (human),Oral Rat Chronic Toxicity,Oral Rat Acute Toxicity ;

Online: 12 December 2023 (12:55:56 CET)

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Preprint ARTICLE | doi:10.20944/preprints202312.0748.v1

Preclinical Pharmacokinetics and Biodistribution of LR004, a Novel Antiepidermal Growth Factor Receptor Monoclonal Antibody

Ying Zheng, Guifang Dou, Shuchen Liu, Zhiyun Meng, Eric I. Tsao, Gang Yu, Xiaoxia Zhu, Ruolan Gu, Zhuona Wu, Yunbo Sun, Peng Han, Hui Gan

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: monoclonal antibody; EGFR; tumor-targeting; pharmacokinetics; radionuclide-based biodistribution; nanoSPECT/CT

Online: 12 December 2023 (05:11:26 CET)

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Preprint ARTICLE | doi:10.20944/preprints202312.0360.v1

Experimental Research on the Effect of Amiodarone on the Healing of Skin Wounds in Rats

Alexandra Grigore, Ana Vatasescu-Balcan, Smaranda Stoleru, Aurelian Zugravu, Elena Poenaru, Miruna Engi, Oana Andreia Coman, Ion Fulga

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: wound healing; potassium channels; amiodarone

Online: 6 December 2023 (10:29:59 CET)

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Preprint ARTICLE | doi:10.20944/preprints202312.0356.v1

Tr-57 Treatment of SUM159 Cells Induces Mitochondrial Dysfunction without Affecting Membrane Potential

Artem Mishukov, Ekaterina Mndlyan, Alexey V. Berezhnov, Margarita Kobyakova, Yana Lomovskaya, Ekhson Holmuhamedov, Irina Odinokova

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: TR-57; SUM159 TNBC cells; respiratory complexes: mitochondrial membrane potential; FoF1-ATPase; IF1; calcium-regulated mitochondrial ATP-Mg/Pi carrier

Online: 6 December 2023 (08:55:20 CET)

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Preprint ARTICLE | doi:10.20944/preprints202311.1938.v1

Drug-induced Anaphylaxis: National Database Analysis

Olga Butranova, Sergey Zyryanov, Anastasia Gorbacheva, Irina Asetskaya, Vitaly Polivanov

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: drug-induced allergy; anaphylaxis; antibiotics; local anesthetics; cyclooxygenase (COX)-inhibitors

Online: 30 November 2023 (04:21:45 CET)

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Preprint ARTICLE | doi:10.20944/preprints202311.1816.v1

Availability of Essential Antimicrobials in Public and Private Sector Facilities: A Cross-Sectional Survey in a District of North India

Niti Mittal, Rakesh Mittal, Sukhbir Singh, Sushila Godara

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: essential antimicrobials; essential medicine list; drug procurement; gap analysis; paediatric antibiotic formulations

Online: 29 November 2023 (11:04:15 CET)

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Preprint ARTICLE | doi:10.20944/preprints202311.1599.v1

Assessing the In Vitro Cytotoxicity, Antitumoral and Antioxidant Properties of Polyphenol‐rich Perilla leaves Extracts

Gigi Adam, Florina Daniela Cojocaru, Liliana Verestiuc, Oana Cioanca, Ingrid Andrada Vasilache, Ana-Maria Adam, Cornelia Mircea, Aurel Nechita, Valeriu Romulus Harabor, Bogdan Huzum, AnaMaria Harabor, Monica Hancianu

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Perilla frutescens; extracts; antioxidant; antitumoral; cytotoxicity

Online: 24 November 2023 (11:33:48 CET)

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Preprint ARTICLE | doi:10.20944/preprints202311.1480.v1

Sensitivity of Human Induced Pluripotent Stem Cells and Thereof Differentiated Kidney Proximal Tubular Cells towards Selected Nephrotoxins

Isaac Musong Mboni-Johnston, Nazih Mohamed Zakari Kouidrat, Cornelia Hirsch, Andreas Georg Weber, Alexander Meißner, James Adjaye, Nicole Schupp

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: hiPSC; differentiation; regeneration; cisplatin; cyclosporin A ;

Online: 23 November 2023 (06:11:48 CET)

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Preprint ARTICLE | doi:10.20944/preprints202311.1192.v1

Disposition Kinetics of Cathinone and Its Metabolites after Oral Administration in Rats

Fahad Y. Sabei, Ibrahim Khardali, Mohamed A. Al-Kasim, Emad S. Shaheen, Magbool Oraiby, Ahmad Alamir, David Banji, Saeed Alshahrani, Abdulmajeed Jali, Mohammad Attafi, Mohammed Y. Albeishy, Ibraheem Attafi

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Cathinone; Cathine; Kinetics; HPLC-IT/MS; Disposition; Organ-specific response; UPLC-QTOF/MS

Online: 20 November 2023 (07:36:02 CET)

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Cathinone is a natural stimulant found in Catha edulis and commonly used in new psychoactive substances. The objective of this study was to examine the disposition kinetics and metabolic profile of cathinone and its metabolite cathine through a single oral dose of cathinone administration in rats. Cathine and cathinone concentrations were identified and quantified using ion trap liquid chromatography (LC-IT/MS), while the metabolic profile was determined using the quadrupole time of flight UPLC-QTOF/MS method in the serum, brain, lung, liver, kidney, and heart over a period of 0, 0.5, 2.5, 6, 12, 24, 48, and 72 hours. The findings revealed a dynamic interplay between the pharmacokinetics of cathinone and its impact on organ-specific biomarkers. The distribution of cathinone and cathine was determined in serum, brain, heart, lung, kidney, and liver. The highest concentration of cathinone was found in the kidney at 1438.6 ug/L. It gradually decreased to 1.97 within 48 hours and disappeared after 72 hours. Within half an hour, cathinone levels in the lungs, liver, and heart were found to be 859, 798.9, and 385.8 ug/L, respectively. However, within 2.5 hours, these levels decreased to 608.1, 429.3, and 309.1 ug/L and kept decreasing until they became undetectable after 24 hours. The concentration of cathinone in the rat brain reduces quickly, dropping to undetectable levels within six hours, with levels decreasing from 712.7 ug/L after just 30 minutes. In the brain and serum, cathine reached its highest levels at 2.5 hours, while in other organs, it peaked at 0.5 hours. This indicates that the conversion of cathinone to cathine is slower in the brain and serum. The study found that cathinone's pharmacokinetics have a significant impact on organ-specific biomarkers. After administering the cathinone, there was a sharp change in biomarker levels, particularly in the liver and brain, during the initial hours. It is essential to investigate the correlation between the changes in biomarkers found in the brain and the levels of cathinone and cathine. The results have significant implications for drug development, pharmacovigilance, and clinical practices involving cathinone. In conclusion, this comprehensive analysis of cathinone's impact on organ-specific biomarkers provides a basis for informed decision-making in medical practices and further research into the cathinone's pharmacological properties.

Preprint ARTICLE | doi:10.20944/preprints202311.0653.v1

Exploring Novel Variants of Cytochrome P450 Reductase Gene (POR) from the Genome Aggregation Database by Integrating Bioinformatic Tools and Functional Assays

Maria Natalia Rojas Velazquez, Søren Therkelsen, Amit V. Pandey

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Cytochrome P450 oxidoreductase; POR; gnomAD, CAH; drug metabolism, steroid hormones; SNV; bioinformatics

Online: 9 November 2023 (15:09:12 CET)

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Preprint ARTICLE | doi:10.20944/preprints202311.0602.v1

First Report and Pathogenicity of Vibrio campbellii (VC_AHPND) Isolated in South Korea

Hee-Jae Choi, Da-Yeon Choi, Ji-Hoon Lee, Jun-Hwan Kim, Yue Jai Kang

Subject: Medicine And Pharmacology, Pharmacology And Toxicology Keywords: Acute hepatopancreatic necrosis disease; Vibrio parahaemolyticus; Vibrio campbellii; Litopenaeus vannamei

Online: 9 November 2023 (07:29:12 CET)

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Medicine and Pharmacology