PreprintArticleVersion 1Preserved in Portico This version is not peer-reviewed
Unraveling the Influence of Six Lupane-, Oleanane-, and Ursane- type Pentacyclic Triterpenes' Structure-Activity Relationship on Non-Small Lung Adenocarcinoma Cells
Version 1
: Received: 3 January 2024 / Approved: 4 January 2024 / Online: 4 January 2024 (07:21:16 CET)
How to cite:
Torres-Sanchez, A.; Torres, G.; Estrada, S.; Pérez, D.; Garcia, C.; Milian, M.; Velazquez, E.; Molina, V.; Delgado, Y. Unraveling the Influence of Six Lupane-, Oleanane-, and Ursane- type Pentacyclic Triterpenes' Structure-Activity Relationship on Non-Small Lung Adenocarcinoma Cells. Preprints2024, 2024010331. https://doi.org/10.20944/preprints202401.0331.v1
Torres-Sanchez, A.; Torres, G.; Estrada, S.; Pérez, D.; Garcia, C.; Milian, M.; Velazquez, E.; Molina, V.; Delgado, Y. Unraveling the Influence of Six Lupane-, Oleanane-, and Ursane- type Pentacyclic Triterpenes' Structure-Activity Relationship on Non-Small Lung Adenocarcinoma Cells. Preprints 2024, 2024010331. https://doi.org/10.20944/preprints202401.0331.v1
Torres-Sanchez, A.; Torres, G.; Estrada, S.; Pérez, D.; Garcia, C.; Milian, M.; Velazquez, E.; Molina, V.; Delgado, Y. Unraveling the Influence of Six Lupane-, Oleanane-, and Ursane- type Pentacyclic Triterpenes' Structure-Activity Relationship on Non-Small Lung Adenocarcinoma Cells. Preprints2024, 2024010331. https://doi.org/10.20944/preprints202401.0331.v1
APA Style
Torres-Sanchez, A., Torres, G., Estrada, S., Pérez, D., Garcia, C., Milian, M., Velazquez, E., Molina, V., & Delgado, Y. (2024). Unraveling the Influence of Six Lupane-, Oleanane-, and Ursane- type Pentacyclic Triterpenes' Structure-Activity Relationship on Non-Small Lung Adenocarcinoma Cells. Preprints. https://doi.org/10.20944/preprints202401.0331.v1
Chicago/Turabian Style
Torres-Sanchez, A., Valerie Molina and Yamixa Delgado. 2024 "Unraveling the Influence of Six Lupane-, Oleanane-, and Ursane- type Pentacyclic Triterpenes' Structure-Activity Relationship on Non-Small Lung Adenocarcinoma Cells" Preprints. https://doi.org/10.20944/preprints202401.0331.v1
Abstract
In recent times, a great interest has been motivated in plant-derived compounds known as phytochemicals. The pentacyclic oleanane-, ursane-, lupane-type triterpenes are phytochemicals that exert significant activities against diseases like cancer. Lung cancer is the leading cause of cancer-related death worldwide. Although chemotherapy is the treatment of choice for lung cancer, its effectiveness is hampered by the dose‐limiting toxic effects and chemoresistance. Herein, we investigated the structure-activity relationship of six pentacyclic triterpenes: oleanolic acid (OleA), ursolic acid (UrA), asiatic acid (AsA), betulinic acid (BeA), betulin (Betu), lupeol (Lupe), on NSCLC A549 cells. From our studies, we confirmed that all these triterpenes showed cytotoxicity in the mid µM range, where BeA showed the strongest effect. Then, we determined that most of these triterpenes induced S-phase and G2/M phase cycle arrest, reactive oxygen species, mitochondrial depolarization, and caspase 3 activation. For chemoresistance markers, we elucidated that most triterpenes downregulated STAT3 and PDL1 genes. In contrast, ursane-type UrA and AsA also induced DNA damage, reactive nitrogen species and autophagy. These results showed that even slight structural changes in these triterpenes can influence the cellular response and mechanistic pathways. This study opens promising perspectives for further research on the pharmaceutical role of phytochemical triterpenoids.
Biology and Life Sciences, Biochemistry and Molecular Biology
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
