A phytochemical survey aiming to acquire pharmacologically active substances has resulted in the isolation of nine new clerodane diterpenoids, named graveospenes A-I (1-9), from the leaves of Casearia graveolens. Spectroscopic methods were employed to establish the structures with their absolute configurations being confirmed by ECD data analysis. A biological evaluation was performed, and compound 1 was found to be cytotoxic to both human lung cancer cells (A549) and human hepatocellular carcinoma cells (HepG2). A mechanism-of-action study on 1 revealed this compound to induce apoptosis of A549 cells and impede them at the G0/G1 stage.
Bibliographical noteFunding Information:
This research was supported financially by the National Key Research and Development Program of China (No. 2018YFA0507204), the National Natural Science Foundation of China (Nos. U1703107 and U1801288), the Natural Science Foundation of Tianjin (No. 19JCYBJC28100), Hundred Young Academic Leaders Program of Nankai University, State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University, No. CMEMR2019-B01), and the open project of Key Laboratory of Xinjiang Uygur Autonomous Region (Nos. 2015KL030 and 2017D04019).
© 2020 American Chemical Society and American Society of Pharmacognosy.
ASJC Scopus subject areas
- Analytical Chemistry
- Molecular Medicine
- Pharmaceutical Science
- Drug Discovery
- Complementary and alternative medicine
- Organic Chemistry