Triterpenoids from the leaves of Dendropanax morbifera Léveille and its cytotoxic activity toward breast MCF-7 and lung A549 cancer cells

Abstract

Dendropanax morbifera Léveille (Araliaceae) is an endemic species growing in the south-western part of South Korea and has been used in folk medicine and health functional food. Several studies have indicated that extract of D. morbifera (DP) has cytotoxic activities on a number of human cancers, such as, breast cancer, lung cancer, hepatoma, and chorioepithelioma. Recently, polyacetylene and triterpene compounds have been isolated from the DP and showed to have anti-complement activity. β-Amyrin, α-amyrin, dendropanoxide, and β-sitosterol are isolated from DP. However, its biological activities in cancer have not yet been clearly elucidated. In this study, we evaluated the anti-cancer activity of isolated triterpenoids from the DP leaves by measuring the levels of cytotoxicity against MCF-7 human breast cancer and A549 human lung cancer cells. Six triterpenoids were isolated from the n-hexane fraction of DP leaves along with the known compounds. β-amyrin (1), α-amyrin (2), olean-12-en-3,24 β-diol (3), dendropanoxide (4), β-sitosterol (5), and stigmasterol (6). Compound 3 and 6 were isolated from DP for the first time. Cytotoxic activities of six compounds were evaluated against two human cancer cell lines by using the MTT in vitro assay. Among them, five compounds (1, 2, 4, 5, and 6) showed moderate cytotoxic activities toward the tested cell lines, and were safe to normal cells. Western blot analysis showed a decreased expression of anti-apoptotic protein Bcl-2 and increased levels of pro-apoptotic protein Bax in MCF-7 and A549 cells treated by β-amyrin and α-amyrin. Flow cytometry analysis confirmed that five compounds (1, 2, 4, 5, and 6) treatment increased populations of sub-G1 (apoptosis) phase. The results of the present study revealed that triterpenoids from DP have the potential for further development as anticancer agents.