title: Novel dammarane-type triterpenes isolated from hydrolyzate of total Gynostemma pentaphyllum saponins.
abstract: In this study, five novel triterpenes were isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum and identified as gypensapogenin H (1), gypensapogenin I (2), gypensapogenin L (3), gypensapogenin J (4) and gypensapogenin K (5), three of which (1-3) possess unprecedented ring A. All the isolated compounds were evaluated for cytotoxic activities in five cell lines and all the tested compounds showed significant anti-cancer activities against a series of human cancer cell lines, while having much weaker effect on the growth of normal cell. Among them, compound 1 showed strong inhibition toward MCF-7 human breast cancer cells (IC50 values 6.85 μM). Further mechanistic study demonstrated that compound 1 significantly induced MCF-7 cell apoptosis. Our results indicated that compound 1 may be a promising lead agent for further study.
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
authors.forename: Xiao-Shu
authors.initials: XS
authors.lastname: Zhang
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
authors.forename: Jia-Qing
authors.initials: JQ
authors.lastname: Cao
authors.affiliation: Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
authors.forename: Chen
authors.initials: C
authors.lastname: Zhao
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
authors.forename: Xu-de
authors.initials: XD
authors.lastname: Wang
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
authors.forename: Xiao-jun
authors.initials: XJ
authors.lastname: Wu
authors.affiliation: School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China. Electronic address: zyq4885@126.com.
authors.forename: Yu-Qing
authors.initials: YQ
authors.lastname: Zhao
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D029774:Gynostemma / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D061986:MCF-7 Cells; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D012503:Saponins / Q000737:chemistry*; D014315:Triterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D000097669:Dammaranes
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D012503:Saponins; D014315:Triterpenes; D000097669:Dammaranes
keywords: Apoptosis; Cytotoxicity; Gynostemma pentaphyllum; Novel triterpenes