title: Cytotoxic and apoptosis-inducing activity of triterpene glycosides from Holothuria scabra and Cucumaria frondosa against HepG2 cells.
abstract: The cytotoxic effects of thirteen triterpene glycosides from Holothuria scabra Jaeger and Cucumaria frondosa Gunnerus (Holothuroidea) against four human cell lines were detected and their cytotoxicity-structure relationships were established. The apoptosis-inducing activity of a more potent glycoside echinoside A (1) in HepG2 cells was further investigated by determining its effect on the morphology, mitochondrial transmembrane potential (Δψm) and mRNA expression levels of the apoptosis-related genes. The results showed that the number of glycosyl residues in sugar chains and the side chain of aglycone could affect their cytotoxicity towards tumor cells and selective cytotoxicity. 1 significantly inhibited cell viability and induced apoptosis in HepG2 cells. 1 also markedly decreased the Δψm and Bcl-2/Bax mRNA express ratio, and up-regulated the mRNA expression levels of Caspase-3, Caspase-8 and Caspase-9 in HepG2 cells. Therefore, 1 induced apoptosis in HepG2 cells through both intrinsic and extrinsic pathway. These findings could potentially promote the usage of these glycosides as leading compounds for developing new antitumor drugs.
authors: Key Laboratory of Animal Virology of Ministry of Agriculture, College of Animal Sciences, Zhejiang University, Hangzhou 310058, China. wjuanjuanhaohao@126.com.
authors: Juanjuan
authors: J
authors: Wang
authors: School of Medicine, Tongji University, Shanghai 200092, China. hanhua@tongji.edu.cn.
authors: Hua
authors: H
authors: Han
authors: Key Laboratory of Animal Virology of Ministry of Agriculture, College of Animal Sciences, Zhejiang University, Hangzhou 310058, China. chenxiangfneg@163.com.
authors: Xiangfeng
authors: X
authors: Chen
authors: Research Center for Marine Drugs, School of Pharmacy, Second Military Medical University, Shanghai 200433, China. yiyanghua@hotmail.com.
authors: Yanghua
authors: Y
authors: Yi
authors: Key Laboratory of Animal Virology of Ministry of Agriculture, College of Animal Sciences, Zhejiang University, Hangzhou 310058, China. sunhx@zju.edu.cn.
authors: Hongxiang
authors: H
authors: Sun
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects*; D020169:Caspases / Q000235:genetics; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D048016:Cucumaria / Q000737:chemistry*; D006027:Glycosides / Q000494:pharmacology*; D006367:HeLa Cells; D056945:Hep G2 Cells; D047332:Holothuria / Q000737:chemistry*; D006801:Humans; D020014:K562 Cells; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D012333:RNA, Messenger / Q000235:genetics; D012616:Sea Cucumbers / Q000737:chemistry; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000494:pharmacology*; D015854:Up-Regulation / Q000187:drug effects; D051028:bcl-2-Associated X Protein / Q000235:genetics
chemical_list: D000970:Antineoplastic Agents; D006027:Glycosides; D012333:RNA, Messenger; D014315:Triterpenes; D051028:bcl-2-Associated X Protein; D020169:Caspases