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Article

Cytotoxic and Apoptosis-Inducing Activity of Triterpene Glycosides from Holothuria scabra and Cucumaria frondosa against HepG2 Cells

1
Key Laboratory of Animal Virology of Ministry of Agriculture, College of Animal Sciences, Zhejiang University, Hangzhou 310058, China
2
School of Medicine, Tongji University, Shanghai 200092, China
3
Research Center for Marine Drugs, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Mar. Drugs 2014, 12(8), 4274-4290; https://doi.org/10.3390/md12084274
Received: 9 February 2014 / Revised: 4 April 2014 / Accepted: 8 April 2014 / Published: 24 July 2014
(This article belongs to the Collection Bioactive Compounds from Marine Invertebrates)
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. View Full-Text
Keywords: Holothuria scabra; Cucumaria frondosa; triterpene glycosides; echinoside A; cytotoxicity; structure-activity relationship; apoptosis; mechanism Holothuria scabra; Cucumaria frondosa; triterpene glycosides; echinoside A; cytotoxicity; structure-activity relationship; apoptosis; mechanism
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MDPI and ACS Style

Wang, J.; Han, H.; Chen, X.; Yi, Y.; Sun, H. Cytotoxic and Apoptosis-Inducing Activity of Triterpene Glycosides from Holothuria scabra and Cucumaria frondosa against HepG2 Cells. Mar. Drugs 2014, 12, 4274-4290. https://doi.org/10.3390/md12084274

AMA Style

Wang J, Han H, Chen X, Yi Y, Sun H. Cytotoxic and Apoptosis-Inducing Activity of Triterpene Glycosides from Holothuria scabra and Cucumaria frondosa against HepG2 Cells. Marine Drugs. 2014; 12(8):4274-4290. https://doi.org/10.3390/md12084274

Chicago/Turabian Style

Wang, Juanjuan, Hua Han, Xiangfeng Chen, Yanghua Yi, and Hongxiang Sun. 2014. "Cytotoxic and Apoptosis-Inducing Activity of Triterpene Glycosides from Holothuria scabra and Cucumaria frondosa against HepG2 Cells" Marine Drugs 12, no. 8: 4274-4290. https://doi.org/10.3390/md12084274

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