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Mar. Drugs 2014, 12(8), 4274-4290; doi:10.3390/md12084274
Article

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

1,†
,
2,†
,
1
,
3
 and
1,*
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 These authors contributed equally to this work.
* Author to whom correspondence should be addressed.
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)
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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.
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
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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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.

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