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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,*
Received: 9 February 2014; in revised form: 4 April 2014 / Accepted: 8 April 2014 / Published: 24 July 2014
(This article belongs to the Special Issue 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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.

Chicago/Turabian Style

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



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