Journal
MARINE DRUGS
Volume 12, Issue 8, Pages 4274-4290Publisher
MDPI
DOI: 10.3390/md12084274
Keywords
Holothuria scabra; Cucumaria frondosa; triterpene glycosides; echinoside A; cytotoxicity; structure-activity relationship; apoptosis; mechanism
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Funding
- Key Scientific and Technological Innovation Team of Zhejiang Province [2010R50031-13]
- Chinese Universities Scientific Fund [2010KLEP007]
- Fundamental Research Funds for the Central Universities [2012FZA6017]
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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 (Delta psi(m)) 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 Delta psi(m) 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.
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