Apoptosis-Inducing Activity of New Pyrazole Emodin Derivatives in Human Hepatocellular Carcinoma HepG2 Cells

A series of new pyrazole derivatives from emodin synthesized in our lab have been shown to have much stronger cytotoxicity than emodin against various tumor cell lines.1) This study was to examine the apoptosis-inducing activity of these new emodin derivatives in human hepatocellular carcinoma HepG2...

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Bibliographic Details
Published in:Biological & Pharmaceutical Bulletin 2007, Vol.30(6), pp.1113-1116
Main Authors: Wang, Xiao-Dong, Gu, Lian-Quan, Wu, Jian-Yong
Format: Article
Language:English
Subjects:
apoptosis
Apoptosis - drug effects
Carcinoma, Hepatocellular - drug therapy
Carcinoma, Hepatocellular - pathology
Caspase 3 - metabolism
caspase-3
Cell Line, Tumor
Cell Nucleus - drug effects
Cell Proliferation - drug effects
Cell Survival - drug effects
DNA Fragmentation - drug effects
Dose-Response Relationship, Drug
Emodin - chemistry
Emodin - metabolism
Emodin - toxicity
emodin derivative
Enzyme Activation - drug effects
Formazans - metabolism
HepG2 cell
Humans
Liver Neoplasms - drug therapy
Liver Neoplasms - pathology
Molecular Structure
Poly(ADP-ribose) Polymerases - metabolism
Tetrazolium Salts - metabolism
Time Factors
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Summary:A series of new pyrazole derivatives from emodin synthesized in our lab have been shown to have much stronger cytotoxicity than emodin against various tumor cell lines.1) This study was to examine the apoptosis-inducing activity of these new emodin derivatives in human hepatocellular carcinoma HepG2 cell culture for a better understanding of their cytotoxic effects on the cancer cells. Several major events in the induction of cell apoptosis, nuclear chromatin condensation, DNA fragmentation, caspase-3 activation and poly ADP-ribose polymerase (PARP) cleavage were detected in the cells after treatment with the compounds at various concentrations. Of the seven emodin derivatives tested at a dose of 10 μM and within a treatment period of 24 h, only compounds 1 and 3 effectively induced all these apoptotic events in the cancer cells. The apoptosis-inducing activity of the compounds showed a positive correlation to their cytotoxic activity, suggesting a close connection between the growth inhibition and apoptosis induction of the cancer cells by these pyrazole emodin derivatives.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.30.1113