3,3',4,5,5'-Pentahydroxy-trans-stilbene, a resveratrol derivative, induces apoptosis in colorectal carcinoma cells via oxidative stress.
Resveratrol exhibits anti-tumor properties against different types of cancer. In this study, several polyhydroxylated resveratrol derivatives were prepared with the aim of discovering new leading compounds with clinical potential for human colon cancer chemotherapy. Among these compounds, 3,3',4,5,5'-pentahydroxy-trans-stilbene (PHS) displayed the most potent cytotoxicity and triggered apoptosis in HT-29 cells as evidenced by increased poly(ADP-ribose) polymerase (PARP) cleavage, elevated levels of cytoplasmic nucleosomes and DNA fragmentation. Further mechanistic analysis revealed that PHS-induced apoptosis was caspase-dependent and mediated by its pro-oxidative action through up-regulation of reactive oxidative species generation and depletion of intracellular glutathione.
Li
Haitao
H
School of Biological Sciences, The University of Hong Kong, Hong Kong, China.
Wu
William Ka Kei
WK
Zheng
Zongping
Z
Che
Chun Tao
CT
Li
Zhi Jie
ZJ
Xu
Dan Dan
DD
Wong
Clover Ching Man
CC
Ye
Cai Guo
CG
Sung
Joseph Jao Yiu
JJ
Cho
Chi Hin
CH
Wang
Mingfu
M
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D015153:Blotting, Western; D015179:Colorectal Neoplasms / Q000378:metabolism* / Q000473:pathology*; D003593:Cytoplasm / Q000378:metabolism; D053938:DNA Fragmentation / Q000187:drug effects; D004797:Enzyme-Linked Immunosorbent Assay; D005978:Glutathione / Q000378:metabolism; D019073:HT29 Cells; D006801:Humans; D009707:Nucleosomes / Q000378:metabolism; D018384:Oxidative Stress / Q000187:drug effects*; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism; D000077185:Resveratrol; D013267:Stilbenes / Q000737:chemistry* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured; D015854:Up-Regulation / Q000187:drug effects
C473468:3,5,3',4',5'-pentahydroxy-stilbene; D000970:Antineoplastic Agents; D009707:Nucleosomes; D013267:Stilbenes; D011065:Poly(ADP-ribose) Polymerases; D005978:Glutathione; D000077185:Resveratrol