Synthesis and structure-activity relationship of cycloberberine as anti-cancer agent

A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The p...

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Bibliographic Details
Published inYao hsüeh hsüeh pao Vol. 48; no. 12; p. 1800
Main Authors Bi, Chong-Wen, Zhang, Cai-Xia, Li, Yang-Biao, Zhao, Wu-Li, Shao, Rong-Guang, Mei, Lin, Song, Dan-Qing
Format Journal Article
LanguageChinese
Published China 01.12.2013
Subjects
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Berberine - analogs & derivatives
Berberine - chemical synthesis
Berberine - chemistry
Berberine - pharmacology
Cell Cycle - drug effects
Cell Proliferation - drug effects
DNA Topoisomerases, Type I - metabolism
Doxorubicin - pharmacology
Drug Resistance, Neoplasm
Hep G2 Cells
Humans
MCF-7 Cells
Molecular Structure
Structure-Activity Relationship
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Summary:A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The primary mechanism showed that cell cycle was blocked at G2/M phase of HepG2 cells treated with 6g using flow cytometry assay. It significantly inhibited the activity of DNA Top I at the concentration of 0.1 mg mL-1. Our results provided a basis for the development of this kind of compounds as novel anti-cancer agents.
ISSN:0513-4870