Synthesis and structure-activity relationship of cycloberberine as anti-cancer agent.
- Author:
Chong-Wen BI
;
Cai-Xia ZHANG
;
Yang-Biao LI
;
Wu-Li ZHAO
;
Rong-Guang SHAO
;
Lin MEI
;
Dan-Qing SONG
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Berberine;
analogs & derivatives;
chemical synthesis;
chemistry;
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
- From:
Acta Pharmaceutica Sinica
2013;48(12):1800-1806
- CountryChina
- Language:Chinese
-
Abstract:
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.
