Synthesis and structure-activity relationship of cycloberberine as anti-cancer agent / 药学学报
Acta Pharmaceutica Sinica
; (12): 1800-1806, 2013.
Article
in Chinese
| WPRIM (Western Pacific)
| ID: wpr-298008
Responsible library:
WPRO
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.
Full text:
Available
Database:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Structure-Activity Relationship
/
Berberine
/
Molecular Structure
/
Doxorubicin
/
Cell Cycle
/
Chemistry
/
DNA Topoisomerases, Type I
/
Drug Resistance, Neoplasm
/
Cell Proliferation
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2013
Document type:
Article