Synthesis and Physiological Activity of Novel Berberine Derivatives
10.13422/j.cnki.syfjx.20192115
- VernacularTitle: 一类新型小檗碱衍生物的合成与生理活性
- Author:
Xiao-fei JIANG
1
;
Jiu-hui LIU
1
;
Hu LI
1
;
Wei ZHANG
2
;
Heng LUO
3
Author Information
1. School of Chemistry and Materials Science, Guizhou Education University, Guiyang 551018, China
2. School of Geography and Tourism, Guizhou Education University, Guiyang 551018, China
3. Key Laboratory of Chemistry for Natural Products of Guizhou Guiyang Province and Chinese Academy of Sciences, Guiyang 550014, China
- Publication Type:Research Article
- Keywords:
berberine;
synthesis;
derivatives;
anti-tumour;
acetylcholinesterase
- From:
Chinese Journal of Experimental Traditional Medical Formulae
2019;25(23):156-164
- CountryChina
- Language:Chinese
-
Abstract:
Objective: TO synthesize novel berberine derivatives with a variety of physiological activities,and study their antitumor activity and acetylcholinesterase inhibitory activity. Method: Berberines with a variety of physiological activities were pieced together isohydroxamic acid,o-phenylenediamine,and sulfhydryl pharmacophore with effects in inhibiting histones and removing acetylases. Totally 7 novel berberine derivatives were obtained by means of organic synthesis. The structures of these derivatives were characterized and confirmed by 1H-NMR,13 C-NMR and MS spectral data.Thiazolyl blue tetrazolium bromide(MTT) method was used in the determination of the cytotoxic activity of HCT116,HepG2,HeLa and CCRF-CEM human cancer cell lines in vitro. Ellman method was used to reveal the inhibitory activities of acetylcholinesterase and butyrylcholinesterase. Result: The results showed that the berberine derivatives containing methyl ketone had good antitumor and acetylcholinesterase inhibitory activities. The results demonstrated that compound 5b had the highest anti-proliferative activity against CCRF-CEM cell line and the acetylcholinesterase inhibitory activities, with IC50=1.48 μmol · L-1 and IC50=0.38 μmol · L-1,respectivly. Conclusion: This paper provides a reference for the synthesis and biological evaluation of this kind of alkaloid derivatives. Compound 5b is a promising candidate drug and worth further study.
