Synthesis and Physiological Activity of Novel Berberine Derivatives / 中国实验方剂学杂志
Chinese Journal of Experimental Traditional Medical Formulae
;
(24): 156-164, 2019.
Article
in Chinese
| WPRIM
| ID: wpr-801779
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Chinese Journal of Experimental Traditional Medical Formulae
Year:
2019
Type:
Article
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