Your browser doesn't support javascript.
loading
Hepatotoxicity of Eight Components of Radix Polygonum multiflorum Thunb. in Rat Liver Microsome System in Vitro / 中国药学杂志
Chinese Pharmaceutical Journal ; (24): 589-593, 2018.
Article in Chinese | WPRIM | ID: wpr-858360
ABSTRACT

OBJECTIVE:

To investigate the hepatic toxicity of 8 monomers in Polygonum multiflorum using a combination of UDPglucuronic acid transferase 1A1(UGT1A1 enzyme).

METHODS:

Bilirubin was used as the substrate for UGT1A1. Incubation method in RLM in vitro was adopted to test the apparent inhibition constants(Ki) of different components. Furthermore the structure-activity relationship between the 8 components and UGT1A1 was analyzed.

RESULTS:

The inhibition effects on UGT1A1 enzyme of the 8 components were in the following sequence emodin-8-O-glc > emodin > citreorosein > (+) -catechin > gallic acid > physcion > rhein > emodin-6-O-glc. Moreover, there was a structure-activity relationship, and it was presumed that the 6-position hydroxyl group is an active and necessary group.

CONCLUSION:

The established method in vitro is stable and feasible. Experimental results shows that the enzyme inhibition has structural selectivity, which provides an experimental basis for predicting the enzyme inhibition activity of the analogues of components of Polygonum multiflorum.

Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Chinese Pharmaceutical Journal Year: 2018 Type: Article

Similar

MEDLINE

...
LILACS

LIS

Full text: Available Index: WPRIM (Western Pacific) Language: Chinese Journal: Chinese Pharmaceutical Journal Year: 2018 Type: Article