Influence of isoliensinine on activity of CYP3A in rats.
- Author:
Li NAN
1
;
Gui-da XUAN
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Cytochrome P-450 CYP3A; metabolism; In Vitro Techniques; Isoquinolines; pharmacology; Male; Microsomes, Liver; drug effects; enzymology; Rats; Rats, Sprague-Dawley; Testosterone; pharmacology
- From: Journal of Zhejiang University. Medical sciences 2012;41(2):178-182
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo investigate the influence of isoliensinine (IL) on CYP3A enzyme activity.
METHODSA mixture metabolic system of liver microsome enzymes in vitro was developed. A HPLC method to test the metabolic activity of CYP3A was established with testosterone as a probe. The activities of CYP3A enzymes were measured with different IL concentrations and incubation time with testosterone.
RESULTSIn mixture metabolic system of liver microsome enzymes, the best incubation concentration of testosterone was 200 μmol/L, the best incubation time was 210 min, in this condition the IC₅₀ of IL for CYP3A inhibition was >1 000 μmol/L.
CONCLUSIONNo significant interaction between IL and CYP3A is detected, which indicates that IL might be used with CYP 3A enzyme substrates.
