학술논문

Effects of the standard extract of Centella asiatica (ECa233) on rat hepatic cytochrome P450.
Document Type
Article
Source
Thai Journal of Pharmaceutical Sciences. Apr2009, Vol. 33 Issue 2/3, p91-100. 10p. 1 Chart, 4 Graphs.
Subject
*CYTOCHROMES
*UMBELLIFERAE
*METABOLIC disorders
*ETIOLOGY of diseases
*LABORATORY rats
*MICROSOMES
*ENZYME activation
*DRUG interactions
*FERTILIZATION in vitro
Language
ISSN
0125-4685
Abstract
Centella asiatica (L.) Urban (Umbelliferae) has been used traditionally in various diseases. The aim of this study was to examine subchronic effects of the standard extract of C. asiatica (ECa233) on hepatic xenobiotic/drug metabolizing enzymes, particularly cytochrome P450 (CYP) such as CYP1A1, CYP1A2, CYP2B1/2B2, CYP2E1 and CYP3A in rats. Both male and female Wistar rats were randomly divided into 4 groups of 10 rats each. Rats in the treatment groups were given orally with ECa233 at 10, 100 and 1,000 mg/kg/day whereas rats in the control group were given distilled water for 90 consecutive days. At the end of treatment, rats were sacrificed and liver microsomes were prepared for enzyme activity assay. The results showed that ECa233 did not affect total CYP content as well as the activities of CYP1A1, CYP1A2, CYP2B1/2B2, CYP2E1 and CYP3A in both male and female rats. Inhibitory effect of ECa233 was examined in vitro, using rat liver microsomes. ECa233 caused a concentration-dependent decrease of the activity of CYP2B1/2B2 (BROD: IC50 = 523 mg/ml, PROD: IC50 = 563 mg/ml) and very slightly effect on CYP1A2 (MROD: IC50 > 1,000 mg/ml). ECa233 had no inhibitory effect on the activities of CYP1A1, CYP2E1 and CYP 3A at concentrations up to 2,000 mg/ml. The inhibitory effect of ECa233 on CYP2B1/2B2 indicated a possibly beneficial effect of the compound regarding the protection of chemical-induced carcinogenesis but the concern regarding the possibilities of drug-drug interaction with the medicines metabolized by these CYPs. Effects of ECa233 on the activities of other CYP isoforms and human liver CYP should be further investigated. [ABSTRACT FROM AUTHOR]