Caffeic acid phenethyl ester의 cytochrome P450 저해 활성 평가

• 영문명: In vitro assessment of cytochrome P450 inhibition by caffeic acid phenethyl ester
• 발행기관: 대한약학회
• 저자명: 류창선(Chang Seon Ryu) 박지은(Ji-Eun Park) 김상겸(Sang Kyum Kim)
• 간행물 정보: 『약학회지』제62권 제2호(2018년), 77~82쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2018.03.30

영문 초록

Caffeic acid phenethyl ester (CAPE) is one of the major active components of propolis showing inhibitory activ-ity against cytochrome P450 (CYP). The purpose of this study was to determine CYP inhibitory potential and metabolic sta-bility of CAPE using human liver microsomes (HLM) for characterization of its metabolic properties. Among CYP isoforms including CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4, CAPE exhibited strong inhibitory potential against CYP1A2 and 2C9, moderate against CYP2E1, 2B6, 2C8, 2C19 and 3A4, and weak against CYP 2D6 and 2A6, based on the IC 50 values. The inhibition of CYP1A2 but not CYP2C9 was increased by preincubation with CAPE and NADPH, suggesting that the CAPE-induced CYP1A2 inhibition may be metabolism-dependent. In metabolic stability study using HLM, CAPE was rapidly hydrolyzed to caffeic acid in a NADPH-independent manner. Caffeic acid exhibited week CYP inhibitory activity, relative to CAPE. These results raise the possibility that CAPE plays a role in propolis-mediated CYP inhibition.

목차

재료 및 실험 방법 (Experimental Methods)

결과 및 고찰 (Results and Discussion)

결 론 (Conclusion)

키워드

cytochrome p450 drug-drug interaction caffeic acid phenethyl ester propolis