Piperine이 간 microsome의 mixed function oxidase(MFO)에 미치는 효과를 검토하였다. Piperine을 100 mg/kg씩 7일간 마우스에 경구투여 한 결과 hexobarbital수면시간을 대조군에 비하여 72% 단축시켰으며 aminopyrine N-demethylase활성 (112.7%), hexobarbital hydroxylase활성 (78.5%) 및 cytochrome p-450(154.2%) 함량을 현저히 증가시켰다. Piperine은 약효를 나타내는 량을 일회 복강내에 주사하였을 때에는 간 효소활성에 변동을 초래하지 않았으나 대량(100 mg/kg, i.p.) 부여하면 aminopyrine 및 hexobaribtal 대사의 억제를 일으켰다. Piperine은 rat의 간 microsome과 작용하여 type I difference spectrum(max. 385 nm, min. 422 nm)을 나타내었고 aminopyrine N-demethylase에 대 하여 상경적 저해(Ki= 0.128 mM), hexobarbital hydroxylase에 대하여 혼합형 저해(Ki= 0.098 mM)를 나타내었으나 aniline hydroxylase 활성에는 아무런 영향을 주지 않았다.
The effect of piperine on hepatic microsomal mixed function oxidases (MFO) was investigated. Piperine, on repeated daily administrations (100mg/kg, p.o. for 7 days) to mice, shortened markedly the duration of hexobarbital induced narcosis (72%) and increased aminopyrine N-demethylase (112.7%) and hexobarbital hydroxylase (78.5%) as well as in the level of cytochrome p-450 (154.2%). At pharmacologically effective doses, it did not affect MFO in vivo, whereas, it produced an inhibition of both aminopyrine and hexobarbital metabolism at a high dose (100 mg/kg, i.p.). Kinetic studies on rat hepatic microsomal enzymes, in vitro, have shown that piperine gave a type I difference spectrum (max. 385nm, min. 422 nm) and appeared to be a competitive inhibitor of aminopyrine N-demethylase and mixed type inhibitor of hexobarbital hydroxylase, the apparent inhibition constants (Ki) of which being 0.128 mM and 0.098 mM, respectively.
