• Title/Summary/Keyword: drug-metabolizing enzyme inhibitors

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Isolation of Hepatic Drug Metabolism Inhibitors from the Seeds of Myristica fragrans

  • Shin, Kuk-Hyun;Kim, Ok-Nam;Woo, Won-Sick
    • Archives of Pharmacal Research
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    • v.11 no.3
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    • pp.240-243
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    • 1988
  • The hexane extract from Nutmeg, the seed of Myristica fragrans significantly inhibited hepatic drug-metabolizing enzyme activity. Through systematic fractionation by $SiO_2$ column and vacuum liquid chromatography monitoring by bioassay, three components, myristicin, (I), licarin-B (II) and dehydrodiisoeugenol (III) were isolated as active principles. Compounds II and III, with a single treatment (200mg/kg, i.p.) showed not only a significant prolongation of hexobarbital-induced sleeping time but also a significant inhibition of aminopyrine N-demethylase and hexobarbital hydroxylase activities in mice. Compounds I and II provoked a sleep episode at a subhypnotic dose of HB, suggesting that they possess CNS-depressant properties.

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Isolation of Hepatic Drug Metabolism Inhibitors from the Rhizomes of Curcuma zedoaria

  • Shin, Kuk-Hyun;Kim, Ok-Nam;Woo, Won-Sick
    • Archives of Pharmacal Research
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    • v.12 no.3
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    • pp.196-200
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    • 1989
  • The methanolic extract of the Rhizome of Curcuma zedoaria exhibited a significant prolongation of hexobarbital (HB)-induced hypnosis. Through liquid chromatography of an ether soluble fraction. monitoring by bioassay, three sequiterpenes, germacrone (A), curzerenone (B) and germacrone epoxide (C) were isolated as active consituents. A single treatment (100-200 mg/kg, i.p.) of each compound showed not only a significant prolongation of HB-induced sleeping time but also a significant inhibition of aminopyrine N-demethylase activity in mice, and further exhibited a typical type I binding spectra with oxidized rat hepatic cytochrome P-450 induced by phenobarbital. All of the compounds provoked a sleep episode at a subhypnotic dose of HB, implying that they possess CNS depressant properties.

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