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  • 标题:In Vitro Inhibitory Effects of Cannabinoids on Progesterone 17α-Hydroxylase Activity in Rat Testis Microsomes
  • 作者:Tatsuya Funahashi ; Hideharu Ikeuchi ; Satoshi Yamaori
  • 期刊名称:Journal of Health Science
  • 印刷版ISSN:1344-9702
  • 电子版ISSN:1347-5207
  • 出版年度:2005
  • 卷号:51
  • 期号:3
  • 页码:369-375
  • DOI:10.1248/jhs.51.369
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The inhibitory effects of three major cannabinoids [ Δ 9-tetrahydrocannabinol (THC), cannabidiol (CBD), cannabinol (CBN)] contained in marijuana, an abused drug, on progesterone 17 α -hydroxylase activity in rat testis microsomes were investigated. Microsomal progesterone 17 α -hydroxylase activity was significantly inhibited in the presence of more than 50 μ M of Δ 9-THC and CBN compared with control activity, and the IC50 values for Δ 9-THC and CBN were estimated to be 42.8 and 32.9 μ M, respectively. CBD showed less but significant inhibitory effects on 17 α -hydroxylase activity at concentrations greater than 100 μ M, and the IC50 value for the cannabinoid was estimated to be 290.9 μ M. Kinetic analysis using double reciprocal plots showed that the type of inhibition by CBN was competitive, whereas that of Δ 9-THC and CBD was the mixed type. These results suggest that the inhibition may be due to metabolic interactions between each cannabinoid and 17 α -hydroxylase.
  • 关键词:cannabinoid;17α-hydroxylase;testis;enzyme inhibition
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