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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Influence of curcumin, capsaicin, and piperine on the rat liver drug-metabolizing enzyme system in vivo and in vitro.
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Influence of curcumin, capsaicin, and piperine on the rat liver drug-metabolizing enzyme system in vivo and in vitro.

机译:姜黄素,辣椒素和胡椒碱在体内和体外对大鼠肝脏药物代谢酶系统的影响。

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摘要

The effect of dietary supplementation of spice-active principles, curcumin (0.2%), capsaicin (0.015%), and piperine (0.02%) on the activities of the liver drug-metabolizing enzyme system was examined. All the 3 dietary spice principles significantly stimulated the activity of aryl hydroxylase. A synergistic action of dietary curcumin and capsaicin with respect to stimulating the activity of aryl hydroxylase was also evidenced when fed in combination. The activity of N-demethylase essentially remained unaffected by dietary curcumin, capsaicin, or their combination, but was significantly lowered as a result of piperine feeding. Uridine dinucleotide phosphate (UDP)-glucuronyl transferase activity was decreased by dietary piperine and the combination of curcumin and capsaicin. NADPH-cytochrome c reductase activity was significantly decreased by dietary piperine. The levels of hepatic microsomal cytochrome P450 and cytochrome b5 were not influenced by any of the dietary spice-active principles. These spice-active principles were also examined for their possible in vitro influence on the components of the hepatic drug-metabolizing enzyme system in rat liver microsomal preparation. Piperine significantly decreased the activity of liver microsomal aryl hydroxylase activity when included in the assay medium at 1 x 10(-6) mol/L, 1 x 10(-5) mol/L, and 1x 10(-4) mol/L level. Lowered activity of N-demethylase was observed in presence of capsaicin or piperine at 1 x 10(-6) mol/L in the assay medium. Hepatic microsomal glucuronyl transferase activity was significantly decreased in vitro by addition of capsaicin or piperine. Capsaicin and piperine brought about significant decrease in liver microsomal cytochrome P450 when included at 1 x 10(-6) mol/L and 1 x 10(-5) mol/L, the effect being much higher in the case of piperine. The results suggested that whereas the 3 spice principles have considerable similarity in structure, piperine is exceptional in its influence on the liver drug-metabolizing enzyme system. The study also indicated that a combination of curcumin and capsaicin does not produce any significant additive effect on the liver drug-metabolizing enzyme system.
机译:检查了饮食中添加的香料活性成分,姜黄素(0.2%),辣椒素(0.015%)和胡椒碱(0.02%)对肝脏药物代谢酶系统活性的影响。这三种饮食香料原则均显着刺激了芳基羟化酶的活性。当组合饲喂时,饮食姜黄素和辣椒素对刺激芳基羟化酶的活性也具有协同作用。 N-脱甲基酶的活性基本上不受饮食姜黄素,辣椒素或其组合的影响,但由于胡椒碱的喂养而大大降低了其活性。饮食胡椒碱和姜黄素和辣椒素的联合使用会降低尿苷磷酸二核苷酸(UDP)-葡萄糖醛酸转移酶的活性。日粮胡椒碱可显着降低NADPH-细胞色素c还原酶的活性。饮食中的任何饮食活性成分均不影响肝微粒体细胞色素P450和细胞色素b5的水平。还研究了这些香料活性成分对大鼠肝微粒体制剂中肝药物代谢酶系统各成分的体外影响。当以1 x 10(-6)mol / L,1 x 10(-5)mol / L和1x 10(-4)mol / L包含在测定培养基中时,胡椒碱显着降低了肝微粒体芳基羟化酶的活性水平。在测定培养基中,在辣椒素或胡椒碱的存在下,以1 x 10(-6)mol / L的浓度观察到N-脱甲基酶活性降低。加入辣椒素或胡椒碱后,肝微粒体葡萄糖醛酸转移酶活性显着降低。当以1 x 10(-6)mol / L和1 x 10(-5)mol / L加入时,辣椒素和胡椒碱显着降低了肝微粒体细胞色素P450,对于胡椒碱而言,效果要高得多。结果表明,尽管这三种香料的原理在结构上具有相当的相似性,但胡椒碱在其对肝脏药物代谢酶系统的影响方面却表现出色。该研究还表明姜黄素和辣椒素的组合不会对肝脏药物代谢酶系统产生任何明显的累加作用。

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