Aneja Ritu, Katyal Anju, Chandra Ramesh
Department of Chemistry, University of Delhi, Delhi, India.
Eur J Drug Metab Pharmacokinet. 2004 Jul-Sep;29(3):157-62. doi: 10.1007/BF03190592.
The modulatory potential of noscapine, an opium alkaloid was assessed on the ethanol-induced changes in hepatic drug metabolizing enzyme systems, glutathione content and microsomal lipid peroxidation. Noscapine was administered orally to male Wistar rats at a dose level of 200 mg/kg bw alone as well as in combination with 50% ethanol (v/v) for 5 days. Noscapine administration was associated with a approximately 91% decrease in hepatic microsomal cytochrome P-450 content. A decline of approximately 36% was observed in the NADPH-cytochrome c reductase activity on noscapine administration. The lowering of cytochrome P-450 levels on noscapine administration was accompanied by a concomitant increase in heme oxygenase activity as well as serum bilirubin levels. Our results indicate that the combination dosage of noscapine and ethanol antagonised the ethanol-induced elevation of cytochrome P-450 levels. Noscapine fed rats had decreased glutathione (GSH) content and enhanced lipid peroxidation compared to control rats as indexed by MDA method. Further, noscapine and ethanol coexposure produced a more pronounced elevation in lipid peroxidation and the glutathione levels also decreased significantly. We speculate on the basis of our results that the significant enhancement of lipid peroxidation on combination dosage of noscapine and ethanol is a consequence of depletion of glutathione to certain critical levels. The inhibition of glutathione-S-transferase (GST) as well as lowering of cytochrome P-450 suggests that the biotransformation of noscapine and ethanol is significantly altered following acute coexposures.
对鸦片生物碱那可丁对乙醇诱导的肝脏药物代谢酶系统、谷胱甘肽含量和微粒体脂质过氧化变化的调节潜力进行了评估。以200mg/kg体重的剂量水平单独给雄性Wistar大鼠口服那可丁,以及与50%乙醇(v/v)联合给药5天。给予那可丁后,肝脏微粒体细胞色素P-450含量下降了约91%。给予那可丁后,NADPH-细胞色素c还原酶活性下降了约36%。给予那可丁后细胞色素P-450水平降低的同时,血红素加氧酶活性以及血清胆红素水平也随之升高。我们的结果表明,那可丁和乙醇的联合剂量拮抗了乙醇诱导的细胞色素P-450水平升高。与对照组大鼠相比,喂食那可丁的大鼠谷胱甘肽(GSH)含量降低,脂质过氧化增强,以丙二醛法为指标。此外,那可丁和乙醇共同暴露导致脂质过氧化更明显升高,谷胱甘肽水平也显著降低。根据我们的结果推测,那可丁和乙醇联合给药后脂质过氧化的显著增强是谷胱甘肽耗竭至某些临界水平的结果。谷胱甘肽-S-转移酶(GST)的抑制以及细胞色素P-450的降低表明,急性共同暴露后那可丁和乙醇的生物转化发生了显著改变。