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O-去甲基文拉法辛对大鼠肝微粒体细胞色素P450酶含量及CYP2D6、CYP3A4活性的影响 被引量：2

Effect of O-desmethylvenlafaxine on the content of cytomicrosome cytochrome P450 (CYP450) enzyme and activity of CYP2D6 and CYP3A4 in rat liver
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摘要 目的研究O-去甲基文拉法辛对大鼠肝微粒体内细胞色素P450(CYP450)含量及CYP2D6、CYP3A4活性的影响。方法生理盐水为对照,大鼠灌胃22.90mg.kg-1.d-1的O-去甲基文拉法辛琥珀酸盐一水合物,连续7d,然后测定其肝微体中CYP450含量及CYP2D6、CYP3A4活性。结果与生理盐水组比较,ODV组CYP450含量和CYP3A4活性无变化(P>0.05),CYP2D6活性明显被抑制(P<0.01)。结论ODV对CYP450含量和CYP3A4活性无影响,但对CYP2D6活性有抑制作用。 Objective To study the effect of O-desmethylverdafaxine （ODV） on the content of cytochrome P450 （CYP450） and activity of CYP2D6 and CYP3A4 in cytomicrosome of rat liver. Methods Bats were given 4.58 mg · kg^-1 · d^-1 ODV monohydrate for 7 days to detect the content of CYP450, activity of CYP2D6 and CYP3A4 in liver microsome taking normal sodium as control group. Results CYP450 content and CYP3A4 activity of liver microsome had no difference （P 〉0.05）, while CYF2D6 activity was significantly reduced （P 〈0.01 ）in ODV group compared with those in control group. Conclusions ODV shows no effect on CYP450 content and CYP3A4 activity, but can inhibit CYP2D6 activity in liver microsomes.
作者 刘明远 杨艳 高瞰 孙严彤 杜晓琳 闫婷婷 顾景凯
机构地区 吉林大学药物代谢研究中心
出处 《中国老年学杂志》 CAS CSCD 北大核心 2007年第7期632-633,共2页 Chinese Journal of Gerontology
关键词 O-去甲基文拉法辛 CYP450 CYP2D6 CYP3A4 O-desmethylvenlafaxine Cytechrome P450 （CYP450） CYP2D6 CYP3A4
分类号 R969.1 [医药卫生—药理学]
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参考文献9

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同被引文献16

  • 1Jiang-quan ZHOU,Zhi-qiang TANG,Jin-nan ZHANG,Jing-cheng TANG.Metabolism and effect of para-toluene-sulfonamide on rat liver microsomal cytochrome P450 from in vivo and in vitro studies[J].Acta Pharmacologica Sinica,2006,27(5):635-640. 被引量：3
  • 2张宁,喻文娟,王翔凌,林茂,邱军强,杨先乐.草鱼肝微粒体的提取及CYP酶活性的测定[J].海洋渔业,2007,29(2):148-152. 被引量：11
  • 3Muth EA, Moyer JA, Haskins JT, et al. Biochemical, neurophysiological, and behavioural effects of Wy-45,233 and other identified metabolites of the antidepressant venlafaxine[J].Drug Dev Res, 1991 ;23 (2) :191-9.
  • 4Deecher DC, Beyer CE, Johnston G, et al. Desvenlafaxine Succinate : A New Serotonin and Norepinephrine Reuptake Inhibitor [J]. J Pharmacol Exp Ther,2006 ;318 (2) :657-65.
  • 5Lowry OH, Rosebrough N J, Fan" AL, et al. Protein measurement with the Folin phenol reagent[J]. J Biol Chem, 1951 ; 193 ( 1 ) : 265-75.
  • 6Rhodes SP, Otten JN, Hingorani GP, et al. Simultaneous assessment of cy- tochrome P450 activity in cultured human hepatocytes for compound-me- diated induction of CYP3A4, CYP2B6, and CYP1 A2 [J]. J Pharmacol Toxicol Methods ,2011 ;63 ( 3 ) :223-6.
  • 7Maliakal PP, Coville PF, Wanwimolruk S. Tea consumption modulates he- patic drug metabolizing enzymes in Wistar rats[ J]. J Pharm Pharmacol, 2001 ;53(4) :569-77.
  • 8Ardjomand-Woelkart K, Kollroser M, Li L, et al. Development and valida- tion of a LC-MS/MS method based on a new 96-well Hybrid-SPETM-pre- cipitation technique for quantification of CYP450 substrates/metabolites in rat plasma[J].Anal Bioanal Chem,2011 ;400(8) :2371-81.
  • 9Pan Y, Abd-Rashid BA, Ismail Z, et aL In vitro modulatory effects of An- drographis panieulata, Centella asiatica and Orthosiphon stamineus on ey- tochrome P450 2C19 ( CYP2C19 ) [J].J Ethnopharmacol, 2011 ; 133 (2) :881-7.
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中国老年学杂志
2007年 第7期

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