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羧酸酯酶与酯类药物代谢 被引量：8

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摘要 哺乳动物羧酸酯酶(Carboxylesterases,CESs,EC3.1.1.1)属于B族酯酶,组成一个多基因家族,其基因产物定位于多种组织的内质网中。CESs参与机体内源性和外源性化合物的水解代谢,并与其他代谢酶或运载体共同作用,极大地影响酯类药物的体内代谢。近年来对于CESs的研究逐步增多,人们将其分为5个亚族,分别为CES1、CES2、CES3、CES4和CES5。人体内参与酯类药物代谢的CESs主要为hCE-1(人类CES1家族同工酶)和hCE-2(人类CES2家族同工酶)。此两种酶在组织分布和对酯类药物代谢特征上存在较大差异,如小肠上皮由于CES2表达会对部分酯类药物的口服吸收产生重要影响。因此在进行酯类药物尤其是酯类前药合成时,必须考虑该类药物的物理化学和生物学性质,结合体内CESs表达特征和活性综合评价才能获得成功。
作者 刘东 张程亮
机构地区 华中科技大学同济医学院附属同济医院药学部
出处 《医药导报》 CAS 2010年第3期332-335,共4页 Herald of Medicine
关键词 酯类药物 羧酸酯酶 药物代谢
分类号 R96 [医药卫生—药理学]
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参考文献20

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同被引文献76

  • 1刘帅兵,丁肖梁,黄晨蓉,薛领,王子腾,缪丽燕.氯吡格雷的体外相互作用研究[J].中国血液流变学杂志,2014(1):12-15. 被引量：1
  • 2王引利,王伟,杜传礼.咪达普利的药理学特性和临床治疗意义[J].心血管病学进展,2005,26(1):21-23. 被引量：6
  • 3夏玉叶,闵旸,盛雨辰.羟基红花黄色素A对大鼠血栓形成和血小板聚集功能的影响[J].中国药理学通报,2005,21(11):1400-1401. 被引量：34
  • 4FUJIWARA Y,MINAMI H.An overview of the recent progress in irinotecan pharmacogenetics[J].Pharmacogenomics,2010,11(3):391-406.
  • 5TAKEMOTO I,ITAGAKI S,CHIBA M,et al.Charac-terization of secretory intestinal transport of the lactone form of CPT-11[J].Cancer Chemother Pharmacol,2006,57(1):129-133.
  • 6HICKS L D,HYATT J L,STODDARD S,et al.Impro-ved,selective,human intestinal carboxylesterase inhibitors designed to modulate 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (Irinotecan; CPT-11) toxicity[J].J Med Chem,2009,52(12):3742-3752.
  • 7VANDE KERKHOF E G,DE GRAAF I A M,GROOTHUIS G M M.In vitro methods to study intestinal drug metabolism[J].Curr Drug Metab,2007,8(7):658-675.
  • 8GUPTA E,VYAS V,AHMED F,et al.Pharmacokinetics of orally administered camptothecins[J].Ann N Y Acad Sci,2000,922:195-204.
  • 9KURITA A,KADO S,MATSUMOTO T,et al.Strepto-mycin alleviates irinotecan-induced delayed-onset diarrhea in rats by a mechanism other than inhibition of beta-glucuronidase activity in intestinal lumen[J].Cancer Chemother Pharmacol,2010.
  • 10HOSOKAWA M.Structure and catalytic properties of carb-oxylesterase isozymes involved in metabolic activation of prodrugs[J].Molecules,2008,13(2):412-431.

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医药导报
2010年 第3期

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