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芳香酶及其抑制剂在妇科领域中的应用
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- Author:
- No author available
- Journal Title:
- CHINESE JOURNAL OF OBSTETRICS AND GYNECOLOGY
- Issue:
- 4
- DOI:
- 10.3760/j.issn:0529-567X.2005.04.022
- Key Word:
- No keyword available
Abstract： @@ 芳香酶是细胞色素P450与还原型尼克酰胺腺嘌呤二核苷酸-细胞色素P450还原酶构成的复合物,是雄激素转化为雌激素过程中的关键酶.芳香酶能作用于不同组织中特异性的雄激素底物,产生不同活性的雌激素,如在脂肪组织中,芳香酶作用的底物为肾上腺皮质产生的雄烯二酮,产物为雌酮;在卵巢组织中主要底物为睾酮,其产物为雌二醇,少部分为由雄烯二酮转化生成的雌酮[1].芳香酶抑制剂(aromatase inhibition, AI)就是通过抑制该酶的活性来阻断雌激素合成的.根据作用机制的不同分两大类:(1)非甾体类AI:通过与亚铁血红素中的铁原子以离子键形式可逆结合,与雄激素竞争酶的活性位点,可逆性地抑制酶活性,即"竞争性抑制剂".(2)甾体类AI:其结构与酶作用的雄激素底物相似,但结合力更强,并以共价键与酶不可逆地结合,使酶永久性失活,即"自杀性抑制",这类抑制剂称为"致死性抑制剂".近年来,有关AI的研究及应用日益广泛,治疗领域不断扩展.现将芳香酶及其抑制剂在妇科领域中的研究进展和应用前景综述如下.
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