不同大鼠组织微粒体对乙酰水杨酸的酶促水解作用中的性别差异。
Sex differences in the enzymatic hydrolysis of acetylsalicylic acid by microsomes from various rat tissues.
作者信息
Vargas Loza A M, Montes de Oca E I, Posadas del Rio F A
机构信息
Departamento de Farmacología y Toxicología, Centro de Investigación y de Estudios Avanzados del I.P.N., México, D.F., Mexico.
出版信息
J Appl Toxicol. 1997 Nov-Dec;17(6):347-51. doi: 10.1002/(sici)1099-1263(199711/12)17:6<347::aid-jat432>3.0.co;2-j.
We studied the in vitro hydrolysis of acetylsalicylic acid (ASA) to salicylic acid (SA) catalysed by microsomal preparations from liver, kidney, small intestine and stomach mucosas and blood serum of adult female and male rats. Hepatic microsomes from male rats had the highest specific activity: 42.3 +/- 6.0 nmol SA mg(-1) min(-1) (mean +/- SEM). Kidney, intestine, stomach and serum activities were 60, 30, 14 and 0.7% with regard to the liver. In contrast, gastric microsomes from female rats showed the highest specific activity: 53 +/- 22.1 nmol SA mg(-1) min(-1) (mean +/- SEM) whereas intestine, liver, kidney and serum activities were 60, 43, 40 and 1.7% with regard to the stomach mucosa. Hepatic, renal and intestinal microsomes had a pH optimum of 5-6. Male rats had Vmax and Km values of 95.5, 83.4 and 29.4 nmol SA mg(-1) min(-1) and 2.9, 1.27 and 6.4 mM, while for female rats they were 54.8, 75.8 and 59.4 nmol SA mg(-1) min(-1) and 2.6, 1.35 and 3.4 mM for hepatic, renal and intestinal microsomes, respectively. Parathion inhibited the hydrolysis of ASA with an IC50 of 1.2 x 10(-5) M for liver and kidney and 5 x 10(6) M for intestine from male rats.
我们研究了成年雌性和雄性大鼠肝脏、肾脏、小肠、胃黏膜及血清的微粒体制剂催化乙酰水杨酸（ASA）体外水解为水杨酸（SA）的过程。雄性大鼠的肝微粒体具有最高的比活性：42.3±6.0 nmol SA mg⁻¹ min⁻¹（平均值±标准误）。肾脏、小肠、胃和血清的活性相对于肝脏分别为60%、30%、14%和0.7%。相比之下，雌性大鼠的胃微粒体表现出最高的比活性：53±22.1 nmol SA mg⁻¹ min⁻¹（平均值±标准误），而小肠、肝脏、肾脏和血清的活性相对于胃黏膜分别为60%、43%、40%和1.7%。肝脏、肾脏和小肠微粒体的最适pH为5 - 6。雄性大鼠肝脏、肾脏和小肠微粒体的Vmax和Km值分别为95.5、83.4和29.4 nmol SA mg⁻¹ min⁻¹以及2.9、1.27和6.4 mM，而雌性大鼠的相应值分别为54.8、75.8和59.4 nmol SA mg⁻¹ min⁻¹以及2.6、1.35和3.4 mM。对硫磷抑制ASA的水解，雄性大鼠肝脏和肾脏的IC50为1.2×10⁻⁵ M，小肠为5×10⁻⁶ M。
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