SPECIES-DIFFERENCES IN HYDROLYSIS OF ISOCARBACYCLIN METHYL-ESTER (TEI-9090) BY BLOOD ESTERASES
SPECIES-DIFFERENCES IN HYDROLYSIS OF ISOCARBACYCLIN METHYL-ESTER (TEI-9090) BY BLOOD ESTERASES
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DOI：
10.1016/0006-2952(95)00071-7
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发表时间：
1995-05-17
影响因子：
5.8
通讯作者：
TSUJI, A
中科院分区：
文献类型：
--
作者：
MINAGAWA, T;KOHNO, Y;TSUJI, A
研究了大鼠、犬和人全血中异碳环素甲酯（TEI-9090）水解及其分离组分的种属差异。大鼠全血中的酯酶活性分别比犬和人全血中的酯酶活性高约100倍和400倍，这归因于高血浆活性。相比之下，TEI-9090在犬和人血液中的水解活性是由于红细胞（RBC），其在人体中的活性受到白蛋白的轻微抑制。在狗中，红细胞膜中的活性是细胞质中的10倍，而在人膜和细胞质中的活性几乎相同。酯酶抑制剂氟磷酸二异丙酯、双对硝基苯磷酸酯（BNPP）、依地孕酮、5，5 '-二硫代双（2-硝基苯甲酸）（DTNB）和对氯汞苯甲酸酯的作用表明，大鼠血浆和红细胞胞液中水解TEI-9090的酯酶分别为羧酸酯酶（CarbE）和芳基酯酶（ArE）。犬血浆和红细胞膜的酯酶为CarbE，红细胞胞浆的酯酶为ArE。人血浆、红细胞膜和胞液中的酯酶活性分别为丁酰胆碱酯酶、CarbE和ArE。
Species differences in the hydrolysis of isocarbacyclin methyl ester (TEI-9090) in whole blood and in its separated components were studied in rats, dogs and human. Esterase activity in rat whole blood was approximately 100 and 400 times higher than that in dog and human whole blood, respectively, and was attributed to high plasma activity. In contrast, TEI-9090 hydrolysis activities in dog and human blood were due to red blood cells (RBC), whose activity in humans was slightly suppressed by albumin. In dogs, activity in RBC membranes was 10 times greater than in the cytosol, while in human membrane and cytosol activity was virtually the same. The effects of the esterase inhibitor diisopropylfluorophosphate, bis-p-nitrophenylphosphate (BNPP), eserine, 5,5'-dithiobis-(2-nitrobenzoic acid) (DTNB) and p-chloromercuribenzo ate showed that the rat plasma and RBC cytosol esterases hydrolysing TEI-9090 were carboxylesterase (CarbE) and arylesterase (ArE), respectively. The esterases in dog plasma and RBC membrane were CarbE, and RBC cytosol esterase was ArE. In humans, the esterase activities in plasma, RBC membrane and cytosol were butyrylcholinesterase, CarbE and ArE, respectively.