Kawai H, Sakamoto F, Taguchi M, Kitamura M, Sotomura M, Tsukamoto G
Pharmaceuticals Research Center, Kanebo Co., Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1991 Jun;39(6):1422-5. doi: 10.1248/cpb.39.1422.
Various 4-arylthiomethyl-2-oxo-1,3-dioxole derivatives IIIa-o were synthesized. Their hydrolysis rates by arylesterase (EC 3.1.1.2) and cholinesterase (EC 3.1.1.8) in human serum were evaluated. Some of them were not hydrolyzed by cholinesterase, but were hydrolyzed easily by arylesterase. Among the substrates, sodium 4-((5-methyl-2-oxo-1,3-dioxol-4-yl)methylthio)benzenesulfonate (IIIg) was selected for its substrate reactivity toward arylesterase and its good water solubility. In addition, neither aliesterase (EC 3.1.1.1), acetylesterase (EC 3.1.1.6) nor cholesterol esterase (EC 3.1.1.13) hydrolyzed the compound. IIIg is thus concluded to be a specific substrate for arylesterase. Our assay system for serum arylesterase using IIIg can be readily applied to an automatic analyzer in the diagnosis of liver cirrhosis.
合成了多种4-芳基硫代甲基-2-氧代-1,3-二氧戊环衍生物IIIa-o。评估了它们在人血清中被芳基酯酶（EC 3.1.1.2）和胆碱酯酶（EC 3.1.1.8）的水解速率。其中一些不被胆碱酯酶水解，但容易被芳基酯酶水解。在这些底物中，4-((5-甲基-2-氧代-1,3-二氧戊环-4-基)甲硫基)苯磺酸钠（IIIg）因其对芳基酯酶的底物反应性和良好的水溶性而被选用。此外，脂肪酶（EC 3.1.1.1）、乙酰酯酶（EC 3.1.1.6）和胆固醇酯酶（EC 3.1.1.13）均不水解该化合物。因此得出结论，IIIg是芳基酯酶的特异性底物。我们使用IIIg的血清芳基酯酶检测系统可很容易地应用于自动分析仪，用于肝硬化的诊断。
