Yang S K, Chen S J, Huang J D
Department of Pharmacology, F. Edward Hébert School of Medicine, Uniformed Services University of the Health Sciences, Bethesda, Maryland.
Chirality. 1995;7(1):40-3. doi: 10.1002/chir.530070108.
A widely utilized pig liver esterase preparation has been found to be derived essentially exclusively from the cytosolic fraction of pig livers. Esterases in cytosol and microsomes prepared from a fresh pig liver hydrolyzed the S- and R-enantiomers of racemic oxazepam 3-acetate (rac-OXA) with specific activity ratios of approximately 2.3:1 and 1:62, respectively. Product formations were analyzed by chiral stationary phase high-performance liquid chromatography. The commercial pig liver esterase preparation showed greater activity toward S-OXA than did the esterases in the cytosolic fraction prepared from fresh pig liver. The results established that (i) esterases contained in microsomes and cytosol of pig liver have opposite enantioselectivity in the hydrolysis of rac-OXA and (ii) the commercial pig liver esterase preparation has a cytosolic origin.
已发现一种广泛使用的猪肝酯酶制剂基本上完全源自猪肝的胞质部分。从新鲜猪肝制备的胞质溶胶和微粒体中的酯酶水解外消旋奥沙西泮3 - 乙酸酯（rac - OXA）的S - 对映体和R - 对映体，比活性分别约为2.3:1和1:62。通过手性固定相高效液相色谱法分析产物形成。市售猪肝酯酶制剂对S - OXA的活性高于从新鲜猪肝制备的胞质部分中的酯酶。结果表明：（i）猪肝微粒体和胞质溶胶中含有的酯酶在rac - OXA水解中具有相反的对映体选择性；（ii）市售猪肝酯酶制剂起源于胞质溶胶。
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