酯酶对己酸17α-羟孕酮的作用。
The effect of esterases on 17alpha-hydroxyprogesterone caproate.
作者信息
Yan Ru, Fokina Valentina, Hankins Gary D V, Ahmed Mahmoud S, Nanovskaya Tatiana N
机构信息
Department of Obstetrics & Gynecology, University of Texas Medical Branch, Galveston, TX, USA.
出版信息
Am J Obstet Gynecol. 2008 Feb;198(2):229.e1-5. doi: 10.1016/j.ajog.2007.07.038. Epub 2007 Oct 22.
OBJECTIVE
The aim of this investigation is to determine whether 17alpha-hydroxyprogesterone caproate is hydrolyzed, in vitro, to 17alpha-hydroxyprogesterone and caproate.
STUDY DESIGN
The in vitro hydrolysis of dual radioactively labeled 17alpha-hydroxy-[3H] progesterone [14C] caproate by human plasma, hepatic and placental S9 fractions as well as recombinant esterases was investigated. The formation of [3H]-17alpha-hydroxyprogesterone and [14C]-caproate were determined with the use of high-performance liquid chromatography equipped with an online radioactivity detector. The presence and activity of carboxylesterase and butyrylcholinesterase in the human-derived preparations was confirmed by the hydrolysis of their prototypic substrates p-nitrophenyl acetate, p-nitrophenyl butyrate, and butyrylthiocholine, respectively.
RESULTS
The aforementioned human-derived preparations hydrolyzed p-nitrophenyl acetate, p-nitrophenyl butyrate, and butyrylthiocholine. However, when 17alpha-hydroxyprogesterone caproate was incubated with the human-derived preparations under identical experimental conditions neither [3H]-17alpha-hydroxyprogesterone nor [14C]-caproate was detected.
CONCLUSION
17Alpha-hydroxyprogesterone caproate is not hydrolyzed in vitro by the esterase enzymes present in human plasma, liver, preterm, or term placenta.
目的
本研究旨在确定己酸17α-羟孕酮在体外是否会水解为17α-羟孕酮和己酸盐。
研究设计
研究了人血浆、肝脏和胎盘S9组分以及重组酯酶对双放射性标记的17α-羟基-[3H]孕酮[14C]己酸盐的体外水解情况。使用配备在线放射性检测器的高效液相色谱法测定[3H]-17α-羟孕酮和[14C]-己酸盐的形成。通过分别水解其原型底物对硝基苯乙酸、对硝基苯丁酸和丁酰硫代胆碱，证实了人源制剂中羧酸酯酶和丁酰胆碱酯酶的存在和活性。
结果
上述人源制剂可水解对硝基苯乙酸、对硝基苯丁酸和丁酰硫代胆碱。然而，在相同实验条件下，将己酸17α-羟孕酮与人源制剂一起孵育时，未检测到[3H]-17α-羟孕酮和[14C]-己酸盐。
结论
人血浆、肝脏、早产或足月胎盘所含的酯酶在体外不会使己酸17α-羟孕酮水解。
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