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In vitro Study of Assumed in vivo Chiral Conversion of Clenbuterol

机译:在体外的体外研究在体内的亚丁醇的手性转化中的研究

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In order to explore the possibility of determining whether clenbuterol (CLB) was ingested unintentionally via meat products contaminated with CLB or taken intentionally for doping purposes by athletes, we conducted an in vitro study assuming in vivo chiral conversion of CLB. Enzymatic reaction using swine liver tissue or chemical reaction in artificial gastric juice was performed to clarify the chiral conversion of CLB enantiomers. LC/UV measurement revealed no chiral conversion in the enzymatic reaction and temperature-dependent chiral conversion in the artificial gastric juice where CLB finally racemized. From the calculated reaction rate, activation energy (Ea ), and activation entropy (ΔS ) in the chiral conversion reaction of R -CLB in artificial gastric juice, we expected that this chiral conversion would proceed slowly because E a was relatively high. After heating at 38°C for 2 h, only approximately 1% of CLB underwent chiral conversion. Therefore, when humans ingest meat products contaminated with CLB having a different enantiomeric ratio, chiral conversion hardly progresses in the stomach and such ingestion would have very little effect on the enantiomeric excess of CLB excreted in urine. This suggests that measuring urinary CLB enantiomeric ratio would reveal whether CLB was ingested unintentionally via CLB-contaminated meat products or taken intentionally.
机译:为了探讨确定是否通过用CLB污染的肉类制品或有意用于掺杂运动员目的的肉类制品来确定是否会摄取克伦甲醇(CLB),假设I>在CLB的体内手性转化中进行了一种在体外研究中进行了一种。 。进行使用猪肝组织或在人造胃液中的化学反应的酶反应,以阐明CLB对映体的手性转化。 LC / UV测量显示在酶促反应中没有手性转化,并且在人造胃液中的温度依赖性手性转化,其中CLB最终造成的。从计算的反应速率,激活能量( ea)和在人造胃液中的手性转化反应中的活化能量(Δs),我们预计这种手性转换将缓慢进行因为 e a相对较高。在38℃加热2小时后,仅大约1%的CLB接受手性转化。因此,当人类摄取含有不同对映体比的CLB污染的肉制品时,手性转化几乎没有进展胃中,这种摄入对尿液排出的CLB的对映体过量影响很小。这表明测量尿CLB对映重量将揭示CLB是否通过CLB污染的肉类产品无意中摄取或有意地摄取。

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