大蒜辣素在大鼠体内转化产物 S-烯丙基巯基-L-半胱氨酸的鉴别

Identification of S-allyl-mercapto-L-cysteine,a transformation product of allicin in rats

目的鉴别大鼠给药后大蒜辣素体内转化产物S-烯丙基巯基-L-半胱氨酸,探讨血浆和皮肤组织中S-烯丙基巯基-L-半胱氨酸的变化情况。方法取SD大鼠,雌雄各半,体重(200±20)g,随机分为8组,分别为空白组及给药后不同时间组,每组每个时间点采用6只大鼠,涂抹大蒜软膏于大鼠背部,分别于0、5、10、15、20、25、30、60 min依次取血液和皮肤组织,UPLC-MS/MS鉴定血液和皮肤组织中大蒜辣素的转化产物S-烯丙基巯基-L-半胱氨酸及变化情况。结果大蒜辣素与半胱氨酸反应产生S-烯丙基巯基-L-半胱氨酸,30 min即可反应90%以上。血浆中转化产物S-烯丙基巯基-L-半胱氨酸在4 h内稳定。UPLC-MS/MS鉴定并确定了皮肤组织和血浆样品大蒜辣素与内源性半胱氨酸的反应产物S-烯丙基巯基-L-半胱氨酸,给予大蒜软膏30 min内血浆和皮肤中S-烯丙基巯基-L-半胱氨酸的浓度逐步增大,60 min时含量降低。结论大蒜辣素可与血浆和组织中的内源性半胱氨酸快速反应,本研究将为大蒜辣素的后续研究提供重要依据。

ObjectiveTo identify the transformation product S-allyl-mercapto-L-cysteine of allicin in rats after administration,and to investigate the changes of S-allyl-mercapto-L-cysteine in plasma and skin tissues.MethodsSD rats,half male and half female,with a body weight of(200±20)g,were randomly divided into 8 groups,which were blank group and groups at different time after administration.6 rats are used at each time point.rats in each group were applied to the back of rats at each time point,and blood and skin tissues were taken successively at 0,5,10,15,20,25,30 and 60 min,respectively.UPLC-MS/MS was used to identify S-allyl mercaptol l-cysteine,the transformation product of allicin,in blood and skin tissues and its changes.ResultsAllicin was stable in the blank solvent for up to 150 minutes and in deproteinized plasma for up to 8 hours.The reaction between allicin and cysteine produced S-allyl-mercapto-L-cysteine,with over 90%of the reaction occurring within 30 minutes.The transformation product S-allyl-mercapto-L-cysteine in plasma was stable within 4 hours.UPLC-MS/MS was used to identified and determined S-allyl-mercapto-L-cysteine,the reaction product of allicin with endogenous cysteine,in both skin tissue and plasma samples.The concentrations of S-allyl-mercapto-L-cysteine in plasma and skin gradually increased within 30 minutes after administration of garlic ointment,and decreased after 60 minutes.ConclusionAllicin can rapidly react with endogenous cysteine in plasma and tissues,and this study provides important evidence for subsequent research on the pharmacokinetics of allicin.