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目的考察没食子酸在大鼠体内对1,2-二氯-4-硝基苯(DCNB)代谢的影响。方法将大鼠随机分为空白组(生理盐水)和没食子酸组(20 mg·kg-1),连续给药14 d,再给予DCNB,不同时间点于眼眶静脉取血,用GC法检测血浆中DCNB的浓度,绘制药时曲线,用DAS3.2.1计算药动学参数。结果 DCNB的线性范围为0.025~10.0μmol·L-1,最低检测限为25nmol·L-1,日内、日间RSD均<10%;5 d内于室温下放置较稳定,提取回收率为85%~90%;没食子酸组的AUC0-∞明显低于空白组的,而Cl/F明显高于空白组的,表明没食子酸在大鼠体内能诱导谷胱甘肽硫转移酶(GST)的活性。结论没食子酸在大鼠体内能明显诱导GST活性,增强DCNB的代谢清除,从代谢角度解释了没食子酸的解毒机制。
Objective To investigate the effect of gallic acid on 1,2-dichloro-4-nitrobenzene (DCNB) metabolism in rats. Methods The rats were randomly divided into blank group (normal saline) and gallic acid group (20 mg · kg-1) for 14 days. DCNB was given to the orbital vein at different time points. In DCNB concentration, draw the drug curve, using pharmacokinetic parameters DAS3.2.1. Results The linear range of DCNB was 0.025 ~ 10.0μmol·L-1, the lowest detection limit was 25nmol·L-1, RSD was less than 10% in day and day, and stable at room temperature within 5 days. The recovery rate of DCNB was 85 % ~ 90%; AUC0-∞ in gallic acid group was significantly lower than that in blank group, while Cl / F was significantly higher than that in blank group, indicating that gallic acid can induce glutathione S-transferase (GST) active. Conclusion Gallic acid can obviously induce GST activity in rats and enhance the clearance of DCNB. The mechanism of the detoxification of gallic acid is explained from the perspective of metabolism.