Simultaneous determination of paeonilactone A and paeonilactone B in rat plasma after oral administration of albiflorin by UPLC/TOF/MS following picolinoyl derivatization

Simultaneous determination of paeonilactone A and paeonilactone B in rat plasma after oral administration of albiflorin by UPLC/TOF/MS following picolinoyl derivatization
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吡啶甲酰基衍生化后 UPLC/TOF/MS 同时测定大鼠口服白花苷后血浆中芍药内酯 A 和芍药内酯 B

DOI:
10.1016/j.jchromb.2017.07.047
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发表时间:
2017-09-01
影响因子:
3
通讯作者:
Wu, Xiuhong
Wu, Xiuhong
中科院分区:
医学3区
文献类型:
--
作者:
Wang, Zhigang;Tang, Shuhan;Wu, Xiuhong

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建立了一种新的高灵敏的分析方法,用于研究中药中最主要的成分之一白花蛇苷的体内代谢。用硫酸酶水解大鼠血浆中的主要代谢物丹皮内酯A和丹皮内酯B,经吡喃甲酰衍生化后,首次用液相色谱质谱联用法成功地检测到了丹皮内酯。以冰片为内标物测定大鼠血浆中丹皮内酯A和丹皮内酯B的浓度。丹皮内酯A和丹皮内酯B表现出不同的药代动力学行为。丹皮内酯A在灌胃给药后8h血药浓度最高达36.4+/-5.6 ng/m L,丹皮内酯B血药浓度在2 h左右达12.4+/-3.4 ng/m L,提示白花丹内酯在大鼠体内的总代谢途径。白花蛇舌草素代谢为丹皮内酯A和丹皮内酯B的硫酸盐,这可能与白花蛇舌草素的生物学效应有关。这种新的分析方法可能有助于阐明含白花苷的中药方剂的临床疗效。
A new highly sensitive analytical method was developed to investigate the in vivo metabolism of albiflorin, one of the most principal components in traditional Chinese medicine. After hydrolyzation with sulfatase, the main metabolites paeonilactone A and paeonilactone B of paeoniflorin in rat plasma were successfully detected for the first time by liquid chromatography mass spectrometry following picolinoyl derivatization. Borneol was used as the internal standard compound to quantify paeonilactone A and paeonilactone B in rat plasma. Paeonilactone A and paeonilactone B show different pharmacokinetic behaviors. The maximum plasma concentration of paeonilactone A reached 36.4 +/- 5.6 ng/mL at about 8 h after oral administration of albiflorin at a dose of 5 mg/kg, while the maximum plasma concentration of paeonilactone B reached 12.4 +/- 3.4 ng/mL at about 2 h. The total metabolic pathway of albiflorin in rats was proposed. Albiflorin was found to be metabolized to the sulfate of paeonilactone A and paeonilactone B which may be responsible for the biological effect of albiflorin. The new analytical method may help to elucidate the clinical efficacy of traditional Chinese formula containing albiflorin.