Han Yan-Qi, Wang Jing, Cui Qing-Xin, Wang Li-Qiang, Cheng Bin-Feng, Zhao Hong-Zhi, Jiang Min, Bai Gang, Luo Guo-An
College of Pharmacy, State Key Laboratory of Medicinal Chemical Biology, Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, 300071, People's Republic of China.
Biomed Chromatogr. 2014 Apr;28(4):554-63. doi: 10.1002/bmc.3069. Epub 2013 Oct 24.
Qishenyiqi dropping pill (QSYQ), is a traditional Chinese medicine (TCM) prescription for treating heart diseases in China. Knowledge concerning the systemic identification of active compounds and metabolic components of QSYQ is generally lacking. Therefore, it is essential to develop a valid method for the analysis of active compounds of the combined prescription and determination of interactions among the herbs. The absorbable compounds and metabolites of QSYQ were profiled using computational chemistry prediction, an improved everted gut sac in vitro experiment, the Caco-2 cell monolayer in vitro test, a rat in vivo experiment and ultra-performance liquid chromatography/diode array detection/quadrupole-time of flight mass spectrum (UPLC/DAD/Q-TOF MS). In total, 42 prototype compounds were recognized as absorbable compounds, and eight metabolites were identified by UPLC/DAD/Q-TOF MS. The absorption rates of phenolic acids and saponins were significantly improved and the absorption of isoflavone was inhibited after compatibility. The volatile oil component had an improved effect on the absorption of other compounds, while its own absorption was inhibited. In conclusion, the present study established a rapid and effective strategy for demonstrating the absorption and metabolism of QSYQ and revealing the compatible relationship among herbs. This investigation can provide a reference for the compatibility of prescriptions and the modernization of TCM.
芪参益气滴丸(QSYQ)是中国用于治疗心脏病的一种中药方剂。目前普遍缺乏关于芪参益气滴丸活性成分和代谢成分系统鉴定的知识。因此,开发一种有效的方法来分析复方活性成分并确定药材之间的相互作用至关重要。采用计算化学预测、改良的外翻肠囊体外实验、Caco-2细胞单层体外试验、大鼠体内实验以及超高效液相色谱/二极管阵列检测/四极杆-飞行时间质谱(UPLC/DAD/Q-TOF MS)对芪参益气滴丸的可吸收成分和代谢产物进行了分析。共识别出42种原型化合物为可吸收成分,并通过UPLC/DAD/Q-TOF MS鉴定出8种代谢产物。配伍后酚酸和皂苷的吸收率显著提高,异黄酮的吸收受到抑制。挥发油成分对其他化合物的吸收有促进作用,但其自身的吸收受到抑制。总之,本研究建立了一种快速有效的策略来阐明芪参益气滴丸的吸收和代谢,并揭示药材之间的配伍关系。本研究可为方剂配伍及中药现代化提供参考。