Hou Mei-Ling, Chang Li-Wen, Lin Chi-Hung, Lin Lie-Chwen, Tsai Tung-Hu
Institute of Traditional Medicine, School of Medicine, National Yang-Ming University, No. 155, Sec. 2, Li-Nong St, Beitou District, Taipei 11221, Taiwan.
Institute of Microbiology and Immunology, National Yang-Ming University, No. 155, Sec. 2, Li-Nong St, Beitou District, Taipei 11221, Taiwan.
Molecules. 2014 Apr 2;19(4):4058-75. doi: 10.3390/molecules19044058.
Rhein (4,5-dihydroxy-9,10-dioxoanthracene-2-carboxylic acid, cassic acid) is a pharmacological active component found in Rheum palmatum L. the major herb of San-Huang-Xie-Xin-Tang (SHXXT), a medicinal herbal product used as a remedy for constipation. Here we have determined multiple bioactive components in SHXXT and investigated the comparative pharmacokinetics of rhein in rats. A sensitive and specific method combining liquid chromatography with electrospray ionization tandem mass spectrometry has been developed and validated to simultaneously quantify six active compounds in the pharmaceutical herbal product SHXXT to further study their pharmacokinetics in rats. Multiple reaction monitoring (MRM) was employed for quantification with switching electrospray ion source polarity between positive and negative modes in a single run. There were no significant matrix effects in the quantitative analysis and the mean recovery for rhein in rat plasma was 91.6%±3.4%. The pharmacokinetic data of rhein demonstrate that the herbal formulae or the single herbal extract provide significantly higher absorption rate than the pure compound. This phenomenon suggests that the other herbal ingredients of SHXXT and rhubarb extract significantly enhance the absorption of rhein in rats. In conclusion, the herbal formulae (SHXXT) are more efficient than the single herb (rhubarb) or the pure compound (rhein) in rhein absorption.
大黄酸（4,5-二羟基-9,10-二氧代蒽-2-羧酸，大黄素）是掌叶大黄中的一种药理活性成分，掌叶大黄是三黄泻心汤（SHXXT）的主要草药，三黄泻心汤是一种用于治疗便秘的草药产品。在此，我们测定了三黄泻心汤中的多种生物活性成分，并研究了大黄酸在大鼠体内的比较药代动力学。我们开发并验证了一种将液相色谱与电喷雾电离串联质谱相结合的灵敏且特异的方法，以同时定量草药产品三黄泻心汤中的六种活性化合物，从而进一步研究它们在大鼠体内的药代动力学。采用多反应监测（MRM）进行定量，在单次运行中在正负极性之间切换电喷雾离子源极性。定量分析中没有显著的基质效应，大鼠血浆中大黄酸的平均回收率为91.6%±3.4%。大黄酸的药代动力学数据表明，草药配方或单一草药提取物的吸收率明显高于纯化合物。这一现象表明，三黄泻心汤的其他草药成分和大黄提取物显著增强了大黄酸在大鼠体内的吸收。总之，在大黄酸吸收方面，草药配方（三黄泻心汤）比单一草药（大黄）或纯化合物（大黄酸）更有效。
