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Abstract: Aim of the study: Huang-Lian-Jie-Du-Tang (HLJDT) is a traditional Chinese medicine with anti-inflammatory use. In the present study, the effects of its component herbs and pure components were observed on eicosanoid generation to find out the contributory components and their precise targets on arachidonic acid (AA) cascade. Materials and methods: By monitoring leukotriene B4 (LTB4), 5-hydroxyeicosatetraenoic acid (5-HETE), and 12-hydroxy-5,8,10-heptadecatrienoic acid (12-HHT), we compared the effects of HLJDT, HLJDT free of one or two component herbs, and water extract of four single component herbs of HLJDT (Rhizoma coptidis, Radix scutellariae, Cortex phellodendri and Fructus gardeniae) on eicosanoid generation in rat elicited peritoneal macrophages. In addition, thirteen pure compounds from HLJDT (baicalin, baicalein, wogonoside, wogonin, berberine, magnoflorine, phellodendrine, coptisine, palmatine, jateorrhizine, crocin, chlorogenic acid, and geniposide) were tested in the macrophages. Furthermore, the efficacies of these thirteen compounds were evaluated on cell-free purified enzymes: leukotriene A4 hydrolase (LTA4H), 5-, 15-lipoxygenase (5-, 15-LO), and cyclo-oxygenase-1/2 (COX-1/2). Moreover, the possible synergetic effect on LO pathway derived LTB4 generation between the active components was also tested in rat peritoneal macrophages. Results: Our experiments showed that Rhizoma coptidis and Radix scutellariae were responsible for the suppressive effect of HLJDT on eicosanoid generation. Some of the pure components including baicalein, baicalin, wogonoside, wogonin, coptisine, and magnoflorine inhibited eicosanoid generation in rat macrophages via LO pathway of AA cascade. Further experiments on cell-free purified enzymes confirmed that Radix scutellariae derived baicalein and baicalin showed significant inhibition on 5-LO and 15-LO, while Rhizoma coptidis derived coptisine showed medium inhibition on LTA4H. On the other hand, no significant inhibition of thirteen components on COX-1/2 was observed. Moreover, the slight synergetic inhibition on LTB4 between baicalein and coptisine was proved in the rat peritoneal macrophages. Conclusions: Baicalein and coptisine, the active components of HLJDT, for the first time are found to interfere with arachidonic acid cascade via inhibition on different points of LO pathway. This finding makes the mechanism of HLJDT clearer and achieves its safer therapeutic application. [Copyright &y& Elsevier]

Abstract: Aim of the study: Tanshinone IIA (T), salvianolic acid B (S) and ginsenoside Rb1 (G) are the three major active ingredients of Compound Danshen Formula (CDF) for its protective effects on myocardial ischemia (MI). In this study, we aimed to investigate therapeutic and synergistic effects of TSG (combination of T, S and G) on MI rats with metabolomic strategy. Materials and methods: MI model were induced in Sprague-Dawley rats by left anterior descending coronary artery ligation. MI rats were respectively administrated T, S, G, TSG and CDF. Plasma was analyzed by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS). Partial least squares discriminate analysis (PLS-DA) models were built to evaluate the therapeutic and synergistic effects of TSG at whole level. 22 MI biomarkers in rat plasma were also investigated to explain that. Results: TSG brings nearly equal therapeutic effects on MI as CDF and it plays more stable regulated action on those 22 identified metabolites than single compound. Conclusions: Overall, there were few methods for the study of synergistic effects of Chinese medicine. Our results suggested that metabolomics offers a new idea for Chinese medicine research. [Copyright &y& Elsevier]