| PART I The Metabolites Research of Andrographolide in RatsAndrographolide , its chemical name as : 2 (3H)-Furanone, 3-[2-[decahydro-6-hydroxy-5 -(hydroxymethyl)-5, 8a-dimethyl-2-methylene-1 -napthalenyl] ethylidene] dihydro-4-hydroxy-, was one of main active constituents of Andrographis paniculate (Burm) Nees (穿心莲) , a famous Traditional Chinese Medicine. It had many bioactivities, such as anti-inflammation, anti-microbe, reducing blood pressure, anti-cancer, et al.In this paper, 14 new metabolites of Andrographolide in rats were found through manifold ways, such as traditional phytochemical separation methods, HPLC/PDA, HPLC/ESI-MS, et al. The structures of metabolites 1 to 13 were determined by means of chemical and spectral analyses as: 14-Deoxy-12(R)-sulfo andrographolide (M-l), 14-Deoxy-12(S)-sulfo andrographolide (M-2), 14-Deoxy-12(R)-sulfo-9(S)-andrographolide (M-3), 14-Sulfo isoandrographolide (M-4), 14-Deoxy-12(R)-sulfo andrographolide 3-sulfate (M-5), 14-Deoxy-12(S)-sulfo andrographolide 3-sulfate (M-6), 14-Sulfo isoandrographolide 3-sulfate (M-7), 14-Deoxy-11,12-didehydro andrographolide (M-8), Isoandrographolide (M-9), 14-Deoxy andrographolide (M-10), 3, 14-Dideoxy andrographolide (M-11), 3, 14, 19-Trimethoxyl andrographolide (M-12), 3, 14, 19-Trimethoxyl isoandrographolide (M-13). All of these were new metabolites. Metabolite 2, 3, 4, 5, 6, 7, 11, 12, 13 were new compounds and metabolite 1 was a new natural compound.A new metabolic reaction named sulfonate reaction of Carbon-Carbon double bond was found in this research, i.e. the β-carbon of α, β-unsaturated carbonyl compounds were attacked by sulphur atom which had lone-pair electrons and formed sulfonic compounds. It may be the main metabolic pathway of Andrographolide in rats. The polarity of the substance increased greatly and could easily be eliminated from body.On the basis of the isolation and determination of the metabolites in urine andfeces, the low polarity metabolites in blood, bile, small intestinal and stomach contents were analyzed by HPLC. 6 low polarity metabolites were found in blood, 3 from small intestinal content and 2 from stomach content. The structures of these metabolites were presumed through HPLC chromatograms, UV spectra and ESI-MS. At the same time, the metabolic pathways of Andrographolide in rats were proposed through above analyses.Metabolite 1 to 7 were sulfonate or sulfate compounds. They had strong polarity and very weak absorptivity in UV spectra (including bottom UV length). These characters made it hard to analyze by HPLC. So HPTLC was performed to analyze them. In the developing agents, paired ion reagent was added and the visualizing reagent with high sensitivity and selectivity was used. A perfect result was obtained to these compounds.No Andrographolide metabolites were detected from bile of rats. This fact suggested that andrographolide was excreted from rats not through the bile, but kidney.The metabolic data and pathways of Andrographolide were obtained through the research and provided the academic evidences for further developing researches of Andrographolide.PART II The Active Constituents Research of Gualou-Xiebai-Baijiu-TangGualou-Xiebai-Baijiu-Tang (瓜蒌薤白白酒汤) is a well-known classic prescription in Traditional Chinese Medical Sciences. It originates from Jingui Yaolue, a great pharmaceutical book written by the famous physician Zhang Zhongjing during Han dynasty. The prescription consists of Trichosanthes kirilo-wii Max. (瓜蒌) and Allium macrostemon Bge.(薤白) and is extracted with wine. In Traditional Chinese Medical Sciences, this prescription is used to activate the blood circulatory system and eliminate stasis. It has been used to treat coronary heart diseases and angina pectoris for several hundred years and has achieved good results in modern clinical practices. In our research, we take the prescription as a whole, and try to find genuine active principles through bioactivity-guided isolation procedures. Then the activeprinciples were t...
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