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Study Of Preparation, Identify And Pharmacokinetics For Alliin And Alliinase

Posted on:2004-01-24Degree:DoctorType:Dissertation
Country:ChinaCandidate:J M ChangFull Text:PDF
GTID:1104360125968701Subject:Pharmacology
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Garlic is the underground bulbs of Allium sativum Linn. Since ancient times garlic has been used worldwide not only as a food but also as a medicine. The preparation of garlic can be cure many disease and use to mainten health. Survey herbal medicine marker of musky and Europe. Since 1998 ,garlic came to be known as "plant gold" .Garlic is eminent in sell and broad effect as medicine, In recent years, garlic research thesises have been exceeded 5000 pieces, The study of garlic arouse human attention, scientists have investigate thoroughly in garlic, heretofore, produce of garlic has been beyonded 30 kinds, but the preparation of garlic in high active component is rare. The aim of this theme of Brown university in USA and Bonn university in Germany and this thesis group for empolder new preparation.1 preparation and identify of alliin, alliinase.The study of active component in garlic is the foundation of new drug research. The chemical component of garlic has many kinds. A great deal of science research indicated: the mostly active component of garlic is the system of alliin-alliinase. Alliin was isolated from the garlic, and was identified the structure by the chemical and spectroscopic data, 13C and 1H-NMR signal of alliin were completely assiged by means of 1H-1H COSY and 13C-1H COSY for the first time. In contrast to alliin of Indofine Chemical Company, Inc.The content of alliin of this experiment is 99.7%. Alliinase was isolated from the garlic, and determined molecular weight by the SDS-PAGE, determined the efficient of alliinase by HPLC.2 determination of ailiin in garlicOwing to the reaction of alliinase catalyse ailiin, the determination of ailiin in garlic is difficult problem, we established a HPLC method in first, used the common ODS column, the mobile phase was methanol: water (3:7) ,detective wavelengh was 220nm. The degree of separation exceeded 1.5. The national drugs standard about the content of garlic adopt determination of allicin and then confer ailiin. USP (2002) adopt derivatization procedure first, and then determinated. The method that we established is more accurate than the national drug's standard. Comparing to USP (2002), it can spare chemical reagent and simplify operation. Two methods were not significant difference by statistics analysis. The contents of ailiin in garlic: ShanDong is 0.74%, HeNan is 1.12%, JiMuSaEr in Xinjiang is 1.5%.3 Pharmacokinetics of ailiinThe series of organosulfur compounds, derived from ailiin, has been reported to have antibiotic activity, and activity against cancer, diabetes, heart disease and stroke, antifungal and etc.. This thesis established two methods of HPLC and HPLC-MS, this methods were reliability and practicability. After oral administration of ailiin 400mg-kg-l to mice. The concentrations of ailiin in plasma fitted two-compartment model, primary parameter of pharmacokinetics was A(-19.658) μg·ml-1, α (1.001) min-1, B(151.801) μg·ml-1, β (0.028) min-1, CL(0.077) mg·min-1·kg-1, K12(0.148) min-1, K21(0.848) min-1, K10(0.032) min-1, Ka(0.427) min-1, t1/2α (0.665) min, t1/2β (27.246) min, t1/2Ka(1.621) min, V(2.375) L·kg-1, AUC(5162.48) μg· min-1·ml-1, tmax(9.19) min, Cmax118.59 μ g·ml-1. After oral administration of alliin 300mg·kg-1 to rat. The concentrations of alliin in plasma fitted two-compartment model, primary parameter of pharmacokinetics was A(84.45) μ g·ml-1, α (0.0258) min-1, B(18.46) μ g.ml-1, β (0.0053) min-1, CL(0.0482) mg·min-1·kg-1, K12(0.00714) min-1, K21(0.00933) min-1, K10(0.01461) min-1, Ka(0.1915) min-1, t1/2α(26.85) min, t1/2β(131.15) min, t1/2Ka(3.62) min, V(3.29)L·kg-1, AUC(6228.48) μg·min-1·ml-1, tmax(14.80) min, Cmax (69.09) μg-ml-1.4 pharmacokinetics of alliin-alliinaseModern research has been proved that active components of garlic are the system of alliin-alliinase. It is essential to study its pharmacokinetics, affirmed alliin+alliinase by HPLC-MS method. The result is that allicin in solution do not transform in 13 hours. Methods developed for the determination of allicin in mice p...
Keywords/Search Tags:garlic, alliin, alliinase, allicin, pharmacokinetics, HPLC, LC-MS.
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