Studies On Foundation Of Effective Compounds Of AiDi Injection

The foundation of active compounds of traditional Chinese medicine (TCM) is thatthey have physiological activity in the body and synergy from the effectivepharmaceutical ingredients and group of their metabolites."Chromatogram-effect"relationship of TCM, which is already internationally accepted as an efficient qualitycontrol technique, is an integral expression of the consitutents in TCM. In this study,focused on the problem of quality control, systemic studies on the chemical constituentsof AiDi injection and the effects of efficacy enhancing and toxicity reducing withcantharidin were carried out. Meanwhile, this study show rational of foundation ofeffective compounds by establshing the "Chromatogram-effect" relationship.Chapter one: the chemical constituents and the development of pharmacology ofPanax ginseng, Astragalus membranceus and Acanthopanax senticosus aresummarized.Chapter two: the chemical constituents of AiDi injection were isolated bychromatography, and their structures were identified by spectroscopic analysis (NMRand MS), At last,22compounds were isolated and identified to be3-O-3’,4’-diacetyl-β-D-xylopyranosyl-6-O-β-D-glucopyranosyl-cycloastragenol (ZA-1),astragaloside IV (ZA-2), astragaloside II (ZA-3), astragaloside I (ZA-4), isoastragalosideI (ZA-5), acetylastragaloside I (ZA-6), ginsenosid-Re (ZA-7), ginsenoside-Rf(ZA-8),ginsenoside-Rg1(ZA-9), ginsenoside-Rb3(ZA-10), notoginsenoside-R4(ZA-11),ginsenoside-Rb1(ZA-12), ginsenoside-Rc (ZA-13), ginsenoside-Rb2(ZA-14),ginsenoside-Rd (ZA-15), Lucyoside H (ZA-16),3-O-β-D-glucopyranosyl(1→4)-β-D-glucopyranosyl(1→3)-α-L-rhamnopyranosyl(1→2)-α-L-arabinopyranosyl oleanolic acid28-O-α-L-rhamnopyranosyl(1→4)-β-D-glucopyranosyl(1→6)-β-D-glucopyranoside(ZA-17),3-O-β-D-glucopyranosyl(1→3)-α-L-rhamnopyranosyl[β-D-glucopyranosyl-(1→4)]-(1→2)-α-L-a r a b i n o p y r a n o s y l o l e a n o l i c a c i d28-O-α-L-arabinopyranosyl(1→4)-β-D-glucopyranosyl(1→6)-β-D-glucopyranoside (ZA-18), syringin (ZA-19), elentheroside E (ZA-20),4-(1,2,3-trihydroxypropyl)-2,6-dimethoxyphenyl-1-O-β-D-glucopyranoside (ZA-21), coniferin (ZA-22). CompoundZA-1was a new compound. Compound ZA-1to ZA-6were originated from Astragalusmembranceus(Fisch) Bge, Compounds ZA-7to ZA-18were originated from Panaxginseng C.A.Mey, and Compounds ZA-19to ZA-22were originated fromAcanthopanax senticosus by LC-MS analysis.Chapter three: the efficacy enhancing and toxicity reducing effects of thosecompunds on tumor (SMMC-7721, U251, Hela) and normal (NRK, QSG-7701) cellswere tested by MTT method. The result show that the effective compounds wereastragaloside IV (ZA-2), astragaloside II (ZA-3), astragaloside I (ZA-4),ginsenoside-Rg1(ZA-9), ginsenoside-Rb1(ZA-12), ginsenoside-Rc (ZA-13),ginsenoside-Rb2(ZA-14), syringin (ZA-19), elentheroside E (ZA-20) and4-(1,2,3-trihydroxypropyl)-2,6-dimethoxyphenyl-1-O-β-D-glucopyranoside (ZA-21).Chapter four and five: to investigate "Chromatogram-effect" relationship of Panaxginseng and Astragalus membranceus. We established the method of contentdetermination of characteristic absorption band in Panax ginseng and Astragalusmembranceus, and the efficacy enhancing and toxicity reducing effects of extact ofPanax ginseng and Astragalus membranceus on tumor and normal cells were tested byMTT method. The "Chromatogram-effect" relationship was suggested to study thefoundation of effective compounds of AiDi injection. The foundation of effectivecompounds may be astragaloside IV (ZA-2), astragaloside II (ZA-3), astragaloside I(ZA-4), ginsenoside-Rb1(ZA-12), ginsenoside-Rc (ZA-13) and ginsenoside-Rb2(ZA-14).Chapter six: discussion.