Panax Quinquefolius Saponin Combination Of Catalytic Hydrogenation Of Its Product Research

Panax quinquefolium L is a kind of valuable tradition drug. It is generally believed that the major bioactive components of it are the ginsenosides. A systematic literature investigation on chemistry and pharmacology of ginsenosides was made in this article, gotten acquainted with the latest research trends in the field. It has been reported to possess of bioactivity in alter cancer cell proliferation, induce apoptosis, and perturb normal cell cycle events, show potential clinical value in cancer therapy.With the deep-going research, problems turn up:Ginsenosides are highly hydrolyzed in acidic conditions as easily as they can, cyclize and change into their epimer ,which maybe influence its o.p. bioavailability and curative effect. Furthermore, the content of ginsenoside-Rg3 and ginsenoside-Rh2 which have strong bioactivity in anti-tumor are low from total ginsenosides. In addition, the bioactivities in anti-tumor are influenced by structure of nuclear parent, the sequence from strong to soft is oleanane>panaxadiol>panaxatriol; in ginsenosides with single glycosyl chain, they were affected by the numbers of glycosyls, the sequence from strong to soft is aglycon>single glycosyl >double glycosyls>three glycosyls>four glycosyls.Researches we have carried out systematically from five aspects: (1) The research in catalytic hydrogenation combinatorial chemistry of ginsenosides. Firstly, ginsenosides-Rb1 and ginsenoside-Re were catalyltic hydrogenated as substrate to established reaction technique, and got two compounds: I, II. Then, total ginsenosides were combinatorial hydrogenated to construct combinatorial compounds storage (GH). (2) The research in combinatorial hydrolyzation of GH. The storage of aglycons and ginsenosides (PH) with stronger anti-tumor activity by the way of controlling the condition were prepared.(3) Established separation methods of column chromatogram and thin-layer chromatogram to separate GH and PH: Silica gel H as stationary phase, BEW(4:1:5) as mobile phase, prepared compounds I, II, III; Inverse C18 as stationary phase,70% ethanol as mobile phase, prepared compound IV; Compound V was prepared with centrifugal thin-layer chromatography. (4) Research in identification of production. Their structures were elucidated by spectroscopic methods, including TLC, HPLC-ELSD, ESI-MS, 1H-NMR., 13C-NMR, DEPT.They are 3β,6β,12β-trihydroxy-3- O-[β-D-glucopyranosyl(2--1)-β-D-glucopyranoside]-20-O-[β-D-glucopyranosyl(6--1) -β-D-glucopyranoside]-20(s)-dammarane;3β,6β,12β-trihydroxy-3-O-[β-D-glucopyranosyl(2--1)-α-L-rhamnose]-20-O-[β-D-glucopyranoside]-20(R)-dammarane;3β,6β,12β- trihydroxy-20(s)-dammarane-20-O-[β-D-glucopyranoside];3β,6β,12β-trihydroxy dammar-20(22)-ene; 3β,6β,12β,20-tetrahydroxy-20(R)-dammarane. (5) Analysis ofhydrolyzed ginsenosides by HPLC-ELSD methods was established. Ethyl cyanide and water as mobile phase gradient eluted. 0～35min,29%～32%B;35～57min,32%B~40%B;57~80min,40%B. Every constituent can be separated from baseline.We established combinatorial chemistry to modify ginsenosides for the first time, established analytic methods of column chromatogram and thin-layer chromatogram, and prepared five compounds: I,II,III,IV,V, they are all new compounds. In addition we established analytic methods of HPLC-ELSD, which provided theoretic base for the research of ginsenosides.