医学ppt课件消化系统药物_2.ppt

Development From Schisandra chinensis (五味子) In the early of 1970s, discover that it lower SGPT Alcohol extract from its fruit kernel, “Schizandrol”（五味子醇，健肝灵） tablet go on the market. serum glutamic-pyruvic transaminase Deoxyschizandrin γ-Schizandrin Schizandrin Aomisin Pseudo-γ-Schizandrin Schisantherin A Neoschisandrin Schisandrol Schisantherin Development of Bifendate No activity Development Intermediate of γ-schisandrin C, Bifendate go on the market 1970s Initial research 1975 1977 1983 Synthesized, and found it hepatoprotective effect Use in clinic Develop new form of drop pill In 1995, accepted in pharmacopoeia Physico-chemical property Characteristic ultraviolet absorption of diphenyl 278±1nm, used for qualitative and quantitative analysis. Hydroxamic acid iron salt test, produce purple product. To check Carboxyl derivatives. Quantitative determination is the formation of a red-purple colouration when chromotropic acid in 75% sulfuric acid reacts with formaldehyde. The colouration is specific to this aldehyde (not produced from ketones and carboxylic acids). chromotropic acid Formaldehyde Chromotropic acid methylenedioxy Conc.H2SO4 formaldehyde Pharmacologic action Lower the activity of Serum Glutamic-Pyruvate Transaminase (SGPT, 血清谷丙转氨酶) , and reinforce the antitoxic function of liver. Clinic： Curative effect is instable GPT may go up after withdrawal, but also down with administration again persistent hepatitis (PH, 迁延性肝炎) GPT(谷丙转氨酶)abnormality for long term Liu Geng-tao Chemical synthesis Ullmann Reaction Methyl Gallate Analogue of Bifendate OH Bicyclol Bifendate Launched in 2001 (百赛诺) Silibinin (水飞蓟宾, 益肝灵) (2R,3R)-3,5,7-trihydroxy-2-[(2R,3R)-3-(4-hydroxy-3-methoxyphenyl)-2-(hydroxymethyl)-2,3-dihydrobenzo[b][1,4]dioxin-6-yl]chroman-4-one Silibinin in clinic It is extracted Silybum marianum(水飞蓟草). It has hepatoprotective properties that protect liver cells against toxins. It has also demonstrated anti-cance