小陷胸汤药效物质基础及配伍机理的研究

项目名称： 小陷胸汤药效物质基础及配伍机理的研究

项目编号： No.30873368

项目类型： 面上项目

立项/批准年度： 2009

项目学科： 轻工业、手工业

项目作者： 裴月湖

作者单位： 沈阳药科大学

项目金额： 35万元

中文摘要： 小陷胸汤始载于张仲景的《伤寒论》，由瓜楼实、黄连和半夏三味中药组成，其制法是先煎瓜楼实，然后再用瓜楼实煎煮液煎煮黄连和半夏。通过本项目的研究表明用瓜楼实煎煮液煎煮黄连可使黄连主要有效成分的溶出增加48%，煎煮黄连和半夏可使黄连主要有效成分的溶出增加41%，半夏无此作用。同时亦可大大增加黄连主要有效成分的吸收和在血液中的浓度。并通过HPLC-MS和与对照品对照的方法阐明了溶出和吸收增加的成分是黄连中的5个主要生物碱类成分。瓜楼实中能增加黄连生物碱溶出、吸收的有效部位是正丁醇提取物和剩余的水溶液，有效部位中的有效成分是一系列DEA类成分（共分离获得9个该类成分）。DEA类成分不仅可增加黄连中主要生物碱的溶出、吸收，而且还能增加大分子化合物的吸收，同时与黄连中的主要有效成分亦有协同作用。对瓜楼实、黄连和半夏三味中药中的成分进行了系统研究，共从中分离鉴定了109个单体化合物，其中新化合物9个，新天然产物2个；从瓜楼实中分离获得的2个新化合物具有免疫抑制作用，推断是小陷胸汤中抗炎的有效成分之一。上述研究结果不仅证实了小陷胸汤制法的科学性，同时亦揭示了该方配伍的科学内涵。

中文关键词： 小陷胸汤；瓜楼实；黄连；半夏；中药复方

英文摘要： Xiao Xianxiong Tang, first recorded in Treatise on Febrile Diseases written by Zhang Zhongjing was compoused of trichosanthis, coptis chinensis and pinellia.We proved that the dissolution rate of the main constituents of coptis chinensis would increase 48% when using the decoction of trichosanthis to extract and the number would be 41% when coptis chinensis and pinellia were extracted together, which could inrease the concentration of the main constituents,five alkaloid determined by HPLC-MS of coptis chinensis in blood. The constituent of trichosanthis which could increase the dissolution and absoption of coptis chinensis is the BuOH extract as well as the water fraction are DEA(9 DEA compounds was isolated). DEA constituent could also increase the absoption of macromolecular. Nine new compounds, two new natural compounds and totally 109 compounds were isolated from trichosanthis, coptis chinensis and pinellia. The two new compounds isolated from trichosanthis showed the bioactivity of immunosuppression, which was considered to be the active constituent of antiinflammatory in Xiao Xianxiong Tang. The results above indicated that the procedure of Xiao Xianxiong Tang is scientific.

英文关键词： Xiao Xianxiong Tang; trichosanthis; coptis chinensis; pinellia;chinese herbal prescription