大黄饮片炮制前后物质基础变化规律研究

目的:通过对大黄生、熟、炭等3种常用饮片化学成分及生物活性的比较研究,揭示饮片炮制前后物质基础的变化规律。方法:采用有机溶剂提取及多种柱色谱分离技术,对掌叶大黄进行系统的化学成分研究,在此基础上对大黄3种饮片进行HPLC指纹图谱定性和主要化学成分的定量分析,并以空白饮片为载体的组分填充模拟炮制方法,进行大黄饮片炮制前后物质基础变化规律的验证。结果:从掌叶大黄共分离鉴定34个化合物,其中4个为新化合物。2个检测波长HPLC指纹图谱及17个主要化学成分的含量比较结果证实,熟大黄、大黄炭与生大黄相比变化显著,泻下作用代表成分蒽醌苷总量分别降低了55%和95%,相反,蒽醌苷元总量分别增加了75%和46%。另外,熟大黄和大黄炭中没食子酸的含量显著增加,分别为生大黄2.4倍和1.3倍。泻下和解热药理实验结果显示生大黄作用最强,而熟大黄和大黄炭基本无泻下作用。结论:通过大黄饮片炮制前后化学成分变化规律的分析,结合饮片主要药理作用的比较,证实基于传统药性理论的苦寒药性是按照生大黄、熟大黄、大黄炭的顺序逐步减弱,基于现代药效学研究的泻下作用强度也按同样的顺序逐步降低。其变化规律与其缩合鞣质、蒽醌苷、苯丁酮苷类化合物含量的递减,没食子酸、蒽醌苷元类化合物含量的变化紧密相关,基本揭示了其药性变化与化学成分变化的相关性。

Study on the variation rules of material basis of Rhubarb after processing

Objective: To reveal the variation rules of Rhubarb after processing,according to comparison of chemical constituents and biological activities in three commonly used pieces from Rhubarb.Methods: we conducted a systematic chemical study on Rheum palmatum L.by organic solvent extraction and chromatographic separation.The HPLC fingerprint and the content of main constituents were used to qualitative and quantitative evaluation respectively.At the same time,a new simulation processing method were used to verify the variation of Rhubarb before and after processing which was taking the blank pieces as the carrier and filled in different chemical constituents.Results: There were thirty-four compounds identified from Rheum palmatum L.including four new compounds.The HPLC fingerprint in two detection wavelengths and the contents of 17 main chemical components among five pieces indicated that the changes were significantly in the braising with liquor and the charring pieces compare with the crude pieces.The content of anthraquinone glycosides were reduced by 55% and 95%,while the total anthraquinone aglycones increased by 75% and 46% in the braising with liquor and the charring pieces.In addition,the content of gallic acid was sharply increased about 2.4 times in the braising pieces.Diarrhea and antipyretic pharmacological experiments showed that the crude pieces have the strongest purgative and febrifuge effect;on the contrary,the braised and the charred pieces had no diarrhea effect.Conclusion: The "bitter and cold" property of Rhubarb is gradually decreased from crude pieces,braising with liquor to charring pieces by the chemical and biological analysis.Meanwhile,the diarrhea intensity which based on the modern pharmacodynamic study is gradually reduced by the same order.The change rules are closely related to the decrease in compound tanning,anthraquinone glucoside,butyrophenone glucoside and the increase in gallic acid,anthraquinone compounds.It has revealed relevance between the property change and the chemical composition changes.