射干的化学成分研究及其药动学初步探索

【作者】 伍实花；

【导师】 张国刚；

【作者基本信息】 沈阳药科大学 ， 天然药物化学， 2008， 硕士

【摘要】 射干是鸢尾科射干属植物射干Belamcanda Chinensis（L.）DC的干燥根茎,为常用中药,具有抗炎、止咳、祛痰等作用。近年来很多国家对其化学成分、药理作用进行了大量深入的研究,进一步阐明了射干临床疗效的内在基础,并在此基础上研发新药和保健用品,已取得相关专利和成果。这充分说明了射干具有确切的作用,前景令人乐观,值得进行深入研究。本文从化学成分及其药动学上对其进行研究与探索。射干中含有丰富的异黄酮,且具有多种药理活性,本文利用硅胶柱色谱,聚酰胺柱色谱,凝胶柱色谱,高效液相色谱,重结晶等多种分离手段对射干的乙醇提取物进行分离,从中分离得到14个化合物。通过波谱解析及理化方法鉴定了其中10个化合物的化学结构。其中异黄酮类化合物5个,甾体类化合物2个,生物碱类化合物1个,三萜类化合物1个,小分子类化合物1个。分别为:次野鸢尾黄素（irisflorentin 1）,白射干素（dichotomitin 2）,野鸢尾黄素（irigenin 3）,鸢尾苷元（tectorigenin 4）,3′,5′-二甲氧基鸢尾素-4′-O-β-D-葡萄糖苷（3′,5′-dimethoxy irisolone-4′-O-β-D-glucoside 5）,β-胡萝卜苷（β-daucosterol 6）,β-谷甾醇（β-sitosterol 7）,尿嘧啶核苷（uridine 8）,环阿尔廷醇（cycloartanol9）,罗布麻宁（apocynin 10）,其中化合物9为首次从该属植物中分离得到的已知化合物。建立了测定大鼠血浆中次野鸢尾黄素含量的RP-HPLC方法,以芹菜素为内标,采用C₁₈色谱柱,甲醇-水（60:40 v/v）为流动相,流速1.0 ml/min,检测波长265 nm。结果未检测到样品,对射干中异黄酮类化合物的药动学特征有了初步的了解,为进一步研制中药复方制剂的药动学行为奠定了基础。更多还原

【Abstract】 The rhizome of Belamcanda chinensis （L.） DC that belongs to Iridacea, It has been used in Chinese herbs for the treatment of antitussive antiinflammatory and expectorant. It has been studied in many countries, on its pharmacological effects. From the results, the innate bases of its clinical effects are clarified further more, according to which, people developed many new medicines and health products. Those strongly speak volumes for its exact effects, and good prospects, so it is worthy of doing further studies on it. The author has investigated and explored the chemical constitutes and pharmacokinetics.The rhizome of Belamcanda chinensis （L.） DC is rich in isoflavonoids, and they have many pharmacological effects. 14 compounds from the ethanol extraction were isolated by silica gel, polyamide, Sephadex LH-20, HPLC, recrystallizing. On the basis of NMR, and measuring physic-chemical characters, 10 chemical structures were elucidated as irisflorentin （1）,dichotomitin（2）,irigenin（3）,tectorigenin （4）, 3’,5’-dimethoxy irisolone-4’-O-β-D-glucoside （5）,β-daucosterol（6）,β-sitosterol（7）, uridine（8）, cycloartanol（9）, apocynin（10）, respectively. Of all these compounds, compound 9 was isolated for the first time from Belamcanda,RP-HPLC method has been developed to determine irisflorentin in rat plasma. Irisflorentin and apigenin （an internal standard） were extracted from plasma using liquid-liquid extraction with acetoacetate, they were separated on a C₁₈ column. Using a mixture of methanol-water （60:40, v/v） as the mobile phase at a flow rate of 1.0 ml/min with UV detection at 265 nm. The Results show that the sample has not been detected. Preliminary understanding the features of pharmacokinetics of isoflavonoids from Belamcanda chinensis （L.） DC. It laid the foundation for future development of the Pharmacokinetics acts of Chinese medicine compound preparation.更多还原