【摘 要】
：
药物与受体的相互作用研究对于揭示药物体内作用的生物学过程具有重要意义，亦是生命科学、化学和临床药理学等领域的热点研究问题之一。β2-肾上腺素受体(β2-AR)是广泛分布于肺和支气管平滑肌的一类受体。本论文采用β2-AR亲和色谱法筛选了黄连的活性成分，并用该法对黄连中盐酸小檗碱和盐酸药根碱与AR的相互作用进行了深入研究。该研究有望为中药活性成分的筛选提供新方法，揭示上述两种生物碱与皮.AR的相互作用机制，对阐明其体内作用的生物学基础具有重要意义。全文共分3章，作者的主要贡献如下： 一、采用β2-A
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药物与受体的相互作用研究对于揭示药物体内作用的生物学过程具有重要意义，亦是生命科学、化学和临床药理学等领域的热点研究问题之一。β2-肾上腺素受体(β2-AR)是广泛分布于肺和支气管平滑肌的一类受体。本论文采用β2-AR亲和色谱法筛选了黄连的活性成分，并用该法对黄连中盐酸小檗碱和盐酸药根碱与AR的相互作用进行了深入研究。该研究有望为中药活性成分的筛选提供新方法，揭示上述两种生物碱与皮.AR的相互作用机制，对阐明其体内作用的生物学基础具有重要意义。全文共分3章，作者的主要贡献如下： 一、采用β2-AR亲和色谱法对黄连水提取物中的活性成分进行了筛选，发现黄连中与β2-AR有特异性作用的活性成分为盐酸小檗碱、盐酸药根碱和盐酸巴马汀等生物碱类物质，有望为中药等复杂体系中药物活性成分的高效筛选提供新途径。 二、用竞争洗脱法，研究了黄连中两种异喹啉类生物碱盐酸小檗碱和盐酸药根碱与固定化β2-AR的相互作用机制，结果表明：盐酸小檗碱与β2-AR 存在一类结合位点，结合常数为2.17×104/M，疏水力是结合过程的主要推动力；盐酸药根碱与β2-AR存在一类作用位点，结合常数为2.54x104/M，氢键或范德华力是结合过程的主要推动力；两种生物碱在β2-AR亲和色谱柱上竞争同一类作用位点。上述研究证明β2-AR亲和色谱能用于研究药物与受体等蛋白的相互作用机制。
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