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Secondary Metabolites Isolated from Perovskia Atriplicifolia and their in vitro Binding Affinity for Human Opioid and Cannabinoid Receptors

机译:从钙钛矿分离的次生代谢产物及其对人阿片和大麻素受体的体外结合亲和力

摘要

Plants and their natural products have been utilized for thousands of years in the treatment of many human diseases. Because of their structural diversity, natural products are ideal lead compounds for drug development. In this thesis, the natural products of the plant Perovskia atriplicifolia were investigated, specifically their in vitro binding affinity to receptors in opioid and cannabinoid classes. Extracts that demonstrated good selective opioid and cannabinoid receptor binding were subjected to bioassay-guided fractionation. Four active compounds were identified from the crude extract in Perovskia atriplicifolia: 1) 5-hydroxy-3’,4’,6,7-tetramethoxy flavone, 2) 5,7-dihydroxy-3’,4’,6,-trimethoxy flavone, 3) 5-hydroxy-4’,6,7-trimethoxy flavone, and 4) 5,7-dihydroxy-4’,6,-dimethoxy flavone. Each compound exhibited good selective δ-opioid receptor binding affinity and was characterized as a flavanoid. ud
机译:植物及其天然产物已经在许多人类疾病的治疗中使用了数千年。由于其结构的多样性,天然产物是药物开发的理想先导化合物。本文研究了植物三叶草的天然产物,特别是它们对阿片类和大麻素类受体的体外结合亲和力。对表现出良好的选择性阿片类药物和大麻素受体结合作用的提取物进行生物测定指导的分离。从三叶草中的粗提物中鉴定出四种活性化合物:1)5-羟基-3',4',6,7-四甲氧基黄酮,2)5,7-二羟基-3',4',6,-三甲氧基黄酮,3)5-羟基-4',6,7-三甲氧基黄酮和4)5,7-二羟基-4',6,-二甲氧基黄酮。每种化合物均表现出良好的选择性δ阿片受体结合亲和力,并被表征为类黄酮。 ud

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    Fitzpatrick Ashli;

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  • 年度 2015
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  • 原文格式 PDF
  • 正文语种 en
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