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Flavonoids from the Genus Euphorbia: Isolation, Structure, Pharmacological Activities and Structure–Activity Relationships

机译:来自大戟属的黄酮类药物:分离,结构,药理活动和结构 - 活动关系

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摘要

Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as d-glucose, l-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.
机译:大戟属的植物广泛分布在南美洲,亚洲和非洲的温带,热带和亚热带地区,建立了阿育吠陀,中国和马来的民族语料记录。本综述报告了2000 - 2012年期间邻近覆盖的异常疗法的分离,发生,植物化学,生物学性质,治疗潜力和结构 - 活性关系,同时识别潜在的未来研究领域,旨在从这些植物开发新的治疗剂。结果表明,提取物和分离的黄酮类化合物具有抗癌,抗增殖,抗疟疾,抗菌,抗炎症,抗炎症,抗肝炎和抗氧化特性,并具有不同的对癌细胞的作用机制。在研究的物种中,已分离出超过80种不同类型的黄酮类化合物。大多数分离的类黄酮是黄酮醇,并包含简单的O替代图案,C-甲基化和戊烯化。其他有糖苷,糖苷键和在C-3或C-7上附着的碳水化合物,并指定为D-葡萄糖,L-鼻窦或葡糖酚。结构 - 活性关系研究表明,C-3或C-7上的羟基甲基化减少了活性,而糖基化失去活性,并且父母骨骼结构对于保留活性至关重要。因此,这些成分可以为新的大戟类的治疗剂提供潜在的替代支架。

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