摘要
COX-2是一种催化花生四烯酸转化为前列腺素的限速步骤的关键酶,在炎症过程中起着关键作用。与其他家族成员不同的是,COX-2在正常生理条件下几乎检测不到,而在人体对损伤或感染的急性炎症反应中具有很强的诱导性。因此,选择性COX-2抑制剂的治疗应用已经被认为是一种减少副作用的有效治疗炎症的方法。目前,传统的和新型的非甾体抗炎药都是通过靶向COX-2治疗炎症性疾病的常用处方药。然而,由于非甾体抗炎药的心血管副作用,寻找这些常用药物的合理替代品是药物化学研究的热点。据报道,天然化合物可抑制COX-2,从而对炎症和某些细胞损伤具有有益作用。本文综述了近年来COX-2抑制剂的天然产物及其衍生物及其结构核心支架的特点、抗炎作用、酶抑制的分子机制以及相关的构效关系。根据结构特征,天然COX-2抑制剂主要分为以下几类:天然酚类、黄酮类、芪类、萜类、醌类和生物碱类。除了抗炎活性外,一些天然来源的膳食COX-2抑制剂也通过靶向COX-2介导的癌变表现出化学预防作用。本文还讨论了这些天然药物在未来癌症预防中的应用。总之,对天然来源的COX-2抑制剂的研究为进一步开发更有效和选择性的COX-2抑制剂铺平了道路。
关键词: COX-2抑制剂,天然产物,黄酮类化合物,萜类化合物,构效关系,抗炎药,抗癌
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