Department of Pharmacology, Faculty of Pharmacy, Erciyes University, Kayseri, Turkey.
Drug Application and Research Center, Erciyes University, Kayseri, Turkey.
Anticancer Agents Med Chem. 2020;20(15):1797-1816. doi: 10.2174/1871520620666200310094646.
Coumarins are the secondary metabolites of some plants, fungi, and bacteria. Coumarins and the hybrid molecules of coumarins are the compounds which have been widely studied for their potential anticancer effects. They belong to benzopyrone chemical class, more precisely benzo-α-pyrones, where benzene ring is fused to pyrone ring. In nature, coumarins are found in higher plants like Rutaceae and Umbelliferae and some essential oils like cinnamon bark oil, cassia leaf oil and lavender oil are also rich in coumarins. The six main classes of coumarins are furanocoumarins, dihydrofuranocoumarins, pyrano coumarins, pyrone substituted coumarins, phenylcoumarins and bicoumarins. As well as their wide range of biological activities, coumarins and the hybrid molecules of coumarins are proven to have an important role in anticancer drug development due to the fact that many of its derivatives have shown an anticancer activity on various cell lines. Osthol, imperatorin, esculetin, scopoletin, umbelliprenin, angelicine, bergamottin, limettin, metoxhalen, aurapten and isopimpinellin are some of these coumarins. This review summarizes the anticancer effects of coumarins and their hybrid molecules including the novel pharmaceutical formulations adding further information on the topic for the last ten years and basically focusing on the structureactivity relationship of these compounds in cancer.
香豆素是一些植物、真菌和细菌的次生代谢产物。香豆素及其杂交分子是具有潜在抗癌作用的研究热点化合物。它们属于苯并吡喃化学类，更准确地说是苯并-α-吡喃酮，其中苯环与吡喃酮环融合。在自然界中，香豆素存在于芸香科和伞形科等高等植物中，肉桂皮油、桂皮叶油和薰衣草油等一些精油也富含香豆素。香豆素主要有六大类：呋喃香豆素、二氢呋喃香豆素、吡喃香豆素、吡喃酮取代香豆素、苯基香豆素和双香豆素。由于香豆素及其杂交分子具有广泛的生物活性，并且其许多衍生物在各种细胞系中表现出抗癌活性，因此它们在抗癌药物开发中被证明具有重要作用。蛇床子素、欧前胡素、花椒毒素、瑞香素、umbelliprenin、当归酸、佛手柑素、柠檬烯、metoxhalen、aurapten 和异佛手柑素等都是香豆素的衍生物。本文综述了香豆素及其杂交分子的抗癌作用，包括新的药物制剂，并在过去十年中对该主题进行了补充，主要集中在这些化合物在癌症中的结构-活性关系。
