cE3c-Centre for Ecology, Evolution and Environmental Changes/Azorean Biodiversity Group & Faculty of Sciences and Technology, University of Azores, Rua Mãe de Deus, 9501-321 Ponta Delgada, Portugal.
Department of Chemistry & QOPNA-Organic Chemistry, Natural Products and Food Stuffs, University of Aveiro, Campus de Santiago, 3810-193 Aveiro, Portugal.
Int J Mol Sci. 2018 Jan 16;19(1):263. doi: 10.3390/ijms19010263.
Cancer is a multistage process resulting in an uncontrolled and abrupt division of cells and is one of the leading causes of mortality. The cases reported and the predictions for the near future are unthinkable. Food and Drug Administration data showed that 40% of the approved molecules are natural compounds or inspired by them, from which, 74% are used in anticancer therapy. In fact, natural products are viewed as more biologically friendly, that is less toxic to normal cells. In this review, the most recent and successful cases of secondary metabolites, including alkaloid, diterpene, triterpene and polyphenolic type compounds, with great anticancer potential are discussed. Focusing on the ones that are in clinical trial development or already used in anticancer therapy, therefore successful cases such as paclitaxel and homoharringtonine (in clinical use), curcumin and ingenol mebutate (in clinical trials) will be addressed. Each compound's natural source, the most important steps in their discovery, their therapeutic targets, as well as the main structural modifications that can improve anticancer properties will be discussed in order to show the role of plants as a source of effective and safe anticancer drugs.
癌症是一个多阶段的过程,导致细胞失控和突然分裂,是导致死亡的主要原因之一。目前报告的病例和对近期的预测是难以想象的。美国食品和药物管理局的数据显示,40%的批准分子是天然化合物或受其启发的化合物,其中 74%用于癌症治疗。事实上,天然产物被认为更具有生物友好性,对正常细胞的毒性更小。在这篇综述中,讨论了具有巨大抗癌潜力的最新和最成功的次生代谢物案例,包括生物碱、二萜、三萜和多酚类化合物。重点介绍那些处于临床试验开发或已用于癌症治疗的案例,因此将涉及紫杉醇和高三尖杉酯碱(临床使用)、姜黄素和 ingenol mebutate(临床试验)等成功案例。将讨论每个化合物的天然来源、发现过程中的重要步骤、它们的治疗靶点,以及可以提高抗癌特性的主要结构修饰,以展示植物作为有效和安全抗癌药物的来源的作用。