Department of Chemistry & QOPNA-Organic Chemistry, Natural Products and Food Stuffs, University of Aveiro, Campus de Santiago, 3810-193 Aveiro, Portugal.
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.
Mar Drugs. 2018 Oct 26;16(11):410. doi: 10.3390/md16110410.
Isolation, finding or discovery of novel anticancer agents is very important for cancer treatment, and seaweeds are one of the largest producers of chemically active metabolites with valuable cytotoxic properties, and therefore can be used as new chemotherapeutic agents or source of inspiration to develop new ones. Identification of the more potent and selective anticancer components isolated from brown, green and red seaweeds, as well as studies of their mode of action is very attractive and constitute a small but relevant progress for pharmacological applications. Several researchers have carried out in vitro and in vivo studies in various cell lines and have disclosed the active metabolites among the terpenoids, including carotenoids, polyphenols and alkaloids that can be found in seaweeds. In this review the type of metabolites and their cytotoxic or antiproliferative effects will be discussed additionally their mode of action, structure-activity relationship and selectivity will also be revealed. The diterpene dictyolactone, the sterol cholest-5-en-3β,7α-diol and the halogenated monoterpene halomon are among the reported compounds, the ones that present sub-micromolar cytotoxicity. Additionally, one dimeric sesquiterpene of the cyclolaurane-type, three bromophenols and one halogenated monoterpene should be emphasized because they exhibit half maximal inhibitory concentration (IC) values between 1⁻5 µM against several cell lines.
分离、寻找或发现新型抗癌药物对于癌症治疗非常重要,海藻是具有有价值细胞毒性的化学活性代谢产物的最大生产者之一,因此可以用作新的化疗药物或开发新药物的灵感来源。从褐藻、绿藻和红藻中分离出更有效和更具选择性的抗癌成分,并研究其作用模式非常有吸引力,这是药理学应用方面的一个小但相关的进展。一些研究人员已经在各种细胞系中进行了体外和体内研究,并披露了海藻中存在的萜类化合物(包括类胡萝卜素、多酚和生物碱)中的活性代谢物。在这篇综述中,将讨论代谢物的类型及其细胞毒性或抗增殖作用,以及它们的作用模式、构效关系和选择性。报道的化合物包括二萜二帖内酯、甾醇胆甾-5-烯-3β,7α-二醇和卤代单萜卤代物,它们具有亚微摩尔级别的细胞毒性。此外,还应强调一种环芳烃型二倍半萜、三种溴酚和一种卤代单萜,因为它们对几种细胞系的半数最大抑制浓度 (IC) 值在 1⁻5µM 之间。