Harry Perkins Institute of Medical Research, QEII Medical Centre, Nedlands and Centre for Medical Research, The University of Western Australia, Crawley, Western Australia 6009, Australia.
Biomedical Research Institute (IRB Lleida). Research Group of Cancer Biomarkers, 25198 Lleida, Spain.
Biomolecules. 2020 Feb 6;10(2):248. doi: 10.3390/biom10020248.
The marine environment represents an outstanding source of antitumoral compounds and, at the same time, remains highly unexplored. Organisms living in the sea synthesize a wide variety of chemicals used as defense mechanisms. Interestingly, a large number of these compounds exert excellent antitumoral properties and have been developed as promising anticancer drugs that have later been approved or are currently under validation in clinical trials. However, due to the high need for these compounds, new methodologies ensuring its sustainable supply are required. Also, optimization of marine bioactives is an important step for their success in the clinical setting. Such optimization involves chemical modifications to improve their half-life in circulation, potency and tumor selectivity. In this review, we outline the most promising marine bioactives that have been investigated in cancer models and/or tested in patients as anticancer agents. Moreover, we describe the current state of development of anticancer marine compounds and discuss their therapeutic limitations as well as different strategies used to overcome these limitations. The search for new marine antitumoral agents together with novel identification and chemical engineering approaches open the door for novel, more specific and efficient therapeutic agents for cancer treatment.
海洋环境代表了抗肿瘤化合物的重要来源,但同时也有很大的探索空间。生活在海洋中的生物合成了各种各样的化学物质,用作防御机制。有趣的是,这些化合物中的很大一部分具有出色的抗肿瘤特性,并已被开发为有前途的抗癌药物,这些药物后来已获得批准或正在临床试验中进行验证。然而,由于对这些化合物的高度需求,需要确保其可持续供应的新方法。此外,海洋生物活性物质的优化是其在临床环境中取得成功的重要步骤。这种优化涉及化学修饰以提高其在循环中的半衰期、效力和肿瘤选择性。在这篇综述中,我们概述了在癌症模型中进行了研究和/或作为抗癌剂在患者中进行了测试的最有前途的海洋生物活性物质。此外,我们描述了抗癌海洋化合物的当前开发状态,并讨论了它们的治疗局限性以及用于克服这些局限性的不同策略。寻找新的抗肿瘤海洋药物以及新的鉴定和化学工程方法为癌症治疗开辟了新的、更特异和更有效的治疗药物的大门。