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撤稿文章:海洋生物碱衍生物及类似物的合成与生物活性

Retracted Article: The synthesis and biological activity of marine alkaloid derivatives and analogues.

作者信息

Zhou Shiyang, Huang Gangliang

机构信息

Chongqing Key Laboratory of Green Synthesis and Application, Active Carbohydrate Research Institute, College of Chemistry, Chongqing Normal University Chongqing 401331 China

Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education, College of Chemistry and Chemical Engineering, Hainan Normal University Haikou Hainan 571158 China.

出版信息

RSC Adv. 2020 Aug 28;10(53):31909-31935. doi: 10.1039/d0ra05856d. eCollection 2020 Aug 26.

Abstract

The ocean is the origin of life, with a unique ecological environment, which has given birth to a wealth of marine organisms. The ocean is an important source of biological resources and tens of thousands of monomeric compounds have been separated from marine organisms using modern separation technology. Most of these monomeric compounds have some kind of biological activity that has attracted extensive attention from researchers. Marine alkaloids are a kind of compound that can be separated from marine organisms. They have complex and special chemical structures, but at the same time, they can show diversity in biological activities. The biological activities of marine alkaloids mainly manifest in the form of anti-tumor, anti-fungus, anti-viral, anti-malaria, and anti-osteoporosis properties. Many marine alkaloids have good medicinal prospects and can possibly be used as anti-tumor, anti-viral, and anti-fungal clinical drugs or as lead compounds. The limited amounts of marine alkaloids that can be obtained by separation, coupled with the high cytotoxicity and low selectivity of these lead compounds, has restricted the clinical research and industrial development of marine alkaloids. Marine alkaloid derivatives and analogues have been obtained rational drug design and chemical synthesis, to make up for the shortcomings of marine alkaloids; this has become an urgent subject for research and development. This work systematically reviews the recent developments relating to marine alkaloid derivatives and analogues in the field of medical chemistry over the last 10 years (2010-2019). We divide marine alkaloid derivatives and analogues into five types from the point-of-view of biological activity and elaborated on these activities. We also briefly discuss the optimization process, chemical synthesis, biological activity evaluation, and structure-activity relationship (SAR) of each of these compounds. The abundant SAR data provides reasonable approaches for the design and development of new biologically active marine alkaloid derivatives and analogues.

摘要

海洋是生命的起源,拥有独特的生态环境,孕育了丰富的海洋生物。海洋是生物资源的重要来源,利用现代分离技术已从海洋生物中分离出数以万计的单体化合物。这些单体化合物大多具有某种生物活性,引起了研究人员的广泛关注。海洋生物碱是一类可从海洋生物中分离得到的化合物。它们具有复杂而特殊的化学结构,但同时在生物活性方面表现出多样性。海洋生物碱的生物活性主要表现为抗肿瘤、抗真菌、抗病毒、抗疟疾和抗骨质疏松等特性。许多海洋生物碱具有良好的药用前景,有可能用作抗肿瘤、抗病毒和抗真菌的临床药物或先导化合物。然而,通过分离获得的海洋生物碱数量有限,加之这些先导化合物的细胞毒性高、选择性低,限制了海洋生物碱的临床研究和产业发展。通过合理的药物设计和化学合成获得海洋生物碱衍生物和类似物,以弥补海洋生物碱的不足,这已成为亟待研发的课题。本文系统综述了过去10年(2010 - 2019年)医学化学领域中海洋生物碱衍生物和类似物的最新研究进展。我们从生物活性的角度将海洋生物碱衍生物和类似物分为五类,并阐述了这些活性。我们还简要讨论了每种化合物的优化过程、化学合成、生物活性评价和构效关系(SAR)。丰富的SAR数据为设计和开发具有新生物活性的海洋生物碱衍生物和类似物提供了合理的途径。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/853b/9056551/2a5cf04633e0/d0ra05856d-f1.jpg

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