Antifouling phenyl ethers and other compounds from the invertebrates and their symbiotic fungi collected from the South China Sea.
Antifouling phenyl ethers and other compounds from the invertebrates and their symbiotic fungi collected from the South China Sea.
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来自无脊椎动物及其共生真菌从南中国海收集的抗染料苯醚和其他化合物。
DOI：
10.1186/s13568-016-0272-2
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发表时间：
2016-12
期刊：
影响因子：
3.7
通讯作者：
Wang CY
中科院分区：
文献类型：
--
作者：
Wang CY;Wang KL;Qian PY;Xu Y;Chen M;Zheng JJ;Liu M;Shao CL;Wang CY
海洋生物源次级代谢产物是发现环境安全的代谢物的潜在来源。本研究对55种海洋次生代谢产物及其衍生物进行了生物活性和安全性评价。这些化合物包括44种从南海海洋无脊椎动物及其共生微生物中分离得到的天然产物和11种结构修饰产物。从2种珊瑚、1种海绵和5种共生真菌中分离得到了天然次生代谢产物，包括苯醚类、萜类、9，11-开环甾类、蒽醌类、生物碱类、核苷类和肽类等。所有分离和合成的化合物进行了测试，其对藤壶藤壶（Amphibalanus）amphitrite达尔文的cyprids的活性。值得注意的是，5个苯基醚衍生物（9，11，13-15）表现出有效的抗幼虫沉降活性，其EC 50值低于3.05 μM，LC 50/EC 50比值高于15。构效关系（SAR）研究表明，苯醚衍生物中乙酰氧基和溴原子的引入可显著提高其抗肿瘤活性。这是首次报道苯醚类化合物对藤壶B的构效关系。安菲里特多溴联苯醚衍生物2，4，6，2′，4′，6′-六溴二间苯二酚（13）具有良好的生物活性，是一种很有前途的环境友好型生物降解剂。本文的在线版本（doi：10.1186/s13568-016-0272-2）包含补充材料，可供授权用户使用。
Marine organism-derived secondary metabolites are promising potential sources for discovering environmentally safe antifouling agents. In present study, 55 marine secondary metabolites and their synthesized derivatives were tested and evaluated for their antifouling activities and security. These compounds include 44 natural products isolated from marine invertebrates and their symbiotic microorganisms collected from the South China Sea and 11 structural modified products derived from the isolated compounds. The natural secondary metabolites, covering phenyl ether derivatives, terpenoids, 9, 11-secosteroids, anthraquinones, alkaloids, nucleoside derivatives and peptides, were isolated from two corals, one sponge and five symbiotic fungi. All of the isolated and synthesized compounds were tested for their antifouling activities against the cyprids of barnacle Balanus (Amphibalanus) amphitrite Darwin. Noticeably, five phenyl ether derivatives (9, 11, 13–15) exhibited potent anti-larval settlement activity with the EC50 values lower than 3.05 μM and the LC50/EC50 ratios higher than 15. The study of structure–activity relationship (SAR) revealed that the introduction of acetoxy groups and bromine atoms to phenyl ether derivatives could significantly improve their antifouling activities. This is the first report on the SAR of phenyl ether derivatives on antifouling activity against barnacle B. amphitrite. The polybrominated diphenyl ether derivative, 2, 4, 6, 2′, 4′, 6′-hexabromo-diorcinol (13), which displayed excellent antifouling activity, was considered as a promising candidate of environmentally friendly antifouling agents. The online version of this article (doi:10.1186/s13568-016-0272-2) contains supplementary material, which is available to authorized users.
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