Graduate School of Environmental Science, Hokkaido University, Sapporo 060-0810, Japan.
Department of Marine Chemistry, Faculty of Marine Sciences, King Abdulaziz University, P.O. Box 80207, Jeddah 21589, Saudi Arabia.
Molecules. 2020 Sep 1;25(17):3986. doi: 10.3390/molecules25173986.
Cyanobacteria are reported as rich sources of secondary metabolites that provide biological activities such as enzyme inhibition and cytotoxicity. Ten depsipeptide derivatives (lyngbyabellins) were isolated from a Malaysian and a Red Sea sp.: lyngbyabellins G (), O (), P (), H (), A (), 27-deoxylyngbyabellin A (), and homohydroxydolabellin (). This study indicated that lyngbyabellins displayed cytotoxicity, antimalarial, and antifouling activities. The isolated compounds were tested for cytotoxic effect against human breast cancer cells (MCF7), for antifouling activity against barnacle larvae, and for antiplasmodial effect towards . Lyngbyabellins A and G displayed potent antiplasmodial effect against , whereas homohydroxydolabellin showed moderate effect. For antifouling activity, the side chain decreases the activity slightly, but the essential feature is the acyclic structure. As previously reported, the acyclic lyngbyabellins are less cytotoxic than the corresponding cyclic ones, and the side chain increases cytotoxicity. This study revealed that lyngbyabellins, despite being cytotoxic agents as previously reported, also exhibit antimalarial and antifouling activities. The unique chemical structures and functionalities of lyngbyabellin play an essential role in their biological activities.
蓝藻被报道为次生代谢产物的丰富来源，这些代谢产物提供了酶抑制和细胞毒性等生物活性。从马来西亚和红海的两种蓝藻中分离得到了十种环肽衍生物（海兔肽）：lyngbyabellin G（）、O（）、P（）、H（）、A（）、27-去氧lyngbyabellin A（）和 homohydroxydolabellin（）。本研究表明，海兔肽具有细胞毒性、抗疟原虫和抗污损活性。分离得到的化合物被测试了对人乳腺癌细胞（MCF7）的细胞毒性、对藤壶幼虫的抗污损活性以及对 的抗疟原虫活性。lyngbyabellin A 和 G 对 表现出很强的抗疟原虫活性，而 homohydroxydolabellin 则表现出中等活性。对于抗污损活性，侧链略微降低了活性，但基本特征是无环结构。如前所述，无环海兔肽的细胞毒性比相应的环状海兔肽低，而侧链则增加了细胞毒性。本研究表明，尽管海兔肽以前被报道为细胞毒性剂，但它们也表现出抗疟原虫和抗污损活性。海兔肽独特的化学结构和功能在其生物活性中起着重要作用。
