Osirisynes G-I, New Long-Chain Highly Oxygenated Polyacetylenes from the Mayotte Marine Sponge Haliclona sp

Osirisynes GI,来自马约特岛海洋海绵 Haliclona sp 的新型长链高氧聚乙炔

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作者:Pierre-Eric Campos, Gaëtan Herbette, Christophe Chendo, Patricia Clerc, Florent Tintillier, Nicole J de Voogd, Eleni-Dimitra Papanagnou, Ioannis P Trougakos, Moran Jerabek, Jérôme Bignon, Géraldine Le Goff, Jamal Ouazzani, Anne Gauvin-Bialecki

Abstract

Chemical study of the CH2Cl2-MeOH (1:1) extract from the sponge Haliclona sp. collected in Mayotte highlighted three new long-chain highly oxygenated polyacetylenes, osirisynes G-I (1-3) together with the known osirisynes A (4), B (5), and E (6). Their structures were elucidated by 1D and 2D NMR spectra and HRESIMS and MS/MS data. All compounds were evaluated on catalase and sirtuin 1 activation and on CDK7, proteasome, Fyn kinase, tyrosinase, and elastase inhibition. Five compounds (1; 3-6) inhibited proteasome kinase and two compounds (5-6) inhibited CDK7 and Fyn kinase. Osirisyne B (5) was the most active compound with IC50 on FYNB kinase, CDK7 kinase, and proteasome inhibition of 18.44 µM, 9.13 µM, and 0.26 µM, respectively.

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