Osirisynes G-I, New Long-Chain Highly Oxygenated Polyacetylenes from the Mayotte Marine Sponge Haliclona sp.
Osirisynes G-I, New Long-Chain Highly Oxygenated Polyacetylenes from the Mayotte Marine Sponge Haliclona sp.
复制标题
DOI：
10.3390/md18070350
复制
发表时间：
2020-07-01
期刊：
影响因子：
5.4
通讯作者：
Gauvin-Bialecki, Anne
中科院分区：
文献类型：
--
作者：
Campos, Pierre-Eric;Herbette, Gaetan;Gauvin-Bialecki, Anne
海绵CH_2Cl_2-MeOH（1：1）提取物的化学研究在马约特收集的研究强调了三种新的长链高度氧化的聚乙炔，奥西里斯烯G-I（1-3）以及已知的奥西里斯烯A（4）、B（5）和E（6）。通过1D和2D NMR谱、HRESIMS和MS/MS数据鉴定了它们的结构。对所有化合物的过氧化氢酶和沉默调节蛋白1活化以及CDK 7、蛋白酶体、Fyn激酶、酪氨酸酶和弹性蛋白酶抑制进行评价。五个化合物（1;3-6）抑制蛋白酶体激酶，两个化合物（5-6）抑制CDK 7和Fyn激酶。Osirisyne B（5）是最具活性的化合物，对FYNB激酶、CDK 7激酶和蛋白酶体抑制的IC（50）分别为18.44 μ M、9.13 μ M和0.26 μ M。
Chemical study of the CH2Cl2-MeOH (1:1) extract from the spongeHaliclonasp. 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 IC(50)on FYNB kinase, CDK7 kinase, and proteasome inhibition of 18.44 mu M, 9.13 mu M, and 0.26 mu M, respectively.