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Halistanol sulfates I and J, new SIRT1-3 inhibitory steroid sulfates from a marine sponge of the genus Halichondria.
The Journal of Antibiotics ( IF 3.3 ) Pub Date : 2018-Feb-01 , DOI: 10.1038/ja.2017.145
Fumiaki Nakamura , Norio Kudo , Yuki Tomachi , Akiko Nakata , Misao Takemoto , Akihiro Ito , Hodaka Tabei , Daisuke Arai , Nicole de Voogd , Minoru Yoshida , Yoichi Nakao , Nobuhiro Fusetani

Two new analogs of halistanol sulfate (1) were isolated from a marine sponge Halichondria sp. collected at Hachijo-jima Island. Structures of these new halistanol sulfates I (2) and J (3) were elucidated by spectral analyses. Compounds 1-3 showed inhibitory activity against SIRT 1-3 with IC50 ranges of 45.9-67.9, 18.9-21.1 and 21.8-37.5 μM, respectively. X-ray crystallography of the halistanol sulfate (1) and SIRT3 complex clearly indicates that 1 binds to the exosite of SIRT3 that we have discovered in this study.

中文翻译:

卤代醇硫酸盐I和J,新的SIRT1-3抑制性类固醇硫酸盐,来自嗜盐菌属的海洋海绵。

从海海绵Halichondria sp。分离到了两个新的硫酸卤代阿司他汀(1)类似物。收集在八丈岛。通过光谱分析阐明了这些新的硫酸金丝胺醇I(2)和J(3)的结构。化合物1-3对SIRT 1-3表现出抑制活性,IC 50范围分别为45.9-67.9、18.9-21.1和21.8-37.5μM。硫酸卤代阿司他汀(1)和SIRT3配合物的X射线晶体学清楚表明,1与我们在本研究中发现的SIRT3的外位结合。
更新日期:2017-11-29
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