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NF-κB Inhibitory and Antibacterial Helvolic and Fumagillin Derivatives from Aspergillus terreus.
Journal of Natural Products ( IF 5.1 ) Pub Date : 2020-03-12 , DOI: 10.1021/acs.jnatprod.9b01190
Kh Ahammad Uz Zaman 1 , Zhenquan Hu 2, 3 , Xiaohua Wu 1 , Shaobin Hou 4 , Jennifer Saito 4 , Tamara P Kondratyuk 1 , John M Pezzuto 1, 5 , Shugeng Cao 1
Affiliation  

Two new helvolic acid analogues (1 and 2) and one new fumagillin derivative containing an octahydroisobenzofuran moiety (3), together with four known compounds (47), were isolated from an Aspergillus terreus, isolated from soil collected from Mauna Kea, the highest mountain in Hawaii. Compound 4 was recorded in SciFinder with a CAS Registry Number of 1379525-35-5, but it was not documented in the cited reference (ACS Chem. Biol. 2012, 7, 137). The structures of compounds 14 were elucidated by NMR spectroscopy and HRMS and ECD analysis. Compounds 5 and 6 showed significant inhibitory activity against NF-κB with IC50 values of 2.7 ± 2.6 and 6.5 ± 0.8 μM, respectively. Compounds 1 and 2 were active against S. aureus with MICs of 6.25 and 6.25 μg/mL, respectively, while compound 5 inhibited E. coli with an MIC of 3.12 μg/mL.

中文翻译:

来自土曲霉的 NF-κB 抑制和抗菌 Helvolic 和 Fumagillin 衍生物。

从土曲霉中分离出两种新的海藻酸类似物(12)和一种含有八氢异苯并呋喃部分的新烟曲霉素衍生物(3),以及四种已知化合物(47)夏威夷最高的山峰。化合物4记录在 SciFinder 中,CAS 登记号为 1379525-35-5,但未记录在引用的参考文献中 ( ACS Chem. Biol . 2012 , 7 , 137)。化合物的结构1 - 4通过核磁共振光谱和 HRMS 和 ECD 分析阐明。化合物56对 NF-κB 显示出显着的抑制活性,IC 50值分别为 2.7 ± 2.6 和 6.5 ± 0.8 μM。化合物12金黄色葡萄球菌具有活性,MIC 分别为 6.25 和 6.25 μg/mL,而化合物5抑制大肠杆菌,MIC 为 3.12 μg/mL。
更新日期:2020-04-24
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