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NF-κB 抑制和抗菌海洛因和黄曲霉素衍生物来自.

NF-κB Inhibitory and Antibacterial Helvolic and Fumagillin Derivatives from .

机构信息

Department of Pharmaceutical Sciences, Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, Hilo, Hawaii 96720, United States.

Warshel Institute for Computational Biology, The Chinese University of Hong Kong, Shenzhen, People's Republic of China.

出版信息

J Nat Prod. 2020 Mar 27;83(3):730-737. doi: 10.1021/acs.jnatprod.9b01190. Epub 2020 Mar 12.

DOI:10.1021/acs.jnatprod.9b01190
PMID:32163285
Abstract

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

摘要

从夏威夷莫纳克亚山采集的土壤中分离得到的,分离得到了两种新的海夫洛酸类似物(和)和一种含有八氢异苯并呋喃部分的新的腐霉酮衍生物(),以及四种已知化合物(-)。化合物在 SciFinder 中记录的 CAS 注册号为 1379525-35-5,但在引用的参考文献(,,137 中没有记载。通过 NMR 光谱和 HRMS 和 ECD 分析阐明了化合物 - 的结构。化合物 和 对 NF-κB 表现出显著的抑制活性,IC 值分别为 2.7 ± 2.6 和 6.5 ± 0.8 μM。化合物 和 对 具有 MIC 值为 6.25 和 6.25 μg/mL 的活性,而化合物 对 的 MIC 值为 3.12 μg/mL。

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