New analogues of brefeldin A from sediment-derived fungus Penicillium sp DT-F29

New analogues of brefeldin A from sediment-derived fungus Penicillium sp DT-F29
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DOI:
10.1080/14786419.2016.1169414
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发表时间:
2016-01-01
影响因子:
2.2
通讯作者:
Ma, Zhong-Jun
Ma, Zhong-Jun
中科院分区:
化学3区
文献类型:
--
作者:
Hu, Zhi-Fei;Qin, Le-Le;Ma, Zhong-Jun

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从沉积物来源的真菌青霉菌的发酵中分离出布雷菲德菌素 A 的四种新类似物,名为 7、7-二甲氧基布雷菲德菌素 C (3)、6-羟基布雷菲德菌素 C (4)、4-epi-15-表-布雷菲德菌素 A (5)、4-epi-8-羟基-15-表-布雷菲德菌素 C (6),以及四种已知类似物 (1、7-9) sp。 DT-F29。这些化合物的结构是在广泛的光谱和化学方法的基础上阐明的。在生物活性测定中,仅化合物1和8对人肺腺癌细胞表现出显着的抑制活性。此外,化合物 1 首次被报道具有重新激活潜伏 HIV 的强大能力,EC50 值为 0.03M。[图表]
Four new analogues of brefeldin A named 7, 7-dimethoxybrefeldin C (3), 6-hydroxybrefeldin C (4), 4-epi-15-epi-brefeldin A (5), 4-epi-8-hydroxy-15-epi-brefeldin C (6), together with four known analogues (1, 7-9) were isolated from a fermentation of the sediment-derived fungus Penicillium sp. DT-F29. The structures of these compounds were elucidated on the basis of extensive spectroscopic and chemical methods. In the bioactivity assays, only compounds 1 and 8 showed significant inhibitory activities against human lung adenocarcinoma cell. In addition, compound 1 was first reported for the potent ability to reactivate latent HIV with EC50 value of 0.03M.[GRAPHICS]