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钩藤真菌内生菌胶孢炭疽菌的次生代谢产物及其PI3K抑制活性

Secondary Metabolites and PI3K Inhibitory Activity of Colletotrichum gloeosporioides, a Fungal Endophyte of Uncaria rhynchophylla.

作者信息

Yang Zhong-Duo, Li Zhi-Jie, Zhao Jun-Wen, Sun Jian-Hui, Yang Li-Jun, Shu Zong-Mei

机构信息

School of Life Science and Engineering, Lanzhou University of Technology, 287 Lan Gong Pin Road, Qi Li He Block, Lanzhou, 730050, Gansu Province, People's Republic of China.

The Provincial Education Key Laboratory of Screening, Evaluation and Advanced Processing of Traditional Chinese Medicine and Tibetan Medicine, School of Life Science and Engineering, Lanzhou University of Technology, Lanzhou, 730050, People's Republic of China.

出版信息

Curr Microbiol. 2019 Jul;76(7):904-908. doi: 10.1007/s00284-019-01707-7. Epub 2019 May 18.

Abstract

In the present study, nine compounds (1-9) were isolated from Colletotrichum gloeosporioides (an endophytic fungus from Uncaria rhynchophylla) which was cultured in wheat bran medium. Their structures were elucidated as 4-Epi-14-hydroxy-10, 23-dihydro-24, 25-dehydroaflavinine (1), 10, 23-Dihydro-24,25 -dehydro-21-oxoaflavinine (2), Ergosterol (3), Ergosterol peroxide (4), Mellein (5), 4, 5-dihydroblumenol A (6), Colletotrichine A (7), Cyclo(L-leucyl-L-leucyl) (8), and Brevianamide F (9) based on NMR spectral data, as well as comparing with previous literature data. This is the first report about the isolation of compounds 1-2, 6, and 8-9 from Colletotrichum genus. All compounds were tested for their phosphoinositide 3-kinase (PI3Kα) inhibitory activity. Compounds 8 and 9 showed potent PI3K α inhibitory activity with IC values of 38.1 and 4.8 µM, respectively, while the other compounds showed very weak activity at a concentration of 20 µg/mL.

摘要

在本研究中,从培养于麦麸培养基中的胶孢炭疽菌(钩藤内生真菌)中分离出9种化合物(1 - 9)。基于核磁共振光谱数据并与先前文献数据比较,确定它们的结构分别为4 - 表 - 14 - 羟基 - 10, 23 - 二氢 - 24, 25 - 脱氢阿弗菌素(1)、10, 23 - 二氢 - 24, 25 - 脱氢 - 21 - 氧代阿弗菌素(2)、麦角甾醇(3)、麦角甾醇过氧化物(4)、蜜环菌素(5)、4, 5 - 二氢布鲁门醇A(6)、炭疽菌素A(7)、环(L - 亮氨酰 - L - 亮氨酰)(8)和短杆菌肽F(9)。这是首次从炭疽菌属中分离出化合物1 - 2、6以及8 - 9的报道。对所有化合物进行了磷酸肌醇3 - 激酶(PI3Kα)抑制活性测试。化合物8和9表现出较强的PI3Kα抑制活性,IC值分别为38.1和4.8 μM,而其他化合物在20 μg/mL浓度下表现出非常弱的活性。

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