Tetramic acid derivatives and polyphenols from sponge-derived fungus and their biological evaluation |
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Authors: | Jun-Feng Wang Xiaochu Qin Fu-Quan Xu Tianyu Zhang Shengrong Liao Xiuping Lin |
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Institution: | 1. CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, RNAM Center for Marine Microbiology, Chinese Academy of Sciences, Guangzhou 510301, P.R. China;2. Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, P.R. China;3. Jiangsu Key Laboratory of Marine Biotechnology, Huaihai Institute of Technology, Lianyungang 222005, P.R. China |
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Abstract: | Fifteen compounds, including two tetramic acid derivatives, penicillenol A1 (1) and penicillenol A2 (2), six polyphenols containing both phenolic bisabolane sesquiterpenoid and diphenyl ether units, expansols A–F (3–8), together with six phenolic bisabolane sesquiterpenoids (9–14) and diorcinol (15), were isolated from the fermentation broth of the marine-derived fungus ZSDS1-F11 isolated from the sponge Phakellia fusca Thiele collected in the Yongxing island of Xisha. Their structures were elucidated mainly by using extensive NMR spectroscopic and mass spectrometric analyses. Compounds 3–5, 7 and 8 showed potent COX-1 inhibitory activity with IC50 values of 5.3, 16.2, 30.2, 41.0 and 56.8 μM, respectively. Meanwhile, compounds 3–8 showed potent COX-2 inhibitory activity with IC50 values of 3.1, 5.6, 3.0, 5.1, 3.2 and 3.7 μM, respectively. In addition, compound 1 exhibited antituberculosis activity with 96.1% inhibition at concentration of 10 μM. |
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Keywords: | marine fungus Phakellia fusca Thiele tetramic acid polyphenol anti-inflammatory activity antituberculosis activity |
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