title: Tetramic acid derivatives and polyphenols from sponge-derived fungus and their biological evaluation.
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.
authors.affiliation: a 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.
authors.forename: Jun-Feng
authors.initials: JF
authors.lastname: Wang
authors.forename: Xiaochu
authors.initials: X
authors.lastname: Qin
authors.forename: Fu-Quan
authors.initials: FQ
authors.lastname: Xu
authors.forename: Tianyu
authors.initials: T
authors.lastname: Zhang
authors.forename: Shengrong
authors.initials: S
authors.lastname: Liao
authors.forename: Xiuping
authors.initials: X
authors.lastname: Lin
authors.forename: Bin
authors.initials: B
authors.lastname: Yang
authors.forename: Juan
authors.initials: J
authors.lastname: Liu
authors.forename: Lishu
authors.initials: L
authors.lastname: Wang
authors.forename: Zhengchao
authors.initials: Z
authors.lastname: Tu
authors.forename: Yonghong
authors.initials: Y
authors.lastname: Liu
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000737:chemistry / Q000302:isolation & purification; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000302:isolation & purification; D005285:Fermentation; D005658:Fungi / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D059808:Polyphenols / Q000737:chemistry* / Q000302:isolation & purification; D011161:Porifera / Q000382:microbiology*; D011760:Pyrrolidinones / Q000737:chemistry* / Q000302:isolation & purification
chemical_list: D000995:Antitubercular Agents; D016861:Cyclooxygenase Inhibitors; D059808:Polyphenols; D011760:Pyrrolidinones; C575093:penicillenol A1; C575092:penicillenol A2; C009435:tetramic acid
keywords: Phakellia fusca Thiele; anti-inflammatory activity; antituberculosis activity; marine fungus; polyphenol; tetramic acid