Seven novel linear polyketides,talaketides A-G(1-7),were isolated from the rice media cultures of the mangrove sed-iment-derived fungus Talaromyces sp.SCSIO 41027.Among these,talaketides A-E(1-5)represented unpreceden...Seven novel linear polyketides,talaketides A-G(1-7),were isolated from the rice media cultures of the mangrove sed-iment-derived fungus Talaromyces sp.SCSIO 41027.Among these,talaketides A-E(1-5)represented unprecedented unsaturated lin-ear polyketides with an epoxy ring structure.The structures,including absolute configurations of these compounds,were elucidated through detailed analyses of nuclear magnetic resonance(NMR)and high-resolution mass spectrometry(HR-MS)data,as well as elec-tronic custom distributors(ECD)calculations.In the cytotoxicity screening against prostate cancer cell lines,talaketide E(5)demon-strated a dose-dependent inhibitory effect on prostate cancer PC-3 cell lines,with an IC50 value of 14.44 μmol·L-1.Moreover,com-pound 5 significantly inhibited the cloning formation of PC-3 cell lines and arrested the cell cycle in S-phase,ultimately inducing ap-optosis.These findings indicate that compound 5 may serve as a promising lead compound for the development of a potential treat-ment for prostate cancer.展开更多
文摘为了研究柱状角孔珊瑚(Goniopora columna)水螅体的次级代谢产物,采用硅胶柱层析、凝胶柱层析及半制备高效液相色谱对柱状角孔珊瑚水螅体粗提物中次级代谢产物进行分离纯化,利用现代波谱技术鉴定其结构,并对获得的次级代谢产物进行非小细胞肺癌A549细胞(non-small cell lung cancer A549 cells, NSCLC)的抗癌活性筛选。结果表明,从柱状角孔珊瑚水螅体中分离鉴定出8种化合物,分别为alkalgoniopora A (1)、茶碱(2)、胸腺嘧啶脱氧核糖核苷(3)、尿嘧啶(4)、胸腺嘧啶(5)、pregna-5,20-dien-3β-ol(6)、cinnamicacid(7)和原儿茶酸(8),其中化合物1为新发现的生物碱。初步细胞毒活性测试显示,化合物1、2和6对NSCLC增殖有较弱的抑制活性,其余化合物对NSCLC增殖无明显抑制活性。
基金supported by the Key-Area Research and Development Program of Guangdong Province(No.2023B1111050008)the National Natural Science Foundation of China(Nos.U23A20528,U20A20101)+1 种基金Guangdong Local Innovation Team Program(No.2019BT02Y262)the Postdoctoral Fellowship Program of CPSF(No.GZC20232777).
文摘Seven novel linear polyketides,talaketides A-G(1-7),were isolated from the rice media cultures of the mangrove sed-iment-derived fungus Talaromyces sp.SCSIO 41027.Among these,talaketides A-E(1-5)represented unprecedented unsaturated lin-ear polyketides with an epoxy ring structure.The structures,including absolute configurations of these compounds,were elucidated through detailed analyses of nuclear magnetic resonance(NMR)and high-resolution mass spectrometry(HR-MS)data,as well as elec-tronic custom distributors(ECD)calculations.In the cytotoxicity screening against prostate cancer cell lines,talaketide E(5)demon-strated a dose-dependent inhibitory effect on prostate cancer PC-3 cell lines,with an IC50 value of 14.44 μmol·L-1.Moreover,com-pound 5 significantly inhibited the cloning formation of PC-3 cell lines and arrested the cell cycle in S-phase,ultimately inducing ap-optosis.These findings indicate that compound 5 may serve as a promising lead compound for the development of a potential treat-ment for prostate cancer.
