| 3 | Griseofulvin enantiomers and bromine-containing griseofulvin derivatives with antifungal activity produced by the mangrove endophytic fungus Nigrospora sp.QQYB1显示文摘Marine microorganisms have long been recognized as potential sources for drug discovery.Griseofulvin was one of the first antifungal natural products and has been used as an antifungal agent for decades.In this study,12 new griseofulvin derivatives[(±)-1-2,(+)-3,(±)-4,10-12,and 14-15]and two new griseofulvin natural products(9 and 16)together with six known analogues[(-)-3,5-8,and 13]were isolated from the mangrove-derived fungus Nigrospora sp.QQYB1 treated with 0.3%NaCl or 2%NaBr in rice solid medium.Their 2D structures and absolute configurations were established by extensive spectroscopic analysis(1D and 2D NMR,HRESIMS),ECD spectra,computational calculation,DP4+analysis,and X-ray single-crystal diffraction.Compounds 1-4 represent the first griseofulvin enantiomers with four absolute configurations(2S,6'S;2R,6'R;2S,6'R;2R,6'S),and compounds 9-12 represent the first successful production of brominated griseofulvin derivatives from fungi via the addition of NaBr to the culture medium.In the antifungal assays,compounds 6 and 9 demonstrated significant inhibitory activities against the fungi Colletotrichum truncatum,Microsporum gypseum,and Trichophyton mentagrophyte with inhibition zones varying between 28 and 41 mm(10μg/disc).The structure-activity relationship(SAR)was analyzed,which showed that substituents at C-6,C-7,C-6'and the positions of the carbonyl and double bond of griseofulvin derivatives significantly affected the antifungal activity. | Ge Zou Wencong Yang Tao Chen Zhaoming Liu Yan Chen Taobo Li Gulab Said Bing Sun Bo Wang Zhigang She | 2024 | Marine Life Science & Technology2024，6，1： | 0 |
| 4 | 海洋天然产物geodin系列衍生物的细胞毒活性评价及构效关系初步研究显示文摘目的评价具有grisan骨架的海洋天然产物geodin(1)及其衍生物(2~26)细胞毒活性,探究其初步构效关系。方法采用MTT法,用人非小细胞肺癌细胞系A549和人肝癌细胞系HepG2、Bel-7402对geodin(1)及其衍生物(2~26)进行了细胞毒活性评价。结果对geodin的4-OH修饰后得到的衍生物中,化合物2~4、6、7、9~18和20~25表现出强到中等程度的细胞毒活性,IC_(50)为0.81~4.78μmol/L。特别是化合物16,对A549和HepG2细胞表现出强效的细胞毒活性,其IC50分别为0.86、0.81μmol/L。结论化合物16是1种潜在的抗癌先导化合物。 | 许颖 陈露 程相成 SAID Gulab 王翠芳 徐同毅 邵长伦 | 2023 | 中国海洋药物2023，42，5： | 0 |
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