Antimicrobial and cytotoxic activities

  • 文章类型: Journal Article
    SumalarinsD-G(1-4),四种先前未描述的卷曲素衍生物,以及两种已知的相关代谢物,curvularin(5)和脱氢curvularin(6),从红树林衍生的真菌summatrense青霉MA-325中分离并鉴定。其中,sumalarinD(1)代表具有5-甲基呋喃-2-基甲基基团的curvularin衍生物的独特实例。根据对NMR和MS数据的分析以及对ECD光谱和NMR的量子化学计算的比较,阐明了它们的结构。和化合物1通过X射线晶体学分析证实。化合物1、2、5和6对水生致病菌溶藻弧菌和哈氏弧菌具有活性,MIC值为4至64μg/mL,而化合物6对肿瘤细胞系5673、HCT116、786-O具有细胞毒性,和Hela,IC50值为3.5、10.6、10.9和14.9μM,分别。
    Sumalarins D-G (1-4), four previously undescribed curvularin derivatives, along with two known related metabolites, curvularin (5) and dehydrocurvularin (6), were isolated and identified from the mangrove-derived fungus Penicillium sumatrense MA-325. Among them, sumalarin D (1) represents a unique example of curvularin derivative featuring a 5-methylfuran-2-yl-methyl group. Their structures were elucidated based on analysis of NMR and MS data as well as comparison of ECD spectra and quantum chemical calculations of NMR, and compound 1 was confirmed by X-ray crystallographic analysis. Compounds 1, 2, 5, and 6 are active against aquatic pathogenic bacteria Vibrio alginolyticus and V. harveyi with MIC values ranging from 4 to 64 μg/mL, while compound 6 is cytotoxic against tumor cell lines 5673, HCT 116, 786-O, and Hela with IC50 values of 3.5, 10.6, 10.9, and 14.9 μM, respectively.
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  • 文章类型: Journal Article
    A highly potent secondary metabolite producing endophytic strain, Streptomyces sp. HUST012 was isolated from the stems of the medicinal plant Dracaena cochinchinensis Lour. Strain HUST012 showed antimicrobial and antitumor activities which were significantly much higher than those of dragon\'s blood extracted from D. cochinchinensis Lour. On further analysis, the strain was found to produce two metabolites, SPE-B11.8 (elucidated to be a novel metabolite (Z)-tridec-7-ene-1,2,13-tricarboxylic acid) and SPE-B5.4 (elucidated as Actinomycin-D). The Minimum Inhibitory Concentration values of SPE-B11.8 against a set of test bacterial organisms (Methicillin-resistant Staphylococcus epidermis ATCC 35984, Methicillin-resistant Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, and Klebsiella pneumoniae ATCC 13883) ranged between 15.63 and 62.5 μg/ml while that for SPE-B5.4 ranged between 0.04 and 2.24 μg/ml. The compound SPE-B11.8 showed cytotoxic effect at 41.63 and 29.54 μg/ml IC 50-values against Hep G2 and MCF-7, respectively, while the compound SPE-B5.4 exhibited stronger activities against them at 0.23 and 0.18 μg/ml IC 50-values.
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