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Characterization of Biomolecules with Antibiotic Activity from Endophytic Fungi Phomopsis Species

机译:生物分子的特征来自内生真菌的抗生素活性

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摘要

Recently, growing interest is devoted to investigation of bioactive secondary metabolites of endophytic fungi. Thus, as an extension to our previous achievements related to antimicrobial potential of endophytic fungi, Phomopsis species isolated from conifer needles was selected as appropriately promising natural source for drug discovery. Its dichloromethane and ethanol extracts considerably inhibited growth of Escherichia coli and Staphylococcus aureus. Moreover, the individual compounds of dichloromethane extract have been separated, collected and purified using semi preparative liquid chromatographic analysis and comprehensively characterized using mass spectrometry (MS) and nuclear magnetic resonance spectroscopy (NMR). Based on their antimicrobial activity and unique structural characteristics in comparison with well-established drugs from the same therapeutic category, two dominant compounds (Z)-(Z)-2-acetoxyprop-1en-1-yl-3-(3-((E)-3,4-dihydroxypent-1-en-1-yl)oxiran-2-yl)acrylate (denoted as 325-3) and (Z)-(Z)-2-acetoxyprop-1en-1-yl 3-(3-((E)-4-hydroxy-3-oxopent-1-en-1-yl)oxiran-2-yl)acrylate (denoted as 325-5) were recognized as valuable leading structures for future discovery of novel antibiotics.
机译:最近,致力于调查生物活性二次代谢物的生物活性次生真菌的兴趣。因此,作为我们以前与内生真菌的抗微生物潜力相关的成果的延伸,选择从针叶树针中分离的Phomopsis物种作为药物发现的适当有前途的自然来源。其二氯甲烷和乙醇提取物显着抑制大肠杆菌和金黄色葡萄球菌的生长。此外,使用半制备液相色谱分析分离,收集和纯化的二氯甲烷提取物的各个化合物,并使用质谱(MS)和核磁共振光谱(NMR)全面表征。基于其抗微生物活性和独特的结构特征,与来自同一治疗类别的良好的药物相比,两个优势化合物(Z) - (Z)-2-乙酰氧基-1en-1-Y1-3-(3 - (( e)-3,4-二羟基型-1-烯-1-烯烃)氧化乙烷-2-基)丙烯酸酯(表示为325-3)和(Z) - (Z)-2-乙酰氧基-1en-1-Y13 - (3 - (((E)-4-羟基-3-氧化-1-烯-1-烯-1-烯)丙烯酸酯(表示为325-5)被认为是有价值的领先结构,以便未来发现小说抗生素。

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