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从海洋链霉菌VITSVK5菌株中提取的5-(2,4-二甲基苄基)吡咯烷-2-酮对人类真菌和细菌病原体的体外活性。

In vitro activity of 5-(2,4-dimethylbenzyl) pyrrolidin-2-one extracted from marine Streptomyces VITSVK5 spp. against fungal and bacterial human pathogens.

作者信息

Saurav Kumar, Kannabiran K

机构信息

Biomolecules and Genetics Division, School of Biosciences and Technology VIT University, Vellore, Tamil Nadu, India.

出版信息

Rev Iberoam Micol. 2012 Jan-Mar;29(1):29-33. doi: 10.1016/j.riam.2011.06.008. Epub 2011 Jul 5.

Abstract

BACKGROUND

Pharmacological screening and usage of natural products for the treatment of human diseases has had a long history from traditional medicine to modern drugs. The majority of modern drugs are reported to be mostly from natural products.

OBJECTIVE

The aim of the present study was to evaluate the inhibitory activity of 5-(2,4-dimethylbenzyl) pyrrolidin-2-one (DMBPO) extracted from marine Streptomyces VITSVK5 spp. isolated from sediment samples collected at Marakkanam coast of Bay of Bengal, India.

METHODS

The lead compound was isolated by bioactive guided extraction and purified by silica gel column chromatography. Structural elucidation of the lead compound was carried out by using UV, FT-IR, (1)H NMR, (13)C NMR, DEPT and HR-MS spectral data.

RESULTS

Systematic screening of isolates for antimicrobial activity lead to identification of a potential strain, Streptomyces VITSVK5 spp. (GQ848482). Bioactivity guided extraction yielded a compound DMBPO and its inhibitory activity was tested against selected bacterial and fungal strains. DMBPO showed maximal activity against Escherichia coli with a MIC value of 187 μg/ml, followed by Klebsiella pneumoniae (MIC of 220 μg/ml and 10.3mm zone of inhibition), Staphylococcus aureus (MIC of >1000 μg/ml and 4.4mm zone of inhibition) and Bacillus subtilis (MIC of 850 μg/ml and 2.6mm zone of inhibition). Furthermore, DMBPO was found to be a potent inhibitor of opportunistic fungal pathogens too. It showed a maximum activity against Aspergillus niger with a MIC value of 1 μg/ml and 28 mm zone of inhibition.

CONCLUSION

The result of this study indicates that DMBPO possess antibiotic activity to selected bacterial and fungal pathogens and exhibited better activity against fungi than bacteria.

摘要

背景

从传统医学到现代药物,天然产物用于治疗人类疾病的药理筛选和应用已有悠久历史。据报道,大多数现代药物主要来源于天然产物。

目的

本研究旨在评估从印度孟加拉湾马勒卡纳姆海岸采集的沉积物样本中分离出的海洋链霉菌VITSVK5 spp. 所提取的5-(2,4-二甲基苄基)吡咯烷-2-酮(DMBPO)的抑制活性。

方法

通过生物活性导向提取分离出先导化合物,并通过硅胶柱色谱法进行纯化。利用紫外光谱、傅里叶变换红外光谱、氢核磁共振谱、碳核磁共振谱、无畸变极化转移增强谱和高分辨质谱光谱数据对先导化合物进行结构解析。

结果

对分离株进行抗菌活性的系统筛选,鉴定出一株潜在菌株,链霉菌VITSVK5 spp.(GQ848482)。生物活性导向提取得到一种化合物DMBPO,并对其针对选定的细菌和真菌菌株的抑制活性进行了测试。DMBPO对大肠杆菌表现出最大活性,最低抑菌浓度(MIC)值为187μg/ml,其次是肺炎克雷伯菌(MIC为220μg/ml,抑菌圈直径为10.3mm)、金黄色葡萄球菌(MIC>1000μg/ml,抑菌圈直径为4.4mm)和枯草芽孢杆菌(MIC为850μg/ml,抑菌圈直径为2.6mm)。此外,DMBPO也被发现是机会性真菌病原体的有效抑制剂。它对黑曲霉表现出最大活性,MIC值为1μg/ml,抑菌圈直径为28mm。

结论

本研究结果表明,DMBPO对选定的细菌和真菌病原体具有抗菌活性,且对真菌的活性优于细菌。

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