首页> 外文期刊>Current Science: A Fortnightly Journal of Research >Microbial transformation of (+)-heraclenin by Aspergillus niger and evaluation of its antiplasmodial and antimicrobial activities.
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Microbial transformation of (+)-heraclenin by Aspergillus niger and evaluation of its antiplasmodial and antimicrobial activities.

机译:黑曲霉对(+)-heraclenin的微生物转化及其抗疟原虫和抗菌活性的评估。

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摘要

Microbial transformation of (+)-heraclenin (1) by Aspergillus niger was studied in growth media to assess its antiplasmodial and antimicrobial activities. It was transformed to (-)-heraclenol (2) as the sole product in a stereospecific manner. The in vitro antiplasmodial activity of compounds 1 and 2 was tested with chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Further, the in vitro antibacterial activity of 1 and 2 against three Grampositive bacteria, Bacillus subtilis, Bacillus sphaericus and Staphylococcus aureus, and three Gram-negative bacteria, Pseudomonas aeruginosa, Escherichia coli and Chromobacterium violaceum was analysed using agar-plate diffusion assay. The same method was employed for the evaluation of antifungal activity against five pathogenic strains of fungi, A. niger, Rhizopus oryzae, Aspergillus flavus, Candida albicans and Saccharomyces cerevisiae. Both furanocoumarins 1 and 2 displayed significant levels of antiplasmodial and moderate levels of antimicrobial activities against the tested pathogenic strains. Compound 2 exhibited two-fold less potent antiplasmodial activity (IC50=6.0 micro g/ml) than the parent compound 1 (IC50=2.5 micro g/ml), whereas no difference was observed in the antimicrobial activity of both furanocoumarins. The oxirane ring was found to be beneficial in terms of antiplasmodial activity.
机译:在生长培养基中研究了黑曲霉对(+)-heraclenin(1)的微生物转化,以评估其抗血浆和抗菌活性。以立体有择的方式将其转化为(-)-海伦醇(2)作为唯一产物。用对氯喹敏感和耐氯喹的恶性疟原虫菌株测试了化合物1和2的体外抗血浆活性。此外,1和2对三种革兰氏阳性细菌枯草芽孢杆菌,球形芽孢杆菌和金黄色葡萄球菌的体外抗菌活性。使用琼脂平板扩散分析法分析了i>和三种革兰氏阴性细菌,分别为铜绿假单胞菌,大肠埃希氏菌和紫罗兰色杆菌。使用相同的方法评估针对五种真菌病原菌 A的抗真菌活性。尼日尔,米根瘤菌,黄曲霉,白色念珠菌和酿酒酵母。呋喃香豆素1和2均显示出显着水平的抗血浆和中等水平的抗微生物活性。化合物2的抗血浆活性(IC 50 = 6.0 micro g / ml)比母体化合物1(IC 50 = 2.5 micro g / ml)低两倍,而两种呋喃香豆素的抗菌活性均未见差异。发现环氧乙烷环在抗血浆活性方面是有益的。

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