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Endophytic fungus Paecilomyces formosus LHL10 produces sester-terpenoid YW3548 and cyclic peptide that inhibit urease and alpha-glucosidase enzyme activities

机译:内生真菌博士霉菌蛋白酶LHL10产生抑制释放脲酶和α-葡糖苷酶活性的Sester-Terpenoid YW3548和环状肽

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Endophytic fungi have been used to obtain novel bioactive secondary metabolites with potential applications in medical and agricultural sectors, which can also act as lead targets for pharmaceutical and medicinal potential. In the present study, the endophytic fungus Paecilomyces formosus LHL10 isolated from the root of cucumber plant was tested for its enzyme inhibitory potential. The ethyl acetate (EtOAc) extract of LHL10 was screened for its inhibitory effect on acetylcholinesterase (AChE), alpha-glucosidase, urease, and anti-lipid peroxidation. The findings suggest that the EtOAc extract from LHL10 possesses significant inhibitory potential against urease and alpha-glucosidase. The EtOAc extract was thus, subjected to advanced column chromatographic techniques for the isolation of pure compounds. The structure elucidation was carried out through spectroscopic analysis and comparison with literature data, and these compounds were confirmed as known a sester-terpenoid (1) and a known cyclic peptide (2). The enzyme inhibition bioassay indicated that Compounds 1 and 2 exhibited remarkable inhibitory rate against alpha-glucosidase and urease, with an IC50 value of 61.80 +/- 5.7, 75.68 +/- 6.2 and 74.25 +/- 4.3, 190.5 +/- 10.31 mu g/g, respectively. Thus, the current study concludes the enzyme inhibitory potential of endophyte LHL10 and provides the basis for further investigations of bioactive compounds, which could be used as potent drugs for enzyme inhibition.
机译:Endophytic真菌已被用于获得具有医学和农业部门的潜在应用的新型生物活性次级代谢产物,这也可以作为药物和药用潜力的铅目标。在本研究中,测试从黄瓜植物根部分离的内生真菌博士学博士素LHL10用于其酶抑制潜力。将LHL10的乙酸乙酯(EtOAc)提取物筛选其对乙酰胆碱酯酶(ACHE),α-葡糖苷酶,脲酶和抗脂质过氧化的抑制作用。研究结果表明,来自LHL10的EtOAc提取物具有对脲酶和α-葡糖苷酶的显着抑制潜力。因此,EtOAc提取物经受高级柱色谱技术,用于分离纯化合物。通过光谱分析和与文献数据进行比较进行结构阐明,并证实了这些化合物,如已知的Sester-Terpenoid(1)和已知的环肽(2)。酶抑制生物测定表明,化合物1和2表现出对α-葡糖苷酶和脲酶的显着抑制率,IC50值为61.80 +/- 5.7,75.68 +/- 6.2和74.25 +/- 4.3,190.5 +/-1031亩分别为g / g。因此,目前的研究总结了内皮内LHL10的酶抑制潜力,为进一步研究生物活性化合物提供了基础,这可以用作酶抑制的有效药物。

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