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一种新型生物活性次生代谢产物的多功能性,来源于. 的内生真菌。

Multi-Function of a New Bioactive Secondary Metabolite Derived from Endophytic Fungus of .

机构信息

Department of Biological Sciences, College of Science, King Faisal University, Al-Ahsa 31982, Saudi Arabia.

Department of Botany and Microbiology, Faculty of Science, Cairo University, Giza 12613, Egypt.

出版信息

J Microbiol Biotechnol. 2023 Jun 28;33(6):806-822. doi: 10.4014/jmb.2206.06010. Epub 2022 Dec 27.

Abstract

In the current study we assessed a new crystallized compound, 5-(1-hydroxybutyl)-4-methoxy-3-methyl-2H-pyran-2-one (C-HMMP), from the endophytic fungus residing in the medicinal plant for its in vitro antimicrobial, antibiofilm, antioxidant, antimalarial, and anti-proliferative properties. The promising compound was identified as C-HMMP through antimicrobial-guided fraction. The structure of C-HMMP was unambiguously confirmed by 2D NMR and HIRS spectroscopic analysis. Antimicrobial property testing of C-HMMP showed it to be effective against a variety of pathogenic bacteria and fungi with MICs ranging from 3.9 to 31.25 μg/ml. The compound displayed excellent antibiofilm activity against , , and . Furthermore, the antimalarial and radical scavenging activities of C-HMMP were clearly dosede-pendent, with IC50 values of 0.15 and 131.2 μg/ml. The anti-proliferative activity of C-HMMP against the HepG-2, HeLa, and MCF-7 cell lines in vitro was investigated by MTT assay, revealing notable anti-proliferative activity with IC50 values of 114.1, 90, and 133.6 μg/ml, respectively. Moreover, C-HMMP successfully targets topoisomerase I and demonstrated beneficial anti-mutagenicity in the Ames test against the reactive carcinogenic mutagen, 2-aminofluorene (2-AF). Finally, the compound inhibited the activity of α-glucosidase and α-amylase with IC50 values of 144.7 and 118.6 μg/ml, respectively. To the best of our knowledge, the identified compound C-HMMP was obtained for the first time from of , and this study demonstrated that C-HMMP has relevant biological significance and could provide better therapeutic targets against disease.

摘要

在目前的研究中,我们评估了一种新的结晶化合物 5-(1-羟基丁基)-4-甲氧基-3-甲基-2H-吡喃-2-酮(C-HMMP),它来源于内生真菌,存在于药用植物中,具有体外抗菌、抗生物膜、抗氧化、抗疟原虫和抗增殖特性。通过抗菌指导分离,确定有前途的化合物为 C-HMMP。通过 2D NMR 和 HIRS 光谱分析明确确定了 C-HMMP 的结构。C-HMMP 的抗菌性能测试表明,它对各种致病细菌和真菌有效,MIC 范围为 3.9 至 31.25μg/ml。该化合物对 、 、 显示出优异的抗生物膜活性。此外,C-HMMP 的抗疟原虫和自由基清除活性明显呈剂量依赖性,IC50 值分别为 0.15 和 131.2μg/ml。通过 MTT 测定法研究了 C-HMMP 对 HepG-2、HeLa 和 MCF-7 细胞系的体外增殖活性,结果表明,该化合物对 HepG-2、HeLa 和 MCF-7 细胞系的增殖活性具有显著的抑制作用,IC50 值分别为 114.1、90 和 133.6μg/ml。此外,C-HMMP 成功靶向拓扑异构酶 I,并在 Ames 试验中对反应性致癌诱变剂 2-氨基芴(2-AF)表现出良好的抗突变性。最后,该化合物对 α-葡萄糖苷酶和 α-淀粉酶的抑制活性分别为 IC50 值为 144.7 和 118.6μg/ml。据我们所知,所鉴定的化合物 C-HMMP 是首次从 中获得的,本研究表明 C-HMMP 具有相关的生物学意义,并可为针对疾病的更好治疗靶点提供依据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b829/10333465/9939865a6405/jmb-33-6-806-f1.jpg

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