从海洋源真菌 Simplicillium sp. SCSIO 41222 的培养液中提取的新肽 Sinulariapeptide F。

IF 2.1 4区医学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Journal of Antibiotics Pub Date : 2024-10-25 DOI:10.1038/s41429-024-00780-w

Yan-Chun He, Meng-Qin Wang, Qing-Qing Tie, Xiao-Wen Huang, Yong-Hong Liu, Yun-Qiu Li, Bin Yang

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引用次数: 0

摘要

从真菌 Simplicillium sp. SCSIO 41222 中分离出了一种名为 sinulariapeptide F（1）的新化合物，以及一种已知的丁内酯（2）和七种已知的肽（3-9）。利用 HRESIMS、核磁共振光谱（1H、13C、HSQC、HMBC）和马菲法确定了它们的结构和绝对构型。评估了所有这些化合物对乙酰胆碱酯酶（AChE）和胰脂肪酶（PL）的抑制活性。化合物 4 和 6 被选中测试其对程序性细胞死亡-1（PD-1）/程序性细胞死亡配体 1（PD-L1）的抑制活性。结果表明，化合物 4 对 PD-1/ PD-L1 具有很强的抑制活性，IC50 值为 0.656 μM。此外，对接分析表明了化合物 4 与蛋白质之间的相互作用，表明 PD-L1 可能是化合物 4 的靶点。

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Sinulariapeptide F, a new peptide from culture broth of marine-derived fungus Simplicillium sp. SCSIO 41222.

One new compound named sinulariapeptide F (1) together with one known butyrolactone (2) and seven known peptides (3-9) were isolated from the fungus Simplicillium sp. SCSIO 41222. Their structures and absolute configurations were established using HRESIMS, NMR spectroscopy (¹H, ¹³C, HSQC, HMBC) and marfey's method. All of these compounds were assessed their inhibitory activity of acetylcholinesterase (AChE) and pancreatic lipase (PL). Compounds 4 and 6 were selected to test for the inhibitory activity against programmed cell death-1 (PD-1)/ programmed cell death-ligand 1 (PD-L1). The results indicated that compound 4 displayed potent inhibition activity against PD-1/ PD-L1 with an IC₅₀ value of 0.656 μM. Furthermore, the docking analysis demonstrated the interactions between 4 and proteins, suggesting PD-L1 to be a probable target for compound 4.

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来源期刊

Journal of Antibiotics 医学-免疫学

CiteScore

6.60

自引率

3.00%

发文量

审稿时长

1 months

期刊介绍： The Journal of Antibiotics seeks to promote research on antibiotics and related types of biologically active substances and publishes Articles, Review Articles, Brief Communication, Correspondence and other specially commissioned reports. The Journal of Antibiotics accepts papers on biochemical, chemical, microbiological and pharmacological studies. However, studies regarding human therapy do not fall under the journal’s scope. Contributions regarding recently discovered antibiotics and biologically active microbial products are particularly encouraged. Topics of particular interest within the journal''s scope include, but are not limited to, those listed below: Discovery of new antibiotics and related types of biologically active substances Production, isolation, characterization, structural elucidation, chemical synthesis and derivatization, biological activities, mechanisms of action, and structure-activity relationships of antibiotics and related types of biologically active substances Biosynthesis, bioconversion, taxonomy and genetic studies on producing microorganisms, as well as improvement of production of antibiotics and related types of biologically active substances Novel physical, chemical, biochemical, microbiological or pharmacological methods for detection, assay, determination, structural elucidation and evaluation of antibiotics and related types of biologically active substances Newly found properties, mechanisms of action and resistance-development of antibiotics and related types of biologically active substances.