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来自[具体来源]的14个氨基酸残基的肽菌素类抗生素velutibol A:其结构与细胞毒性评估

14-Residue peptaibol velutibol A from : its structural and cytotoxic evaluation.

作者信息

Singh Varun Pratap, Pathania Anup Singh, Kushwaha Manoj, Singh Samsher, Sharma Vandana, Malik Fayaz A, Khan Inshad A, Kumar Anil, Singh Deepika, Vishwakarma Ram A

机构信息

Medicinal Chemistry Division, CSIR-Indian Institute of Integrative Medicine Canal Road Jammu 180 001 India

Department of Biotechnology, Faculty of Sciences, Shri Mata Vaishno Devi University Katra Jammu and Kashmir 182320 India.

出版信息

RSC Adv. 2020 Aug 24;10(52):31233-31242. doi: 10.1039/d0ra05780k. eCollection 2020 Aug 21.

DOI:10.1039/d0ra05780k
PMID:35520634
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9056410/
Abstract

Velutibol A (1), a new 14-residue peptaibol was isolated from the Himalayan cold habitat fungus . The structural characterization was carried out by 1D and 2D NMR studies, and tandem mass studies, and Marfey's method aided in determining the stereochemistry of the amino acids. The CD analysis revealed folding of the peptide in a 3-helical conformation. The intramolecular H-bonding was determined by an NMR-VT experiment. Cytotoxic evaluation was carried out against a panel of cancer cell lines. The cell cycle assay was carried out on human myeloid leukaemia (HL-60) cells and revealed the formation of apoptotic bodies and DNA damage in a dose-dependent manner. Three other peptaibols namely velutibol B (2), velutibol C (3), and velutibol D (4) were also isolated in trace amounts from the psychotropic fungus and characterized through tandem mass spectroscopy and Marfey's analysis.

摘要

Velutibol A(1)是一种从喜马拉雅寒冷栖息地真菌中分离出的新的含14个残基的肽菌素。通过一维和二维核磁共振研究、串联质谱研究进行结构表征,马尔费方法有助于确定氨基酸的立体化学。圆二色分析表明该肽呈α-螺旋构象折叠。通过核磁共振变温实验确定分子内氢键。对一组癌细胞系进行细胞毒性评估。在人髓性白血病(HL-60)细胞上进行细胞周期分析,结果显示以剂量依赖方式形成凋亡小体和DNA损伤。还从该精神活性真菌中微量分离出另外三种肽菌素,即velutibol B(2)、velutibol C(3)和velutibol D(4),并通过串联质谱和马尔费分析进行表征。

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