Synthesis and biological evaluation of nectriatide derivatives, potentiators of amphotericin B activity

IF 2.1 4区医学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY

Journal of Antibiotics Pub Date : 2024-01-24 DOI:10.1038/s41429-023-00700-4

Kenichiro Nagai, Keisuke Kobayashi, Ryosuke Miyake, Yukino Sato, Reiko Seki, Takashi Fukuda, Akiho Yagi, Ryuji Uchida, Taichi Ohshiro, Hiroshi Tomoda

引用次数: 0

Abstract

Nectriatide 1a, a naturally occurring cyclic tetrapeptide, has been reported to a potentiator of amphotericin B (AmB) activity. In order to elucidate its structure-activity relationships, we synthesized nectriatide derivatives with different amino acids in solution-phase synthesis and evaluated AmB-potentiating activity against Candida albicans. Among them, C-and N-terminal protected linear peptides were found to show the most potent AmB-potentiating activity.

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作为两性霉素 B 活性增效剂的内酯肽衍生物的合成和生物学评价。

据报道，内曲肽 1a 是一种天然环状四肽，可增强两性霉素 B（AmB）的活性。为了阐明其结构-活性关系，我们用溶液相合成法合成了不同氨基酸的内曲肽衍生物，并评估了其对白色念珠菌的 AmB 增效活性。结果发现，其中 C 端和 N 端受保护的线性肽具有最强的 AmB 促效活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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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.