由链霉菌 TMPU-20A065 产生的新型脂质霉素同系物--在家蚕感染模型中具有疗效的抗分枝杆菌复合制剂

IF 2.1 4区 医学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Journal of Antibiotics Pub Date : 2024-05-08 DOI:10.1038/s41429-024-00724-4
Akiho Yagi, Mayu Fujiwara, Mayu Sato, Yuzu Abe, Ryuji Uchida
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摘要

从链霉菌 TMPU-20A065 的培养液中分离出了 3 种新的脂质霉素同系物(1、2 和 4)以及 14 种已知的脂质霉素(3 和 5-17),作为抗分枝杆菌复合菌剂。通过核磁共振和质谱等光谱分析,阐明了脂质霉素的结构。化合物 1、2 和 4 属于含硫酸基团和甲基戊二酸的 I 型脂质霉素,结构中的酰基侧链各不相同。化合物 1-17 在体外具有抗阿维菌素和细胞内阿维菌素的活性,其 MIC 值介于 2.0 和 64 μg ml-1 之间。此外,1-17 还在体内模拟家蚕感染模型中发挥了强大的治疗作用,其 ED50 值介于 0.12 和 3.7 μg larva-1 g-1 之间。
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New liposidomycin congeners produced by Streptomyces sp. TMPU-20A065, anti-Mycobacterium avium complex agents with therapeutic efficacy in a silkworm infection model
Three new liposidomycin congeners (1, 2, and 4), together with 14 known liposidomycins (3 and 5–17), were isolated from the culture broth of Streptomyces sp. TMPU-20A065 as anti-Mycobacterium avium complex agents. The structures of liposidomycins were elucidated by spectroscopic analyses, including NMR and MS. Compounds 1, 2, and 4 belong to type-I liposidomycin-containing sulfate groups and methylglutaric acid, each with a different acyl side chain in the structure. Compounds 1–17 exhibited in vitro anti-M. avium and M. intracellulare activities with MIC values ranging between 2.0 and 64 μg ml−1. Furthermore, 1–17 exerted potent therapeutic effects in an in vivo-mimic silkworm infection model with ED50 values ranging between 0.12 and 3.7 μg larva−1 g−1.
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来源期刊
Journal of Antibiotics
Journal of Antibiotics 医学-免疫学
CiteScore
6.60
自引率
3.00%
发文量
87
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.
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