Division of Natural Product Chemistry, Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai, Miyagi, 981-8558, Japan.
J Antibiot (Tokyo). 2024 Jul;77(7):412-421. doi: 10.1038/s41429-024-00724-4. Epub 2024 May 8.
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. Furthermore, 1-17 exerted potent therapeutic effects in an in vivo-mimic silkworm infection model with ED values ranging between 0.12 and 3.7 μg larva g.
从链霉菌 TMPU-20A065 的发酵液中分离到三个新的脂多霉素类似物（1、2 和 4）和 14 个已知的脂多霉素（3 和 5-17），它们是抗鸟分枝杆菌复合体的药物。通过包括 NMR 和 MS 在内的光谱分析阐明了脂多霉素的结构。化合物 1、2 和 4 属于含有硫酸基团和甲基戊二酸的 I 型脂多霉素，其结构中均有不同的酰侧链。化合物 1-17 对体外鸟分枝杆菌和胞内分枝杆菌表现出抗活性，MIC 值在 2.0 到 64 μg/ml 之间。此外，化合物 1-17 在体内模拟蚕感染模型中具有很强的治疗效果，ED 值在 0.12 到 3.7 μg 幼虫 g 之间。
