发现了诺西肽、灰黄霉素和壮观霉素是抗鸟分枝杆菌复合体的有效抗分枝杆菌药物。
Discovery of Nosiheptide, Griseoviridin, and Etamycin as Potent Anti-Mycobacterial Agents against Mycobacterium avium Complex.
机构信息
Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo 108-8641, Japan.
Medicinal Research Laboratories, School of Pharmacy, Kitasato University, Tokyo 108-8641, Japan.
出版信息
Molecules. 2019 Apr 16;24(8):1495. doi: 10.3390/molecules24081495.
complex (MAC) is a serious disease mainly caused by and Although the incidence of MAC infection is increasing worldwide, only a few agents are clinically used, and their therapeutic effects are limited. Therefore, new anti-MAC agents are needed. Approximately 6600 microbial samples were screened for new anti-mycobacterial agents that inhibit the growth of both M. avium and M. intracellulare, and two culture broths derived from marine actinomycete strains OPMA1245 and OPMA1730 had strong activity. Nosiheptide (1) was isolated from the culture broth of OPMA1245, and griseoviridin (2) and etamycin (viridogrisein) (3) were isolated from the culture broth of OPMA1730. They had potent anti-mycobacterial activity against . and with minimum inhibitory concentrations (MICs) between 0.024 and 1.56 μg/mL. In addition, a combination of 2 and 3 markedly enhanced the anti-mycobacterial activity against both M. avium and M. intracellulare. Furthermore, a combination 2 and 3 had a therapeutic effect comparable to that of ethambutol in a silkworm infection assay with .
分枝杆菌复合体（MAC）是一种严重的疾病，主要由 和 引起。尽管全球 MAC 感染的发病率正在上升，但临床上仅使用少数几种药物，且其治疗效果有限。因此，需要新的抗 MAC 药物。我们对大约 6600 个微生物样本进行了筛选，以寻找新的抗分枝杆菌药物，这些药物既能抑制 和 的生长，又有两种来自海洋放线菌菌株 OPMA1245 和 OPMA1730 的培养物具有很强的活性。从 OPMA1245 的培养液中分离出了诺西肽（1），从 OPMA1730 的培养液中分离出了灰绿霉素（2）和埃他霉素（viridogrisein）（3）。它们对 和 具有很强的抗分枝杆菌活性，最低抑菌浓度（MIC）在 0.024 到 1.56 μg/mL 之间。此外，2 和 3 的联合使用显著增强了对 和 的抗分枝杆菌活性。此外，在感染家蚕的实验中，2 和 3 的联合使用具有与乙胺丁醇相当的治疗效果。
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