重新发现四霉素作为一种针对耐药革兰氏阳性菌的广谱强效抗生素。
Rediscovery of Tetronomycin as a Broad-Spectrum and Potent Antibiotic against Drug-Resistant Gram-Positive Bacteria.
作者信息
Kimishima Aoi, Tsuruoka Iori, Kanto Hiroki, Tsutsumi Hayama, Arima Naoaki, Sakai Kazunari, Sugamata Miho, Matsui Hidehito, Watanabe Yoshihiro, Iwatsuki Masato, Honsho Masako, Naher Kamrun, Inahashi Yuki, Hanaki Hideaki, Asami Yukihiro
机构信息
Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
O̅mura Satoshi Memorial Institute, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
出版信息
ACS Omega. 2023 Mar 14;8(12):11556-11563. doi: 10.1021/acsomega.3c00651. eCollection 2023 Mar 28.
Tetronomycin (), first isolated from a cultured broth of sp. by Juslen . in 1974, is a polycyclic polyether compound. However, the biological activity of has not been thoroughly examined. In this study, we found that exhibits more potent antibacterial activity than two well-known antibacterial drugs (vancomycin and linezolid) and is effective against several drug-resistant clinical isolates including methicillin-resistant and vancomycin-resistant . Furthermore, we reassigned the C NMR spectra of and performed a preliminary structure-activity relationship study of to synthesize a chemical probe for target identification, which implied different targets based on its ionophore activity.
四环素霉素（）于1974年由尤斯伦首次从 的培养液中分离出来，是一种多环多醚化合物。然而，其生物活性尚未得到充分研究。在本研究中，我们发现它比两种著名的抗菌药物（万古霉素和利奈唑胺）具有更强的抗菌活性，并且对几种耐药临床分离株有效，包括耐甲氧西林 和耐万古霉素 。此外，我们重新确定了其碳核磁共振光谱，并对其进行了初步的构效关系研究，以合成用于靶点鉴定的化学探针，这暗示了基于其离子载体活性的不同靶点。
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