Tohyama Shigehiro, Nukui Seiji, Hatano Masaki, Hayashi Chigusa, Momose Isao, Igarashi Masayuki
Institute of Microbial Chemistry (BIKAKEN), Shinagawa-ku, Tokyo, Japan.
Funakoshi Co. Ltd., Bunkyo-ku, Tokyo, Japan.
J Antibiot (Tokyo). 2025 Jun 18. doi: 10.1038/s41429-025-00841-8.
Fluostatins are a class of compounds having four unique ring systems. They were originally isolated as dipeptidyl peptidase III (DPP3) inhibitors, and various derivatives and activities have been reported. In this study, fluostatin A, which is difficult to prepare by fermentative production, was effectively prepared by the transformation of fluostatin B. A new derivative, fluostatin Y, and a new naturally occurring derivative, fluostatin B2, were obtained, and their structures were determined. Furthermore, the bioactivity, DPP3 inhibitory activity, and antibacterial and cytotoxic activities were examined.
氟他汀类化合物是一类具有四个独特环系的化合物。它们最初作为二肽基肽酶III（DPP3）抑制剂被分离出来，并且已经报道了各种衍生物和活性。在本研究中，通过氟他汀B的转化有效地制备了难以通过发酵生产制备的氟他汀A。获得了一种新的衍生物氟他汀Y和一种新的天然存在的衍生物氟他汀B2，并确定了它们的结构。此外，还检测了它们的生物活性、DPP3抑制活性以及抗菌和细胞毒性活性。
