Irie Kensuke, Jeelani Ghulam, Nozaki Tomoyoshi, Iwasaki Arihiro
Department of Applied Chemistry, Chuo University, 1-13-27 Kasuga, Bunkyo-ku, Tokyo 112-8551, Japan.
Department of Biomedical Chemistry, Graduate School of Medicine, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8654, Japan.
J Nat Prod. 2024 Sep 27;87(9):2292-2301. doi: 10.1021/acs.jnatprod.4c00733. Epub 2024 Aug 15.
Pemuchiamides A and B ( and ) were isolated from a marine sp. cyanobacterium collected from Pemuchi Beach on Hateruma Island, Japan. Although and existed as a complex mixture of rotamers in chloroform-, detailed analyses of their 2D NMR and tandem mass spectra revealed their planar structures, respectively. The absolute configurations of and were established via the degradation and derivatization reactions. Pemuchiamide A () exhibited potent growth-inhibitory activity against , the causative organism of African sleeping sickness, while showed 10-fold weaker activity than . This result indicates that the presence of a hydroxy group at the C-3 position of the 4-aminobutanoic acid moiety negatively affects antitrypanosomal activity.
佩穆酰胺A和B（ 和 ）是从采自日本波照间岛佩穆奇海滩的一种海洋蓝藻细菌中分离得到的。尽管 和 在氯仿中以旋转异构体的复杂混合物形式存在，但对它们的二维核磁共振和串联质谱进行详细分析后分别揭示了它们的平面结构。 和 的绝对构型通过降解和衍生化反应得以确定。佩穆酰胺A（ ）对非洲昏睡病的病原体 表现出强大的生长抑制活性，而 表现出的活性比 弱10倍。这一结果表明，4-氨基丁酸部分C-3位上羟基的存在会对抗锥虫活性产生负面影响。
