新型抗疟呋罗色酮类似物由真菌菌株 Fusarium sp. FKI-9521 产生。
New antimalarial fusarochromanone analogs produced by the fungal strain Fusarium sp. FKI-9521.
机构信息
Ōmura Satoshi Memorial Institute, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
出版信息
J Antibiot (Tokyo). 2023 Jul;76(7):384-391. doi: 10.1038/s41429-023-00617-y. Epub 2023 Apr 12.
Two new antimalarial compounds, named deacetyl fusarochromene (1) and 4'-O-acetyl fusarochromanone (2), were discovered from the static fungal cultured material of Fusarium sp. FKI-9521 isolated from feces of a stick insect (Ramulus mikado) together with three known compounds fusarochromanone (3), 3'-N-acetyl fusarochromanone (4), and 5 (fusarochromene or banchromene). The structures of 1 and 2 were elucidated as new analogs of 3 by MS and NMR analyses. The absolute configurations of 1, 2, and 4 were determined by chemical derivatization. All five compounds showed moderate in vitro antimalarial activity against chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum strains, with IC values ranging from 0.08 to 6.35 µM.
两种新的抗疟化合物，命名为去乙酰 fusarochromene（1）和 4'-O-乙酰 fusarochromanone（2），是从真菌 Fusarium sp. FKI-9521 的静态培养物中分离出来的，该真菌是从竹节虫（Ramulus mikado）的粪便中分离出来的，同时还分离出了三种已知化合物 fusarochromanone（3）、3'-N-乙酰 fusarochromanone（4）和 5（fusarochromene 或 banchromene）。通过 MS 和 NMR 分析，1 和 2 的结构被阐明为 3 的新类似物。1、2 和 4 的绝对构型通过化学衍生化确定。所有五种化合物对氯喹敏感和氯喹耐药的恶性疟原虫株均表现出中等体外抗疟活性，IC 值范围为 0.08 至 6.35 μM。
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