Ui Hideaki, Shiomi Kazuro, Suzuki Hideaki, Hatano Hiroko, Morimoto Hiromi, Yamaguchi Yuichi, Masuma Rokuro, Sunazuka Toshiaki, Shimamura Hiroyuki, Sakamoto Kimitoshi, Kita Kiyoshi, Miyoshi Hideto, Tomoda Hiroshi, Omura Satoshi
Kitasato Institute for Life Sciences and Graduate School of Infectious Control Sciences, Kitasato University, Minato-ku, Tokyo 108-8641, Japan.
J Antibiot (Tokyo). 2006 Dec;59(12):785-90. doi: 10.1038/ja.2006.103.
A new NADH-fumarate reductase inhibitor, verticipyrone, was isolated from the cultured broth of a fungus, Verticillium sp. FKI-1083. The structure was established as (E)-2-methoxy-3,5-dimethyl-6-(3-methyl-2-undecenyl)-4H-pyran-4-one. Verticipyrone exhibited an IC50 value of 0.88 nM against NADH-fumarate reductase of Ascaris suum. Verticipyrone inhibited both Ascaris and bovine heart complex I, and its synthetic analogue, 8,9-dihydro-8-hydroxyverticipyrone, showed good selectivity against Ascaris complex I.
一种新的烟酰胺腺嘌呤二核苷酸（NADH）-延胡索酸还原酶抑制剂——轮枝孢吡喃酮，是从真菌轮枝菌属FKI-1083的培养液中分离得到的。其结构确定为（E）-2-甲氧基-3,5-二甲基-6-（3-甲基-2-十一碳烯基）-4H-吡喃-4-酮。轮枝孢吡喃酮对猪蛔虫NADH-延胡索酸还原酶的半数抑制浓度（IC50）值为0.88纳摩尔。轮枝孢吡喃酮可抑制猪蛔虫和牛心脏的复合体I，其合成类似物8,9-二氢-8-羟基轮枝孢吡喃酮对猪蛔虫复合体I表现出良好的选择性。
