由绿粘帚霉 BF-0440 产生的固醇 O-酰基转移酶新抑制剂 Voluhemins。
Voluhemins, new inhibitors of sterol O-acyltransferase, produced by Volutella citrinella BF-0440.
机构信息
Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
Medicinal Research Laboratories, School of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
出版信息
J Antibiot (Tokyo). 2020 Nov;73(11):748-755. doi: 10.1038/s41429-020-0327-0. Epub 2020 May 29.
New compounds, designated voluhemins A (1) and B (2), are isolated from the culture broth of the fungal strain Volutella citrinella BF-0440 along with structurally related known NK12838 (3). Spectroscopic data, including 1D and 2D NMR, elucidated their structures. Compounds 1-3 have a common indoline-diterpene core and two additional isoprenyl moieties. Compounds 1 and 3 contain a hemiaminal unit, while 2 is O-methylated 1. Their inhibitory activities toward sterol O-acyltransferase (SOAT) 1 and 2 isozymes in SOAT1- and SOAT2-expressing Chinese hamster ovary (CHO) cells show that 2 selectively inhibits the SOAT2 isozyme.
新化合物，命名为 voluhemins A（1）和 B（2），从真菌菌株 Volutella citrinella BF-0440 的发酵液中分离得到，同时还分离到结构相关的已知化合物 NK12838（3）。光谱数据，包括 1D 和 2D NMR，阐明了它们的结构。化合物 1-3 具有共同的吲哚二萜核心和两个额外的异戊二烯部分。化合物 1 和 3 含有半亚胺单元，而 2 是 O-甲基化的 1。它们对甾醇 O-酰基转移酶（SOAT）1 和 2 同工酶的抑制活性在 SOAT1 和 SOAT2 表达的中国仓鼠卵巢（CHO）细胞中表明，2 选择性抑制 SOAT2 同工酶。
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