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7-氯脂他汀,一种由海洋来源的曲霉NKH-007产生的固醇O-酰基转移酶抑制剂。

7-Chlorofolipastatin, an inhibitor of sterol O-acyltransferase, produced by marine-derived Aspergillus ungui NKH-007.

作者信息

Uchida Ryuji, Nakajyo Kento, Kobayashi Keisuke, Ohshiro Taichi, Terahara Takeshi, Imada Chiaki, Tomoda Hiroshi

机构信息

Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.

Graduate School of Marine Science and Technology, Tokyo University of Marine Science and Technology, Tokyo, Japan.

出版信息

J Antibiot (Tokyo). 2016 Aug;69(8):647-51. doi: 10.1038/ja.2016.27. Epub 2016 Mar 16.

DOI:10.1038/ja.2016.27
PMID:26980608
Abstract

A new depsidone, named 7-chlorofolipastatin, and five known structurally related depsidones were isolated from the culture broth of the marine-derived fungus Aspergillus ungui NKM-007 by solvent extraction and HPLC using an octadecylsilyl column. The structure of 7-chlorofolipastatin was elucidated by various spectroscopic data including 1D and 2D NMR spectroscopy. 7-Chlorofolipastatin inhibited sterol O-acyltransferase (SOAT) 1 and 2 isozymes in cell-based and enzyme assays using SOAT1- and SOAT2-expressing Chinese hamster ovary (CHO) cells.

摘要

通过溶剂萃取和使用十八烷基硅烷柱的高效液相色谱法,从海洋来源真菌爪曲霉NKM - 007的培养液中分离出一种名为7 - 氯脂他汀的新型缩酚酸环醚酮和五种已知的结构相关缩酚酸环醚酮。通过包括一维和二维核磁共振光谱在内的各种光谱数据阐明了7 - 氯脂他汀的结构。在使用表达SOAT1和SOAT2的中国仓鼠卵巢(CHO)细胞进行的基于细胞和酶的测定中,7 - 氯脂他汀抑制了固醇O - 酰基转移酶(SOAT)1和2同工酶。

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