New verticilides, inhibitors of acyl-CoA:cholesterol acyltransferase, produced by Verticillium sp FKI-2679
New verticilides, inhibitors of acyl-CoA:cholesterol acyltransferase, produced by Verticillium sp FKI-2679
复制标题
DOI：
10.1038/ja.2012.12
复制
发表时间：
2012-05-01
影响因子：
3.3
通讯作者：
Tomoda, Hiroshi
中科院分区：
文献类型：
--
作者：
Ohshiro, Taichi;Matsuda, Daisuke;Tomoda, Hiroshi
土壤分离物Verticillium sp. FKI-2679在使用表达ACAT 1和ACAT 2的CHO细胞的基于细胞的测定中被发现产生酰基辅酶A：胆固醇酰基转移酶（ACAT）抑制剂。通过溶剂萃取、ODS柱层析、硅胶柱层析和制备HPLC等方法，从该真菌发酵液中分离得到3个新化合物，分别为轮枝孢内酯A2、A3和B1，并与已知化合物轮枝孢内酯A1一起沿着分离得到。结构鉴定表明这些化合物为新的环状缩酚肽。Verticilides A1、A2、A3和B1对ACAT 2表现出一定程度的选择性，IC（50）比观察到的对ACAT 1的效力高8.5-11倍。The Journal of Antibiotics（2012）65，255-262; doi：10.1038/ja.2012.12; 2012年3月14日在线发表
Verticillium sp. FKI-2679, a soil isolate, was found to produce inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT) in a cell-based assay using ACAT1- and ACAT2-expressing CHO cells. Three new compounds, verticilides A2, A3 and B1, were isolated along with a known compound, verticilide A1, from the fermentation broth of the fungus by solvent extraction, ODS column chromatography, silica gel column chromatography and preparative HPLC. Structure elucidation showed that these compounds were new cyclic depsipeptide. Verticilides A1, A2, A3 and B1 showed a degree of selectivity towards ACAT2, with IC(50)s 8.5-11-fold more potent than observed against ACAT1. The Journal of Antibiotics (2012) 65, 255-262; doi:10.1038/ja.2012.12; published online 14 March 2012