小鼠腹腔巨噬细胞内胆固醇酯再形成的选择性抑制剂——FO-6979-P9

A selective inhibitor of the reformation of cholesterol ester in mouse peritoneal macrophages FO 6979 P9

ＦＯ－６９７９－Ｐ９是在从真菌培养液筛选巨噬细胞泡沫化抑制剂过程中获得的，其对小鼠腹腔巨噬细胞中胆固醇酯再形成的抑制ＩＣ５０为０．３８ｍｇ／Ｌ（０．７８μｍｏｌ／Ｌ），而对甘油三酯和磷脂的再形成无显著抑制作用。真菌Ｂｅａｕｖｅｒｉａｓｐ．ＦＯ－６９７９静置培养１４ｄ后，经有机溶媒提取，常压ＯＤＳ柱层析和制备ＨＰＬＣ柱层析分离得到ＦＯ－６９７９－Ｐ９纯品。又经过测定其ＦＡＢＭＳ、ＵＶ、１Ｈ－ＮＭＲ、１３Ｃ－ＮＭＲ、１Ｈ－１ＨＣＯＳＹ、ＤＥＰＴ、ＨＭＱＣ和ＨＭＢＣ等光谱数据。

During our screening programme of inhibitor to the reformation of cholesterol ester in mouse peritoneal macrophages, we found the FO 6979 P9 which exhibited a IC 50 =0.38 mg/L (0.78 μmol/L) of inhibition to the reformation of cholesterol ester in mouse peritoneal macrophages but no inhibition effect on the reformation of triacylglycerol and phospholipides. The culture broth of Beauveria sp. FO 6979 for 14 days in static state was extracted by organic solvent, isolated by ODS column and HPLC column chromatography. Based on spectral data of FABMS, UV, 1 H NMR, 13 C NMR, 1 H 1H COSY, FO 6979 P9 was identified as Beauveriolide Ⅰ with a structure of cyclodepsipeptide.