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使用一个含有人ＶＣＡＭ－１基因启动子和荧光素酶编码基因的转染细胞株，从微生物代谢产物中筛选能够抑制由ＴＮＦ－α诱导的ＶＣＡＭ－１表达的活性物质。在筛选过程中，应用有机溶媒萃取、ＯＤＳ柱层析及ＨＰＬＣ等方法，从一株放线菌ＫＳ－５５５５的发酵液中分离到了ＫＳ－５５５５－Ｅ、Ｆ、Ｇ３种生物活性物质。它们对与人ＶＣＡＭ－１基因的启动子相连接的荧光素酶基因的表达显示出较强的抑制活性，其ＩＣ５０值分别为０．３２、０．１４、０．１９μｍｏｌ／Ｌ。经各种理化特性及ＵＶ、ＭＳ、ＨＰＬＣ等分析，确定化合物ＫＳ－５５５５－Ｅ、Ｆ、Ｇ分别与脂酰ＣｏＡ合成抑制剂ｔｒｉａｃｓｉｎＣ、Ｄ、Ａ的结构相同。
A transfected cell line containing the human VCAM-1 gene promoter and luciferase encoding gene was used to screen microbial metabolites for an active substance capable of inhibiting the expression of VCAM-1 induced by TNF-α. During the screening process, KS-5555-E, F, G bioactive substances were isolated from the fermentation broth of actinomyces strain KS-5555 by using organic solvent extraction, ODS column chromatography and HPLC. They showed strong inhibitory activity on the expression of luciferase gene linked to the promoter of human VCAM-1 gene with IC50 values of 0.32, 0.14 and 0.19 μmol / L, respectively. The compounds KS-5555-E, F and G were identified as triacsinC, D and A respectively by various physicochemical properties and UV, MS and HPLC analysis.