ABSTRACT The selectivity of microbial inhibitors of acyl-CoA : cholesterol acyltransferase (ACAT) toward the two isozymes, ACAT1 and ACAT2, was assessed in cell-based assays. Purpactin A

(IC50 values of ACAT1 _vs_. IC50 values of ACAT2; 2.5 μM _vs_. 1.5 μM), terpendole C (10 μM _vs_. 10 μM), glisoprenin A (4.3 μM _vs_. 10 μM), spylidone (25 μM _vs_. 5.0 μM) and synthetic

CL-283,546 (0.1 μM _vs_. 0.09 μM) inhibited ACAT1 and ACAT2 to similar extents. Beauveriolides I (0.6 μM _vs_. 20 μM) and III (0.9 μM _vs_. >20 μM) inhibited ACAT1 rather selectively,

while pyripyropenes A (>80 μM _vs_. 0.07 μM), B (48 μM _vs_. 2.0 μM), C (32 μM _vs_. 0.36 μM) and D (38 μM _vs_. 1.5 μM) showed selective inhibition against ACAT2. In particular,

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references AUTHOR INFORMATION AUTHORS AND AFFILIATIONS * School of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan Hiroshi Tomoda * Kitasato Institute for

Life Sciences and Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan Taichi Ohshiro & Satoshi Ōmura * Atherosclerosis

Research Program, Wake Forest University School of Medicine, Winston-Salem, 27157, NC, USA Lawrence L Rudel Authors * Taichi Ohshiro View author publications You can also search for this

author inPubMed Google Scholar * Lawrence L Rudel View author publications You can also search for this author inPubMed Google Scholar * Satoshi Ōmura View author publications You can also

search for this author inPubMed Google Scholar * Hiroshi Tomoda View author publications You can also search for this author inPubMed Google Scholar CORRESPONDING AUTHOR Correspondence to

Hiroshi Tomoda. RIGHTS AND PERMISSIONS Reprints and permissions ABOUT THIS ARTICLE CITE THIS ARTICLE Ohshiro, T., Rudel, L., Ōmura, S. _et al._ Selectivity of Microbial Acyl-CoA :

cholesterol Acyltransferase Inhibitors toward Isozymes. _J Antibiot_ 60, 43–51 (2007). https://doi.org/10.1038/ja.2007.6 Download citation * Received: 12 September 2006 * Accepted: 21

December 2006 * Issue Date: 01 January 2007 * DOI: https://doi.org/10.1038/ja.2007.6 SHARE THIS ARTICLE Anyone you share the following link with will be able to read this content: Get

shareable link Sorry, a shareable link is not currently available for this article. Copy to clipboard Provided by the Springer Nature SharedIt content-sharing initiative KEYWORDS * acyl-CoA

: cholesterol acyltransferase * isozyme * microbial inhibitors * lipid droplet accumulation * pyripyropene * beauveriolide * atherosclerosis