Purpactins, new inhibitors of acyl-CoA:cholesterol acyltransferase produced by Penicillium purpurogenum. I. Production, isolation and physico-chemical and biological properties
| Autor: | Hiroyuki Nishida, Shigenobu Okuda, Jing Cao, Rokuro Masuma, Satoshi Omura, Hiroshi Tomoda |
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| Rok vydání: | 1991 |
| Předmět: |
Sterol O-acyltransferase
Penicillium purpurogenum High-performance liquid chromatography Cell Line chemistry.chemical_compound Column chromatography Heterocyclic Compounds Drug Discovery Animals Chromatography High Pressure Liquid Benzofurans Pharmacology biology Cholesterol Macrophages Penicillium biology.organism_classification Enzyme assay Rats Biochemistry chemistry Enzyme inhibitor Fermentation Microsomes Liver biology.protein Microsome Chromatography Thin Layer Heterocyclic Compounds 3-Ring Sterol O-Acyltransferase |
| Zdroj: | The Journal of Antibiotics. 44:136-143 |
| ISSN: | 1881-1469 0021-8820 |
| DOI: | 10.7164/antibiotics.44.136 |
| Popis: | Penicillium purpurogenum FO-608, a soil isolate, was found to produce a series of new inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). Three active compounds, designated purpactins, A, B and C, were isolated from the fermentation broth of the producing strain by solvent extraction, silica gel column chromatography and HPLC. Purpactins inhibit ACAT activity in an enzyme assay system using rat liver microsomes with IC50 values of 121 approximately 126 microM. Purpactin A also inhibited cholesterol ester formation in J 774 macrophages, indicating the inhibition of ACAT activity in the living cells by purpactin A. |
| Databáze: | OpenAIRE |
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