Funalenone, a Novel Collagenase Inhibitor Produced by Aspergillus niger

• Published in: Journal of antibiotics Vol. 52; no. 12; pp. 1095 - 1100
• Main Authors: INOKOSHI, JUNJI, SHIOMI, KAZURO, MASUMA, ROKURO, TANAKA, HARUO, YAMADA, HARUKI, OMURA, SATOSHI
• Format: Journal Article
• Language: English
• Published: TOKYO JAPAN ANTIBIOTICS RESEARCH ASSOCIATION 01.12.1999; JAPAN ANTIBIOT RES ASSN; Japan Antibiotics Research Association
• Subjects: Antibacterial agents; Antibiotics (antibacterial agents, antifungal agents); Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Applied microbiology; Aspergillus niger; Aspergillus niger - classification; Aspergillus niger - metabolism; Bacteria - drug effects; Biological and medical sciences; Biotechnology & Applied Microbiology; collagenase inhibitors; Fermentation; funalenone; Fundamental and applied biological sciences. Psychology; Immunology; Ketones - chemistry; Ketones - isolation & purification; Ketones - pharmacology; Life Sciences & Biomedicine; Matrix Metalloproteinase Inhibitors; Medical sciences; Microbiology; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Polycyclic Compounds - chemistry; Polycyclic Compounds - isolation & purification; Polycyclic Compounds - pharmacology; Protease Inhibitors - chemistry; Protease Inhibitors - isolation & purification; Protease Inhibitors - pharmacology; Science & Technology; RHEUMATOID-ARTHRITIS; METALLOPROTEINASES; Enzyme; Microbial collagenase; Phenalene derivatives; Enzyme inhibitor; Metalloendopeptidases; NMR spectrometry; Fermentation; In vitro; Biological activity; Fungi; Peptidases; Antibiotic; Aspergillus niger; Microorganism culture; Hydrolases; Fungi Imperfecti; Antibacterial agent; Physicochemical properties; Thallophyta; Structural analysis
• ISSN: 0021-8820; 1881-1469
• DOI: 10.7164/antibiotics.52.1095

Funalenone, a phenalene compound that inhibits type I collagenase (MMP-1), was isolated from mycelium of Aspergillus niger FO-5904 by solvent extaction, ODS column chromatography, Sephadex LH-20 column chromatography and reversed phase HPLC. Funalenone inhibited 50% of type I collagenase activity at a concentration of 170 μM, but inhibited 18.3% and 38.7% against 72kDa and 92kDa type IV collagenase, respectively, at a concentration of 400 μM.