Arachidonate 12-lipoxygenases with reference to their selective inhibitors
- Department of Food and Nutrition, Faculty of Home Economics, Kyoto Women's University, Imakumano, Higashiyama-ku, Kyoto 605-8501 (Japan)
- Faculty of Life and Environmental Science, Shimane University, Matsue, Shimane 690-8504 (Japan)
- Department of Biochemistry, School of Medicine, Kagawa University, Miki-cho, Kita-gun, Kagawa 761-0793 (Japan)
Lipoxygenase is a dioxygenase recognizing a 1-cis,4-cis-pentadiene of polyunsaturated fatty acids. The enzyme oxygenates various carbon atoms of arachidonic acid as a substrate and produces 5-, 8-, 12- or 15-hydroperoxy eicosatetraenoic acid with a conjugated diene chromophore. The enzyme is referred to as 5-, 8-, 12- or 15-lipoxygenase, respectively. Earlier we found two isoforms of 12-lipoxygenase, leukocyte- and platelet-type enzymes, which were distinguished by substrate specificity, catalytic activity, primary structure, gene intron size, and antigenicity. Recently, the epidermis-type enzyme was found as the third isoform. Attempts have been made to find isozyme-specific inhibitors of 12-lipoxygenase, and earlier we found hinokitol, a tropolone, as a potent inhibitor selective for the platelet-type 12-lipoxygenase. More recently, we tested various catechins of tea leaves and found that (-)-geotechnical gallate was a potent and selective inhibitor of human platelet 12-lipoxygenase with an IC{sub 5} of 0.14 {mu}M. The compound was much less active with 12-lipoxygenase of leukocyte-type, 15-, 8-, and 5-lipoxygenases, and cyclo oxygenases-1 and -2.
- OSTI ID:
- 20793188
- Journal Information:
- Biochemical and Biophysical Research Communications, Vol. 338, Issue 1; Other Information: DOI: 10.1016/j.bbrc.2005.08.214; PII: S0006-291X(05)01939-X; Copyright (c) 2005 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved; Country of input: International Atomic Energy Agency (IAEA); ISSN 0006-291X
- Country of Publication:
- United States
- Language:
- English
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