STUDIES ON LIPOXYGENASE INHIBITORS I. MY3-469 (3-METHOXYTROPOLONE), A POTENT AND SELECTIVE INHIBITOR OF 12-LIPOXYGENASE, PRODUCED BY STREPTOVERTICILLIUM HADANONENSE KY11449
- Resource Type
- Journal Article
- Authors
- HIROSHI KASE; KUNIKATSU SHIRAHATA; SHIGETO KITAMURA; TAKAO IIDA
- Source
- The Journal of Antibiotics. 1986, 39(4):589
- Subject
- Language
- English
- ISSN
- 0021-8820
1881-1469
Streptoverticillium hadanonense KY11449 was found to produce a 12-lipoxygenase inhibitor MY3-469. The compound was purified by chromatography on Diaion HP-10, charcoal, Sephadex LH-20 and crystallization. The chemical structure of MY3-469 was determined to be 3-methoxytropolone on the basis of its physico-chemical properties. The half maximal inhibitory concentration (IC50) of MY3-469 against bovine platelet 12-lipoxygenase was 1.8×10-6 M. The compound did not inhibit bovine platelet cyclooxygenase at 10-3 M and showed weak inhibition (IC50 2.8×10-4) against 5-lipoxygenase of rat basophilic leukemia cells. The results indicate that MY3-469 is a potent and selective inhibitor of 12-lipoxygenase.