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5-Lipoxygenase inhibition by acetyl-11-keto-β-boswellic acid (AKBA) by a novel mechanism
H Safayhi1, E R Sailer, H P Ammon
1Department of Pharmacology, Institute for Pharmaceutical Sciences, University of Tuebingen, Auf der Morgenstelle 8, D-72076 Tuebingen, Germany.
Abstract:
Acetyl-11-keto-β-boswellic acid (AKAB) from Boswellia serrata and B. carterii acts directly on purified 5-lipoxygenase of human blood leukocytes at a selective site for pentacyclic triterpenes that is different from the arachidonate substrate binding site. The pentacyclic triterpene ring is crucial for binding to the enzyme, whereas functional groups (11-keto function in addition to a hydrophilic group on C 4 of ring A) are essential for the 5-lipoxygenase activity.
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