Inhibition of 5-hydroxy-eicosatetraenoic acid (5-HETE) formation in intact human neutrophils by naturally-occurring diarylheptanoids: inhibitory activities of curcuminoids and yakuchinones.
Various diarylheptanoids including curcumin, bis (3,4-dihydroxy-cinnamoyl) methane, and yakuchinones A & B were screened and found to be potent inhibitors of 5-HETE production by intact human neutrophils, with respective IC50 values of 8.0, 4.4, 5.4, and 4.0 microM. These diarylheptanoids were found to be more potent than BW-755C, Phenidone, and AA-861. We have confirmed a previous report that several of these diarylheptanoids inhibit cyclooxygenase. Thus, curcuminoids and yakuchinones are more accurately characterized as dual inhibitors of arachidonic acid metabolism.
Flynn
D L
DL
Rafferty
M F
MF
Boctor
A M
AM
D002396:Catechols / Q000494:pharmacology*; D003474:Curcumin / Q000031:analogs & derivatives / Q000494:pharmacology*; D006139:Guaiacol / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D006893:Hydroxyeicosatetraenoic Acids / Q000096:biosynthesis*; D066298:In Vitro Techniques; D009504:Neutrophils / Q000378:metabolism*
D002396:Catechols; D006893:Hydroxyeicosatetraenoic Acids; C022022:5-hydroxy-6,8,11,14-eicosatetraenoic acid; D006139:Guaiacol; C042566:yakuchinone-A; D003474:Curcumin