Inhibition of LTB4 binding to human neutrophils by nordihydroguaiaretic acid.
Nordihydroguaiaretic acid (NDGA) was investigated for its ability to interact with leukotriene B4 receptors on human polymorphonuclear leukocytes (hPMNs). 3H-LTB4 binding to specific receptors was reduced in a dose-dependent manner with maximal reduction at 100 microM NDGA and an IC50 of about 50 microM. Binding of another inflammatory stimulus. N-formyl-norleucyl-leucyl-phenylalanine (FNLP) was not affected by similar treatment. Chemotaxis and enzyme release stimulated by LTB4 and oligopeptide were inhibited by NDGA. In addition, LTB4-triggered inflammation in vivo in mice was inhibited by systemic administration of NDGA. These data suggest that LTB4 receptor antagonism may contribute to inhibition of inflammation by NDGA.
Maloff
B L
BL
Medical Products Department, E. I. DuPont de Nemours and Company, Inc., Wilmington, De 19898.
Fefer
D
D
Cooke
G M
GM
Ackerman
N R
NR
D000818:Animals; D002396:Catechols / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D007249:Inflammation / Q000139:chemically induced / Q000517:prevention & control; D007975:Leukotriene B4 / Q000378:metabolism* / Q000494:pharmacology; D009637:Masoprocol / Q000494:pharmacology*; D051379:Mice; D009504:Neutrophils / Q000187:drug effects* / Q000378:metabolism; D011971:Receptors, Immunologic / Q000187:drug effects; D018102:Receptors, Leukotriene B4
D002396:Catechols; D011971:Receptors, Immunologic; D018102:Receptors, Leukotriene B4; D007975:Leukotriene B4; D009637:Masoprocol