Probing the activity differences of simple and complex brominated aryl compounds against 15-soybean, 15-human, and 12-human lipoxygenase.
Lipoxygenases (LO) have been implicated in asthma, immune disorders, and various cancers. As a consequence of these broad biological implications, there is great interest in understanding the effects of naturally occurring and environmental contaminants against its activity. On the basis of our earlier studies indicating that polybrominated diphenol ethers are potent inhibitors to mammalian 15-LO, we expanded our structure-activity study to include marine-derived brominated phenol ethers (including a newly discovered tribrominated diphenyl ether), dioxins, and bastadins, as well as the synthetic brominated fire retardants, brominated bisphenol A (BBPA), and polybrominated diphenyl ethers (PBDEs). We report herein the effects of 21 simple and complex organobromine compounds against human platelet 12-LO, human reticulocyte 15-LO, and soybean 15-LO-1.
Segraves
Erika N
EN
Department of Chemistry and Biochemistry, University of California, Santa Cruz, California 95064, USA.
Shah
Rachana R
RR
Segraves
Nathaniel L
NL
Johnson
Tyler A
TA
Whitman
Stephanie
S
Sui
Jennifer K
JK
Kenyon
Victor A
VA
Cichewicz
Robert H
RH
Crews
Phillip
P
Holman
Theodore R
TR
D000818:Animals; D001092:Arachidonate 12-Lipoxygenase / Q000737:chemistry; D001093:Arachidonate 15-Lipoxygenase / Q000737:chemistry; D001792:Blood Platelets / Q000737:chemistry; D004147:Dioxins / Q000737:chemistry; D004785:Environmental Pollutants / Q000032:analysis*; D005411:Flame Retardants / Q000032:analysis; D006801:Humans; D006842:Hydrocarbons, Brominated / Q000737:chemistry*; D016859:Lipoxygenase Inhibitors; D010636:Phenols / Q000737:chemistry; D010647:Phenyl Ethers / Q000737:chemistry; D011075:Polybrominated Biphenyls / Q000737:chemistry; D011161:Porifera; D012156:Reticulocytes / Q000737:chemistry; D013025:Glycine max; D013329:Structure-Activity Relationship
D004147:Dioxins; D004785:Environmental Pollutants; D005411:Flame Retardants; D006842:Hydrocarbons, Brominated; D016859:Lipoxygenase Inhibitors; D010636:Phenols; D010647:Phenyl Ethers; D011075:Polybrominated Biphenyls; D001092:Arachidonate 12-Lipoxygenase; D001093:Arachidonate 15-Lipoxygenase