Human mast cells take up and hydrolyze anandamide under the control of 5‐lipoxygenase and do not express cannabinoid receptors
[摘要] Human mast cells (HMC-1) take up anandamide (arachidonoyl-ethanolamide, AEA) with a saturable process (K m=200±20 nM, V max=25±3 pmol min−1 mg protein−1), enhanced two-fold over control by nitric oxide-donors. Internalized AEA was hydrolyzed by a fatty acid amide hydrolase (FAAH), whose activity became measurable only in the presence of 5-lipoxygenase, but not cyclooxygenase, inhibitors. FAAH (K m=5.0±0.5 μM, V max=160±15 pmol min−1 mg protein−1) was competitively inhibited by palmitoylethanolamide. HMC-1 cells did not display a functional cannabinoid receptor on their surface and neither AEA nor palmitoylethanolamide affected tryptase release from these cells.
[发布日期] [发布机构]
[效力级别] [学科分类] 生物化学/生物物理
[关键词] Anandamide;Endocannabinoid;Inflammation;Lipoxygenase;Nitric oxide;Tryptase;AEA;anandamide (arachidonoylethanolamide);AM404;N-(4-hydroxy-phenyl)-arachidonoylamide;ATFMK;arachidonoyl-trifluoromethyl-ketone;CB1/2R;type 1/2 cannabinoid receptor;CP55.940;5-(1;1′-dimethyheptyl)-2-[1R;5R-hydroxy-2R-(3-hydroxy-propyl)cyclohexyl]phenol;ETYA;5;8;11;14-eicosatetraynoic acid;FAAH;fatty acid amide hydrolase;GAR-AP;goat anti-rabbit alkaline phosphatase conjugate;HMC;human mast cells;MES;2-[N-morpholino]ethanesulfonic acid;MK886;3-[1-(p-chlorobenzyl)-5-(isopropyl)-3-tert-butylthioindol-2-yl]-2;2-dimethyl propanoic acid;NO;nitric oxide;NOS;nitric oxide synthase;PBS;phosphate-buffered saline;PEA;palmitoylethanolamide;RP-HPLC;reversed phase high performance liquid chromatography;SNAP;S-nitroso-N-acetylpenicillamine;SNP;sodium nitroprusside;TGPL;N-p-tosyl-Gly-Pro-Lys-p-nitroanilide [时效性]
