Department of Pharmacology and Toxicology, Medical College of Wisconsin, Milwaukee, Wisconsin 53226, USA.
Am J Physiol Heart Circ Physiol. 2011 Mar;300(3):H725-35. doi: 10.1152/ajpheart.00696.2009. Epub 2010 Dec 30.
Arachidonic acid (AA) metabolites function as EDHFs in arteries of many species. They mediate cyclooxygenase (COX)- and nitric oxide (NO)-independent relaxations to acetylcholine (ACh). However, the role of AA metabolites as relaxing factors in mouse arteries remains incompletely defined. ACh caused concentration-dependent relaxations of the mouse thoracic and abdominal aorta and carotid, femoral, and mesentery arteries (maximal relaxation: 57 ± 4%, 72 ± 4%, 82 ± 3%, 80 ± 3%, and 85 ± 3%, respectively). The NO synthase inhibitor nitro-L-arginine (L-NA; 30 μM) blocked relaxations in the thoracic aorta, and L-NA plus the COX inhibitor indomethacin (10 μM) inhibited relaxations in the abdominal aorta and carotid, femoral, and mesenteric arteries (maximal relaxation: 31 ± 10%, 33 ± 5%, 41 ± 8%, and 73 ± 3%, respectively). In mesenteric arteries, NO- and COX-independent relaxations to ACh were inhibited by the lipoxygenase (LO) inhibitors nordihydroguaiaretic acid (NDGA; 10 μM) and BW-755C (200 μM), the K(+) channel inhibitor apamin (1 μM), and 60 mM KCl and eliminated by endothelium removal. They were not altered by the cytochrome P-450 inhibitor N-methylsulfonyl-6-(2-propargyloxyphenyl)hexanamide (20 μM) or the epoxyeicosatrienoic acid antagonist 14,15-epoxyeicosa-5(Z)-enoic acid (10 μM). AA relaxations were attenuated by NDGA or apamin and eliminated by 60 mM KCl. Reverse-phase HPLC analysis revealed arterial [(14)C]AA metabolites that comigrated with prostaglandins, trihydroxyeicosatrienoic acids (THETAs), hydroxyepoxyeicosatrienoic acids (HEETAs), and hydroxyeicosatetraenoic acids (HETEs). Epoxyeicosatrienoic acids were not observed. Mass spectrometry confirmed the identity of 6-keto-PGF(1α), PGE(2), 12-HETE, 15-HETE, HEETAs, 11,12,15-THETA, and 11,14,15-THETA. AA metabolism was blocked by NDGA and endothelium removal. 11(R),12(S),15(S)-THETA relaxations (maximal relaxation: 73 ± 3%) were endothelium independent and blocked by 60 mM KCl. Western immunoblot analysis and RT-PCR of the aorta and mesenteric arteries demonstrated protein and mRNA expression of leukocyte-type 12/15-LO. Thus, in mouse resistance arteries, 12/15-LO AA metabolites mediate endothelium-dependent relaxations to ACh and AA.
花生四烯酸(AA)代谢物在许多物种的动脉中作为 EDHF 发挥作用。它们介导对乙酰胆碱(ACh)的环氧化酶(COX)和一氧化氮(NO)独立的松弛作用。然而,AA 代谢物作为小鼠动脉中舒张因子的作用仍未完全确定。ACh 引起小鼠胸主动脉和腹主动脉以及颈动脉、股动脉和肠系膜动脉的浓度依赖性松弛(最大松弛:分别为 57 ± 4%、72 ± 4%、82 ± 3%、80 ± 3%和 85 ± 3%)。NO 合酶抑制剂硝基-L-精氨酸(L-NA;30 μM)阻断了胸主动脉的松弛作用,而 L-NA 加 COX 抑制剂吲哚美辛(10 μM)抑制了腹主动脉和颈动脉、股动脉和肠系膜动脉的松弛作用(最大松弛:分别为 31 ± 10%、33 ± 5%、41 ± 8%和 73 ± 3%)。在肠系膜动脉中,ACh 引起的非 NO 和非 COX 依赖性松弛被脂氧合酶(LO)抑制剂 nordihydroguaiaretic acid(NDGA;10 μM)和 BW-755C(200 μM)、钾通道抑制剂 apamin(1 μM)和 60 mM KCl 抑制,并被内皮细胞去除消除。它们不受细胞色素 P-450 抑制剂 N-甲基磺酰基-6-(2-丙烯氧基苯)己酰胺(20 μM)或环氧二十碳三烯酸拮抗剂 14,15-环氧二十碳五烯酸(10 μM)的影响。AA 松弛作用被 NDGA 或 apamin 减弱,并被 60 mM KCl 消除。反相高效液相色谱分析显示动脉中与前列腺素、三羟二十碳三烯酸(THETAs)、羟基环氧二十碳三烯酸(HEETAs)和羟二十碳四烯酸(HETEs)共迁移的 [14C]AA 代谢物。未观察到环氧二十碳三烯酸。质谱证实了 6-酮-PGF(1α)、PGE(2)、12-HETE、15-HETE、HEETAs、11,12,15-THETA 和 11,14,15-THETA 的身份。NDGA 和内皮细胞去除阻断了 AA 代谢。11(R),12(S),15(S)-THETA 松弛(最大松弛:73 ± 3%)是内皮细胞非依赖性的,被 60 mM KCl 阻断。主动脉和肠系膜动脉的 Western 免疫印迹分析和 RT-PCR 显示白细胞 12/15-LO 的蛋白和 mRNA 表达。因此,在小鼠阻力动脉中,12/15-LO AA 代谢物介导对 ACh 和 AA 的内皮依赖性松弛作用。