Turk J, Wolf B A, Comens P G, Colca J, Jakschik B, McDaniel M L
Biochim Biophys Acta. 1985 Jun 14;835(1):1-17. doi: 10.1016/0005-2760(85)90023-2.
Deuterium-labelled standards of four regionally isomeric epoxyeicosatrienoic acids (EETs) and their hydrolysis products, the dihydroxyeicosatrienoic acids (DHETs), have been prepared and analyzed by capillary column gas chromatography (GC)-negative ion (NI)-methane chemical ionization (MCI)-mass spectrometry (MS) as the pentafluorobenzyl esters. As little as 40 pg of these compounds were readily visualized by these methods, and the deuterium-labelled standards were used in a stable isotope dilution mass spectrometric assay which was linear from near the detection limit over several orders of magnitude. NADPH-dependent synthesis of both EETs and DHETs from arachidonate by hepatic microsomal cytochrome P-450-mono-oxygenase activity was demonstrable with these methods and was significantly suppressed by the compound BW755C (500 microM), but not by eicosa-5,8,11,14-tetraynoic acid (ETYA, 20 microM) or by nordihydroguaiaretic acid (NDGA, 50 microM). All three compounds suppress glucose-induced insulin secretion and 12-hydroxyeicosatetraenoic acid (12-HETE) synthesis by isolated pancreatic islets with similar concentration dependence. Microsomes derived from isolated pancreatic islets synthesized less than 3% of the EET and DHET compounds as a comparable amount of hepatic microsomes. Intact islets synthesized less than 3% by mass of the EET and DHET compounds compared to the mass of 12-HETE produced by the islets. Islets also failed to convert 3H-labelled arachidonate to 3H-labelled EETs or DHETs under conditions where conversion to [3H]12-HETE and to [3H]prostaglandin E2 (but not to [3H]leukotriene C4, D4, or E4) was clearly demonstrable. Neither exogenous EETs nor leukotriene C4 stimulated insulin secretion from the isolated islets or reversed the suppression of glucose-induced secretion by the lipoxygenase inhibitor BW755C. The cytochrome P-450-monooxygenase inhibitor, metyrapone (50 microM), did not influence insulin secretion from the isolated islets under conditions where the lipoxygenase inhibitor, NDGA, suppressed glucose-induced secretion. These observations argue against the recently suggested hypothesis that EETs derived from arachidonate by monooxygenase action participate in glucose-induced insulin secretion by isolated pancreatic islets.
已制备了四种区域异构体环氧二十碳三烯酸(EETs)及其水解产物二羟基二十碳三烯酸(DHETs)的氘标记标准品,并通过毛细管柱气相色谱(GC)-负离子(NI)-甲烷化学电离(MCI)-质谱(MS)分析其五氟苄酯。通过这些方法,低至40皮克的这些化合物都能很容易地被检测到,并且氘标记标准品被用于一种稳定同位素稀释质谱分析中,该分析在从接近检测限到几个数量级的范围内呈线性。用这些方法可证明肝微粒体细胞色素P-450单加氧酶活性从花生四烯酸依赖NADPH合成EETs和DHETs,并且该活性被化合物BW755C(500微摩尔)显著抑制,但不受二十碳-5,8,11,14-四炔酸(ETYA,20微摩尔)或去甲二氢愈创木酸(NDGA,50微摩尔)抑制。所有这三种化合物以相似的浓度依赖性抑制分离的胰岛的葡萄糖诱导的胰岛素分泌和12-羟基二十碳四烯酸(12-HETE)的合成。与相当量的肝微粒体相比,分离的胰岛来源的微粒体合成的EET和DHET化合物不到3%。与胰岛产生的12-HETE的质量相比,完整的胰岛合成的EET和DHET化合物的质量不到3%。在能清楚证明向[3H]12-HETE和[3H]前列腺素E2(但不向[3H]白三烯C4、D4或E4)转化的条件下,胰岛也未能将3H标记的花生四烯酸转化为3H标记的EETs或DHETs。外源性EETs和白三烯C4均未刺激分离的胰岛分泌胰岛素,也未逆转脂氧合酶抑制剂BW755C对葡萄糖诱导分泌的抑制作用。在脂氧合酶抑制剂NDGA抑制葡萄糖诱导分泌的条件下,细胞色素P-450单加氧酶抑制剂美替拉酮(50微摩尔)不影响分离的胰岛的胰岛素分泌。这些观察结果与最近提出的假说相悖,该假说认为通过单加氧酶作用从花生四烯酸衍生的EETs参与分离的胰岛的葡萄糖诱导的胰岛素分泌。