Marcocci C, Luini A, Santisteban P, Grollman E F
Endocrinology. 1987 Mar;120(3):1127-33. doi: 10.1210/endo-120-3-1127.
Ca2+-dependent and TSH-, norepinephrine (NE)-, and A23187-induced iodide (I-) efflux from FRTL-5 rat thyroid cells is inhibited by quinacrine and trifluoroperazine, agents that inhibit phospholipase A2 activity. Furthermore, I- efflux can be stimulated by an activator of phospholipase A2 activity, melittin. Phospholipase A2 action releases arachidonic acid from phospholipids; arachidonic acid enhances I- efflux in FRTL-5 cells. Inhibitors of arachidonic acid metabolism via the lipoxygenase pathway, 5,8,11,14-eicosatetraynoic acid and nordihydroguaiaretic acid, and via the cytochrome P450-linked epoxygenase pathway, piperonyl butoxide and 2-diethylaminoethyl-2,2-diphenyl valerate, but not an inhibitor of the cyclooxygenase pathway, indomethacin, can inhibit TSH-, NE-, and A23187-induced I- efflux. TSH, NE, and arachidonic acid stimulation of I- efflux in FRTL-5 cells is associated with increased iodination of thyroglobulin, which is blocked by 10 microM 5,8,11,14-eicosatetraynoic acid and 50 microM piperonyl butoxide. The data thus suggest that TSH- and NE-induced I- efflux from FRTL-5 thyroid cells involves lipoxygenase and/or epoxygenase metabolites of arachidonic acid, released from phospholipids upon Ca2+-dependent activation of phospholipase A2. Since this process is associated with the iodination of thyroglobulin, TSH- and NE-induced I- efflux in FRTL-5 cells may represent the transport of I- from the cell into the follicular lumen in vivo.
钙依赖性以及促甲状腺激素(TSH)、去甲肾上腺素(NE)和A23187诱导的碘离子(I-)从FRTL-5大鼠甲状腺细胞外流受到奎纳克林和三氟拉嗪的抑制,这两种药物可抑制磷脂酶A2的活性。此外,磷脂酶A2活性的激活剂蜂毒素可刺激I-外流。磷脂酶A2的作用是从磷脂中释放花生四烯酸;花生四烯酸可增强FRTL-5细胞中的I-外流。通过脂氧合酶途径(5,8,11,14-二十碳四烯酸和去甲二氢愈创木酸)以及细胞色素P450连接的环氧化酶途径(胡椒基丁醚和2-二乙氨基乙基-2,2-二苯基戊酸)的花生四烯酸代谢抑制剂,而非环氧化酶途径的抑制剂吲哚美辛,可抑制TSH、NE和A23187诱导的I-外流。TSH、NE和花生四烯酸对FRTL-5细胞中I-外流的刺激与甲状腺球蛋白碘化增加有关,这被10微摩尔的5,8,11,14-二十碳四烯酸和50微摩尔的胡椒基丁醚所阻断。因此,数据表明TSH和NE诱导的I-从FRTL-5甲状腺细胞外流涉及花生四烯酸的脂氧合酶和/或环氧化酶代谢产物,这些产物在磷脂酶A2的钙依赖性激活后从磷脂中释放出来。由于这一过程与甲状腺球蛋白的碘化有关,TSH和NE诱导的FRTL-5细胞中I-外流可能代表体内I-从细胞向滤泡腔的转运。