Depauw H, De Wolf M, Van Dessel G, Lagrou A, Hilderson H J, Dierick W
RUCA-Laboratory for Human Biochemistry, University of Antwerp, Belgium.
Biochim Biophys Acta. 1990 May 9;1024(1):41-8. doi: 10.1016/0005-2736(90)90206-4.
Gangliosides (GM1, GT1b, GD3) were incorporated in bovine thyroid plasma membranes using the nonspecific lipid transfer protein from beef liver. The transfer of GT1b or GD3 in the presence of 16 units of transfer protein was twice as high as that of GM1. However, taking into account the spontaneous exchange (approximately 8% for GT1b or GD3 and 1% for GM1) the transfer protein seemed to be more effective for GM1. Incorporation of these gangliosides in bovine thyroid plasma membranes caused a concentration dependent inhibition of the TSH-stimulated adenylate cyclase activity. The forskolin-stimulated adenylate cyclase activity was not significantly affected by ganglioside modification of the plasma membranes, indicating that the gangliosides do not act at the level of the catalyst of adenylate cyclase. Binding experiments on the other hand revealed that TSH binding to bovine thyroid plasma membranes was inhibited with the same order of efficacy (GT1b greater than GD3 greater than GM1) and to the same extent as their inhibitory effect on TSH stimulation. Therefore, this indicates that the ganglioside induced drop in TSH binding might be an important factor in the decrease in TSH-stimulated adenylate cyclase activity. Incorporation of GT1b or GD3 (approximately 11 nmol) in bovine thyroid plasma membranes, however, also induced a substantial decrease in cholera toxin-stimulated adenylate cyclase activity (approximately 30%) and to a lesser degree a decrease in NaF-stimulated activity (approximately 17%), whereas GM1 incorporation did not significantly affect these stimulated activities. These latter inhibitory effects were paralleled by changes in fluorescence steady-state anisotropy: GT1b modification of the plasma membranes provoked a slight increase in TMA-DPH anisotropy, whereas the anisotropy of DPH was substantially enhanced after incorporation of GD3 or GT1b. These results suggest that gangliosides might also interfere with the coupling between the alpha-subunit of the stimulatory GTP-binding regulatory protein and the catalyst of the adenylate cyclase system by affecting the membrane fluidity.
利用来自牛肝的非特异性脂质转运蛋白,将神经节苷脂(GM1、GT1b、GD3)掺入牛甲状腺质膜中。在存在16个单位转运蛋白的情况下,GT1b或GD3的转运量是GM1的两倍。然而,考虑到自发交换(GT1b或GD3约为8%,GM1约为1%),转运蛋白对GM1似乎更有效。这些神经节苷脂掺入牛甲状腺质膜会导致对促甲状腺激素(TSH)刺激的腺苷酸环化酶活性产生浓度依赖性抑制。福斯可林刺激的腺苷酸环化酶活性不受质膜神经节苷脂修饰的显著影响,这表明神经节苷脂并非作用于腺苷酸环化酶的催化水平。另一方面,结合实验表明,TSH与牛甲状腺质膜的结合受到抑制,其抑制效力顺序相同(GT1b>GD3>GM1),且抑制程度与它们对TSH刺激的抑制作用相同。因此,这表明神经节苷脂诱导的TSH结合下降可能是TSH刺激的腺苷酸环化酶活性降低的一个重要因素。然而,在牛甲状腺质膜中掺入GT1b或GD3(约11 nmol)也会导致霍乱毒素刺激的腺苷酸环化酶活性大幅下降(约30%),对氟化钠刺激的活性下降程度较小(约17%),而掺入GM1对这些刺激活性没有显著影响。这些后期的抑制作用与荧光稳态各向异性的变化平行:质膜的GT1b修饰导致TMA-DPH各向异性略有增加,而掺入GD3或GT1b后,DPH的各向异性大幅增强。这些结果表明,神经节苷脂可能还通过影响膜流动性来干扰刺激性GTP结合调节蛋白的α亚基与腺苷酸环化酶系统催化物之间的偶联。