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4,6-O-亚乙基-α-D-吡喃葡萄糖(亚乙基葡萄糖)对人红细胞的渗透作用

The permeation of human red cells by 4,6-O-ethylidene- -D-glucopyranose (ethylidene glucose).

作者信息

Baker G F, Widdas W F

出版信息

J Physiol. 1973 May;231(1):129-42. doi: 10.1113/jphysiol.1973.sp010224.

Abstract
  1. The glucose derivative 4, 6-O-ethylidene-alpha-D-glucopyranose (ethylidene glucose) was found to inhibit glucose exit competitively but its penetration into human red cells was unaffected by glucose in the medium.2. In penetrating red cells ethylidene glucose followed diffusion type kinetics without any evidence of saturation up to 360 mM. Besides its penetration being unaffected by glucose, 10(-5)M phloretin, which powerfully inhibits the facilitated transfer of hexoses, did not inhibit penetration.3. Red cells incubated with 1-fluoro-2, 4-dinitrobenzene (FDNB) until glucose exit was reduced by 95% showed no slowing of penetration by ethylidene glucose.4. The potentiation of the development of FDNB inhibition by sugars in the incubating medium was absent when ethylidene glucose was used and there was a slight protective action. Cells pre-incubated with 76 mM ethylidene glucose did not show an uphill transfer from 4 mM-[(14)C]glucose in the outside medium in contrast to cells pre-incubated in 76 mM glucose or in 76 mM 3-O-methyl glucose.5. The possibility that ethylidene glucose penetrated human red cells by simple diffusion was supported by its penetration of guinea-pig red cells at similar rates, by the occurrence of osmotic haemolysis in isosmotic solutions which was unaffected by copper ions and by the relatively high ether/water partition of the compound.
摘要
  1. 发现葡萄糖衍生物4,6-O-亚乙基-α-D-吡喃葡萄糖(亚乙基葡萄糖)能竞争性抑制葡萄糖外流,但培养基中的葡萄糖对其进入人红细胞的过程没有影响。

  2. 在进入红细胞的过程中,亚乙基葡萄糖遵循扩散型动力学,在高达360 mM的浓度下均未出现饱和迹象。除了其进入过程不受葡萄糖影响外,10^(-5)M的根皮素虽能强烈抑制己糖的易化转运,但并不抑制其进入。

  3. 用1-氟-2,4-二硝基苯(FDNB)孵育红细胞直至葡萄糖外流减少95%,此时亚乙基葡萄糖的进入速度并未减慢。

  4. 使用亚乙基葡萄糖时,孵育培养基中的糖对FDNB抑制作用发展的增强作用消失,且有轻微的保护作用。与预先在76 mM葡萄糖或76 mM 3-O-甲基葡萄糖中孵育的细胞不同,预先用76 mM亚乙基葡萄糖孵育的细胞在外界培养基中4 mM - [(14)C]葡萄糖存在时并未出现上坡转运。

  5. 亚乙基葡萄糖以简单扩散方式进入人红细胞这一可能性得到了以下证据的支持:它以相似速率进入豚鼠红细胞;在等渗溶液中发生的渗透溶血不受铜离子影响;以及该化合物相对较高的醚/水分配系数。

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