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乙醛酸化合物作为缺氧细胞的放射增敏剂。

Glyoxylic compounds as radiosensitizers of hypoxic cells.

作者信息

Cornago M P, Lopez Zumel M C, Alvarez M V, Izquierdo M C

机构信息

Instituto Química Física Rocasolano, CSIC, Madrid, Spain.

出版信息

Biochem Med Metab Biol. 1990 Jun;43(3):253-62. doi: 10.1016/0885-4505(90)90032-v.

Abstract

The radiosensitizing effect of five glyoxal derivatives on the survival of TC-SV40 cells has been measured, under aerobic and hypoxic conditions. A toxicity study was previously performed in order to use nontoxic concentrations. The OER for the TC-SV40 cells was 2.74. None of the glyoxylic compounds showed radiosensitizing activity under aerobic conditions while in hypoxia their radiosensitizing factors decreased in the order phenylglyoxylic acid (1.68 at 8 x 10(-3) mole dm-3) greater than phenylglyoxal (1.55 at 5 x 10(-6) mole dm-3) greater than 2-2' furil (1.48 at 5 x 10(-5) mole dm-3) greater than glyoxylic acid (1.39 at 1 x 10(-3) mole dm-3) greater than glyoxal (1.30 at 5 x 10(-5) mole dm-3). The dose-modifying factors were also determined at two equimolar concentrations 5 x 10(-5) and 5 x 10(-6) mole dm-3. A concentration effect was noticed for all the compounds although their relative radiosensitizing activity kept, independently of the concentration, the same order noted above. Glyoxals with aromatic or heterocyclic rings exert a greater radiosensitization than the others. The acidic compounds have less radiosensitizing activity than their aldehydic counterparts. Interaction of these glyoxals with NPSH cellular groups was tested and the low degree of inhibition shows that this mechanism would contribute very little, if any, to the radiosensitization effect.

摘要

在需氧和缺氧条件下,已测定了五种乙二醛衍生物对TC - SV40细胞存活的放射增敏作用。此前进行了毒性研究以使用无毒浓度。TC - SV40细胞的氧增强比为2.74。在需氧条件下,没有一种乙醛酸化合物表现出放射增敏活性,而在缺氧条件下,它们的放射增敏因子按以下顺序降低:苯乙醛酸(8×10⁻³摩尔/立方分米时为1.68)>苯乙二醛(5×10⁻⁶摩尔/立方分米时为1.55)>2,2'-糠偶酰(5×10⁻⁵摩尔/立方分米时为1.48)>乙醛酸(1×10⁻³摩尔/立方分米时为1.39)>乙二醛(5×10⁻⁵摩尔/立方分米时为1.30)。还在5×10⁻⁵和5×10⁻⁶摩尔/立方分米这两个等摩尔浓度下测定了剂量修正因子。尽管所有化合物的相对放射增敏活性与浓度无关保持上述相同顺序,但仍观察到了浓度效应。带有芳环或杂环的乙二醛比其他乙二醛具有更大的放射增敏作用。酸性化合物的放射增敏活性低于其醛类对应物。测试了这些乙二醛与细胞内NPSH基团的相互作用,低程度的抑制表明该机制对放射增敏作用的贡献极小(如果有贡献的话)。

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