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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Inhibition of gelatinase B (matrix metalloproteinase-9) by dihydrolipoic acid.
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Inhibition of gelatinase B (matrix metalloproteinase-9) by dihydrolipoic acid.

机译：二氢硫辛酸对明胶酶B（基质金属蛋白酶9）的抑制作用。

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摘要

Alpha-lipoic acid (LA) is a disulphide-containing fatty acid that is absorbed from the diet and transported to tissues. Once it has been taken up by mammalian cells, LA is reduced to dihydrolipoic acid (DHLA), a vicinal dithiol, and rapidly effluxed into the extracellular milieu. We hypothesized that DHLA may be an effective inhibitor of human gelatinase B (GelB). Purified human GelB was incubated with 0 to 200 micromol/L DHLA, and residual enzyme activity was measured by HPLC using a fluorogenic substrate (matrix metalloproteinase substrate III). DHLA inhibited GelB in a dose-dependent fashion with an IC50 of 20 micromol/L. Oxidation of DHLA resulted in a loss of DHLA's capacity to inhibit GelB. The DHLA-mediated inhibition of GelB was independent of the zinc concentration in the reaction buffer. DHLA had no inhibitory effect on gelatinase A. Zymographs of activated neutrophil lysates demonstrated that higher concentrations of DHLA also prevent the activation of GelB proenzyme. Bronchoalveolar lavage fluid from mice fed a diet enriched with LA showed significantly increased GelB inhibitory capacity (p = 0.0002 vs. regular diet). We conclude that DHLA can modulate neutrophil-derived GelB activity through direct inhibition of enzyme activity and by preventing the activation of GelB proenzyme.
机译：α-硫辛酸（LA）是一种含有二硫化物的脂肪酸，可从饮食中吸收并运输到组织中。一旦被哺乳动物细胞吸收，LA就还原为邻二硫醇二氢硫辛酸（DHLA），并迅速外排到细胞外环境中。我们假设DHLA可能是人类明胶酶B（GelB）的有效抑制剂。将纯化的人GelB与0至200 micromol / L DHLA孵育，并使用荧光底物（基质金属蛋白酶底物III）通过HPLC测定残留的酶活性。 DHLA以剂量依赖性方式抑制GelB，IC50为20 micromol / L。 DHLA的氧化导致DHLA抑制GelB的能力丧失。 DHLA介导的GelB抑制与反应缓冲液中锌浓度无关。 DHLA对明胶酶A无抑制作用。活化的嗜中性粒细胞裂解物的酶谱仪显示，较高浓度的DHLA也会阻止GelB酶的活化。饲喂富含LA的饮食的小鼠支气管肺泡灌洗液显示出明显的GelB抑制能力增强（相对于常规饮食，p = 0.0002）。我们得出的结论是，DHLA可以通过直接抑制酶活性并通过阻止GelB酶的活化来调节中性粒细胞衍生的GelB活性。

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