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首页> 外文期刊>Journal of applied toxicology >L-lactate reduces in vitro the inhibition of butyrylcholinesterase (BChE) by paraoxon (E 600).
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L-lactate reduces in vitro the inhibition of butyrylcholinesterase (BChE) by paraoxon (E 600).

机译：L-乳酸乳酸在体外减少了副福丹（E 600）的抑制丁酰胆碱酯酶（BCHE）。

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摘要

Intoxication with the organophosphorus compound paraoxon (POX), an inhibitor of serine hydrolases, is frequent. Oximes are the only enzyme reactivators clinically available. Serendipitous observation led us to the hypothesis that lactate might attenuate some of the POX effects. In vitro effects of lactate on the inhibition of butyrylcholinesterase (BChE) by POX were assessed in plasma of 12 healthy human volunteers. The determinations were repeated using different lactate and different POX concentrations. The BChE activity determinations were performed in the following settings: (i) baseline untreated plasma (BL); (ii) after addition of POX to plasma (pl+POX); (iii) after POX and plasma were incubated and then lactate was added (pl+POX/lact); (iv) after addition of lactate to plasma (pl+lact); (v) after lactate and plasma were incubated and then POX was added (pl+lact/POX); (vi) after lactate and POX were incubated and then added to plasma (lact+POX/pl). In the micro- and millimolar ranges, lactate is able to abolish in vitro the inhibition of BChE by POX in human plasma when added to plasma prior to POX or when incubated with POX prior to addition to plasma. Lactate added to plasma after POX has no protective effect. In a second set of experiments, the effect of lactate on BChE activity was determined. At high millimolar concentrations, lactate itself inhibits BChE to an extent comparable to POX. Lactate is a mixed inhibitor of BChE, being able to interfere with the enzyme-substrate complex (inhibition constant for the enzyme-inhibitor-substrate complex K'I(EIS) = 81 mM) and the enzyme (inhibition constant for the enzyme-inhibitor complex K(I) (EI) = 26 mM).
机译：用有机磷化合物副植物（POX）的中毒，丝氨酸水解酶的抑制剂频繁。肟是临床上可用的唯一酶反应试剂。 Serendipitoy观察使我们致前的假设可能会衰减一些痘效应。在12个健康人志愿者的血浆中评估乳酸对乳酸对丁酰胆碱酯酶（BCHE）抑制的体外作用。使用不同的乳酸和不同的痘浓度重复测定。在以下设置中进行BCHE活性测定：（i）基线未处理等离子体（BL）; （ii）加入痘血浆（PL + POX）后; （III）孵育POx和血浆后，然后加入乳酸（PL + POX / LACT）; （iv）加入乳酸血浆（PL + Lact）后; （v）孵育乳酸和血浆后，然后加入POx（PL + LACT / POX）; （VI）孵育乳酸和痘后，然后加入血浆（Lact + POX / PL）中。在微量和毫米范围内，当在POx之前或者在血浆之前加入血浆时，乳酸乳酸盐能够在体血浆中通过POX抑制BCHE。痘痘后添加到血浆中的乳酸没有保护作用。在第二组实验中，确定了乳酸对BCHE活性的影响。在高毫摩尔浓度下，乳酸本身抑制BCHE与POX相当的程度。乳酸盐是BCHE的混合抑制剂，能够干扰酶 - 衬底复合物（酶抑制剂 - 底物复合物K'i（EIS）= 81mm的抑制常数）和酶（酶抑制剂的抑制常数复合K（I）（EI）= 26毫米）。

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