新型潜在抗黑素抑制剂、自旋标记三氮杂烯和亚硝基源对酪氨酸酶多巴氧化酶活性的调节作用。

Cancer biochemistry biophysics Pub Date : 1999-07-01
V Gadjeva, A Zheleva, E Raikova
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引用次数: 0

摘要

用Bumett的分光光度法研究了新合成的烷基化自旋标记三氮杂烯和自旋标记亚硝基脲衍生物对蘑菇酪氨酸酶多巴氧化酶活性的调节作用(Burnett et al., 1967)。自旋标记的三氮杂烯对酪氨酸酶的多巴氧化酶活性均表现出活化作用,而临床使用的不含氮氧化物部分的三氮杂烯(DTIC)则表现出抑制作用。在相同的实验条件下,自旋标记的氨基酸亚硝基脲表现出双重作用——在酶反应开始时具有激活作用,在反应后期具有抑制作用。推导出自旋标记化合物的活化作用是由氮氧化物部分引起的,而所有化合物的抑制作用都取决于它们的半衰期。本研究一方面有助于进一步明确新化合物的作用机制,另一方面对其抗黑色素瘤活性的初步预测具有重要意义。
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Modulating effect of new potential antimelanomic agents, spin-labeled triazenes and nitrosoureas on the DOPA-oxidase activity of tyrosinase.

The modulating effect of newly synthesized alkylating spin labeled triazene and spin labeled nitrosourea derivatives on the DOPA-oxidase activity of mushroom tyrosinase has been investigated by Bumett's spectrophotometric method (Burnett et al., 1967). All spin labeled triazenes have exhibited activating effect on DOPA-oxidase activity of tyrosinase, whereas clinically used triazene (DTIC), which does not contain nitroxide moiety, have showed inhibiting effect. At the same experimental conditions the spin labeled aminoacid nitrosoureas have showed dual effect - activating, in the beginning of the enzyme reaction and inhibiting later on. It is deduced that the activating effect of the spin labeled compounds is due to the nitroxide moiety and the inhibiting effect of all compounds depends on their half-life time. This study might contribute to make more clear the mechanism of action of the new compounds and on the other hand would come in quite useful as a preliminary prognosis for their antimelanomic activity.

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