氨溴索作为一氧化氮依赖性可溶性鸟苷酸环化酶激活的抑制剂。
Ambroxol as an inhibitor of nitric oxide-dependent activation of soluble guanylate cyclase.
作者信息
Severina I S, Bussygina O G, Pyatakova N V, Khropov Y V, Krasnoperov R A
机构信息
Institute of Biomedical Chemistry, Russian Academy of Medical Sciences, 10 Pogodinskaya str., 119832, Moscow, Russia.
出版信息
Eur J Pharmacol. 2000 Oct 27;407(1-2):61-4. doi: 10.1016/s0014-2999(00)00739-1.
The influence of ambroxol on the activity of human platelet soluble guanylate cyclase and rat lung soluble guanylate cyclase was investigated. Ambroxol in the concentration range from 0.1 to 10 microM had no effect on the basal activity of both enzymes and slightly enhanced it at 50 and 100 microM. Ambroxol inhibited in a concentration-dependent manner the sodium nitroprusside-induced activation of both enzymes. The IC(50) values for inhibition by ambroxol of sodium nitroprusside-stimulated human platelet soluble guanylate cyclase and rat lung soluble guanylate cyclase were 3.9 and 2.1 microM, respectively. Ambroxol did not influence the stimulation of soluble guanylate cyclase by protoporphyrin 1X. Thus, it is possible that the molecular mechanism of the therapeutic action of ambroxol involves the inhibition of nitric oxide (NO)-dependent activation of soluble guanylate cyclase.
研究了氨溴索对人血小板可溶性鸟苷酸环化酶和大鼠肺可溶性鸟苷酸环化酶活性的影响。浓度范围为0.1至10微摩尔的氨溴索对两种酶的基础活性均无影响，而在50和100微摩尔时略有增强。氨溴索以浓度依赖性方式抑制硝普钠诱导的两种酶的激活。氨溴索抑制硝普钠刺激的人血小板可溶性鸟苷酸环化酶和大鼠肺可溶性鸟苷酸环化酶的IC（50）值分别为3.9和2.1微摩尔。氨溴索不影响原卟啉1X对可溶性鸟苷酸环化酶的刺激。因此，氨溴索治疗作用的分子机制可能涉及抑制一氧化氮（NO）依赖性的可溶性鸟苷酸环化酶激活。
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