Nielsen Vance G, Bazzell Charles M
Department of Anesthesiology, The University of Arizona College of Medicine, 1501 North Campbell Avenue, P.O. Box 245114, Tucson, AZ, 85724-5114, USA.
J Thromb Thrombolysis. 2017 Feb;43(2):203-208. doi: 10.1007/s11239-016-1442-4.
A complication of defibrinogenation therapy with snake venom enzymes such as ancrod is hypofibrinogenemia associated bleeding secondary to no human-derived inhibitor being available to inactivate or diminish the activity of such enzymes. Of interest, ancrod contains a critical histidine residue without which enzymatic activity is inhibited, and carbon monoxide has been demonstrated to inhibit biomolecular function by interacting with histidine moieties in ion channels. We tested the hypothesis that exposure of three different snake venoms containing serine proteases with thrombin-like activity (which included ancrod) to carbon monoxide derived from carbon monoxide releasing molecule-2 would diminish their effects on plasmatic coagulation as assessed by thrombelastography. In the case of the Malayan pit viper and Eastern diamondback rattlesnake venoms, carbon monoxide diminished the effects of thrombin-like activity. In contrast, timber rattlesnake venom demonstrated enhancement of "thrombin-generating" activity with simultaneous loss of thrombin-like activity in response to carbon monoxide exposure. These findings may serve as the rational basis for not just continuing to investigate the potential of snake venom enzymes as clinical defibrinogenating agents, but to also to assess the potential to stop such agents from becoming a catalytic "runaway train" by judicious application of a biochemical "brake" such as carbon monoxide.
使用诸如安克洛酶等蛇毒酶进行去纤维蛋白原治疗的一个并发症是低纤维蛋白原血症伴发的出血,这是由于没有可用于使此类酶失活或降低其活性的人源抑制剂。有趣的是,安克洛酶含有一个关键的组氨酸残基,没有该残基酶活性就会受到抑制,并且一氧化碳已被证明可通过与离子通道中的组氨酸部分相互作用来抑制生物分子功能。我们测试了这样一个假设:将三种含有具有凝血酶样活性的丝氨酸蛋白酶的不同蛇毒(其中包括安克洛酶)暴露于一氧化碳释放分子-2产生的一氧化碳中,通过血栓弹力图评估,会减弱它们对血浆凝血的影响。就马来亚蝮蛇毒和东部菱斑响尾蛇毒而言,一氧化碳减弱了凝血酶样活性的影响。相比之下,粗鳞响尾蛇毒在暴露于一氧化碳后显示出“凝血酶生成”活性增强,同时凝血酶样活性丧失。这些发现不仅可以作为继续研究蛇毒酶作为临床去纤维蛋白原制剂潜力的合理依据,还可以作为通过明智地应用诸如一氧化碳这样的生化“刹车”来评估阻止此类制剂成为催化“失控列车”潜力的合理依据。