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徐长卿(Cynanchum paniculatum)作为一种传统中草药,被广泛应用于毒蛇咬伤治疗,然而其疗效的科学实验证据缺乏,治疗的分子机制也不清楚.本文采用有机溶剂萃取、柱层析及高效液相色谱法(HPLC)相结合,从徐长卿中筛选出和分离得到一个功效组分,经质谱和核磁共振鉴定为丹皮酚原苷.动物活体实验与组织病理切片观察表明,该组分显著地抑制尖吻蝮(Deinagkistrodon acutus)蛇毒引起的出血、水肿及肌肉组织坏死等活性.体外酶活检测显示,丹皮酚原苷可以抑制尖吻蝮蛇毒水解纤维蛋白原活性和PLA2活性.进一步采用分子模拟软件技术,揭示出丹皮酚原苷是通过与蛇毒中主要成分金属蛋白酶和PLA2发生相互作用,从而抑制尖吻蝮蛇毒发挥致伤作用.本研究首次揭示了中草药徐长卿治疗蛇伤的分子机制,为中医治疗毒蛇咬伤使用徐长卿找到了科学实验证据,也为蛇伤药物的研发提供了新的思路.
As a traditional Chinese herbal medicine, Cynanchum paniculatum has been widely used in the treatment of snake bites, however, the lack of scientific evidence for its curative effect and the molecular mechanism of its treatment are still unclear.In this paper, organic solvent extraction, column chromatography and high performance liquid chromatography Chromatography (HPLC), a functional component was screened and isolated from Xuchangqing, identified as paeonol glycosides by mass spectrometry and nuclear magnetic resonance.The observation of animal experiments and histopathological sections showed that this component was significantly inhibited Deinagkistrodon acutus venom caused by bleeding, edema and muscle tissue necrosis activity in vitro enzyme assay showed that paeonol glycosides can inhibit the Agkistrodon disintegrin fibrinogen hydrolysis activity and PLA2 activity further molecular modeling Software technology revealed that paeonol propeptide glycosides through the interaction with the major components of the metalloproteinase and PLA2, thereby inhibiting the acutissimus venom play a role in injury.This study for the first time revealed the Chinese herbal medicine Xu Zhangqing molecular mechanism of treatment of snakebite, For Chinese medicine treatment of snake bites using Xu Changqing found scientific experimental evidence, but also for snakebite drug development New ideas.