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Analgesic and toxic effects of venenum bufonis and its constituent compound cinobufagin: A comparative study.
Neurotoxicology and Teratology ( IF 2.6 ) Pub Date : 2019-03-31 , DOI: 10.1016/j.ntt.2019.03.004
Longsheng Xu 1 , Shizhen Wang 2 , Hui Shen 1 , Qingli Feng 1 , Xiaoping Zhang 1 , Huadong Ni 1 , Ming Yao 1
Affiliation  

OBJECTIVE In this study, we aimed to compare the analgesic and toxic effects of Venenum Bufonis (VB) with those of cinobufagin (CBG), a monomer isolated from VB, to provide the experimental basis for further research and development of VB. METHODS After intragastric administration, the analgesic activities of VB and CBG were compared using the hot plate test and acetic acid-induced writhing test. Their side effects were also compared using hepatotoxicity, acute toxicity, cytotoxicity, and hemolytic toxicity tests, as well as by evaluating their effects on rat heart rate. RESULTS In the hot plate test, both drugs prolonged paw withdrawal latency; however, CBG-treated mice exhibited significantly longer latency than VB-treated mice. In the acetic acid-induced writhing test, both drugs inhibited mouse writhing; however, the inhibitory effects of CBG were stronger. In addition, VB significantly increased serum aspartate aminotransferase (AST) levels, whereas CBG did not these levels. The LD50 of VB and CBG was 36.25 and 4.78 mg/kg, respectively. Both drugs increased the heart rate with CBG exhibiting stronger effects. Moreover, results showed that the cytotoxicity of CBG was more dose-dependent than that of VB. Both VB and CBG showed low hemolytic toxicity. CONCLUSIONS Both VB and CBG exhibited analgesic effects and low hemolytic toxicity; however, the latter showed stronger analgesic activity and less hepatotoxicity. Additionally, both VB and CBG increased the heart rate; however, CBG had stronger effects and higher acute toxicity.

中文翻译:

布氏venenum及其组成成分西诺蟾蜍精的镇痛和毒性作用:一项比较研究。

目的在本研究中,我们旨在比较蟾蜍委内瑞拉(VB)和从VB分离出的丁香蟾蜍精(CBG)的镇痛和毒性作用,从而为进一步研究和开发VB提供实验依据。方法胃内给药后,采用热板试验和乙酸诱导的扭体试验比较VB和CBG的镇痛活性。还使用肝毒性,急性毒性,细胞毒性和溶血毒性测试,以及评估它们对大鼠心率的影响,比较了它们的副作用。结果在热板试验中,两种药物均延长了爪子的退缩潜伏期。但是,CBG处理的小鼠比VB处理的小鼠表现出更长的潜伏期。在乙酸诱导的扭体试验中,两种药物均能抑制小鼠扭体。然而,CBG的抑制作用更强。此外,VB显着提高了血清天冬氨酸转氨酶(AST)的水平,而CBG则没有这些水平。VB和CBG的LD50分别为36.25和4.78 mg / kg。两种药物均能增加心率,CBG表现出更强的作用。此外,结果表明,CBG的细胞毒性比VB更具剂量依赖性。VB和CBG均显示出低溶血毒性。结论VB和CBG均具有镇痛作用和低溶血毒性。然而,后者显示出更强的止痛活性和较低的肝毒性。此外,VB和CBG均可提高心率。然而,CBG的作用更强,急性毒性更高。而CBG没有这些水平。VB和CBG的LD50分别为36.25和4.78 mg / kg。两种药物均能增加心率,CBG表现出更强的作用。此外,结果表明,CBG的细胞毒性比VB更具剂量依赖性。VB和CBG均显示出低溶血毒性。结论VB和CBG均具有镇痛作用和低溶血毒性。然而,后者显示出更强的止痛活性和较低的肝毒性。此外,VB和CBG均可提高心率。然而,CBG的作用更强,急性毒性更高。而CBG没有这些水平。VB和CBG的LD50分别为36.25和4.78 mg / kg。两种药物均能增加心率,CBG表现出更强的作用。此外,结果表明,CBG的细胞毒性比VB更具剂量依赖性。VB和CBG均显示出低溶血毒性。结论VB和CBG均具有镇痛作用和低溶血毒性。然而,后者显示出更强的止痛活性和较低的肝毒性。此外,VB和CBG均可提高心率。然而,CBG的作用更强,急性毒性更高。VB和CBG均显示出低溶血毒性。结论VB和CBG均具有镇痛作用和低溶血毒性。然而,后者显示出更强的止痛活性和较低的肝毒性。此外,VB和CBG均可提高心率。然而,CBG的作用更强,急性毒性更高。VB和CBG均显示出低溶血毒性。结论VB和CBG均具有镇痛作用和低溶血毒性。然而,后者显示出更强的止痛活性和较低的肝毒性。此外,VB和CBG均可提高心率。然而,CBG的作用更强,急性毒性更高。
更新日期:2019-11-01
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