Department of Anesthesiology and Pain Medicine, The First Affiliated Hospital of Jiaxing University, Jiaxing 314001, China.
Department of Basic Medical Sciences, Jiangsu College of Nursing, Huai'an 223001, China.
Neurotoxicol Teratol. 2019 May-Jun;73:49-53. doi: 10.1016/j.ntt.2019.03.004. Epub 2019 Mar 31.
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.
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.
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 LD 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.
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.
本研究旨在比较蟾酥(VB)与从 VB 中分离得到的单体华蟾酥毒基(CBG)的镇痛作用和毒性作用,为 VB 的进一步研究和开发提供实验依据。
通过灌胃给药,采用热板试验和醋酸诱导扭体试验比较 VB 和 CBG 的镇痛活性。通过肝毒性、急性毒性、细胞毒性和溶血毒性试验以及评估它们对大鼠心率的影响比较它们的副作用。
在热板试验中,两种药物均延长了小鼠的舔足潜伏期;然而,CBG 处理组的潜伏期明显长于 VB 处理组。在醋酸诱导的扭体试验中,两种药物均抑制了小鼠的扭体反应;然而,CBG 的抑制作用更强。此外,VB 显著增加了血清天冬氨酸氨基转移酶(AST)水平,而 CBG 没有升高这些水平。VB 和 CBG 的 LD 分别为 36.25 和 4.78 mg/kg。两种药物均增加了心率,其中 CBG 的作用更强。此外,结果表明 CBG 的细胞毒性比 VB 更具剂量依赖性。VB 和 CBG 均表现出低溶血毒性。
VB 和 CBG 均具有镇痛作用和低溶血毒性;然而,后者具有更强的镇痛活性和更低的肝毒性。此外,VB 和 CBG 均增加了心率;然而,CBG 的作用更强,急性毒性更高。