天然产物研究与开发 ›› 2018, Vol. 30 ›› Issue (5): 761-766.doi: 10.16333/j.1001-6880.2018.5.006

所属专题: No.2

• 研究论文 • 上一篇    下一篇

蓑衣莲酮硫酸酯对对乙酰氨基酚诱导小鼠急性肝损伤的保护作用

蔺良才1,2, 赵菲菲1,2, 王敏1,2, 陈海东1,2, 徐国波1,2, 廖尚高1,2*   

  1. 1贵州医科大学药学院 药用植物功效与利用国家重点实验室, 贵阳 550025;2贵州医科大学教育部民族药与中药开发应用工程研究中心,贵阳 550004
  • 出版日期:2018-06-04 发布日期:2018-06-04
  • 基金资助:

    国家自然科学基金(81260506);贵州省优秀青年科技人才项目(2015-32)

Protection of Auriculatone Sulphate Against APAP-induced Acute Liver Injury in Mice

LIN Liang-cai1,2, HAO Fei-fei1,2, WANG Min1,2, CHEN Hai-dong1,2, XU Guo-bo1,2, LIAO Shang-gao1,2*   

  1. 1School of Pharmacy & State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University,Guizhou 550025, China;2Engineering Research Center for the Development and Application of Ethnic Medicine and TCM(Ministry of Education), Guiyang 550004, China
  • Online:2018-06-04 Published:2018-06-04

摘要: 蓑衣莲酮硫酸酯(Auriculatone sulphate,AS)是天然保肝活性化合物蓑衣莲酮的前药。为评估AS的保肝作用,课题采用小鼠腹腔注射300 mg/kg的对乙酰氨基酚(APAP)复制小鼠急性肝损伤模型,通过静脉注射给予25 mg/kg的AS,测定给药后小鼠血清中的谷草转氨酶(AST)、谷丙转氨酶(ALT)和乳酸脱氢酶(LDH)的含量变化,从肝损伤水平初步了解AS对肝脏的保护作用;通过测定肝组织中丙二醛(MDA)和谷胱甘肽(GSH)的水平以及超氧化物歧化酶(SOD)活性的变化,了解AS对氧化损伤的保护作用;通过小鼠肝组织的病理学检查,直观评价AS通过静脉注射给药后对肝脏的保护作用。研究结果显示,静脉注射AS能够显著降低血清中ALT、AST和LDH的水平,使其趋近于正常水平(P<0.001)。与模型组相比,AS不但可以显著降低肝脏中MDA的水平(P<0.001),而且显著增加GSH水平和SOD的活性(P<0.001)。病理学检查显示,AS能显著改善APAP对肝组织的破坏,使肝组织的结构趋近于正常。综上,静脉注射AS可有效保护小鼠免受APAP诱导小鼠急性肝损伤,其保护作用可能与抑制肝脏氧化损伤有关。

关键词: 蓑衣莲酮硫酸酯, 静脉注射, 对乙酰氨基酚肝损伤, 保肝作用

Abstract: Auriculatone sulphate(AS)was a prodrug of auriculatone that is a natural hepatoprotective compound.In order to evaluate the hepatoprotective effect of AS,an acetaminophen(APAP)-induced acute liver injury model of mice was established by intraperitoneal administration of 300 mg/kg APAP.The hepatoprotective effect of AS(25 mg/kg)was initially evaluated by determining its inhibitory effect on the increases of serum alanine aminotransferase(ALT),aspartate aminotransferase(AST)and lactate dehydrogenase(LDH)induced by APAP.The protective effect of AS against oxidative damage was assessed by measuring the levels of malondialdehyde(MDA)and glutathione(GSH)and testing the activity of superoxide dismutase(SOD)in the liver tissue.Histochemical analysis of liver tissue was also conducted to evaluate the hepatoprotective effect of AS.The results showed that intravenous pretreatment with AS significantly prevented the liver tissue from APAP-induced injury,and retained the serum ALT,AST and LDH levels close to those of the control group(P<0.001).When compared with the APAP group,AS pretreatment significantly decreased the hepatic level of MDA(P<0.001),and increased the hepatic level of GSH as well as the activity of SOD(P<0.001).Histochemical examinations showed that AS treatment significantly improved the pathological changes of liver tissues.In conclusion,intravenous administration of AS effectively protected mouse against APAP-induced liver injury and the protection might involve its inhibition of liver tissue oxidative damage.

Key words: auriculatone sulfate, intravenous injection, acetaminophen-induced liver injury, hepatoprotection  

中图分类号: 

R285 R965