摘要
为了研究博落回中6种主要生物碱别隐品碱、原阿片碱、血根碱、白屈菜红碱、二氢血根碱和二氢白屈菜红碱对大鼠和猪肝胞液醌氧化还原酶2(NQO2)的影响,初步筛选出对大鼠或猪NQO2具有诱导或抑制作用的生物碱,探讨其在畜禽体内的代谢机制,建立了大鼠和猪NQO2体外孵育体系,以槲皮素为阳性对照,噻唑蓝(MTT)为底物,阳性对照物和待测化合物分别与空白组肝胞液孵育,初步筛选出具有诱导或抑制作用的生物碱。结果显示:博落回中的6种主要生物碱对大鼠和猪NQO2的抑制类型均是可逆性反竞争性抑制,其中原阿片碱和血根碱对大鼠和猪肝胞液NQO2具有较强的抑制作用;原阿片碱对雄性大鼠、雌性大鼠和猪NQO2的抑制常数分别为29.26、93.84和18.35μmol·L-1,半数抑制浓度(IC50)分别为(39.80±2.42)、(203.65±0.20)和(309.20±0.83)μmol·L-1;血根碱对雄性大鼠、雌性大鼠和猪NQO2的抑制常数分别为54.87、23.34和151.3μmol·L-1,IC50分别为(160.67±5.77)、(148.00±6.62)和(118.25±0.11)μmol·L-1;别隐品碱和二氢白屈菜红碱对雌性大鼠NQO2无抑制作用,二氢血根碱对猪NQO2的抑制作用非常微弱。研究结果为博落回中原阿片碱和血根碱的临床应用提供了一定的理论基础。
In order to study the effects of six main alkaloids in Macleaya cordata,such as allocryptopine,protopine,sanguinarine,chelerythrine,dihydrosanguinarine and dihydrochelerythrine,on quinone oxidoreductase 2(NQO2)in the liver cytosols of rats and pigs,alkaloids with inducing or inhibiting effects on NQO2 in rats or pigs were preliminarily screened out,and their metabolic mechanism in livestock and poultry was discussed.In this study,rat NQO2 and pig NQO2 were incubated in vitro with quercetin as the positive control and thiazole blue(MTT)as the substrate.The positive control and the compounds to be tested were incubated with the hepatocyte fluid of the blank group,and the alkaloids with inducing or inhibiting effects were screened out.The results showed that the inhibition types of 6 alkaloids in Macleaya cordata to NQO2 in rats and pigs were reversibly anticompetitive.Among the alkaloids,proto opioid and sanguinarine had strong inhibitory effects on NQO2 in the cytosol of rats and pigs.The inhibitory constants of proto opioid to NQO2 in male rats,female rats and pigs were 29.26,93.84 and 18.35μmol·L-1,respectively,and IC50 were(39.80±2.42),(203.65±0.2)and(309.20±0.83)μmol·L-1,respectively.The inhibition constants of sanguinarine on NQO2 in male,female and pig were 54.87,23.34 and 151.3μmol·L-1,respectively,and IC50 were(160.67±5.77),(148.00±6.62)and(118.25±0.11)μmol·L-1,respectively.The inhibitory effects of allosapine,chelerythrine and dihydrochelerythrine on NQO2 of female rats were weak,while that of dihydrohaemorrhizine on NQO2 of pigs was weak.The above results indicated that the main alkaloids of Macleaya cordata,protopine and sanguinarine,had a strong inhibitory effect on NQO2 in rats and pigs,which provided a theoretical basis for clinical application.
作者
陈敏
张卓亿
刘兆颖
CHEN Min;ZHANG Zhuoyi;LIU Zhaoying(College of Veterinary Medicine,Hunan Agricultural University,Changsha 410128,China)
出处
《畜牧与兽医》
北大核心
2020年第2期40-46,共7页
Animal Husbandry & Veterinary Medicine
基金
湖南省杰出青年基金项目(2017JJ1017)
国家级大学生创新创业训练计划项目(G(S)CX1702)
湖南省大学生创新项目(SCX1702)
湖南农业大学大学生创新项目(XCX17003).
作者简介
第一作者:陈敏(1997-),女,本科生;通信作者:刘兆颖,副教授,研究方向为兽医药理学与毒理学,E-mail:liu_zhaoying@sina.com。
