木犀草素对大鼠肝肾组织中11β-羟基类固醇脱氢酶的影响  

Effect of Luteolin on 11β-Hydroxysteroid Dehydrogenase in Rat Liver and Kidney

作　　者：邓斌[1] 洪晓丹[1] 姚秋燕[1] 韦炳华[1] DENG Bin HONG Xiao-dan YAO Qiu-yan WEI Bing-hua(Department of Pharmacy, The First Affiliated Hospital of Sun Yat-sen University, Guangzhou 510080, China)

机构地区：[1]中山大学附属第一医院药学部,广东广州510080

出　　处：《中山大学学报（医学科学版）》2017年第5期685-692,共8页Journal of Sun Yat-Sen University:Medical Sciences

基　　金：广东省中医药局项目(20131145)

摘　　要：【目的】考察木犀草素对大鼠组织11β-羟基类固醇脱氢酶(11β-HSD)基因表达、蛋白表达和酶活性的影响。【方法】24只雄性大鼠随机分为4组,称重后灌胃给予1%羧甲基纤维素钠溶液或木犀草素低(5 mg/kg)、中(10 mg/kg)、高(20 mg/kg)剂量组连续14 d后,取肝、肾等糖皮质激素靶组织,采用定量RT-PCR法测定大鼠肝肾组织11β-HSD Ⅰ及11β-HSD Ⅱ基因表达,Western Blot法测定大鼠肝肾组织11β-HSD Ⅰ和11β-HSD Ⅱ蛋白表达,以代谢产物泼尼松、泼尼松龙的生成速率表示酶活性。【结果】木犀草素显著诱导肝脏组织11β-HSD Ⅰ基因表达,抑制11β-HSD Ⅱ基因表达;显著抑制肾脏11β-HSD Ⅰ基因表达,诱导11β-HSD Ⅱ基因表达。木犀草素给药组对肝11β-HSD Ⅰ蛋白表达呈明显的上调趋势,对肝11β-HSD Ⅱ蛋白表达呈明显的下调趋势;对肾11β-HSD Ⅱ蛋白表达呈明显的上调趋势,对肾11β-HSD Ⅰ蛋白表达呈明显的下调趋势。木犀草素明显诱导肝11β-HSD Ⅰ、肾11β-HSD Ⅱ活性。【结论】木犀草素可通过影响大鼠肝肾组织中11β-HSD Ⅰ和11β-HSD Ⅱ基因表达、蛋白表达和酶活性,影响糖皮质激素体内活化及肝肾组织中激素水平。【Objective】To investigate the effect of Luteolin on m RNA expression,protein expression and enzyme activity of 11β-Hydroxysteroid Dehydrogenase（11β-HSD）in rats.【Methods】Twenty-four rats were randomly divided into 4 groups and orally administrated with vehicle（1 % CMC-Na solution）or Luteolin（5,10 or 20 mg/kg daily）for 14 days. Gene expression of 11β-HSD Ⅰ and 11β-HSD Ⅱ in liver and kidney was determined with quantitative RT-PCR method. Protein expression was determined with quantitative Western Blot method. The enzyme activity was expressed as the production rate of metabolites of prednisone and prednisolone.【Results】Luteolin significantly induced gene expression of 11β-HSD Ⅰ and inhibited gene expression of 11β-HSD Ⅱ in liver tissues,significantly inhibited gene expression of 11β-HSD Ⅰ and induced gene expression of 11β-HSD Ⅱ in kidney tissues. Luteolin obviously up-regulated protein expression of 11β-HSD Ⅰ and down-regulated protein expression of 11β-HSD Ⅱ in liver tissues,down-regulated protein expression of 11β-HSD Ⅰ and up-regulated protein expression of 11β-HSD Ⅱ in kidney tissues. Luteolin significantly induced activity of 11β-HSD Ⅰ in liver and 11β-HSD Ⅱ in kidney.【Conclusions】Luteolin could change the activity of corresponding enzyme through affecting gene expression,protein expression and enzyme activity of 11β-HSD Ⅰ and 11β-HSD Ⅱ in liver and kidney tissues in rat,and affect in vivo activation of glucocorticoids and hormone level in liver and kidney.

关 键 词：木犀草素 11Β-羟基类固醇脱氢酶 基因表达 蛋白表达 酶活性 

分 类 号：R9[医药卫生—药学]