中国临床药理学杂志
中國臨床藥理學雜誌
중국림상약이학잡지
The Chinese Journal of Clinical Pharmacology
2015年
16期
1648-1651
,共4页
苏启表%韦桂宁%王来友%廖丽贞%赵杰%李国标%李卫东
囌啟錶%韋桂寧%王來友%廖麗貞%趙傑%李國標%李衛東
소계표%위계저%왕래우%료려정%조걸%리국표%리위동
拟黑多刺蚁乙醇提取物石油醚部位%抗痛风活性%细胞色素P450酶
擬黑多刺蟻乙醇提取物石油醚部位%抗痛風活性%細胞色素P450酶
의흑다자의을순제취물석유미부위%항통풍활성%세포색소P450매
petroleum ether fraction of ethanol extracts of polyrhachisvicina Roger%antigout activity%cytochrome P450
目的:拟黑多刺蚁乙醇提取物石油醚部位对大鼠肝微粒体细胞色素P450酶的影响。方法健康SD雄性大鼠随机分为6组,拟黑多刺蚁乙醇提取物石油醚部位低、中、高3个剂量组(实验组,分别相当于药材1,2,4 g? kg-1)、地塞米松阳性对照组、苯巴比妥阳性对照组、空白对照组,每组3只。实验组大鼠分别灌胃给予拟黑多刺蚁乙醇提取物石油醚部位低、中、高3个剂量,每天一次,连续10 d;地塞米松阳性对照组大鼠腹腔给予地塞米松100 mg? kg-1,每天一次,连续4 d;苯巴比妥阳性对照组大鼠腹腔给予苯巴比妥80 mg? kg-1,每天一次,连续3 d;空白对照组大鼠给予等量0.9%氯化钠,均灌胃给药,每天一次,连续10 d。取肝组织,用液质联用、荧光高效液相色谱、反转录-聚合酶链反应、免疫印迹杂交方法分别检测细胞色素P450酶活性,基因表达和蛋白表达的变化。结果拟黑多刺蚁乙醇提取物石油醚部位低、中、高剂量均能显著性提高CYP1A2 mRNA水平、蛋白表达水平以及酶活性,且呈剂量依赖性。结论拟黑多刺蚁乙醇提取物石油醚部位对大鼠 CYP1 A2有诱导作用,提示其可能与CYP1A2底物、诱导剂或抑制剂发生药物相互作用。
目的:擬黑多刺蟻乙醇提取物石油醚部位對大鼠肝微粒體細胞色素P450酶的影響。方法健康SD雄性大鼠隨機分為6組,擬黑多刺蟻乙醇提取物石油醚部位低、中、高3箇劑量組(實驗組,分彆相噹于藥材1,2,4 g? kg-1)、地塞米鬆暘性對照組、苯巴比妥暘性對照組、空白對照組,每組3隻。實驗組大鼠分彆灌胃給予擬黑多刺蟻乙醇提取物石油醚部位低、中、高3箇劑量,每天一次,連續10 d;地塞米鬆暘性對照組大鼠腹腔給予地塞米鬆100 mg? kg-1,每天一次,連續4 d;苯巴比妥暘性對照組大鼠腹腔給予苯巴比妥80 mg? kg-1,每天一次,連續3 d;空白對照組大鼠給予等量0.9%氯化鈉,均灌胃給藥,每天一次,連續10 d。取肝組織,用液質聯用、熒光高效液相色譜、反轉錄-聚閤酶鏈反應、免疫印跡雜交方法分彆檢測細胞色素P450酶活性,基因錶達和蛋白錶達的變化。結果擬黑多刺蟻乙醇提取物石油醚部位低、中、高劑量均能顯著性提高CYP1A2 mRNA水平、蛋白錶達水平以及酶活性,且呈劑量依賴性。結論擬黑多刺蟻乙醇提取物石油醚部位對大鼠 CYP1 A2有誘導作用,提示其可能與CYP1A2底物、誘導劑或抑製劑髮生藥物相互作用。
목적:의흑다자의을순제취물석유미부위대대서간미립체세포색소P450매적영향。방법건강SD웅성대서수궤분위6조,의흑다자의을순제취물석유미부위저、중、고3개제량조(실험조,분별상당우약재1,2,4 g? kg-1)、지새미송양성대조조、분파비타양성대조조、공백대조조,매조3지。실험조대서분별관위급여의흑다자의을순제취물석유미부위저、중、고3개제량,매천일차,련속10 d;지새미송양성대조조대서복강급여지새미송100 mg? kg-1,매천일차,련속4 d;분파비타양성대조조대서복강급여분파비타80 mg? kg-1,매천일차,련속3 d;공백대조조대서급여등량0.9%록화납,균관위급약,매천일차,련속10 d。취간조직,용액질련용、형광고효액상색보、반전록-취합매련반응、면역인적잡교방법분별검측세포색소P450매활성,기인표체화단백표체적변화。결과의흑다자의을순제취물석유미부위저、중、고제량균능현저성제고CYP1A2 mRNA수평、단백표체수평이급매활성,차정제량의뢰성。결론의흑다자의을순제취물석유미부위대대서 CYP1 A2유유도작용,제시기가능여CYP1A2저물、유도제혹억제제발생약물상호작용。
Objective To study the effect of the petroleum ether fraction of ethanol extracts of Polyrhachisvicina Roger with antigout activity on liver microsomal cytochrome P450 in rats.Methods Healthy male SD rats were randomly divided into six groups (3 rats of each group):three groups of the petroleum ether fraction of ethanol extracts of Polyrhachisvi-cina Roger ( test groups, the low dose group, the middle dose group and the high dose group with equivalent to 1, 2, 4 g? kg -1, respectively), two positive control groups and one blank control group.The rats in the low dose, the middle dose and the high dose test groups were adminis-tered daily by gavage at corresponding dose of the petroleum ether frac-tion of ethanol extracts of Polyrhachisvicina Roger for 10 consecutive days.The rats in positive control groups were treated by dexamethasone ( 100 mg? kg-1? d-1 , ip, daily for 4 days ) or phenobarbital ( 80 mg? kg-1? d-1 , ip, daily for 3 days ) .Blank control rats received equivalent volume of sterile normal saline daily by gavage for 10 consecu-tive days.The levels of CYP450 activity, mRNA, protein in rat liver mi-crosome were analyzed by LC/MS/MS or RP-HPLC-FLD, RT-PCR, Western blot, respectively.Results CYP1A2 activity, protein expression and mRNA levels were increased signifi-cantly in a dose-dependent manner with the petroleum ether fraction of ethanol extracts of Polyrhachisvicina Roger at low, middle and high dose, respectively.Conclusion The petroleum ether fraction of ethanol extracts of Polyrhachis-vicina Roger can induce CYP1A2 in rats, suggesting the potential of drug-drug interactions between the petroleum ether fraction of ethanol extracts of Polyrhachisvicina Roger and the inducers, inhibitors, or substrates of CYP1A2.