龙利叶止咳活性部位筛选及其作用机制研究
|
摘要
目的对龙利叶的止咳作用进行研究,筛选其活性部位,并初步研究其止咳作用机制。方法制备龙利叶75%乙醇、石油醚、醋酸乙酯、正丁醇、95%乙醇部位提取物,采用改良寇氏法研究龙利叶不同提取部位的急性毒性;采用氨水引咳法制备小鼠模型,用序贯法求出引起半数小鼠咳嗽的喷雾时间,进行止咳活性部位的筛选;采用辣椒素引咳实验,通过观察龙利叶各部位提取物对小鼠阿片受体激动作用和对ATP敏感性钾通道(KATP)的作用,探讨其作用机制。结果龙利叶75%乙醇、醋酸乙酯、正丁醇和95%乙醇部位对小鼠的半数致死剂量(LD_(50))分别为浸膏7.30、17.00、69.68、75.88 g/kg;石油醚部位最大耐受量为浸膏117.71 g/kg;75%乙醇部位和醋酸乙酯部位具有止咳作用,其止咳作用与激动中枢系统的阿片受体和KATP通道有关。结论 75%乙醇和醋酸乙酯部位为龙利叶止咳活性部位,其止咳机制与激动中枢系统的阿片受体和KATP通道有关。
Objective To study the antitussive effect of Sauropus spatulifolius, screen the active part of its antitussive effect, and study its antitussive mechanism. Methods The acute toxicity of different extraction sites of S. spatulifolius were studied by modified Karber's method; The model was made with ammonia liquor to induce cough. The spray time that caused half of the mice to cough was calculated by sequential method with aim to screen the active sites. Capsaicin was used to induce cough, and the mechanism of action of extracts from various parts of S. spatulifolius on opioid receptor and ATP-sensitive potassium channel(KATP) of mice was explored.Results The LD_(50) of 75% ethanol, ethyl acetate, n-butanol, and 95% ethanol extracts was 7.30, 17.00, 69.68, and 75.88 g/kg,respectively; The maximum tolerance dose(MTD) of petroleum ether extracts was 117.71 g/kg; Extracts from 75% ethanol and ethyl acetate had antitussive effects, and its antitussive effect was related to opioid receptor and KATP pathway. Conclusion The fractions from 75% ethanol and ethyl acetate are the active parts of S. spatulifolius for relieving cough, and its antitussive mechanism is related to the KATP pathway and opioid receptors in the excited central system.
Objective To study the antitussive effect of Sauropus spatulifolius, screen the active part of its antitussive effect, and study its antitussive mechanism. Methods The acute toxicity of different extraction sites of S. spatulifolius were studied by modified Karber's method; The model was made with ammonia liquor to induce cough. The spray time that caused half of the mice to cough was calculated by sequential method with aim to screen the active sites. Capsaicin was used to induce cough, and the mechanism of action of extracts from various parts of S. spatulifolius on opioid receptor and ATP-sensitive potassium channel(KATP) of mice was explored.Results The LD_(50) of 75% ethanol, ethyl acetate, n-butanol, and 95% ethanol extracts was 7.30, 17.00, 69.68, and 75.88 g/kg,respectively; The maximum tolerance dose(MTD) of petroleum ether extracts was 117.71 g/kg; Extracts from 75% ethanol and ethyl acetate had antitussive effects, and its antitussive effect was related to opioid receptor and KATP pathway. Conclusion The fractions from 75% ethanol and ethyl acetate are the active parts of S. spatulifolius for relieving cough, and its antitussive mechanism is related to the KATP pathway and opioid receptors in the excited central system.
引文
[1]中国药典[S].一部.2015.
[2]国家中医药管理局《中华本草》编委会.中华本草(第四册)[M].上海:上海科学技术出版社,2006.
[3]中国科学院植物研究所.中国植物志[M].北京:中国科学院植物所,2005.
[4]《全国中草药汇编》编写组.全国中草药汇编下册[M].第2版.北京:人民卫生出版社,2006.
[5]广西壮族自治区革命委员会卫生局.广西本草下册[M].北京:人民卫生出版社,1974.
[6]张国熙,叶锡洪,林胜英,等.千龙合剂对小鼠肺炎双球菌的药效学研究[J].新中医,2002,32(4):35.
[7]邓汉华,邓景云,孔令深,等.千龙汤治疗间质性肺炎62例日[J].新中医,1999,29(11):42.
[8]史筱冰,赵不潜,潘俊辉,等.天龙茶治疗急性支气管炎的临床观察[J].现代临床医学生物工程学杂志,1997,3(2):126.
[9]丘琴,甄汉深,王莹,等.龙利叶根急性毒性和抗炎作用的研究[J].中国实验方剂学杂志,2013,19(2):286-288.
[10]丘琴,黄培倩,甄汉深,等.龙利叶茎急性毒性和抗炎作用的研究[J].时珍国医国药,2016,27(3):541-542.
[11]陈奇.中药药理研究方法学[M].第3版.北京:人民卫生出版社,2011.
[12]甄汉深,刘蓉,丘琴,等.龙利叶抗炎镇痛作用的研究[J].中国实验方剂学杂志,2013,19(9):270-273.
[13]王孝勋,黄茂春,赵旭,等.序贯法研究广西不同产地对叶百部总生物碱对小鼠的止咳作用[J].中华中医药杂志,2012,27(7):1935-1937.
[14]刘宾,江南.序贯法研究甘草酸二铵对小鼠止咳作用[J].中国医院药学杂志,2009,29(10):820-822.
[15]陈奇.中药药理实验方法[M].北京:人民卫生出版社,1994.
[16]唐慧勤,龙颖,董威,等.产地、生长期、商品规格等不同因素对罗汉果止咳作用的影响[J].中草药,2015,46(20):3051-3054.
[17]杨冰月,李敏,任敏,等.基于灰色关联度分析法对半夏及其炮制品总有机酸止咳作用的谱-效关系研究[J].中草药,2016,47(13):2301-2307.
[18]晏子俊,罗燕秋,李作燕,等.暗紫贝母及浙贝母镇咳作用的化学刺激引咳法比较[J].时珍国医国药,2012,23(10):2522-2525.
[19]徐启贵,李勤耕,田睿,等.羟丙哌嗪衍生物的合成及其镇咳活性[J].中国药物化学杂志,2005,15(2):85-88.
[20]Undem B J,Carr M J,Kollarik M.Physiology and plasticity of putative cough fibres in the guinea pig[J].Pulm Pharmacol Ther,2002,15(3):193-198.
[21]陈晓芳.枇杷花醇提物镇咳、平喘、祛痰作用及其机制研究[D].兰州:兰州大学,2011.
[22]Orita K,Kamei J.Involvement of ATP-sensitive K+channels in the anti-tussive effect of moguisteine[J].Eur J Pharmacol,2000,395(2):161-164.
[2]国家中医药管理局《中华本草》编委会.中华本草(第四册)[M].上海:上海科学技术出版社,2006.
[3]中国科学院植物研究所.中国植物志[M].北京:中国科学院植物所,2005.
[4]《全国中草药汇编》编写组.全国中草药汇编下册[M].第2版.北京:人民卫生出版社,2006.
[5]广西壮族自治区革命委员会卫生局.广西本草下册[M].北京:人民卫生出版社,1974.
[6]张国熙,叶锡洪,林胜英,等.千龙合剂对小鼠肺炎双球菌的药效学研究[J].新中医,2002,32(4):35.
[7]邓汉华,邓景云,孔令深,等.千龙汤治疗间质性肺炎62例日[J].新中医,1999,29(11):42.
[8]史筱冰,赵不潜,潘俊辉,等.天龙茶治疗急性支气管炎的临床观察[J].现代临床医学生物工程学杂志,1997,3(2):126.
[9]丘琴,甄汉深,王莹,等.龙利叶根急性毒性和抗炎作用的研究[J].中国实验方剂学杂志,2013,19(2):286-288.
[10]丘琴,黄培倩,甄汉深,等.龙利叶茎急性毒性和抗炎作用的研究[J].时珍国医国药,2016,27(3):541-542.
[11]陈奇.中药药理研究方法学[M].第3版.北京:人民卫生出版社,2011.
[12]甄汉深,刘蓉,丘琴,等.龙利叶抗炎镇痛作用的研究[J].中国实验方剂学杂志,2013,19(9):270-273.
[13]王孝勋,黄茂春,赵旭,等.序贯法研究广西不同产地对叶百部总生物碱对小鼠的止咳作用[J].中华中医药杂志,2012,27(7):1935-1937.
[14]刘宾,江南.序贯法研究甘草酸二铵对小鼠止咳作用[J].中国医院药学杂志,2009,29(10):820-822.
[15]陈奇.中药药理实验方法[M].北京:人民卫生出版社,1994.
[16]唐慧勤,龙颖,董威,等.产地、生长期、商品规格等不同因素对罗汉果止咳作用的影响[J].中草药,2015,46(20):3051-3054.
[17]杨冰月,李敏,任敏,等.基于灰色关联度分析法对半夏及其炮制品总有机酸止咳作用的谱-效关系研究[J].中草药,2016,47(13):2301-2307.
[18]晏子俊,罗燕秋,李作燕,等.暗紫贝母及浙贝母镇咳作用的化学刺激引咳法比较[J].时珍国医国药,2012,23(10):2522-2525.
[19]徐启贵,李勤耕,田睿,等.羟丙哌嗪衍生物的合成及其镇咳活性[J].中国药物化学杂志,2005,15(2):85-88.
[20]Undem B J,Carr M J,Kollarik M.Physiology and plasticity of putative cough fibres in the guinea pig[J].Pulm Pharmacol Ther,2002,15(3):193-198.
[21]陈晓芳.枇杷花醇提物镇咳、平喘、祛痰作用及其机制研究[D].兰州:兰州大学,2011.
[22]Orita K,Kamei J.Involvement of ATP-sensitive K+channels in the anti-tussive effect of moguisteine[J].Eur J Pharmacol,2000,395(2):161-164.
© 2004-2018 中国地质图书馆版权所有 京ICP备05064691号 京公网安备11010802017129号 地址：北京市海淀区学院路29号 邮编：100083 电话：办公室：(+86 10)66554848；文献借阅、咨询服务、科技查新：66554700 |