刺人参苷的药效学研究
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摘要
刺人参(Oplopanax elatus Nakai)系五加科刺参属多年生落叶灌木。分布于中国东北、俄罗斯、朝鲜三国境内。其根茎入药,具有滋补强壮、调节血压、兴奋中枢神经等功效,有类似人参的作用,是一种极具有开发前途的药用植物。近年来由于资源破坏,刺人参处于濒危状态,已列为国家二级保护植物。
本文制备刺人参总皂苷并研究了其对大鼠的心血管系统、呼吸系统及小鼠中枢神经系统的作用,通过测定大鼠体内的单胺类物质变化,初步探讨了其调节血压的机理。主要包括以下几个方面:
1.从植物形态、生态环境、化学成分、药理活性和临床应用等方面综述了刺人参的最新研究进展。
2.用回流提取法,将刺人参干燥叶用8倍量60%的乙醇回流提取3次,每次30min,减压过滤,浓缩回流液;选用D101大孔树脂对提取物进行纯化处理,每克大孔树脂上样量不超过6g(以生药计),水洗后,先用4倍柱体积20%乙醇除杂,再以6倍柱体积60%乙醇1倍柱体积每小时流速洗脱,收集60%乙醇部分,干燥制得刺人参总皂苷。
3.研究了刺人参总苷对wistar大鼠心血管系统、呼吸系统的作用并测定了大鼠血清中单胺类物质的含量,结果表明静脉注射刺人参总皂苷对大鼠心率、呼吸频率及呼吸幅度无明显影响,与对照组比较无显著性差异;高剂量刺人参皂苷(70 mg/kg)可使大鼠平均动脉压降低,而低剂量刺人参皂苷(17.5 mg/kg)可使大鼠平均动脉压升高,表明刺人参皂苷对大鼠血压产生双向调节的作用;本实验初步证明刺人参总皂苷的升压作用可被α受体阻断剂酚妥拉明对抗,并不被β受体阻断剂普萘洛尔所阻断,说明升压作用可能与α受体有关,提示刺人参总苷可能直接作用于α受体,激动α受体引起血压升高;测定大鼠体内的单胺类物质变化结果表明大鼠血清中NE、DA浓度在给药后与对照组比较没有显著性差异,而5-HT浓度在给药后降低,其中给药组与对照组比较有显著性差异,提示刺人参总皂苷可能抑制5-HT释放或促进其灭活,从而引起大鼠血压的变化,说明刺人参总皂苷对血压作用的机理比较复杂,有待进一步研究。
4.研究了刺人参总皂苷对小鼠中枢神经系统的影响,结果表明刺人参总皂苷对戊巴比妥钠小鼠睡眠有协同作用;刺人参总苷对小鼠机能协调运动、一般行为、自发活动无明显影响,与对照组比较无显著性差异,说明刺人参总皂苷对中枢神经系统无明显影响。
Oplopanax elatus Nakai is a perennial deciduous shrub of Araliaceae, and distributes in northeast of China , Russia and Korea. Oplopanax elatus Nakai, whose roots and stems are used as medicine, has various effects such as invigoration, adjusting blood pressure , stimulating central nervous system. The activities are similar with those of ginseng. Oplopanax elatus Nakai has bright future as medicinal plants. Because of resource damadge, Oplopanax elatus Nakai has been in endangered status recently, already listed as secondary protective plant of our country.
The scholars at home and abroad have done a lot of studies on plant morphology, ecological environment, characteristic properties of biology and chemical constituents of Oplopanax elatus Nakai. It was discovered that layerage and cuttage are good ways to breed Oplopanax elatus Nakai quickly in order to provide stable source for clinical application. The chemical constituents research of Oplopanax elatus Nakai, important to pharmacological activity and clinical application, showed that Oplopanax elatus Nakai contains saponins, volatile oils, fatty acids, anthraquinones, flavones, microelements, ect. The research on pharmacology of Oplopanax elatus Nakai was rarely reported. There are only some about volatile oils on antisepticize, antiinflammatory, etc. The pharmacology research of other chemical constituents have not been reported systematically.
In this article we studied the preparation technology and pharmacology -- circulation system, respiratory system of rats and central nervous system of mice -- of total saponins extracted from Oplopanax elatus Nakai. We also studied the mechanism of adjusting blood pressure by determination of monoamines in the blood serum. The results included several parts below:
1. Referring to the related literature, We reviewed studies on plant morphology, ecological environment, characteristic properties of biology, chemical constituents, pharmacology and clinical application of Oplopanax elatus Nakai.
2. The technology to extract total saponins from the leaves of Oplopanax elatus Nakai is reflux extration with 60% ethanol(8 folds) for 3 times, half an hour once. The purification technology is: loading amount should be no more than 6g dried herb for per gram macroporous resin; 4BV 20% ethanol is needed to get rid of impuries, then 6BV 60% ethanol elute the column at the rate of 1BV/h.
3. We studied pharmacological effects of total saponins on the circulation system such as blood pressure , heart rate and respiratory system such as respiratory rate, repiratory extent of rats. The total saponins has no obvious influence on heart rate, repiratory rate and respiratory range of rats. The result indicates that blood pressure increased after injection of total saponins (17.5 mg/kg), decreased slightly afer injection of total saponins (70 mg/kg), which showed two-way regulation to blood pressure of rats. The effect of elevating blood pressure was antagonized by phentolamine and was not antagonized by propranolol. The above result indicates the elevating blood pressure effect has some relations withα-acceptor, and total saponins may agitate it to make blood pressure increase. The concentration of blood serum monoamine, DA, NE and 5-HT was meansured. The result showed that the concentration of NE and DA in the blood serum of the administration group had no significant difference with that of the control group. But the concentration of 5-HT was lower. This phenomenon indicates that the variation of blood pressure is related with 5-HT.
4. We studied the effects of total saponins on nervous system such as normal behavior, locomotor activity and coordinated motion of mice. The result showed that total saponins prolonged the sleeping time of mice injected pentobarbital sodium and had no influence on normal behavior and coordinated motion of mice. This indicates total saponins has no effect on the central nervous system of mice.
The studies on the preparation and pharmacology of total saponins provide scientific data for drug developing, and are meaningful to improve medical value of Oplopanax elatus Nakai.
本文制备刺人参总皂苷并研究了其对大鼠的心血管系统、呼吸系统及小鼠中枢神经系统的作用,通过测定大鼠体内的单胺类物质变化,初步探讨了其调节血压的机理。主要包括以下几个方面:
1.从植物形态、生态环境、化学成分、药理活性和临床应用等方面综述了刺人参的最新研究进展。
2.用回流提取法,将刺人参干燥叶用8倍量60%的乙醇回流提取3次,每次30min,减压过滤,浓缩回流液;选用D101大孔树脂对提取物进行纯化处理,每克大孔树脂上样量不超过6g(以生药计),水洗后,先用4倍柱体积20%乙醇除杂,再以6倍柱体积60%乙醇1倍柱体积每小时流速洗脱,收集60%乙醇部分,干燥制得刺人参总皂苷。
3.研究了刺人参总苷对wistar大鼠心血管系统、呼吸系统的作用并测定了大鼠血清中单胺类物质的含量,结果表明静脉注射刺人参总皂苷对大鼠心率、呼吸频率及呼吸幅度无明显影响,与对照组比较无显著性差异;高剂量刺人参皂苷(70 mg/kg)可使大鼠平均动脉压降低,而低剂量刺人参皂苷(17.5 mg/kg)可使大鼠平均动脉压升高,表明刺人参皂苷对大鼠血压产生双向调节的作用;本实验初步证明刺人参总皂苷的升压作用可被α受体阻断剂酚妥拉明对抗,并不被β受体阻断剂普萘洛尔所阻断,说明升压作用可能与α受体有关,提示刺人参总苷可能直接作用于α受体,激动α受体引起血压升高;测定大鼠体内的单胺类物质变化结果表明大鼠血清中NE、DA浓度在给药后与对照组比较没有显著性差异,而5-HT浓度在给药后降低,其中给药组与对照组比较有显著性差异,提示刺人参总皂苷可能抑制5-HT释放或促进其灭活,从而引起大鼠血压的变化,说明刺人参总皂苷对血压作用的机理比较复杂,有待进一步研究。
4.研究了刺人参总皂苷对小鼠中枢神经系统的影响,结果表明刺人参总皂苷对戊巴比妥钠小鼠睡眠有协同作用;刺人参总苷对小鼠机能协调运动、一般行为、自发活动无明显影响,与对照组比较无显著性差异,说明刺人参总皂苷对中枢神经系统无明显影响。
Oplopanax elatus Nakai is a perennial deciduous shrub of Araliaceae, and distributes in northeast of China , Russia and Korea. Oplopanax elatus Nakai, whose roots and stems are used as medicine, has various effects such as invigoration, adjusting blood pressure , stimulating central nervous system. The activities are similar with those of ginseng. Oplopanax elatus Nakai has bright future as medicinal plants. Because of resource damadge, Oplopanax elatus Nakai has been in endangered status recently, already listed as secondary protective plant of our country.
The scholars at home and abroad have done a lot of studies on plant morphology, ecological environment, characteristic properties of biology and chemical constituents of Oplopanax elatus Nakai. It was discovered that layerage and cuttage are good ways to breed Oplopanax elatus Nakai quickly in order to provide stable source for clinical application. The chemical constituents research of Oplopanax elatus Nakai, important to pharmacological activity and clinical application, showed that Oplopanax elatus Nakai contains saponins, volatile oils, fatty acids, anthraquinones, flavones, microelements, ect. The research on pharmacology of Oplopanax elatus Nakai was rarely reported. There are only some about volatile oils on antisepticize, antiinflammatory, etc. The pharmacology research of other chemical constituents have not been reported systematically.
In this article we studied the preparation technology and pharmacology -- circulation system, respiratory system of rats and central nervous system of mice -- of total saponins extracted from Oplopanax elatus Nakai. We also studied the mechanism of adjusting blood pressure by determination of monoamines in the blood serum. The results included several parts below:
1. Referring to the related literature, We reviewed studies on plant morphology, ecological environment, characteristic properties of biology, chemical constituents, pharmacology and clinical application of Oplopanax elatus Nakai.
2. The technology to extract total saponins from the leaves of Oplopanax elatus Nakai is reflux extration with 60% ethanol(8 folds) for 3 times, half an hour once. The purification technology is: loading amount should be no more than 6g dried herb for per gram macroporous resin; 4BV 20% ethanol is needed to get rid of impuries, then 6BV 60% ethanol elute the column at the rate of 1BV/h.
3. We studied pharmacological effects of total saponins on the circulation system such as blood pressure , heart rate and respiratory system such as respiratory rate, repiratory extent of rats. The total saponins has no obvious influence on heart rate, repiratory rate and respiratory range of rats. The result indicates that blood pressure increased after injection of total saponins (17.5 mg/kg), decreased slightly afer injection of total saponins (70 mg/kg), which showed two-way regulation to blood pressure of rats. The effect of elevating blood pressure was antagonized by phentolamine and was not antagonized by propranolol. The above result indicates the elevating blood pressure effect has some relations withα-acceptor, and total saponins may agitate it to make blood pressure increase. The concentration of blood serum monoamine, DA, NE and 5-HT was meansured. The result showed that the concentration of NE and DA in the blood serum of the administration group had no significant difference with that of the control group. But the concentration of 5-HT was lower. This phenomenon indicates that the variation of blood pressure is related with 5-HT.
4. We studied the effects of total saponins on nervous system such as normal behavior, locomotor activity and coordinated motion of mice. The result showed that total saponins prolonged the sleeping time of mice injected pentobarbital sodium and had no influence on normal behavior and coordinated motion of mice. This indicates total saponins has no effect on the central nervous system of mice.
The studies on the preparation and pharmacology of total saponins provide scientific data for drug developing, and are meaningful to improve medical value of Oplopanax elatus Nakai.
引文
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[2]Zhurba O V, Fomenko K P. Ecological area and growing conditions of Oplopanax elatus in the primorie region[J]. Rastitel`nye Resursy, 1980, 16(3): 364-373.
[3]吉林省中医中药研究院.长白山植物药志[M].长春:吉林人民出版社, 1982: 785.
[4]宋朝枢.中国珍稀濒危保护植物[M].北京:中国林业出版社, 1989: 344.
[5]陈霞,王广树,李红,等.刺人参皂苷对大鼠血压的影响[J].白求恩医科大学学报, 1997, 23(5): 475-476.
[6]杨野.刺人参的形态和生态观察[J].特产科学实验, 1980, (2): 4-7.
[7]Simonova O N.Flowering charaeteristics of Oplopanax elatus Nakai. Rastitel`nye Resursy, 1984, 20(3): 371-375.
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