新疆一枝蒿黄酮及其抑菌、降血糖活性研究
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摘要
新疆一枝蒿(Artemisia rupestris L.)是新疆特有的一种药用植物,具有抗肿瘤、保肝、抗氧化、解毒和抗过敏等药理作用,有很高的开发利用价值。文献报道新疆一枝蒿中含有倍半萜类、黄酮类、苷类、挥发油类、酚类和氨基酸等化学成分。黄酮类化合物是新疆一枝蒿发挥药效的主要成分,对其含量进行测定并优化提取工艺是该药材应用的重要途径。为此,本研究对新疆一枝蒿的抑菌活性、总黄酮的提取及工艺优化、降血糖活性及化学成分等方面作了较系统的研究,以期有效控制新疆一枝蒿药材质量,主要研究内容和实验结果概述如下:
1、通过体外抑菌试验研究了新疆一枝蒿的水及醇提取物对10种供试菌的抑制活性,并采用试管预试法对新疆一枝蒿的抑菌活性物质进行了初步分离。结果表明新疆一枝蒿的水提物及醇提物具有广谱的抗菌作用,无水乙醇提取物的抗菌效果最好,且新疆一枝蒿提取物对G+的抑菌效果优于G-;化学成分系统预试表明,新疆一枝蒿的活性成分可能为香豆素类、苷类和黄酮类等。
2、采用超声法提取新疆一枝蒿总黄酮,通过响应面法分析,得到提取新疆一枝蒿总黄酮的最佳工艺条件:乙醇体积分数76.0%,料液比1:11,超声时间32min。在最佳工艺条件下,新疆一枝蒿总黄酮得率为4.50%,比优化前提高了34.0%。
3、采用四氧嘧啶构建糖尿病小鼠模型,观察新疆一枝蒿对KM小鼠体重、血糖、SOD以及MDA变化,并对其组织形态进行观察,探究新疆一枝蒿提取液对糖尿病KM小鼠的影响。结果表明:新疆一枝蒿总黄酮具有降血糖活性,最佳的使用剂量为67.5mg/kg。
4、为了进一步地了解新疆一枝蒿的降血糖化学成分,以便更全面的综合利用这种植物资源,开发糖尿病新药,本文运用高效液相色谱法和质谱联用技术(HPLC-MS)分离测定新疆一枝蒿黄酮类化学成分,并对金丝桃苷和木犀草素的含量进行测定,这些黄酮类化合物丰富的生理活性为新疆一枝蒿所表现出来的多方面的药理作用提供了物质基础。
Artemisia rupestris L. is a rare endemic plant of Xinjiang. It is widely known of antitumor, protecting liver, antioxida, detoxification and anti-hypersusceptibility obout the plant. A search showed that the active compounds responsible for the activity of A. rupestris L. are sesquiterpenoids, flavonoids, glycosides, essential oil, phenolics, lipids and amino acid compounds. Among these metabolites, flavonoids were considered the main active constituent, flavonoids determination and flavonoids extraction from A. rupestris L. would provide information about its utilization for commercial production. In this paper, studying on the antibacterial effect, extraction, hypoglycemic activity and chemical composition of flavonoids in the A. rupestris L.,
The main reseach contants and results in the paper are concluded as follows:
1. The antimicrobial activities of water and ethanol extracts from A. rupestris L. to ten bacteria were investigated. And the antibacterial active components were selected by the tube preliminary test. The results indicated that the water and ethanol extracts inhibited significantly the growth of a wide range of bacteria. The antimicrobial efficacy of absolute ethanol extracts from A. rupestris L. is remarkable and its inhibitory effect on G+ is better than G-. A preliminary test of chemical constituents showed that its active components may be conmarins, glycoside and flavone, etc.
2. Total flavonoids were extracted from A. rupestris L. by ultrasonic extraction. The optimum extraction conditions were confirmed by response surface analysis as follows: methanol concentration 76.0%, material-liquid ratio 1:11, ultrasonic time 32 min. Under these conditions, the extraction rate of total flavonoids was 4.50%, which was increased 34.0% compared with the original conditions.
3. In order to investigate hypoglycemic effect of the flavonoids in A. rupestris L., we established diabetic model rats induced by alloxan,study effect of KM body weight, blood glucose, SOD and MDA, and its morphology was observed. The results suggest flavonoids of A. rupestris L. can decrease the level of giucose, the optimal dosage is 67.5mg/kg.
4. To study the anti-diabetic chemical consituents and utilize the resource of A. rupestris L.. The flavonoids compounds were determined by HPLC-MS, and the quality of hyperin and luteolin were determined. Rich physiological activity of flavonoids provided the material basis for A. rupestris L. pharmacological effects.
1、通过体外抑菌试验研究了新疆一枝蒿的水及醇提取物对10种供试菌的抑制活性,并采用试管预试法对新疆一枝蒿的抑菌活性物质进行了初步分离。结果表明新疆一枝蒿的水提物及醇提物具有广谱的抗菌作用,无水乙醇提取物的抗菌效果最好,且新疆一枝蒿提取物对G+的抑菌效果优于G-;化学成分系统预试表明,新疆一枝蒿的活性成分可能为香豆素类、苷类和黄酮类等。
2、采用超声法提取新疆一枝蒿总黄酮,通过响应面法分析,得到提取新疆一枝蒿总黄酮的最佳工艺条件:乙醇体积分数76.0%,料液比1:11,超声时间32min。在最佳工艺条件下,新疆一枝蒿总黄酮得率为4.50%,比优化前提高了34.0%。
3、采用四氧嘧啶构建糖尿病小鼠模型,观察新疆一枝蒿对KM小鼠体重、血糖、SOD以及MDA变化,并对其组织形态进行观察,探究新疆一枝蒿提取液对糖尿病KM小鼠的影响。结果表明:新疆一枝蒿总黄酮具有降血糖活性,最佳的使用剂量为67.5mg/kg。
4、为了进一步地了解新疆一枝蒿的降血糖化学成分,以便更全面的综合利用这种植物资源,开发糖尿病新药,本文运用高效液相色谱法和质谱联用技术(HPLC-MS)分离测定新疆一枝蒿黄酮类化学成分,并对金丝桃苷和木犀草素的含量进行测定,这些黄酮类化合物丰富的生理活性为新疆一枝蒿所表现出来的多方面的药理作用提供了物质基础。
Artemisia rupestris L. is a rare endemic plant of Xinjiang. It is widely known of antitumor, protecting liver, antioxida, detoxification and anti-hypersusceptibility obout the plant. A search showed that the active compounds responsible for the activity of A. rupestris L. are sesquiterpenoids, flavonoids, glycosides, essential oil, phenolics, lipids and amino acid compounds. Among these metabolites, flavonoids were considered the main active constituent, flavonoids determination and flavonoids extraction from A. rupestris L. would provide information about its utilization for commercial production. In this paper, studying on the antibacterial effect, extraction, hypoglycemic activity and chemical composition of flavonoids in the A. rupestris L.,
The main reseach contants and results in the paper are concluded as follows:
1. The antimicrobial activities of water and ethanol extracts from A. rupestris L. to ten bacteria were investigated. And the antibacterial active components were selected by the tube preliminary test. The results indicated that the water and ethanol extracts inhibited significantly the growth of a wide range of bacteria. The antimicrobial efficacy of absolute ethanol extracts from A. rupestris L. is remarkable and its inhibitory effect on G+ is better than G-. A preliminary test of chemical constituents showed that its active components may be conmarins, glycoside and flavone, etc.
2. Total flavonoids were extracted from A. rupestris L. by ultrasonic extraction. The optimum extraction conditions were confirmed by response surface analysis as follows: methanol concentration 76.0%, material-liquid ratio 1:11, ultrasonic time 32 min. Under these conditions, the extraction rate of total flavonoids was 4.50%, which was increased 34.0% compared with the original conditions.
3. In order to investigate hypoglycemic effect of the flavonoids in A. rupestris L., we established diabetic model rats induced by alloxan,study effect of KM body weight, blood glucose, SOD and MDA, and its morphology was observed. The results suggest flavonoids of A. rupestris L. can decrease the level of giucose, the optimal dosage is 67.5mg/kg.
4. To study the anti-diabetic chemical consituents and utilize the resource of A. rupestris L.. The flavonoids compounds were determined by HPLC-MS, and the quality of hyperin and luteolin were determined. Rich physiological activity of flavonoids provided the material basis for A. rupestris L. pharmacological effects.
引文
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