中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
玫瑰花多酚片制备工艺及其功效评价和石榴花多酚提取物生物活性研究

文献类型:学位论文

作者徐建军
答辩日期2019-05-27
授予单位中国科学院大学
授予地点北京
导师阿吉艾克拜尔·艾萨
关键词玫瑰花多酚 制备工艺 抗疲劳 石榴花多酚 抗炎
学位名称博士
学位专业有机化学
目次

Rosa rugosa Thunb.and Punica granatum L. are widely planted in the world that formed abundant and characteristic resources in Xinjiang, which are used as medicinal materials for ethnic medicine with a long history of use. Both of them contain abundant polyphenol, flavonoids and volatile oils that attributed to their biological activities. In recent years, the research on Rosae rugosae flos and flowers of Punica granatum mainly focused on the bioactivity like anti-oxidation, hypoglycemic of active polyphenol. Our earlier research have presented that total polyphenol of Rosae rugosae flos have positive the anti-fatigue effect. Punica granatum flower Polyphenol also has positive the anti-inflammation activity. In order to study the anti-fatigue effect and anti-inflammatory active of polyphenol in Rosae rugosae flos and flowers of Punica granatum. Therefore, in this paper, the anti-fatigue effect of Rosae rugosae flos polyphenol from Xinjiang Rosae rugosae flos was extracted, purified by macroporous resin, forming process of tablets, enlargement experiment, pilot-scale production, anti-fatigue efficacy and safety evaluation, repetitive stability and quality standard of preparations. The anti-inflammatory activity of Punica granatum flower Polyphenol was studied in depth. The results are as follows: 1. The preparation process of Rosae rugosae flos polyphenol extract was studied by single factor, orthogonal design experiment, static adsorption and dynamic adsorption of HPD600 macroporous resin and enlarged verification experiment of macroporous resin process.The optimum extraction process was: 50% ethanol for extraction, liquid to solid ratio of 1:25 (mL/g), warm immersion 45 ℃ of 4 hours, extracted 2 times, filtrated and combinated at below 60 ℃, and finally concentrated in vacuum (-0.08 Mpa) to relative density of 1.10-1.20. The purification process of Rosae rugosae flos polyphenol by HPD 600 macro-porous resin was studied by static adsorption test and dynamic adsorption amplification test. The results showed that the optimum conditions are: the pH of Rosae rugosae flos crude extract should be controlled at 3, the concentration of NaCl was 0.5 mol/L, the concentration of polyphenol was 2.50-3.6 mg/mL, The sample loading is 7 BV and the flow rate was 3 BV/h, The purified water was 5 BV, the flow rate was 3 BV/h,the eluent was 50% ethanol, the elution flow rate was 4 BV/h, and the amount of eluent was 5 BV. After vacuum concentration and cold drying red powder solid was obtained, and the polyphenol content was about 60%. 2. The preparation process of Rosae rugosae flos polyphenol tablets was optimized and verified by pilot production. After investigating the main-auxiliary ratio, filler, disintegrating agent, wetting agent, lubricant, mixing time and drying time of process parameters, through single factor, orthogonal experiment, laboratory scale-up experiment and pilot production, the final prescription technology: 52% Rosae rugosae flos polyphenol, 21% mannitol and microcrystalline cellulose, crospovidone (extra) 5%, magnesium stearate 1%, 95% ethanol with appropriate proportion. Rosae rugosae flos polyphenol materials were crushed and sieved 100 mesh. And accessory materials such as mannitol, microcrystalline cellulose, cross-linked polyvinyl ketone and magnesium stearate were sifted 100 mesh. According to prescription technology, raw materials were mixed evenly, wetting agent of 95% ethanol was added to make suitable soft materials. wet granules of 14 mesh were dried at 45 ℃ for 120 minutes, while granules were mixed and pressed into tablets that weighing as 0.5 g. 3. The purity of Rosae rugosae flos polyphenol and the standard of Rosae rugosae flos tablets were studied. Fingerprint analysis of Rosae rugosae flos polyphenol purifier were carried out, and the content of polyphenol components and flavonoid components were determined. Gallic acid,Ellagic acid,Hyperoside and isoquercitrin were chosen to control the quality of its purified products. In order to better control the quality of Rosae rugosae flos tablet, the quality standard of Rosae rugosae flos tablet was established. The above results show that the production process is easy to operate, reproducible and stable, and the method is simple and applicable, which is suitable for industrial conversion production. 4. The efficacy and safety of Rosae rugosae flos polyphenol tablets were evaluated. The results of weight-bearing swimming test, serum urea and hepatic glycogen test in mice were positive, while the results of blood lactic acid test in mice were negative. The results showed that Rosae rugosae flos Polyphenol Tablets had the function of alleviating physical fatigue. In terms of safety experimental research, acute toxicity test shows that it is actually non-toxic. Three genetic toxicity tests: Ames test of Rosae rugosae flos Polyphenol tablets, micronucleus test of bone marrow cells in mice and sperm abnormality test in mice were all negative. The 30-day feeding test of rats showed that all the indexes had no significant effect. 5. The anti-inflammatory effect of Punica granatum flower Polyphenol was studied. LPS-induced RAW 264.7 cell model was used. It was found that the polyphenol extract from flowers of Punica granatum could inhibit the production of pro-inflammatory mediators PGE2, NO, TNF-α, IL-1β and IL-6. The main reason is that it prevents the degradation of IκBα and nuclear transfer of NF-κB p65 in RAW 264.7 cells induced by LPS, and inhibited the phosphorylation of MAPKs pathway. Based on the above results, it can be concluded that the polyphenol extract from flowers of Punica granatum can be used as a potential anti-inflammatory drug for inflammation-related diseases. This study provides a good guiding significance for the application and development of Rosae rugosae flos in the fields of medicine, health food and industrial transformation from experiment. Punica granatum flower Polyphenol provide a basis for further study of anti-inflammatory drugs.

页码153
源URL[http://ir.xjipc.cas.cn/handle/365002/6000]  
专题新疆理化技术研究所_资源化学研究室
推荐引用方式
GB/T 7714
徐建军. 玫瑰花多酚片制备工艺及其功效评价和石榴花多酚提取物生物活性研究[D]. 北京. 中国科学院大学. 2019.

入库方式: OAI收割

来源:新疆理化技术研究所

浏览0
下载0
收藏0
其他版本

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。