四种药用植物活性成分的系统研究
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摘要
本文系统研究了青牛胆、金果榄、芫花和西南文殊兰四种药用植物的化学成分，共鉴定了97个化合物，其中13个新化合物。采用小鼠耳肿胀模型和小鼠扭体模型对青牛胆和金果榄进行抗炎镇痛活性的跟踪筛选；建立了HPLC-DAD和HPLC-ESI-MS-MS联用的方法同时定性和定量39批不同来源的金果榄药材中的8个指标性成分；建立了一类基于遗传算法的中药组效关系发现算法；建立了LC／MS／MS方法研究古伦宾在大鼠体内药代动力学参数和生物利用度；古伦宾具有显著的抗炎活性，我们对其抗炎机制做了初步的探讨；对金果榄药材基源植物的资源状况和生态环境进行系统调查；采用小鼠耳肿胀实验、小鼠扭体模型和大鼠弗氏完全佐剂性关节炎法对芫花进行抗炎、镇痛和抗关节炎活性的跟踪筛选；采用四氮唑盐(Methyl-Thiazol-Tetrozolium，MTT)还原法对西南文殊兰进行细胞毒活性跟踪筛选。
This dissertation describes the chemical and pharmacology study of Tinospora sagittata (Oliv.)Gagnep, Tinospora capillipes Gagnep, Daphne genkwa Sieb. et Zucc.and Crinum latifalium L.. From thefour medicinal plants, 97 compounds in total were obtained and indentificated, including 13 newcompounds. The bio-assay guided isolation of anti-inflammatory and analgesic activity of T. sagittata andT. capillipes were perfermed. Futhermore, High-performance liquid chromatography (HPLC) coupled withelectrospray tandem mass spectrometry (ESI-MS-MS) and diode array detection (DAD) was employed toidentify and simultaneously determine eight major ingredients in Radix Tinosporae. Genetic algorithmbased approaches were established to study the quantitative composition-activity relationship of RadixTinosporae. A method of HPLC coupled with tandem mass spectrometry (LC/MS/MS) was established forthe determination of columbin in plasma.The method was further applied to assess pharmacokinetics ofcolumbin after intravenous administration and oral administration in rats. The mechanism ofanti-inflamatation of colubin was also discussed. The bionomics and resources of Radix Tinosporae wereinvestigated. The bio-assay guided isolation of anti-inflammatory, analgesic and anti-arthritis activity of D.genkwa were perfermed. The bio-assay guided isolation of cytotoxin activity of C. latifalium was assessedby MTT method.
This dissertation describes the chemical and pharmacology study of Tinospora sagittata (Oliv.)Gagnep, Tinospora capillipes Gagnep, Daphne genkwa Sieb. et Zucc.and Crinum latifalium L.. From thefour medicinal plants, 97 compounds in total were obtained and indentificated, including 13 newcompounds. The bio-assay guided isolation of anti-inflammatory and analgesic activity of T. sagittata andT. capillipes were perfermed. Futhermore, High-performance liquid chromatography (HPLC) coupled withelectrospray tandem mass spectrometry (ESI-MS-MS) and diode array detection (DAD) was employed toidentify and simultaneously determine eight major ingredients in Radix Tinosporae. Genetic algorithmbased approaches were established to study the quantitative composition-activity relationship of RadixTinosporae. A method of HPLC coupled with tandem mass spectrometry (LC/MS/MS) was established forthe determination of columbin in plasma.The method was further applied to assess pharmacokinetics ofcolumbin after intravenous administration and oral administration in rats. The mechanism ofanti-inflamatation of colubin was also discussed. The bionomics and resources of Radix Tinosporae wereinvestigated. The bio-assay guided isolation of anti-inflammatory, analgesic and anti-arthritis activity of D.genkwa were perfermed. The bio-assay guided isolation of cytotoxin activity of C. latifalium was assessedby MTT method.
引文
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