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UM E-Theses Collection (澳門大學電子學位論文庫)

Title

Study on chemical constituents and qualitative & quantitative analysis of Rhizoma coptidis

English Abstract

Rhizoma coptidis (family Ranunculaceae), Huang-Lian in Chinese, is a famous Traditional Chinese Medicine. It is used in China as an antimicrobial in the treatment of dysentery, gastroenteritis as well as other inflammatory conditions. Furthermore, its anticancer activities had been a focus recently. Thus, it is potential to research and develop Chinese Traditional Medicine "Huang-Lian" to remedy the cancer. However, studies on chemical constituents and quality control of Rhizoma coptidis were limited, which cannot guarantee its safety and efficacy. Therefore, the chemical compositions and analytical method of Rhizoma coptidis will be studied in this thesis. The thesis contained four chapters: Chapter 1 reviewed on the chemical constituents, pharmacology and the quality control studies of Rhizoma coptidis. Chapter 2 is focused on chemical studies of Coptis chinensis recorded in "China Pharmacopoeia" (2005 Ed.). 1. Seventeen compounds had been isolated from the ethanol extract of Coptis chinensis by various chromatographic methods. Their structures were elucidated using spectral and chemical methods as 8-oxyberberine (1), 8-oxocoptisine (2), 8-oxo-epiberberine (3), 6-([1,3]dioxolo[4,5-glisoquinoline-5-carbonyl)-2,3-dimethoxy-benzoic acid methyl ester (4), corydaldine (5), noroxyhydrastineine (6), 6,7-methylencdioxy-1(2H)-isoquinolinone (7), coptinin A (8), coptinin B (0), coptinin C (10), coptinin D (11), neocoptinin A (12), neocoptinin B (13), neocoptinin C (14), woorenoside II (15), woorenol (16) and ferulic acid (17). Compounds 8~14 are new compounds and named as coptinin A~D and neocoptinin A~C, respectively. Compounds 1~7, 15 and 16 were isolated from this plant for the first time. The quality control method (both qualitative & quantitative analysis by CZE for Rhizoma coptidis was developed in Chapter 3. Optimization of extraction conditions: Pressurized liquid extraction (PLE) was used for extraction. The optimized conditions were: particle size, 80-100 mesh; solvent, 70% methanol; temperature, 150 °C; static extraction time, 10 min; pressure, 1500 p.s.i. Optimization of CZE-UV conditions: A fused-silica capillary (64.5 cm × 75 um I.D., 56 cm effective length) was used throughout the study. The effects of the experimental parameters of CZE had been optimized by using central composite design (CCD). The best separation of nine compounds could be obtained within 15 min using 60 mM borate buffer (pH 9.9 containing 22% acetontrile as modifier, while separation voltage was 20 kV and temperature was at 30 °C. Result: A CZE method was developed for simultaneous determination of five alkaloids and four lignans in Rhizoma coptidis. The developed method is accurate, simple and reproducible.

Chinese Abstract

毛茛科植物黄连为常用中药,作为一类抗菌剂,用于治疗痢疾、肠胃炎以及其它炎症。近几年,黄连的抗癌活性也受到广泛的关注。从资源广泛的传统中药黄连中研究开发治疗癌症的药物,具有广阔的前景。相对的,对于黄连化学成分和质量控制方面研究的局限,制约了其使用的安全性和有效性。因此,本论文针对黄连的化学成分及其分析方法展开了研究。 全文共分四章。 第一章是有关黄连研究的文献综述,包括黄连的化学成分和药理学研究,以及黄连质量控制方法的研究进展。 第二章对中国药典(2005版)收载的毛茛科植物黄连(Coptis chinensis Franch)的化学成分进行了研究。包括: 1.运用多种层析分离手段从黄连中分离了 17 个化合物,并通过波谱学和化学方法鉴定了它们的结构为:8-氧化小檗碱 (8-oxyberberine, 1),8-氧化黄连碱(8-0xocoptisine, 2),8-氧化表小樂碱 (8-0x0-epiberberine, 3), 6-(1133] dioxolo[4,5-gJisoquinoline-5-carbonyl)-2,3-dimethoxy-benzoicacid methvlester (4), corydaldine (5), noroxyhydrastineine (6), 6,7-methylenedioxy-1 (2FD-isoquinolinone (⑦),黄连木脂素 A (coptinin A,8),黄连木脂素 B (coptininB,9),黄连木脂素 C (coptinin C, 10),黄连木脂素 D (coptinin D,11),黄连新木脂素 A (neocoptinin ^,12),黄连新木脂素 B (neocoptinin B, 13),黄连新木脂素 C (neocoptinin C, 14), woorenoside I (15),woorenol (16) 和阿魏 H@ (ferulic acid, 17). 2.化合物 8~14 为新化合物;化合物 1~7,15 和 16 为首次从本植物中分离得到。第三章是应用 CZE 对黄连药材定性定量分析质量控制方法的研究。包括: 黄连中有效成分的加压溶剂提取条件(包括药材粉径、溶剂种类、提取温度和提取时间)的优化,结果为:粒径为 80-100 目数的药材在压强 1500 p.s.i.,温度 120°c 的条件下用 70% 甲醇提取 1次(10分钟)。CZE 条件的优化:64.5cm × 75wm 熔融石英毛细管柱,有效长度 56cm。利用星点设计(CCD)优化了分离条件:电压20kV;温度 30°C;缓冲液 50mM 硼砂溶液-乙腈(78:22),调pF 9.9。 建立了同时测定黄连中 5 种生物碱和 4 种木脂素的区带毛细管电泳分析方法,此方法简单精确且重复性好。

Issue date

2007.

Author

Wang, Wei

Faculty
Institute of Chinese Medical Sciences
Degree

M.Sc.

Subject

Coptis -- Therapeutic use.

Materia medica, Vegetable -- China -- Analysis.

Supervisor

王一濤

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Location
1/F Zone C
Library URL
991000541299706306