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In-vitro studies on the intestinal absorption mechanisms of quercetin and related glycosides.

Ying Zheng. / Thesis submitted in: October 2001. / Thesis (M.Phil.)--Chinese University of Hong Kong, 2002. / Includes bibliographical references (leaves 84-90). / Abstracts in English and Chinese. / ABSTRACT --- p.ii / 中文摘要 --- p.iv / ACKNOWLEDGEMENTS --- p.vi / TABLE OF CONTENTS --- p.vii / LIST OF FIGURES --- p.x / LIST OF TABLES --- p.xii / ABBREVIATIONS --- p.xiii / Chapter CHAPTER 1. --- Introduction --- p.1 / Chapter 1.1. --- Rationale of the Study --- p.2 / Chapter 1.2. --- Flavonoids --- p.3 / Chapter 1.2.1. --- Introduction --- p.3 / Chapter 1.2.2. --- Potential Health Effects --- p.5 / Chapter 1.2.3. --- Absorption Studies --- p.6 / Chapter 1.3. --- Drug Absorption --- p.9 / Chapter 1.3.1. --- Pathways and Mechanisms of Intestinal Absorption --- p.9 / Chapter 1.3.2. --- Transporters Potentially Involved in the Absorption of Flavonoids --- p.11 / Chapter 1.3.2.1. --- Glucose Transporters --- p.11 / Chapter 1.3.2.2. --- Multidrug Resistance Systems --- p.13 / Chapter 1.3.2.2.1. --- P-glycoprotein --- p.13 / Chapter 1.3.2.2.2. --- Non-P-glycoprotein Efflux Mechanisms --- p.15 / Chapter 1.4. --- In vitro Models to Study Absorption --- p.15 / Chapter 1.4.1. --- Ussing Chamber --- p.16 / Chapter 1.4.2. --- Cultured Cells --- p.17 / Chapter 1.4.2.1. --- Choice of Cells --- p.17 / Chapter 1.4.2.2. --- Caco-2 Cell Monolayers as in vitro Model --- p.18 / Chapter 1.4.2.3. --- Correlation Between in vivo Absorption and in vitro Permeability Coefficients --- p.19 / Chapter 1.4.3. --- Everted Gut Sacs --- p.20 / Chapter 1.4.4. --- Brush Border Membrane Vesicles (BBMVs) --- p.20 / Chapter 1.4.5. --- In situ Experiments --- p.21 / Chapter 1.5. --- Aims and Scope of the Present Study --- p.23 / Chapter CHAPTER 2. --- Materials & Methods --- p.25 / Chapter 2.1. --- Materials --- p.26 / Chapter 2.1.1. --- Chemicals --- p.26 / Chapter 2.1.2. --- Materials for Cell Culture --- p.27 / Chapter 2.1.3. --- Instruments --- p.28 / Chapter 2.1.4. --- Animals --- p.28 / Chapter 2.2. --- Methods --- p.29 / Chapter 2.2.1. --- Preformulation Studies on Selected Flavonoids --- p.29 / Chapter 2.2.1.1. --- Determination of Stability --- p.29 / Chapter 2.2.1.2. --- Thermal Analysis --- p.29 / Chapter 2.2.1.3. --- Determination of Solubility --- p.29 / Chapter 2.2.1.4. --- Determination of Partition Coefficient --- p.30 / Chapter 2.2.2. --- Validation of in vitro Models --- p.30 / Chapter 2.2.2.1. --- Ussing Chamber --- p.30 / Chapter 2.2.2.1.1. --- Tissue Preparation --- p.30 / Chapter 2.2.2.1.2. --- Electrical Measurements --- p.31 / Chapter 2.2.2.1.3. --- Experimental Protocols --- p.31 / Chapter 2.2.2.1.4. --- Calculations of Permeability --- p.32 / Chapter 2.2.2.2. --- Caco-2 Cell Monolayers --- p.32 / Chapter 2.2.2.2.1. --- Preparation of Caco-2 Cell Monolayers --- p.32 / Chapter 2.2.2.2.2. --- Validation of Caco-2 Cell Monolayers --- p.32 / Chapter 2.2.2.2.3. --- Calculation of Permeability --- p.34 / Chapter 2.2.3. --- Transport Studies of Selected Flavonoids --- p.34 / Chapter 2.2.4. --- Brush Border Membrane Vesicles (BBMVs) --- p.35 / Chapter 2.2.4.1. --- Preparation of BBMVs --- p.35 / Chapter 2.2.4.2. --- Uptake of D-glucose by BBMVs --- p.38 / Chapter 2.2.4.3. --- Counting of 3H-D-glucose in BBMVs --- p.39 / Chapter 2.2.4.4. --- Calculation of Glucose Uptake --- p.39 / Chapter 2.2.4.5. --- Total Protein Assay --- p.40 / Chapter 2.2.5. --- Analytical Methods --- p.41 / Chapter 2.2.5.1. --- HPLC Analysis --- p.41 / Chapter 2.2.5.1.1. --- HPLC Analysis of Quercetin and Related Glycosides --- p.41 / Chapter 2.2.5.1.2. --- HPLC-MS Analysis of Degradation Products --- p.41 / Chapter 2.2.5.1.3. --- HPLC Analysis of Propranolol --- p.42 / Chapter 2.2.5.2. --- UV Analysis --- p.42 / Chapter 2.2.5.3. --- Fluorescence Analysis --- p.42 / Chapter 2.2.5.4. --- Analysis of Radiolabeled Markers --- p.42 / Chapter 2.2.6. --- Statistical Analysis --- p.42 / Chapter CHAPTER 3. --- Results & Discussions --- p.44 / Chapter 3.1. --- Preformulation Studies on Selected Flavonoids --- p.45 / Chapter 3.1.1. --- Stability --- p.45 / Chapter 3.1.2. --- Thermal Analysis --- p.52 / Chapter 3.1.3. --- Aqueous Solubility --- p.58 / Chapter 3.1.4. --- Partition Coefficient --- p.61 / Chapter 3.2. --- Validation of in vitro Models --- p.62 / Chapter 3.2.1. --- Selection of Marker Compounds --- p.62 / Chapter 3.2.2. --- Validation of Ussing Chamber --- p.63 / Chapter 3.2.3. --- Validation of Caco-2 Cell Monolayers --- p.64 / Chapter 3.2.3.1. --- Integrity of Caco-2 Cell Monolayers --- p.64 / Chapter 3.2.3.2. --- Permeabilities of Marker Compounds --- p.65 / Chapter 3.2.3.3. --- Selection of in vitro Models --- p.66 / Chapter 3.2.3.3. --- Validation of Sodium/Glucose Cotransporter (SGLT1) --- p.66 / Chapter 3.3. --- Transport Studies of Quercetin and Related Flavonoids --- p.67 / Chapter 3.3.1. --- Direction of Transport --- p.67 / Chapter 3.3.2. --- Concentration Dependence --- p.69 / Chapter 3.3.3. --- Inhibition of P-gp by Verapamil --- p.71 / Chapter 3.3.4. --- Metabolism of Quercetin in Caco-2 Cells --- p.72 / Chapter 3.3.5. --- Studies of Quercetin-3-glucoside with Sugar Transporters --- p.73 / Chapter 3.4. --- Uptake of D-glucose by Brush Border Membrane Vesicles (BBMVs) --- p.75 / Chapter CHAPTER 4. --- Conclusions --- p.80 / References --- p.83

Identiferoai:union.ndltd.org:cuhk.edu.hk/oai:cuhk-dr:cuhk_323852
Date January 2002
ContributorsZheng, Ying, Chinese University of Hong Kong Graduate School. Division of Pharmacy.
Source SetsThe Chinese University of Hong Kong
LanguageEnglish, Chinese
Detected LanguageEnglish
TypeText, bibliography
Formatprint, xiii, 90 leaves : ill. ; 30 cm.
RightsUse of this resource is governed by the terms and conditions of the Creative Commons “Attribution-NonCommercial-NoDerivatives 4.0 International” License (http://creativecommons.org/licenses/by-nc-nd/4.0/)

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