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Establishment and Optimization of the LC-MS-Based Strategy for Screening of Passively Establishment and optimization of the LC-MS-based strategy for screening of passively absorbed açaí and maca constituents for CYP3A4 inhibition by Thankhoe Abram Rants’o A thesis submitted to the Graduate Faculty of Auburn University in partial fulfillment of the requirements for the Degree of Master of Science Auburn, Alabama August 5, 2017 Keywords: liquid chromatography-mass spectrometry, açaí, maca, intestinal absorption, CYP3A4 inhibition, metabolism Copyright 2017 by Thankhoe Abram Rants’o Approved by Angela I. Calderón, Chair, Associate Professor of Drug Discovery and Development Randall Clark, Professor of Drug Discovery and Development Jack DeRuiter, Professor of Drug Discovery and Development Forrest Smith, Associate Professor of Drug Discovery and Development Abstract The escalation of cancer morbidity and mortality has increased the use of botanical dietary supplements among cancer patients undergoing chemotherapy. Euterpe oleracea Mart. (açaí) berry and Lepidium meyenii Walpers (maca) root are some of the most common botanical dietary supplements used concomitantly with anticancer agents. CYP3A4 is an important enzyme in the metabolism and clearance of anticancer agents. While often used for their scientific claims against cancer, the supplements may also cause botanical-drug pharmacokinetic interactions of which one is through CYP3A4 inhibition. Consideration of bioavailable constituents of botanical dietary supplements has been identified as a route to counteract the discrepancy between preclinical and clinical botanical-drug interaction data. Passive absorption is the most common mechanism of absorption for medicines in the market. The goal of this study is to screen passively absorbable açaí berry and maca root constituents and their Phase I and Phase II metabolites for CYP3A4 inhibition. Chapter one is an overview of cancer prevalence, treatment, botanical dietary supplements use and the herbal-drug interactions. The chapter also goes into the chemical characterization of açaí berry and maca root extracts. Chapter two describes in detail, the methods used in açaí and maca plant extracts fingerprinting, establishment of intestinal passive absorption model, metabolism and CYP3A4 inhibition assays. The experimental work used LC-MS and other orthogonal confirmatory assays. Chapter three presents the results, discussion and conclusions. The findings of this study, after identifying the extracts with moderate to strong CYP3A4 inhibition, suggest that açaí and maca ii botanical dietary supplements have a potential to cause significant botanical-drug interactions in the clinical setting. iii Acknowledgements Above all, I thank God for the everlasting protection, love and perfect guidance He gave to me throughout this journey. I am more than thankful to my family that had faith to let me leave my country and follow my passion but never ceased to support me every second. I therefore dedicate this work to my father, Mr. Motlatsi Rants’o, my mother, Mrs ‘Majane Rants’o, my brother Jane Rants’o and my sister ‘Majapi Rants’o. Their love and care kept me going even through the tough times. My hearty acknowledgements go to the Fulbright Scholarship that generously sponsored all my tuition and living costs. I believe that without Fulbright I wouldn’t have set my foot on the land of destiny, United States of America. I want to thank the US Embassy in Lesotho that helped me with all preparations to come to the US and constantly supported me during my stay. I am grateful of my Fulbright advisors, Ms. Megan Ames and Ms. ‘Mathabang Fanyane who always ensured that I had all I needed to reach the completion of my study. I want to take this opportunity to thank my academic advisor, Dr. Angela Calderón for giving me an opportunity to join her great lab and for her constant guidance, support, encouragement and for making me realize my potential. I here observe my committee members who tirelessly helped me not only through my research but also in the academic courses. I highly thank Dr. Jack Deruiter who stimulated my passion into the career of drug discovery through his Advanced Medicinal Chemistry courses that also happened to be the major part of my research. I greatly thank Dr. Randall Clark who has helped me understand my research better and been always most welcoming supportive. In the same way, my sincere regards go to Dr. Forrest Smith for his valuable input that always gave me a direction in analyzing my research data. I would like to also extend my gratitude to our collaborators, Dr. Richard Hansen and Dr. Jingjing Qian who are tirelessly complementing this project by searching for population-based statistical reports of the findings of this research. I would also like to thank Dr. Richard van iv Breemen from University of Illinois at Chicago who has always been responsive to the questions I had in the designing of the experiments of this research. I thank also the following undergraduate students who carried out some of the experiments with me during their designated times in the lab. These are Amanda Schellenberger, Lane McLendon, Da Jung and Rebecca Keller. I also like to thank them for letting me mentor and train them. I am indebted to the Auburn University Research Initiative in Cancer (AURIC) for the financial support to this project. I want to thank my friends and colleagues Logan Neel and Ibtisam Ibtisam whom we took classes together and encouraged each other through out. My sincere gratitude to Logan Neel whom we shared great and bad moments. Again, I would like to thank my friends Mansour Alturki, Rene Fuanta and Ahmed Almalki who have always been by my side throughout. I would like to thank Dr. David Riese and Mrs Jennifer Johnston for not only monitoring my academic stability but also my well-being and making sure that I reach my goals. Again, I would like to thank Chris Smith and Kaleia Williams for always being ready to help and making me feel free and welcome. Finally, I give my regards to Tamika Fields and her colleagues in the Office of Information Technology in the school for working closely with me in the most secure management of my data and software installations for my data analysis. v Table of Contents Abstract ......................................................................................................................................... ii Acknowledgments ....................................................................................................................... iv List of Figures .............................................................................................................................. xi List of Tables ............................................................................................................................. xiii List of Abbreviations ................................................................................................................. xv Chapter 1: Literature review ........................................................................................................ 1 1.1 Introduction ................................................................................................................ 1 1.2 Botanical dietary supplement use in the United States ............................................... 3 1.2.1 Use of botanical dietary supplements among cancer patients ................................. 5 1.2.2 Euterpe oleracea Mart. (açaí) .................................................................................. 5 1.2.3 Lepidium meyenii Walpers (maca)........................................................................... 9 1.3 Botanical-drug pharmacokinetic interactions ........................................................... 11 1.3.1 Importance of determination of intestinal absorption of botanical constituents .... 13 1.3.2 Relevance of Phase I and Phase II metabolism of botanical constituents ............. 14 1.3.3 CYP3A4 metabolic enzyme and significance in botanical-drug interactions ....... 15 1.7 Project rationale ........................................................................................................ 16 1.8 Research objectives ................................................................................................... 17 Chapter 2: Establishment and optimization of the LC-MS-based strategy for screening of passively absorbed plant extract constituents for CYP3A4 inhibition ..................... 18 vi 2.1 Introduction ............................................................................................................... 17 2.2 Materials and methods .............................................................................................. 19 2.2.1 Chemicals ............................................................................................................... 19 2.2.1.1 Identity of the plant materials ............................................................................. 20 2.2.1.2 Açaí and maca plant standard compounds……………………………………...24 2.2.2 Plant extracts preparation ....................................................................................... 24 2.2.2.1 Açaí plant extracts............................................................................................... 25 2.2.2.1.1 Dichloromethane and methanol extracts……………………………………...25 2.2.2.1.2 Acidic methanol extracts...................................................................................25 2.2.2.2 Maca plant extracts ............................................................................................
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