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Phytochemical Investigation of Turraea Robusta, Turraea Nilotica and Ekebergia Capensis for Antiplasmodial and Cytotoxic Compounds

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Phytochemical Investigation of Turraea Robusta, Turraea Nilotica and Ekebergia Capensis for Antiplasmodial and Cytotoxic Compounds UNIVERSITY OF NAIROBI PHYTOCHEMICAL INVESTIGATION OF TURRAEA ROBUSTA, TURRAEA NILOTICA AND EKEBERGIA CAPENSIS FOR ANTIPLASMODIAL AND CYTOTOXIC COMPOUNDS. BY BEATRICE NJERI IRUNGU I80/80299/2010 A Thesis Submitted in Fulfilment of the Requirements for Award of the Degree of Doctor of Philosophy in Chemistry of the University of Nairobi 2014 i DECLARATION I declare tha t this thesis is my original work and has not been submitted elsewhere for examination or award of a degree. Signature.................................................... Date......................................... Beatrice Njeri Irungu I80/80299/2010 Department of Chemistry School of Physical Sciences University of Nairobi This thesis is submitted for examination with our approval as research supervisors Signature Date Professor Jacob Midiwo ................... ................. Department of Chemistry University of Nairobi P.O Box 30197-00100, Nairobi-Kenya [email protected] Professor Abiy Yenesew ……………… …………… Department of Chemistry University of Nairobi P.O Box 30197-00100, Nairobi-Kenya [email protected] Dr. Jennifer Orwa ........................ ........................ Kenya Medical Research Institute Centre for Traditional Medicine and Drug Research P.O. Box 54840-00200, Nairobi- Kenya [email protected] ii DEDICATION This thesis is dedicated to my husband Kimani Maina for enduring this long process with me, always offering support and love. our children Maina Kimani and Nyawira Kimani Though too young to understand what mum was going through, you supported me in your own little ways. I pray that this will serve as an encouragement as you walk through your academic pathways. iii ACKNOWLEDGEMENT The road towards a doctorate degree is not walked alone. Thus, this project would not have been possible without the support of my supervisors/mentors, friends and colleagues, to only some of whom it is possible to give particular mention here. Above all, I thank God for the precious gift of life, health and strength to continue and stay focussed especially when the end seemed far out of sight. To my principal supervisors and mentors Professor Jacob Midiwo and Professor Abiy Yenesew: I am grateful for all the support you gave me. Your invaluable guidance helped me in the course of my PhD research and write-up of this thesis. Thank you for shaping my scientific thinking. Dr Jennifer Orwa: Thank you for your encouragement and accepting to be a Principal Investigator to this project and a supervisor at KEMRI where the project was carried out. Professor Máté Erdélyi: Thank you for accepting me in your group at the Department of Chemistry and Molecular Biology, University of Göteborg, Sweden and for financial support. I was able to acquire NMR and LC/MS data. Dr Matthias Heydenreich: Thank you for 1D and 2D NMR and MS data Fellow PhD students at CTMDR, Messers Charles Muthaura and Mr. Antony Radol: Thank you for your company, advice and encouragement. To Dr Omar Sabah and Mr. Francis Kimani: Malaria laboratory CBRD-KEMRI: Thank you for all the antiplasmodial data. Messrs Nicholas Adipo, Kenneth Murega and Ibrahim Kirema: I will be forever thankful for all the technical assistance you gave me. Director KEMRI is acknowledged for providing facilities for this research. I express my gratitude to UNICEF/UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases (TDR) for the financial support. Last but not least to my parents, Peter Irũngũ and Helina Wambũi; thanking you for your love and bringing me up to be the woman I am today. iv ABSTRACT In an effort to identify antiplasmodial and/or cytotoxic secondary metabolites, three African medicinal plants, Ekebergia capensis, Turraea nilotica and Turraea robusta were investigated for antiplasmodial and cytotoxic compounds. Except for T. nilotica, the other plants were selected on the basis of previous reports on antiplasmodial activities of crude extracts. A combination of different chromatographic techniques including preparative HPLC was employed in isolation of compounds. The characterization of compounds was done using 1D and 2D NMR as well as MS analyses. The crude extracts and the isolated compounds were evaluated for antiplasmodial activity against the chloroquine- resistant (W2) and chloroquine-sensitive (D6) strains of Plasmodium falciparum using a semiautomated micro dilution technique which measures the ability of the compounds to inhibit the incorporation of (G-3H) hypoxanthine into the malaria parasite. They were also evaluated for cytotoxicity properties against African green monkey kidney (vero), using a rapid colourimetric assay that employs 3- (4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) as a viability indicator. Selectivity index (SI) defined as IC50 (Vero cells) / IC50 (P. falciparum) was also determined. A total of twenty six compounds were isolated. From the stem bark of Turraea robusta seven compounds were isolated of which acetoxy-7-deacetylazadirone (28) and 11-epi-toonacilin (62) were new to the species whereas azadironolide (192) was new to the genus. Turraea nilotica leaves, root and stem bark yielded twelve compounds of which five [mzikonone (17), azadirone (19), acetoxy-7- deacetylazadirone (28), 1α,3α-diaacety-7α-tigloylvilasinin (40) and hipidol B (96)] were new to the species and four [toonapubesins (194) and phytosterols (195-197)] were new to the genus. From the root bark and leaves of Ekebergia capensis ten compounds were isolated with two glycoflavonoids (199-200) being new to the genus and a new natural product, 3-oxo-12β-hydroxy-oleanan-28,13β- olide (198). Azadironolide (192) displayed the highest antiplasmodial activity with an IC50 of 1.1 and 2.4 μM against W2 and D6 strains respectively, with a SI > 10.5. This compound can be evaluated further for its antimalarial activity in a mouse model. The rest of the compounds displayed moderate to low antiplasmodial activities with IC50 ranging 14.4-205 μM against the two P. falciparum strains with low selectivity index (< 10). The low SI values indicate that the observed moderate antiplasmodial activity may be due to general cytotoxicity rather than the activity against the parasites. This motivated further cytotoxicity investigation on cancerous cell lines, mouse breast cancer (4T1), human larynx carcinoma (HEp2) and human breast cancer (MDA-MB-231). Six compounds were cytotoxic to cell lines 4T1 and HEp2 (IC50 < 20 μM) with oleanonic acid (160) being the most cytotoxic to HEp2 cell line with an IC50 value of 1.4 μM. v Interaction of oleanonic acid (160) isolated as a major compound from E. capensis, with five triterpenoids; 2,3,22,23-tetrahydroxy-2,6,10,15,19,23- hexamethyl-6,10,14,18- tetracosatetraene (151), 2-hydroxymethyl-2,3,22,23- tetrahydroxy-6,10,15,19,23-pentamethyl-6,10,14,18 tetracosatetraene (152), ekeberin A (158), oleanolic acid (159) and 3-epi-oleanolic acid (161) was evaluated against vero and HEp2 cell lines. No appreciable synergism was observed. Structure-Activity–Evaluation by acetylating niloticin (25), piscidinol A (27) and oleanolic acid (159) was carried out. The derivatives were evaluated for cytotoxicity activity where niloticin acetate (201) and piscidinol A diacetate (203) were of lower activity than the parent molecules while oleanolic acid acetate (202) was seven folds more active than oleanolic acid. vi TABLE OF CONTENTS DECLARATION .............................................................................................................. ii DEDICATION ................................................................................................................. iii ACKNOWLEDGEMENT ............................................................................................... iv ABSTRACT ..................................................................................................................... v TABLE OF CONTENTS ................................................................................................ vii LIST OF TABLES ......................................................................................................... xiii LIST OF FIGURES ........................................................................................................ xv LIST OF ABBREVIATIONS and ACRONYMS .......................................................... xvi CHAPTER ONE ............................................................................................................... 1 INTRODUCTION ............................................................................................................ 1 1.1. GENERAL OVERVIEW .............................................................................. 1 1.2. Statement of the Problem .............................................................................. 4 1.3. Objectives...................................................................................................... 5 1.3.1. General Objective .................................................................................. 5 1.3.2. Specific objectives ................................................................................. 5 1.4. Justification ................................................................................................... 6 CHAPTER TWO .............................................................................................................. 7 LITERATURE REVIEW ................................................................................................. 7 2.1. Background on Malaria ................................................................................
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