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Diabetes Mellitus; University of Nigeria Research Publications OKONTA, Jegbefume Matthew Author PG/Ph.D/99/27325 Evaluation of the Antidiabetic Activity of the Seed Title Extract of Picralima Nitida Stapf (Apocyanaceae) Pharmaceutical Sciences Faculty Faculty Pharmacology and Toxicology Department Department January, 2007 Date Signature Signature EVALUATION OF THE ANTIDIABETIC ACTIVITY OF THE SEED EXTRACT OF Picralima nitida STAPF (APOCYANACEAE) OKONTA, JEGBEFUME MATTHEW (PG/Ph.D/99/27325) DEPARTMENT OF PHARMACOLOGY AND TOXICOLOGY, FACULTY OF PHARMACEUTICAL SCIENCES UNIVERSITY OF NIGERIA, NSUKKA JANUARY 2007 EVALUATION OF THE ANTIDIABETIC ACTIVITY OF THE SEED EXTRACT OF Picralima nitida STAPF (APOCYANACEAE) OKONTA, JEGBEFUME MATTHEW (PGlPh.Dl99127325) A THESIS SUBMITTED TO THE DEPARTMENT OF PHARMACOLOGY AND TOXICOLOGY, FACULTY OF PHARMACEUTICAL SCIENCES, UNIVERSITY OF NIGERIA, NSUKKA IN PARTIAL FULFILLMENT OF THE REQUIREMENTS FOR THE AWARD OF DOCTOR OF PHILOSOPHY (Ph.D) DEGREE IN PHARMACOLOGY SUPERVISOR PROF*CJY-AGUWA DEPARTMENT OF CLINICAL PHARMACY AND PHARMACY MANAGEMENT, FACULTY OF PHARMACEUTICAL SCIENCES, UNIVERSITY OF NIGERIA, NSUKKA. CERTIFICATION Okonta Jegbefume Matthew, a postgraduate student with registration number PG/Ph.D/99/27325 has satisfactorily completed the requirement for the award of the degree of Doctor of Philosophy (Ph. D) of the Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences. The research embodied in this thesis is original and has not been submitted in part or in full for the award of any other Diploma or Degree of this or any other University Head of Departmknt, ? External Examiner . ,. 4. <.-1. , ., ,. ' DEDICATION To My precious mother in law, Late Madam Lucy Nka; All that suffered Diabetes mellitus; All that is suffering Diabetes mellitus, All that will suffer Diabetes mellitus, And To my beloved wife, Lillian and my son, Chidera For their understanding, support and prayers. ACKNOWLEDGEMENT I am sincerely obligated to Prof. C. Nze Aguwa, my supervisor, whose patience, fatherly guidance and timely material assistance immensely contributed to the completion of this research work. In his numerous trips within and outside the country, he brought all he deemed needful for this research work; these were evidence of his commitment to my successful completion of this work. Thank you, Sir. May I also express my sincere gratitude to Prof.I.U.Asuzu of Dept of Vet. Pharmacology and Physiology for the free access to his academic materials especially scientific papers; Prof.A.A.Ubachukwu of Dept of Physics and Astronomy and Prof. M.1.Uguru of Dept of Crop Sciences for their spiritual and academic assistance. Thank you for those your 'how far have you gone with your work? And we are praying for you' after every church service. My beloved brother, indeed and in need, Dr Vincent Chikwendu Ejere, I am not unmindful of your vested interest in my well being. In the days of my sojourn in Central America, you stood out for my young family and me. My siblings: Vincent, Andy, Mabeje, Nelzo and Catho, I aq gat:@ 49 you for all your encouraging calls and text messages. God bless all of you. 1 cannot forget my colleagues, Drs Okoli, Obonga, Ofokansi, Esimone, Okorie, Odoh and Nwodo; and Pharmacists Udeogaranya, Obitte, Ndu, Ezea, Omeje, the Okoyes, Nworu and Madu for both their spoken and unspoken encouragements. The encouragements that I got from my senior colleagues and my teachers in the persons of Prof. P A. Akah, Dr C.V. Ukwe, Prof. M.U. Adikwu, Prof. S.I. Ofoefule, Dr C.E. Ibezim, Dr C.O. Ezugwu and my precious friend, Dr V.C. Okorie cannot go without acknowledgement. I thank you all. The earnest contributions of Mr Tochi Okonkwo and Igboeme Sabastin in the laboratory work stage of this research is worthy of mention. Only God will reward you enough for the sleepless nights we shared together in the Laboratory. I am grateful to Dr Q. Zao of the Xavier-Tulane Coordinated Instrumentation Facility, Tulane University, New Orleans, USA for the 500 mHz NMR Spectra that formed a part of the Spectra data described in this thesis. I am very grateful to my soul mate, my precious wife and friend, Lillian for all her moral, emotional, and academic support while this research work lasted. Also my son Chidera is not left out in this shower of appreciation. His curiosity gave me great joy as a father. Finally, I am also grateful to my God for the health he granted my family and I, and peace that past all understanding even during some very trying moments, while this work lasted. Okonta, J.M. University of Nigeria, Nsukka.2007 ABSTRACT This study investigated the antidiabetic effect of the seed extracts of Picralima nitida in rats treated with alloxan monohydrate at 120 mgkg intraperitoneally. Methanol extract (ME, 5 gkg) caused 20.0 % maximal reduction of mean fasting blood glucose levels in normoglycemic rats while glyburide (5 mgkg) caused 25.9 % maximal reduction. In the alloxanized rats, ME caused 49.7% maximal reduction in the mean fasting blood glucose levels while glyburide caused 71.9% maximal reduction in the mean blood glucose levels after per oral administration. The blood glucose lowering effect of the extract commenced at the first hour and climaxed at twelve hour. The alkaloids extract of Picralima nitida seed given i.p. caused increase in fasting blood glucose levels while the glycosides extract reduced the blood glucose levels in normoglycemic and hyperglycemic rats though not in dose-dependent pattern. Glycosides extract caused significant (p < 0.05) reduction of 38.6 % (250 mgkg) and 22.9% (500 mgkg) of the fasting blood glucose levels in normoglycemic, and 64.4% (250 mgkg) and 39.0 % (500 mgkg) in the hyperglycemic rats. The glycosides extract maintained reduced fasting b1~~)d,.glqcoselevels for 24 h which is indicative of long duration of action. On subchronic (10 days) treatment of hyperglycemic rats, glycosides extract (250 mgkg) caused 82.99 % while glyburide (5 mgkg) caused 60.81% reduction of mean blood glucose levels. The n-butanol fractions (F7>F5>F4>Fs) showed consistent reduction of the fasting blood glucose levels of diabetic rats in the following order, 84.58 %, 80.88 %, 76.83 % and 66.92% while the glyburide caused 86.14 %. These fractions that exhibited significant blood glucose lowering action for 24 hours and F7 has the most persistent hypoglycemic effect. The fraction E of F7 caused 89.17 % maximal reduction of the mean fasting blood glucose levels of treated rats while the standard drug, glyburide caused 79.66% reduction. The peak mean blood glucose concentration achieved after glucagon administration was reduced by the glycosides fractions like glybwide did. They respectively caused reduction in mean blood glucose levels in the following order E>F7>F5. From the fraction E of the seed extract of Picralima nitida, that had the highest hypoglycemic activity, was isolated a hydrophilic triterpenoidal saponin; 2a, 3a 16a, 23- tetrahydroxyloleana-5, 13 (1 8)-dien-28-oic acid which may be the enatiomer of Mimusic acid obtained from the Mimusops elengi. In conclusion, it may be stated that the high hypoglycemic activity of the seed extract of Picralima nitida resides in the hydrophilic triterpenoidal saponins which may have achieved this through reduction of hepatic overproduction of glucose or increase in glucagon catabolism, and inhibition of gastric emptying in diabetic conditions. .. 11 .. 111 iv v vii ix xiv xvi xix CHAPTER TWO: MATERIALS AND METHODS 2.3.1 Fractionation of Alkaloids and Glycosides from methanolic extract------------- 47 2.4.3 Chemical identification of the respective spots of Fraction F7 bE--------------- 49 2.4.4 Determination of the Nuclear Magnetic Resonance (NMR) and Mass Spectrophotometry (MS) of Fraction F7 bE spots-------------------------------- 49 2.6.2 Effects of methanol (ME) and chloroform (CHE) extracts of Picralima nitida seed on mean fasting blood glucose levels in normal rats---------------------------- 5 1 2.6.6 Effect of alkaloids (AKF) and glycosides fractions of methanol extract of Picralima nitida on mean fasting blood glucose levels in normal rats-------------------- 53 2.6.8 Effect of aqueous (AQP) and chloroform (CHP) phases of glycosides fraction of Picralima nitida on mean fasting blood glucose levels in alloxanized rats---- 54 2.6.9 Prolonged treatment effect of q-Bum01 extract (nBF) of glycosides fraction of Picralima nitida on mean fasting blood glucose levels in alloxanized rat--- 54 2.7.1 Effects of chromatographic fractions (F4-8) of nBF of Picralima nitida on mean fasting blood glucose level in alloxanized rats----------------------------------- 55 2.7.2 Effects of chromatographic fractions (F4,+8) of nBF of Picralima nitida on mean fasting blood glucose levels in glucagon-induced hyperglycemic rats------- 56 2.8 Preparation of Calibration Curve of Phenol Red in Glucose solution------------ 58 CHAPTER THREE: RESULTS Phytochemical analysis of extracts and fractions----------------------------- 60 Effect of methanol (ME) and chloroform (CHE) extracts of Picralima nitida on mean fasting blood glucose levels in normal rats----------------------------- 72 Effect of methanol (ME) extract of Picralima nitida on mean fasting blood glucose levels in normoglycemic and alloxanized rats------------------------ 72 Effect of methanolic extract of Picralima nitida seeds on mean blood glucose levels of rats orally fed with glucose..................................................... 73 , . .. Effect of alkaloids (Alk) and glycosides (gly) fractions
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