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ETHNOPHARMACOLOGICAL RELEVANCE: Dennettia tripetala Baker f. belonging to the family Annonaceae is an important food and medicinal plant used in some local communities in Southwest Nigeria. AIMS OF THE STUDY: The study aims at determining the chemical composition of the essential oil of different morphological parts of D. tripetala, the memory enhancing and anticholinesterase activities as well as the antimicrobial properties. MATERIALS AND METHODS: Essential oil of the morphological parts namely the fresh fruits, dried fruits, dried seeds and fresh leaves were obtained by hydrodistillation and analysed by GC-FID and GC-MS. The oil samples were evaluated for memory enhancement using Y-maze and in vitro anticholinesterase activities. The antimicrobial properties were also evaluated by nutrient broth method. RESULTS: GC analysis identifies ß-ocimene, linalool, ß-phenylnitroethane and humulene as common constituents of the fresh fruits, dried fruits, dried seeds and fresh leaves. ß-Phenylnitroethane (BPNE) was the predominant constituent of all the parts; with the dried seed containing 87.4% BPNE, followed by the dried fruit (78.1%), fresh leaf (62.9%) and the fresh fruit content was 61.6%. The second most predominant constituent, linalool, was highest in the fresh fruit (29.9%), followed by the fresh leaf (16.0%), the dried fruit (14.9%) and the dried seed had least linalool content (8.8%). (Z)- ß-Ocimene and humulene were other common components. The seed oil and BPNE exhibited high memory enhancing activities in the Y-maze test. However, the seed oil exhibited the best inhibition against the test bacteria and it had a broad spectrum of antimicrobial activity. Bioactivities demonstrated by the various essential oils were not solely due to BPNE; rather, synergistic effects of other components are quite obvious. CONCLUSION: The most abundant component - ß-phenylnitroethane of D. tripetala was totally responsible for its memory enhancing properties but could not solely account for its antimicrobial activity.
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Annonaceae , Antiinfecciosos/farmacología , Inhibidores de la Colinesterasa/farmacología , Aprendizaje/efectos de los fármacos , Aceites Volátiles/farmacología , Animales , Bacterias/efectos de los fármacos , Bacterias/crecimiento & desarrollo , Candida/efectos de los fármacos , Candida/crecimiento & desarrollo , Ratones , Pruebas de Sensibilidad MicrobianaRESUMEN
BACKGROUND: Beta (ß)-endorphins are endogenous neuropeptides found in the plasma and cerebrospinal fluid (CSF) of humans but there have been reports of the relationship between the plasma and CSF ß-endorphin levels in different clinical conditions. However, the relationship between ß-endorphin levels in the plasma and CSF of children with cerebral malaria (CM) has not been reported. AIM: To determine the relationship between ß-endorphin levels in the CSF and plasma of children with CM. SETTINGS AND DESIGN: This cross-sectional study involved 40 children, aged between 6 months and 14 years, admitted with a diagnosis of CM at the Obafemi Awolowo University Teaching Hospitals Complex (OAUTHC), Ile-Ife, Nigeria. MATERIALS AND METHODS: One milliliter (mL) of venous blood and 1mL of CSF obtained from each subject at admission were used to determine the ß-endorphin levels using enzyme-linked immunosorbent assay (ELISA) method. STATISTICAL ANALYSIS: Bivariate linear regression was used to determine the association between plasma and CSF ß-endorphin levels using the correlation coefficient (r), coefficient of determination (R 2), and P values. RESULTS: The plasma ß-endorphin levels significantly positively correlated with CSF ß-endorphin (r = 0.568, P = 0.001) such that for every unit rise in plasma ß-endorphin, CSF ß-endorphin rose by 0.252 pmol/L (confidence interval: 0.132-0.371 pmol/L). CONCLUSION: The finding of positive correlation between plasma and CSF ß-endorphin levels in this study suggests a possible direct link between plasma and CSF in CM, probably from the disruption of the blood-brain barrier that has been reported in CM.
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This study evaluated the ameliorative and prophylactic effects of 2 different doses of polyphenolic-rich fraction of Garcinia kola (PPRFGk) seeds on the histology and hormones of pituitary-testicular axis of male Wistar rats. Thirty-five male Wistar rats (150-200 g) were divided into 7 groups of 5 rats each. Groups I and II were given distilled water (0.5 mL/day) for 8 days followed by propylene glycol (0.2 mL/d) and 600 mg/kg of PPRFGk, respectively, for 21 days. Group III received sodium arsenate (8 days), left untreated for 21 days. Groups IV and V received sodium arsenate (20 mg/kg) for 8 days followed by PPRFGk (300 and 600 mg/kg, respectively) for 21 days. Groups VI and VII received PPRFGk (300 and 600 mg/kg, respectively) for 21 days followed by sodium arsenate (20 mg/kg) for 8 days. Rats were killed by cervical dislocation 24 hours after the last dose and their blood collected through cardiac puncture. Blood sera were assayed for the levels of follicle-stimulating hormone (FSH), luteinizing hormone (LH), and testosterone using immunoassay techniques. Histology of the pituitary gland and testes was carried out. A significant reduction was observed in the concentration of FSH in groups IV, V, VI, and VII in comparison with groups I and II. The concentrations of both LH and testosterone showed significant decreases in groups IV, V, VI, and VII in comparison with group I. Group III presented with the lowest serum hormonal concentrations. Photomicrographs of the pituitary gland revealed greatly reduced basophils in group III and mildly reduced basophils in groups IV, VI, and VII in comparison with groups I and II. Group V revealed hypercellularized and distorted basophils. Photomicrographs of the testes showed detachment of the seminiferous tubules from the basement membrane and disruption of the interstitial space which was worse in group III, moderate in groups V and VI, and mild in group VII. In conclusion, PPRFGk effected a dose-dependent reversal and prevention of the perturbations caused by arsenate in rats.
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Spondias mombin has been used in traditional medicine for the management of several diseases, including memory loss. This study aimed to evaluate the cholinesterase inhibitory activity of the methanol extract of the leaves and its derived fractions, as well as carry out detailed phytochemical investigations leading to the isolation and characterization of bioactive compounds from the plant. The acetyl cholinesterase (AChE) and butyryl cholinesterase (BUChE) inhibitory activities were evaluated by colorimetric and thin-layer chromatography bioautographic assay techniques. The ethyl acetate fraction was most active against both enzymes, with percentage inhibition of 58.10 ± 1.08% and 52.66 ± 1.34% against AChE and BUChE, respectively. Three compounds, namely, botulin, campesterol and phytol, with IC50 of 0.88 µg/mL (AChE), 4.67 µg/mL (BuChE); 1.89 µg/mL (AChE), 4.08 µg/mL (BuChE) and 12.51 µg/mL (AChE), 23.89 µg/mL (BuChE), respectively, were isolated from the supernatant of the ethyl acetate fraction. The isolated cholinesterase inhibitory compounds correlate with the known memory-enhancing property of the plant and thus support one of its uses in ethnomedicine.
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OBJECTIVES: Cerebral malaria (CM) is the most lethal form of malaria, yet its pathogenesis is not fully understood. Cytoadherence, sequestration, alterations in cytokine expression, inflammation, and microvascular obstruction are all hypothesized to be important in the aetio-pathogenesis of coma which characterizes cerebral malaria and the death which sometimes result. Beta (ß)-endorphin has been postulated to be involved in the pathogenetic processes of inflammation and cytokine expression, although the exact role is unknown. The aim of this study was to determine the levels of ß-endorphin in cerebrospinal fluid (CSF) and plasma of children with CM and compare the levels of ß-endorphin in the plasma of children with CM with that of apparently healthy age- and sex-matched controls at Ile-Ife, Nigeria. MATERIALS AND METHODS: Additional to the standard investigation for CM, CSF and venous blood samples were obtained from the subjects for the determination of ß-endorphin levels. RESULTS: Forty children with CM were studied along with forty age- and sex-matched controls. The mean CSF ß-endorphin (± SD) level for the children with CM was 1.8 ± 0.9 pmol/L. The mean plasma ß-endorphin levels at admission (3.1 ± 2.0 pmol/L) and discharge (4.1 ± 3.3 pmol/L) were higher in children with CM than in the control subjects (2.7 ± 0.7 pmol/L). However, only the mean plasma ß-endorphin levels at discharge was significantly higher than that of controls (p = .012). CONCLUSION: Children with CM had higher mean plasma ß-endorphin levels compared to the controls and there was increased production of ß-endorphins in children with CM during the course of the illness.
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Malaria Cerebral/sangre , Malaria Cerebral/líquido cefalorraquídeo , betaendorfina/sangre , betaendorfina/líquido cefalorraquídeo , Envejecimiento/sangre , Envejecimiento/líquido cefalorraquídeo , Biomarcadores/sangre , Biomarcadores/líquido cefalorraquídeo , Análisis Químico de la Sangre , Temperatura Corporal/fisiología , Niño , Desarrollo Infantil/fisiología , Preescolar , Ensayo de Inmunoadsorción Enzimática , Femenino , Humanos , Lactante , Malaria Cerebral/terapia , Masculino , Caracteres Sexuales , Resultado del TratamientoRESUMEN
ABSTRACT The leaves of Pycnanthus angolensis (Welw.) Warb., Myristicaceae, are used as memory enhancer and anti-ageing in Nigerian ethnomedicine. This study aimed at evaluating the cholinesterase inhibitory property as well as isolates the bioactive compounds from the plant. The acetylcholinesterase and butyrylcholinesterase inhibitory potentials of extracts, fractions, and isolated compounds were evaluated by colorimetric and TLC bioautographic assay techniques. The extract inhibited both enzymes with activity increasing with purification, ethyl acetate fraction being most active fraction at 65.66 ± 1.06% and 49.38 ± 1.66% against acetylcholinesterase and butyrylcholinesterase, respectively while the supernatant had 77.44 ± 1.18 inhibition against acetylcholinesterase. Two new bioactive compounds, (2E, 18E)-3,7,11,15,18-pentamethylhenicosa-2,18-dien-1-ol (named eluptol) and [12-(4-hydroxy-3-methyl-oxo-cyclopenta-1,3-dien-1yl)-11-methyl-dodecyl](E)-3-(3,4-dimethylphenyl)prop-2-enoate (named omifoate A) were isolated from the plant with IC50 of 22.26 µg/ml (AChE), 34.61 µg/ml (BuChE) and 6.51 µg/ml (AChE), 9.07 µg/ml (BuChE) respectively. The results showed that the plant has cholinesterase inhibitory activity which might be responsible for its memory enhancing action, thus justifying its inclusion in traditional memory enhancing preparations.
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African animal trypanosomosis (AAT) is a disease of concern with ravaging effects on the health of both animals and livestock in tropical Africa. This study investigates the anti-trypanosomal activities of Anogeissus leiocarpus (ALE) and Vitelleria paradoxa (VPE) stem bark extracts and also determines the toxicological profile of the active plant, with a view to establishing the anti-trypanosomal potential and safety of the plants. Laboratory mice (19 g 26 g) and rats (140 g 165 g) obtained from the Animal house, Faculty of Pharmacy, OAU, Ile-Ife were used for the study. The animals were treated according to the standard set criteria for animal use and care. VPE showed neither trypanocidal nor trypanostatic activities while ALE was found to be trypanostatic at 62.5 and 125 mg/kg body weight. However, the partitioned aqueous fraction of ALE was found to demonstrate comparable anti-trypanocidal effect as Diminal (standard agent). In conclusion, the ethanolic extract of A. leiocarpus possesses antitrypanosomal effect through the relative suppression or delay in parasite establishment in trypanosome-infected mice. The toxicological study of A. leiocarpus stem bark extract revealed that it is relatively safe for use in cattle and other grazing animals.
La tripanosomiasis africana de los animales es una enfermedad de preocupación que causa estragos sobre la salud de los animales y el ganado en África tropical. Este estudio investiga las actividades anti-tripanosomal de Anogeissus leiocarpus (ALE) y Vitelleria paradoxa (VPE) del tallo y extractos de corteza. También determina el perfil toxicológico de la planta activa, con el fin de establecer el potencial anti-tripanosomal y la seguridad de las plantas. Ratones de laboratorio (19 g - 26 g) y ratas (140 g - 165 g) obtenidos del Bioterio de la Facultad de Farmacia de la OUA, se utilizaron para el estudio. Los animales fueron tratados de acuerdo con los criterios estándar establecido para el uso y cuidado de animales. VPE mostró actividades no tripanocidas ni tripanostáticas mientras que en ALE se encontró que era tripanostático a 62,5 y 125 mg/kg de peso corporal. Sin embargo, se encontró que la fracción acuosa de ALE demostró un efecto anti-tripanocida comparable como Diminal (agente estándar). En conclusión, el extracto etanólico de A. leiocarpus posee efecto sobre tripanosomas a través de la supresión relativa o retraso en la creación de parásitos en ratones infectados con tripanosomosis. El estudio toxicológico del extracto de corteza del tallo A. leiocarpus reveló que es relativamente seguro para su uso en el ganado y otros animales de pastoreo.
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Animales , Ratones , Ratas , Combretaceae/química , Extractos Vegetales/uso terapéutico , Sapotaceae/química , Tripanocidas/uso terapéutico , Tripanosomiasis Africana/tratamiento farmacológico , Pruebas de Toxicidad , TrypanosomaRESUMEN
BACKGROUND: Flavonoid-rich aqueous fraction of methanolic extract of Hibiscus sabdariffa calyx was evaluated for its anti-hepatotoxic activities in streptozotocin-induced diabetic Wistar rats. METHODS: Diabetes Mellitus was induced in Wistar rats by a single i.p injection of 80 mg/kg b.w. streptozotocin (STZ) dissolved in 0.1 M citrate buffer (pH 6.3). RESULTS: The ameliorative effects of the extract on STZ-diabetes induced liver damage was evident from the histopathological analysis and the biochemical parameters evaluated in the serum and liver homogenates. Reduced levels of glutathione (GSH), catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) (3.76 ± 0.38 µM, 0.42 ± 0.04 U/L, 41.08 ± 3.04 U/ml, 0.82 ± 0.04 U/L respectively) in the liver of diabetic rats were restored to a near normal level in the Hibiscus sabdariffa-treated rats (6.87 ± 0.51 µM, 0.72 ± 0.06 U/L, 87.92 ± 5.26 U/ml, 1.37 ± 0.06 U/L respectively). Elevated levels of aspartate amino transferase (AST), alanine amino transferase (ALT) and alkaline phosphatase (ALP) in the serum of diabetic rats were also restored in Hibiscus sabdariffa -treated rats. Examination of stained liver sections revealed hepatic fibrosis and excessive glycogen deposition in the diabetic rats. These pathological changes were ameliorated in the extract-treated rats. CONCLUSION: The anti-hepatotoxic activity of Hibiscus sabdariffa extract in STZ diabetic rats could be partly related to its antioxidant activity and the presence of flavonnoids.
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Diabetes Mellitus Experimental/tratamiento farmacológico , Hibiscus/química , Hepatopatías/tratamiento farmacológico , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Animales , Diabetes Mellitus Experimental/sangre , Diabetes Mellitus Experimental/enzimología , Diabetes Mellitus Experimental/patología , Enzimas/sangre , Hígado/química , Hígado/efectos de los fármacos , Hígado/patología , Hepatopatías/metabolismo , Hepatopatías/patología , Masculino , Distribución Aleatoria , Ratas , Ratas WistarRESUMEN
The cardioprotective property of Spondias mombin (SM) was investigated and compared with that of the ACE inhibitor, ramipril. Alterations to markers of myocardial injury and indices of antioxidant capacity by isoproterenol (ISP) intoxication were significantly corrected in groups treated with SM. The inflammatory index was increased by 24% in ISP-intoxicated group compared with control (P < 0.001) but reduced in the groups administered ISP and treated with 100 or 250 mg/kg SM by 17% (P < 0.001) and 11% (P < 0.05) respectively. Serum lactate dehydrogenase activity and cholesterol level which were significantly increased in ISP-intoxicated group compared with control were reduced in groups administered ISP and treated with SM. Serum phosphate levels in groups administered ISP and treated with SM were significantly lower than values obtained for the ISP-intoxicated group (P < 0.001). Tissue catalase and superoxide dismutase activities as well as glutathione level were significantly increased in groups administered ISP and treated with SM compared to ISP-intoxicated group while MDA and nitrite levels were decreased. Disruption in the structure of cardiac myofibrils by ISP intoxication was reduced by treatment with SM. Comparable results were obtained for ramipril. These results are indicative of the potent cardioprotective property of SM.
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Anacardiaceae , Inhibidores de la Enzima Convertidora de Angiotensina/farmacología , Fármacos Cardiovasculares/farmacología , Infarto del Miocardio/prevención & control , Isquemia Miocárdica/prevención & control , Fenómeno de no Reflujo/prevención & control , Extractos Vegetales/farmacología , Ramipril/farmacología , Animales , Catalasa/metabolismo , Colesterol/sangre , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Glutatión/metabolismo , Isoproterenol , L-Lactato Deshidrogenasa/sangre , Masculino , Malondialdehído/metabolismo , Infarto del Miocardio/inducido químicamente , Infarto del Miocardio/metabolismo , Infarto del Miocardio/patología , Infarto del Miocardio/fisiopatología , Isquemia Miocárdica/metabolismo , Isquemia Miocárdica/patología , Isquemia Miocárdica/fisiopatología , Miocardio/metabolismo , Miocardio/patología , Nitritos/metabolismo , Fenómeno de no Reflujo/metabolismo , Fenómeno de no Reflujo/patología , Fenómeno de no Reflujo/fisiopatología , Fosfatos/sangre , Hojas de la Planta , Ratas , Ratas Sprague-Dawley , Superóxido Dismutasa/metabolismo , Factores de TiempoRESUMEN
Plants have been found to be useful as memory enhansers as well as antiaging. Twenty two of such plants from sixteen families were investigated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities using the in vitro Ellman's spectrophotometric and in situ bioautographic methods with physostigmine as standard. At least three morphological parts were examined for each of the plants investigated and the test concentration was 42.5 µg/ mL. Some plants were active on both enzymes though with some morphological parts being more active than others. The root bark of Spondias mombin showed the highest activity to the two enzymes; 64.77 percent and 83.94 percent on AChE and BuChE respectively. Other plant parts of the selected plants exhibited some remarkable selectivity in their actions. Those selectively active against AChE were Alchornia laxiflora stem bark (41.12 percent) and root bark, Callophyllum inophyllurn root bark (56.52 percent). The leaves of C. jagus (74.25 percent), Morinda lucida leaves (40.15 percent), Peltophorum pterocarpum leaves and stem bark (49.5 percent and 68.85 percent, respectively), physiostigmine gave 90.31 percent inhibition. Generally higher activities were found against BuChE. Bombax bromoposenze leaves, root bark and stem bark were particularly active. The inhibition was over 80 percent. Other selective plant parts are the leaves Antiaris africana, Cissampelos owarensis aerial parts (78.96 percent), Combretum molle leaves and stem bark (90.42 percent and 88.13 percent, respectively), Dioscorea dumentorum root bark and tuber (over 87 percent), G. kola leaves, Markhamia tomentosa root bark, Pycnanthus angolensis stem bark and Tetrapleura tetraptera leaves. Most of these plants are taken as food or are food ingredients in Nigeria and may account for the low incidence of Alzheimer's disease in the country and may play certain roles in the mediation of the disease.
As plantas podem ser úteis para estimular a memória, bem como serem usadas para combater o envelhecimento. Vinte e duas plantas, de dezesseis famílias, foram investigadas in vitro oara verificar sua atividade inibidora das enzimas acetilcolinesterase (AChE) e butirilcolinesterase (BuChE) pelo método espectrofotométrico de Ellman in situ e métodos de bioautografia utilizando fisostigmina como padrão. Pelo menos três partes morfológicas de cada planta foram analisadas e a concentração de ensaio foi de 42,5 µg/mL. Algumas plantas foram ativas em ambas as enzimas, embora com algumas partes mais ativas que outras. A casca da raiz de Spondias mombin apresentou a maior atividade as duas enzimas, 64,77 por cento para AChE e 83,94 por cento para BuChE. Outras partes das plantas selecionadas apresentaram boa seletividade em suas ações. As plantas seletivamente ativos contra AChE foram as casca do caule e casca da raiz de Alchornia laxiflora (41,12 por cento), e casca da raiz de Callophyllum inophyllurn (56,52 por cento). As folhas de C. jagus (74,25 por cento), folhas de Morinda lucida (40,15 por cento), folhas e casca do caule de Peltophorum pterocarpum (49,5 por cento e 68,85 por cento, respectivamente), physiostigmine inibiu 90,31 por cento. Em geral, atividades melhoras foram apresentadas contra BuChE. Folhas, casca da raiz e casca do caule Bombax bromoposenze foram particularmente ativos. A inibição foi acima de 80 por cento. Outras partes de algumas espécies também foram seletivas, como as partes aéreas de Antiaris africana, Cissampelos owarensis (78,96 por cento), folhas e casca do caule de Combretum molle (90,42 por cento e 88,13 por cento, respectivamente), casca da raiz e de tubérculos de Dioscorea dumentorum (mais de 87 por cento), folhas de G cola, cascas de raiz de Markhamia tomentosa, casca do caule de Pycnanthus angolensis e folhas de Tetrapleura tetraptera. A maioria destas plantas são utilizadas como alimentos ou ingredientes alimentares na Nigéria e podem ser responsáveis pela baixa incidência da doença de Alzheimer no país e desempenhar determinadas funções na mediação da doença.
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Methanolic extracts of 10 selected Nigerian medicinal plants-Psidium guajava, Alstonia boonei, Cassia alata, Newbouldia laevis, Spondias mombin, Globimetula cupulatum, Chromolaena odorata, Securidaca longepedunculata, Ocimum gratissimum, and Morinda lucida-widely used in ethnomedicine, were assessed for phytochemical constituents and antioxidant and free radical scavenging activities using seven different antioxidant assay methods. Phytochemical screening gave positive tests for steroids, terpenoids, and cardiac glycosides, alkaloids, saponins, tannins, and flavonoids contained in the extracts. P. guajava contained the highest amount of total phenolics (380.08 +/- 4.40 mg/L gallic acid equivalents), and the highest amounts of total flavonoids were found in the leaf extracts of C. alata (275.16 +/- 1.62 microg/mL quercetin equivalents [QE]), C. odorata (272.12 +/- 2.32 microg/mL QE), and P. guajava (269.72 +/- 2.78 microg/mL QE). Percentage 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity was highest in S. mombin (88.58 +/- 3.04%) and P. guajava (82.79 +/- 2.84%) and compared with values obtained for ascorbic acid and gallic acid. All the extracts, generally, had low nitric oxide radical scavenging activities, and G. cupulatum had the highest hydroxyl radical scavenging activity (63.84 +/- 0.97%). The extracts in general demonstrated high lipid peroxidation inhibitory activity, with only M. lucida (38.74 +/- 1.99%) and A. boonei (47.16 +/- 0.59%) being exceptions. The reductive potential was highest in P. guajava (0.79 +/- 0.04) and least in S. longepedunculata (0.26 +/- 0.00). DPPH assay correlated well with total phenolic contents (r(2) = 0.76) and reductive potential (r(2) = 0.81) and fairly with lipid peroxidation inhibitory activity (r(2) = 0.51). There was a good correlation between total phenolic contents and reductive potential (r(2) = 0.79) and a fair correlation between total phenolic contents and lipid peroxidation inhibitory activity (r(2) = 0.55). These results suggest that the methanolic extracts of the studied plant parts possess significant antioxidant and radical scavenging activities that may be due to the phytochemical content of the plants and as such make them potential candidates as natural chemoprophylactic agents. In addition, multiple assay methods should be used in comparing antioxidant capacities of samples to have a reliable result.