Ursane-Type Triterpenes, Phenolics and Phenolic Derivatives from Globimetula braunii Leaf.

Globimetula braunii is a hemi-parasitic plant used in African ethnomedicine for the management of microbial infections, rheumatic pain and tumors amongst others. We report the isolation and characterization of eight compounds with their antioxidant and antimicrobial activities. The air-dried powdered leaf was macerated in EtOH/H20 (4:1). The extract was solvent-partitioned into n-hexane, EtOAc, n-BuOH and aqueous fractions. The fractions were screened for their antioxidant properties, using DPPH, FRAP, TAC and FIC assays. Antimicrobial analysis was performed using the micro-broth dilution method. The active EtOAc fraction was purified for its putative compounds on a repeated silica gel column chromatography monitored with TLC-bioautography. The isolated compounds were characterized using spectroscopic methods of UV, FT-IR, NMR and MS. Eight compounds (1-8) were isolated and characterized as 13,27-cycloursane (1), phyllanthone (2), globraunone (3), three phenolics: methyl 3,5-dihydroxy-4-methoxybenzoate (4), methyl 3-methyl-4-hydroxybenzoate (5) and guaiacol (6), as well as two phenol derivatives: 4-formaldehyde phenone (7) and 6-methoxy-2H-inden-5-ol (8). The study identified 4 and 6 as natural antioxidant compounds with potential as antimicrobial agents.

Iron deficiency, still a rarity in children with sickle cell anemia in Ile-Ife, Nigeria

ABSTRACT In this study, children with sickle cell anemia were evaluated for iron deficiency. Serum ferritin and free erythrocyte protoporphyrin free erythrocyte protoporphyrin (FEP) levels, mean corpuscular volume mean corpuscular volume (MCV) and mean corpuscular hemoglobin mean corpuscular hemoglobin (MCH) were used in determining their iron status. The study was done at Pediatric Hematology Outpatient Clinic of the Obafemi Awolowo University Teaching Hospitals' Complex, Ile-Ife. Forty-eight HbSS subjects in steady state and 48 apparently well age and sex matched HbAA controls were evaluated. Serum ferritin less than 25 ng/dL FEP greater than cut off for age, mean corpuscular volume MCV and mean corpuscular hemoglobin MCH less than cut off for age were regarded as indicating iron deficiency. Serum ferritin values ranged from 34.2 to 3282.9 µg/L, with a mean of 381.2 (1.0), median 180 µg/L; which was significantly higher than the controls (p = 0.000). FEP was lower in the subjects but none was iron deficient compared with the controls. The mean corpuscular hemoglobin MCH of subjects was significantly lower than the controls. Subjects had lower mean corpuscular volume MCV compared with controls. Iron deficiency was not detected in any of the subjects with sickle cell anemia in comparison to a prevalence of 43.75% in the controls. Iron deficiency anemia (IDA) was found in 16.7% of the controls, using the WHO cut off for anemia which is hemoglobin concentration of <11 g/dl. While a high prevalence of iron deficiency was noted in the control group, patients with sickle cell anemia were largely iron sufficient, despite their anemia. Iron supplementation remains unnecessary as part of routine management of children with sickle cell anemia in our practice.

Iron deficiency, still a rarity in children with sickle cell anemia in Ile-Ife, Nigeria.

In this study, children with sickle cell anemia were evaluated for iron deficiency. Serum ferritin and free erythrocyte protoporphyrin free erythrocyte protoporphyrin (FEP) levels, mean corpuscular volume mean corpuscular volume (MCV) and mean corpuscular hemoglobin mean corpuscular hemoglobin (MCH) were used in determining their iron status. The study was done at Pediatric Hematology Outpatient Clinic of the Obafemi Awolowo University Teaching Hospitals' Complex, Ile-Ife. Forty-eight HbSS subjects in steady state and 48 apparently well age and sex matched HbAA controls were evaluated. Serum ferritin less than 25ng/dL FEP greater than cut off for age, mean corpuscular volume MCV and mean corpuscular hemoglobin MCH less than cut off for age were regarded as indicating iron deficiency. Serum ferritin values ranged from 34.2 to 3282.9µg/L, with a mean of 381.2 (1.0), median 180µg/L; which was significantly higher than the controls (p=0.000). FEP was lower in the subjects but none was iron deficient compared with the controls. The mean corpuscular hemoglobin MCH of subjects was significantly lower than the controls. Subjects had lower mean corpuscular volume MCV compared with controls. Iron deficiency was not detected in any of the subjects with sickle cell anemia in comparison to a prevalence of 43.75% in the controls. Iron deficiency anemia (IDA) was found in 16.7% of the controls, using the WHO cut off for anemia which is hemoglobin concentration of <11g/dl. While a high prevalence of iron deficiency was noted in the control group, patients with sickle cell anemia were largely iron sufficient, despite their anemia. Iron supplementation remains unnecessary as part of routine management of children with sickle cell anemia in our practice.

Memory enhancing, anticholinesterase and antimicrobial activities of ß-phenylnitroethane and essential oil of Dennettia tripetala Baker f.

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.

Anticholinesterase constituents from the leaves of Spondias mombin L. (Anacardiaceae).

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.

Studies of the antitrypanosomal and toxicological properties of Anogeissus leiocarpus (Dc.) Guill. & Perr. (Combretaceae) and Vitellaria paradoxa C. F. Gaertn (Sapotaceae) in mice / Estudios de las propiedades antitripanosómicas y toxicológicas de Anogeissus leiocarpus (Dc). Guill. & Perr. (Combretaceae) y Vitellaria paradoxa C. F. Gaertn (Sapotaceae) en ratones

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.

Anti-hepatotoxic activities of Hibiscus sabdariffa L. in animal model of streptozotocin diabetes-induced liver damage.

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.

Evaluation of antioxidant potential of methanolic leaf extract of Anacardium Occidentale (Linn) on the testes of streptozotocin-induced diabetic wistar rats

Anacardium occidentale is a plant with reported anti-diabetic and antioxidant properties. The objective of this work was to determine the effects of Anacardium occidentale leaf extract (AOLE) on the activities of glucose-6-phosphate dehydrogenase (G-6-PDH), thiobarbituric acid reactive substances (TBARS) and anti-oxidant enzymes (Glutathione peroxidase, GPx and superoxide dismutase, SOD) in the testicular homogenate of streptozotocin-induced diabetic rats. Forty (40) wistar rats (Rattus norvegicus) were randomly divided into four experimental groups. Diabetes was induced by a single intraperitoneal injection of Streptozotocin (70 mg/kg b.w.). Five days after the confirmation of hyperglycemia, Groups A and B were treated with 300 mg/kg b.w of the extract and 1 I.U/kg b.w. insulin respectively. Groups C and D served as hyperglycemic and normal controls respectively. Animals were sacrificed 16 days after treatment. Our study showed that AOLE ameliorated the level of TBARS and improved the activities of G-6-PDH, SOD and GPx in the testes of extract-treated rats (AU)

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Ramipril-like activity of Spondias mombin linn against no-flow ischemia and isoproterenol-induced cardiotoxicity in rat heart.

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.

Acetylcholinesterase and butyrylcholinesterase inhibitory activity of some selected Nigerian medicinal plants / Atividade inibitória da acetilcolinesterase e butirilcolinesterase de algumas plantas medicinais da Nigéria

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.

Evaluation of antioxidant and free radical scavenging capacities of some Nigerian indigenous medicinal plants.

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.

Anti hyperglycemic activities of Annona muricata (Linn).

This study was designed to determine the effects of methanolic extracts of Annona muricata (Linn) on the blood glucose level of streptozotocin-induced diabetic Wistar rats. Thirty adult Wistar rats were randomly assigned into three groups (A, B and C) of ten rats each. Group A was the control, Group B was untreated hyperglycemic group and group C was A. muricata-treated group. Hyperglycemia was induced in groups B and C by a single intraperitoneal injection of 80 mg/kg streptozotocin dissolved in 0.1 M citrate buffer. The control group was intraperitoneally injected with equivalent volume of citrate buffer and all the animals were monitored for four weeks. Daily intra peritoneal injection of 100 mg/kg A. muricata was administered to group C rats for two weeks and the animals were monitored for another two weeks. The data obtained were analyzed with descriptive and inferential statistics. The result showed a mean body weight of 206 +/- 7.74 g, 173.29+/-5.13 g and 197 +/- 5.62 g respectively for the control, untreated diabetic and A. muricata-treated diabetic group, and a mean blood glucose concentration of 3.78 +/- 0.190 mmol/L, 21.64 +/- 2.229 mmol/L and 4.22 +/- 0.151 mmol/L for the control, untreated diabetic and treated diabetic groups respectively. A significant difference exists between the blood glucose concentrations of treated and untreated hyperglycemic groups of rats. The result of this study demonstrated that A. muricata possesses anti-hyperglycemic activities.