Involvement of the Benzodiazepine Site in the Anticonvulsant Activity of Tapinanthus globiferus against Pentylenetetrazole-induced Seizures in Mice.

Tapinanthus globiferus is often referred to as an all-purpose herb for the treatment of stroke and epilepsy. The present study investigates the anticonvulsant effect of methanolic leaf extract, active fractions, and lupeol (isolate) of Tapinanthus globiferus in mice as well as the underlying mechanisms. Following phytochemical studies of T. globiferus, preliminary assays were performed to evaluate MLE-induced toxic effect and behavioral changes. The pentylenetetrazol (70 mg/kg, i. p.)-induced seizure was evaluated in mice that were pretreated orally with vehicle 10 mL/kg, MLE (4, 20, or 100 mg/kg), fractions (F1 to F6), lupeol 10 mg/kg or diazepam (3 mg/kg). Methanolic leaf extract preserved neuron viability as well as the relative organ weight, and hematological and biochemical parameters. The behavioral endpoints, neuromuscular coordination, and sensory response parameters revealed a dose-dependent effect of methanolic leaf extract. This extract, active fractions, lupeol, and diazepam potentiated the hypno-sedative effect of the barbiturate and attenuated PTZ-induced acute seizure. This antiseizure effect was completely reversed by flumazenil 2 mg/kg (benzodiazepine site antagonist). Altogether, the benzodiazepine site-mediated anticonvulsant effects of methanolic leaf extract, active fractions, and lupeol corroborate traditional application of T. globiferus against epilepsy.

Neuroprotective flavonoids of the leaf of Antiaris africana Englea against cyanide toxicity.

ETHNOPHARMACOLOGICAL RELEVANCE: Different parts of Antiaris africana Englea (Moraceae) are used traditionally for the treatment of various diseases, including epilepsy and other nervous system disorders. AIMS OF THIS STUDY: The current study was designed to evaluate the neuroprotective activity of flavonoids isolated from A. africana against potassium cyanide (KCN)-induced oxidative damage in brain homogenate. MATERIALS AND METHODS: Dried and ground leaves of A. africana were extracted with methanol and fractioned into n-hexane (HFA), dichloromethane (DFA), ethyl acetate (EFA) and methanol (MFA). Each fraction was assessed for neuroprotective potential by anticholinesterase activity test. The fraction with the best anticholinesterase activity was subjected to various chromatographic techniques through bioassay-guided fractionation to isolate the bioactive compounds. The protective ability of the extract, fractions and compounds against Potassium cyanide (KCN)-induced mitochondrial damage in rat brain homogenate was evaluated. Structures of the isolated compounds were determined using 1D and 2D NMR, mass spectrometry and by comparison with literature data. RESULTS AND DISCUSSION: The ethyl acetate fraction showed the best anticholinesterase activity with an IC50 of 23.23 ± 1.12 µg/ml. Quercetin and a biflavonoid glucoside identified as 3'-4'-bisquercetin-3ß-D-diglucoside from this fraction displayed a remarkable antioxidant activity in the DPPH assay and showed significant (P < 0.05) increase in the activity of dehydrogenase inhibited by KCN in a concentration dependent manner. However, quercetin was more effective in reducing the MDA level and acetylcholinesterase activity that were elevated by KCN. CONCLUSION: Quercetin and the bisquercetin-diglucoside isolated from the leaves of A. Africana for the first time, are major contributors to the observed neuroprotective property of the plant which supports its folkloric usage in the management of seizures, epilepsy and other neurological disorders.

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.

Neuropharmacological profile and chemical analysis of fresh rhizome essential oil of Curcuma longa (turmeric) cultivated in Southwest Nigeria.

BACKGROUND: Curcuma longa (turmeric) is commonly used as spice and also used to treat fever, cough and febrile convulsions in Nigeria. This study determined the chemical composition of the essential oil of C. longa and evaluated its neuropharmacological activity in mice. METHODS: Essential oil of C. longa (EOCL) fresh rhizome was obtained by hydrodistillation and its chemical composition determined by GC-MS. Acute toxicity (LD50) profile of the essential oil was determined orally (p.o.) and intraperitoneally (i.p.); and the EOCL (50-200 mg/kg, i.p.) was evaluated for its behavioural, anxiolytic, sedative and anticonvulsant activities using appropriate models in Albino mice (Vom Strain, Jos, Nigeria). RESULTS: Analysis of the oil showed the presence of 23 compounds with turmerone (35.9%) being the major component. The LD50 values obtained for the mice were 2154 mg/kg, p.o., and 693 mg/kg, i.p. The EOCL (50-200 mg/kg, i.p.) caused significant (p < 0.01) inhibition of rearing {F(4,20) = 9} and locomotor {F(3,16) = 42} activity; decreased head dips in hole board {F (4,20) = 4}; increased the time spent in the open arms of the elevated pus maze {F (4,20) = 9}; prolonged total sleeping time {F (4,20) = 21} induced by ketamine injection, and protected mice against pentylenetetrazol-induced convulsions. CONCLUSION: The major component of the essential oil of this C. longa species was turmerone; the oil was slightly toxic orally but moderately toxic intraperitoneally in mice; exhibited significant anxiolytic, sedative and anticonvulsant activities in mice.

New glucose esters from the fresh leaves of Jacaranda mimosaefolia.

From the fresh leaves of Jacaranda mimosaefolia were isolated Phytoquinoids 1-4 established as beta-D-glucopyranose 2-benzeneacetatel,6-bis(1-hydroxy-4-oxo-2,5-cyclohexadiene-1-acetate), for which the name Jacaranoside is proposed; beta-D-glucopyranose 2-(4-hydroxybenzeneacetate) 1,6-bis(1-hydroxy-4-oxo-2,5-cyclohexadiene-1-acetate), for which the name Jacarandol is proposed; beta-D-glucopyranose 2-benzeneacetate 1-(1-hydroxy-4-oxo-2,5-cyclohexadiene-1-acetate) and beta-D-glucopyranose 1,6-bis (1-hydroxy-4-oxo-2,5-cyclohexadiene-1-acetate) respectively.

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.