Phytochemical and anticonvulsant screening of three medicinal plants used in the treatment of epilepsy in the south-western part of Nigeria

The burden of epilepsy in developing countries made medicinal plants like Xylopia aethiopica fruit; Khaya grandifoliola, Alstonia boonei etc an alternative source in epilepsy management in the south-western part of Nigeria. The aim of the study was to provide pharmacological rationale for the ethnomedicinal use of the plants in epilepsy management. The oral medial lethal dose of methanol stem bark extracts of Alstonia boonei (MEAB) and Khaya grandifoliola (MEKG) and methanol fruit extract of Xylopia aethiopica (MEXAF) were done in accordance with the Organization for Economic Cooperation Development guideline. Quantitative and qualitative phytochemical profiling of the extracts was done. Anticonvulsant screening was carried out on the extracts (doses: 75, 150 and 300 mg/kg) using the pentylenetetrazole (PTZ)-induced seizure and maximum electroshock tests (MEST). Results showed that the MEXAF has the highest amount of phytochemicals except for saponins in MEKG; and MEAB with the least amount (but higher alkaloid) than MEKG. The TLC showed different bands of spots of the extracts. In the PTZ test, MEXAF showed 100 % protection against mortality at 300 mg/kg; MEAB with 66.67 % protection at 75 mg/kg and MEKG 0 % protection. MEAB, MEKG and MEXAF nonsignificantly increased the onset of seizure and latency to death. In the MEST, MEXAF, MEKG and MEAB at 75 mg/kg protected 50, 33.3 and 16.67% of the animals against tonic hind limb extension respectively and nonsignificantly (p˃0.05) decreased the recovery time at a dose of 75 mg/kg. It was concluded that the extracts possess anticonvulsant activities hence, the pharmacological credence for the ethnomedicinal use of these plants in treating epilepsy.

Nanoemulsion containing essential oil from Xylopia ochrantha Mart. produces molluscicidal effects against different species of Biomphalaria (Schistosoma hosts)

BACKGROUND This work describes a chemical study of the essential oil from leaves of Xylopia ochrantha, an endemic Annonaceae species from Brazil, and its activity against Biomphalaria species. Considering its poor solubility in aqueous medium, the essential oil was nanoemulsified to evaluate its action on controlling some mollusc species of genus Biomphalaria, snail hosts of Schistosoma mansoni that causes schistosomiasis, which mainly affects tropical and subtropical countries. OBJECTIVES The main aims of this work were to analyse the chemical composition of essential oil from X. ochrantha, and to evaluate the effect of its nanoemulsion on molluscs of genus Biomphalaria and their oviposition. METHODS Chemical analysis was performed by gas chromatography coupled to mass spectrometry. Nanoemulsions were prepared by a low energy method and characterised by particle size and polydispersity index. Biological assays evaluating the mortality of adult species of B. glabrata, B. straminea and B. tenagophila and their ovipositions upon contact with the most stable nanoemulsion during 24 and 48 h were performed. FINDINGS Chemical analysis by mass spectrometry revealed the majority presence of bicyclogermacrene and germacrene D in the essential oil. The formulation with a hydrophilic-lipophilic balance (HLB) of 9.26 was the most suitable for the oil delivery system. This nanoemulsion caused the mortality in B. tenagophila, B. straminea and B. glabarata of different sizes at levels ranging from 50 to 100% in 48 h. Additionally, the formulation could inhibit the development of deposited eggs. CONCLUSION Thus, these results suggest the use of nanoemulsified essential oil from X. ochrantha as a possible alternative in controlling some Biomphalaria species involved in the schistosomiasis cycle.

Ultrastructural and immunohistochemical effects of aqueous leave extract of Xylopia aethiopica on the stomach in streptozotocin-induced diabetic rats / Efectos ultraestructurales e inmunohistoquímicos del extracto acuoso de la hoja Xylopia aethiopica en el estómago de ratas diabéticas inducidas por estreptozotocina

Gastrointestinal pathology in diabetic patients has become a source of concern in recent times. The aim of this study was to investigate the ultrastructural and immunohistochemical effects of aqueous leaf extract of Xylopia aethiopica on the stomach in streptozotocin-induced diabetic rats. This study was conducted using thirty adult Wistar rats. The animals were divided into three groups (n= 10). Group A was the control animals (administered with equivalent volume of citrate buffer), group B was diabetic animals induced by a single intraperitoneal injection of streptozotocin dissolved in citrate buffer (65 mg/kg) and group C was diabetic animals treated with 200 mg/kg body weight of aqueous leave extract of X. aethiopica for twenty five days. At the expiration of the study, all the animals in each of the groups were sacrificed and the stomach excised and fixed in both 10 % formol and karnovsky fixatives immunohistochemical, light microscopic and electron microscopic studies respectively. The results showed a gradual decline (P<0.05) in the blood glucose level in the extract treated group as against the increment in untreated diabetic group. There was a distortion of the glandular mucosa and epithelium in the untreated diabetic group vis-à-vis the extract treated and control groups. The immunohistochemical staining and percentage immunoreactivity of the stomach of untreated diabetic group showed that the immunoexpression of H+/K+-ATPase were sparse and significantly (p<0.000) lower compared with the control group. There was a better staining pattern for H+/K+-ATPase gastric proton pump in the group treated with aqueous leaf extract of X. aethiopica as compared with the untreated diabetic group. The ultrastructural studies of untreated diabetic group revealed a reduction in the density of mitochondria as compared with the control group. Treatment with leaf extract of X. aethiopica increased the mitochondrial density as well as uniform dispersal of chromatin. It is concluded that diabetes causes gastric pathology thus resulting in morphological changes in the gastric histo-architecture and parietal cells. The aqueous leaf extract of X. aethiopica enhances the recovery/restoration of these defects in streptozotocin induced diabetic rats and as such, may play a significant role in the management of complications associated with diabetes mellitus.

La enfermedad gastrointestinal en pacientes diabéticos se ha convertido en una fuente de preocupación en los últimos tiempos. El objetivo fue investigar los efectos ultraestructurales e inmunohistoquímicos de extracto acuoso de la hoja de Xylopia aethiopica en el estómago de ratas con diabetes inducida por estreptozotocina. Se utilizaron 30 ratas Wistar adultas, divididas en tres grupos (n= 10). El Grupo A, control (se le administró un volumen equivalente de tampón de citrato); el Grupo B, animales diabéticos inducidos por una sola inyección intraperitoneal de estreptozotocina disuelta en tampón de citrato (65 mg/kg) y el Grupo C, animales diabéticos con 200 mg/kg peso corporal tratados con extracto acuoso de X. aethiopica durante 25 d. Luego, todos los animales fueron sacrificados, se les extirpó el estómago y fijó en formol al 10 % y en fijador Karnovsky para anticuerpos monoclonales contra la bomba de protones gátrica H+/K+-ATPasa; las muestras se observaron mediante microscopías óptica y electrónica. Los resultados mostraron una disminución gradual (P<0,05) en el nivel de glucosa en sangre del grupo tratado con el extracto, contra un incremento en el grupo diabético no tratado. Hubo una distorsión de la mucosa glandular y el epitelio en el grupo diabético no tratado vis-à-vis los grupos tratados con extracto y el de control. La tinción inmunohistoquímica del estómago del grupo diabético no tratado, mostró escasas células parietales inmunorreactivas en el grupo diabético no tratado comparado con el grupo control. Hubo un mejor patrón de tinción en la bomba de protones gátrica H+/K+-ATPasa en el grupo tratado con el extracto de hoja acuosa de X. aethiopica, en comparación con el grupo diabético no tratado. Los estudios ultraestructurales del grupo diabético no tratado revelaron una reducción en la densidad de las mitocondrias en comparación con el grupo control. El tratamiento con extracto de hoja de X. aethiopica aumentó la densidad mitocondrial, así como la dispersión uniforme de la cromatina. Se concluye que la diabetes causa una enfermedad gástrica que genera cambios morfológicos en la histoarquitectura de las células parietales gástricas. El extracto de hoja acuosa de X. aethiopica mejora la recuperación/restauración de estos defectos en ratas diabéticas inducidas por estreptozotocina y, como tal, puede jugar un rol significativo en el tratamiento de las complicaciones asociadas con la diabetes mellitus.

Plantas do Gênero Xylopia: Composição Química e Potencial Farmacológico / Plants of the Xylopia Genus: Chemical Composition and Pharmacological Potential

RESUMO A família Annonaceae possui representantes de grande interesse medicinal e o gênero Xylopia é um dos que merecem destaque. Composta por aproximadamente 160 espécies distribuídas na América do Sul, América central, África e Ásia, as espécies desse gênero podem ser arbustivas ou arbóreas. No Brasil são encontradas nas regiões Norte, Nordeste, Centro-Oeste e Centro Sul. Este gênero produz uma variedade de metabólitos incluindo alcalóides, amidas, lignóides, acetogeninas e terpenóides e têm sido investigados como fonte potencial de acetogeninas, compostos esses que apresentam uma ampla variedade de propriedades biológicas com destaque para: citotóxica, antitumoral, antiparasitária, antimicrobial, inseticida e antimalarial. Neste estudo, efetuou-se uma revisão das principais espécies de Xylopiaencontradas no Brasil, já estudadas e descritas na literatura, abordando os aspectos químico-farmacológicos, destacando os constituintes químicos isolados bem como a ação farmacológica evidenciada.

ABSTRACT The family Annonaceae has representatives of great medical interest, and the Xylopia species deserves attention. The Xylopia genus is composed by approximately 160 species, with geographic distribution in tropical and subtropical regions of America, Africa and Asia. This genus can present shrubs or trees. In Brazil, they can be found at the North, North-west, Central-West and Central-South Regions. The phytochemical investigations resulted mainly in the isolation of alkaloids, diterpenos, quinolines and acetogenins, with the latter presenting very interesting biological properties such as the cytotoxic, antiprotozoal and the insecticide activities.This study aimed to review the botanical, chemical and pharmacological aspects of the Xylopia genus found in Brazil, highlighting the chemical components, as the well-known pharmacological effect .

Effects of environmental conditions associated to the cardinal orientation on the reproductive phenology of the cerrado savanna tree Xylopia aromatica (Annonaceae)

The Brazilian cerrado has undergone an intense process of fragmentation, which leads to an increase in the number of remnants exposed to edge effects and associated changes on environmental conditions that may affect the phenology of plants. This study aimed to verify whether the reproductive phenology of Xylopia aromatica (Lam.) Mart. (Annonaceae) differs under different light conditions in a cerrado sensu stricto (a woody savanna) of southeastern Brazil. We compared the reproductive phenology of X. aromatica trees distributed on east and south cardinal faces of the cerrado during monthly observations, from January 2005 to December 2008. The east face had a higher light incidence, higher temperatures and canopy openness in relation to south face. X. aromatica showed seasonal reproduction at both faces of the cerrado, but the percentage of individuals, the synchrony and duration of phenophases were higher at the east face. The study demonstrated the influence of the environmental conditions associated to the cardinal orientation of the cerrado faces on the phenological pattern of X. aromatica. Similar responses may be observed for other species, ultimately affecting patterns of floral visitation and fruit production, which reinforces the importance of considering the cardinal direction in studies of edge effects and fragmentation.

O cerrado brasileiro vem sofrendo um processo intenso de fragmentação, que levou ao aumento de remanescentes sujeitos aos efeitos de borda e a alterações nas condições ambientais que podem afetar a fenologia das plantas. O objetivo deste trabalho foi verificar se a fenologia reprodutiva de Xylopia aromatica (Lam.) Mart. (Annonaceae) difere sob diferentes condições de luz em um cerrado sensu stricto no sudeste do Brasil. Comparamos a fenologia reprodutiva de árvores de X. aromatica distribuídas nas faces leste e sul do cerrado, observadas mensalmente de janeiro de 2005 a dezembro de 2008. A face leste apresentou maior incidência de luz, temperaturas e aberturas do dossel em relação à face sul. X. aromatica apresentou reprodução sazonal em ambas as faces do cerrado, mas a porcentagem de indivíduos, sincronia e duração das fenofases foram maiores na face leste. O estudo demonstrou a influência das condições ambientais associadas à orientação cardeal das faces do cerrado no padrão fenológico de X. aromatica. Respostas similares poderão ser observadas em outras espécies de cerrado, afetando os padrões de visitação floral e produção de frutos, o que reforça a importância de considerarmos a orientação cardeal nos estudos de efeitos de borda e fragmentação.

Spatial patterns of a tropical tree species growing under an eucalyptus plantation in South-East Brazil / Padrões espaciais de uma espécie arbórea tropical crescendo sob o dossel de um plantio de eucalipto no Sudeste brasileiro

The objectives of this study were to evaluate the influence of propagules source and the implication of tree size class on the spatial pattern of Xylopia brasiliensis Spreng. individuals growing under the canopy of an experimental plantation of eucalyptus. To this end, all individuals of Xylopia brasiliensis with diameter at soil height (dsh) > 1 cm were mapped in the understory of a 3.16 ha Eucalyptus spp. and Corymbia spp. plantation, located in the municipality of Lavras, SE Brazil. The largest nearby mature tree of X. brasiliensis was considered as the propagules source. Linear regressions were used to assess the influence of the distance of propagules source on the population parameters (density, basal area and height). The spatial pattern of trees was assessed through the Ripley K function. The overall pattern showed that the propagules source distance had strong influence over spatial distribution of trees, mainly the small ones, indicating that the closer the distance from the propagules source, the higher the tree density and the lower the mean tree height. The population showed different spatial distribution patterns according to the spatial scale and diameter class considered. While small trees tended to be aggregated up to around 80 m, the largest individuals were randomly distributed in the area. A plausible explanation for observed patterns might be limited seed rain and intra-population competition.

Os objetivos deste estudo foram avaliar a influência da fonte de propágulo e a implicação de diferentes classes de tamanho sobre o padrão de distribuição espacial de indivíduos de Xylopia brasiliensis Spreng. crescendo sob o dossel de um plantio experimental de eucalipto. Para isso, todos os indivíduos de X. brasiliensis com diâmetro à altura do solo (das) > 1 cm foram mapeados em uma área de 3,16 ha no sub-bosque de um plantio de Eucalyptus ssp. e Corymbia spp., localizado no município de Lavras, MG. O maior e mais próximo indivíduo reprodutivo de X. brasiliensis foi considerado como fonte de propágulos. Foram utilizadas regressões lineares para avaliar a influência da fonte de propágulos sobre parâmetro populacionais (densidade, área basal e altura). O padrão de distribuição espacial das árvores foi avaliado por meio da função K de Ripley. O padrão geral demonstrou que a distância da fonte de propágulo teve forte influência sobre a distribuição espacial das árvores, principalmente as menores, indicando que quanto mais próximo à fonte de propágulos, maior a densidade e menor a altura das árvores. A população demonstrou diferentes distribuições espaciais de acordo com a escala analisada. Enquanto árvores menores tenderam a estar agregadas até uma escala de 80 m, os maiores indivíduos estavam aleatoriamente distribuídos na área. Uma explicação plausível para os padrões observados poderia ser a limitação espacial da chuva de sementes e a competição intraespecífica.

Leaf development in Xylopia aromatica (Lam) Mart. (Annonaceae): implications for palatability to Stenoma scitiorella Walker 1864 (Lepidoptera: Elachistidae) / Crescimento foliar em Xylopia aromatica (Lam) Mart. (Annonaceae): implicações sobre a palatabilidade para lagartas de Stenoma scitiorella Walker 1864 (Lepidoptera: Elachistidae)

Variations in specific foliar mass and water content, nitrogen, soluble carbohydrates and tannins were studied during the growth and maturation processes of the Xylopia aromatica leaves, to determine the effects of such alterations on the herbivory of Stenoma scitiorella caterpillars. This work was carried out in the physiognomy of the typical cerrado of the Parque Estadual de Vassununga, Gleba Pé-de Gigante, Santa Rita do Passa Quatro, São Paulo State, Brazil. While nutritional quality (water and nitrogen) decreases during expansion and maturation of Xylopia aromatica leaves, the chemical (tannins) and physical (sclerophylly) defenses are raised. In agreement with the observations on herbivory, the results support the hypothesis that the reduction in palatability and increase in chemical defenses of Xylopia aromatica leaves account for the caterpillars' preference for young expanding leaves.

Com o objetivo de avaliar os efeitos do crescimento e do amadurecimento de folhas de Xylopia aromatica sob o ataque de lagartas de Stenoma scitiorella, foram estudados a variação da área, massa foliar específica, bem como os teores de água, nitrogênio, hidratos de carbono e taninos durante estes processos. O trabalho foi desenvolvido numa fisionomia de cerrado stricto sensu na Gleba Pé-de-Gigante do Parque Estadual de Vassununga, localizado no município de Santa Rita do Passa Quatro, Estado de São Paulo, Brasil. A expansão e o amadurecimento das folhas de Xylopia aromatica resultaram na redução da qualidade nutricional e no aumento de defesas químicas e físicas. Concordando com as observações realizadas sobre a herbivoria, os resultados permitem supor que a redução na palatabilidade das folhas pode explicar a preferência das lagartas por folhas jovens ainda no início do processo de expansão.