Jatonik polyherbal mixture induced rat liver MMPT pore opening in normal Wistar rat: In vitro and in vivo studies / 中草药·英文版

OBJECTIVE@#To assess acute toxicity, the in vitro and in vivo effects of methanol and ethyl acetate extracts (JME and JEE) of Jatonik polyherbal mixture on some mitochondria-related parameters and their effect on the activity of some liver enzymes.@*METHODS@#Acute toxicity of JME and JEE was determined using Lorke's method. In vitro and in vivo opening of the mitochondrial membrane permeability transition pore (MMPT pore) was spectrophotometrically assayed. Production of malondialdehyde (MDA) as an index of lipid peroxidation and the activity of mitochondrial ATPase was evaluated in vitro and in vivo and the effect of JME and JEE on the activity of liver enzymes such as alkaline phosphatase (ALP), aspartate and alanine aminotransferase (AST and ALT) and gamma-glutamyl transferase (GGT) was also investigated.@*RESULTS@#JME had an LD50 of 3 808 mg/kg b.w whereas JEE had an LD50 greater than 5 000 mg/kg b.w. of rats. After the rats have been fed with both extracts, a photomicrograph of a piece of liver tissue showed no apparent symptoms of toxicity. From the in vitro and in vivo studies, both extracts prompted intact mitochondria to open their MMPT pores. When compared to the control, lipid peroxide product release and ATPase activity were significantly increased (P < 0.05) in vitro and in vivo. The activities of AST, ALT, and GGT were all reduced at 50 mg/kg when treated with JME, but the activity of AST was considerably enhanced when treated with JEE (P < 0.05). The results revealed that both JME and JEE of the Jatonik polyherbal mixture had low toxicity, profound MMPTpore induction, and enhanced ATPase activity, but an increased MDA production.@*CONCLUSION@#Jatonik extracts may be a promising target for drug development in diseases where there is dysregulation of apoptosis, however, further studies are needed to better clarify the molecular mechanism involved in these phenomena.

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 .

Phytochemical, Nutrient Composition and Serum Lipid Lowering Effect of Xylopia aethiopica Fruit.

Aims: The present study was carried out to evaluate the effects of Xylopia aethiopica on serum lipids in fed rats. Also the quantitative phytochemical and nutrient composition was investigated. Study Design: Quantitative phytochemical, proximate analysis and in vivo effect on serum lipid profile. Place and Duration of Study: Department of Biochemistry, College of Natural Sciences, Michael Okpara University of Agriculture, Umudike Abia State, between June 2013 and September 2013. Methodology: The fruit were cut into small piece, dried and ground into powder. The quantitative phytochemical and proximate nutrient analyses of the powder sample were determined using standard methods. The serum lipid lowering effects of the powdered fruit in rats was determined by feeding different groups of rats with graded levels (5, 10, 20 and 50%) of the powdered fruit incorporated in their feed for 21 consecutive days and the effects on the total cholesterol, triglyceride, LDL-C, and HDL-C were compared with a negative control. Results: The fruit sample produced significant (p<0.05) concentration-dependent decrease in the total serum cholesterol, triglyceride, LDL-C and VLDL-C levels and increase in serum HDL-C level in fed groups of rats when compared to the control group. The phytochemical analysis showed that the sample contained tannins (4.96%), flavonoids (0.81%), saponins (2.93%) and alkaloids (1.24%). The proximate analysis of the nutrient composition of powdered Xylopia aethiopica sample showed the presence of moisture, lipid, crude fibre, crude protein, ash and nitrogen free extracts in the following proportion 6.32, 12.54, 14.51, 0.91, 2.31 and 63.41% respectively. Conclusion: The fruit sample demonstrated good hypolipidemic effects which may suggest that the consumption of Xylopia aethiopica fruit may help in the reduction of the incidence of hyperlipidemia related diseases in patients.

Effect of Xylopia aethiopica, Fiscus mucuso and Anthocleista vogelli Extracts on Some Biochemical Parameters Following Ethanol-induced Toxicity.

The objective of the study was to comparatively verify the effects of aqueous extracts of three plants on some biochemical parameters following ethanol administration with a view to ascertaining the role of the extracts in ameliorating ethanol toxicity. A total of forty rats were divided into eight groups (n=5). Group A were control rats; Group B were administered with absolute ethanol; Group C were ethanol administered rats treated with Xylopia aethiopica; Groups D were ethanol administered rats treated with Fiscus mucuso, Group E were ethanol administered rats treated with Anthocleista vogelli; Group F were normal rats administered orally with Xylopia aethiopica; Group G were normal rats administered orally with Fiscus mucuso; Group H were normal rats administered orally with Anthocleista vogelli. At the end of the experimental period, the animals were sacrificed and serum was obtained for total protein, uric acid, creatinin, urea, aspartate aminotrasferase (AST) and alanine aminotransferase (ALT) analysis using respective research kits. The result showed that Xylopia aethiopica had protective effect on the kidney as compared with Fiscus mucuso and Anthocleista vogelli treated rats. Also, The AST and ALT was lowered with the beginning of Xylopia aethiopia treatment. The total protein, creatinin and urea were slightly (p>0.05) affected with ethanol, an effect which was normalized with the beginning of extract treatment. It can be concluded that Xylopia aethiopica had a better reno-protective and hepatoprotective effect than Anthocleista vogelli and Fiscus mucuso extract as evident in its ameliorative role on the biochemical profiles.

Xylopioxyde and other bioactive kaurane-diterpenes from Xylopia aethiopica Dunal (Annonaceae).

A new cytotoxic ent-kaurane-type diterpene named xylopioxyde (16,17-epoxy-15-oxo-ent-kauran-19-oic acid) has been isolated from the fruits of Xylopia aethiopica Dunal (Annonaceae) together with three known compounds, namely 15α-acetoxy-ent-kaur-16-en-19 oic acid (xylopic acid), 15-oxo-ent-kaur-16-en-19-oic acid and ent-kaur-16-en-19-oic acid. Xylopic acid, obtained in a good amount, has been successively converted in moderate to good yields into 15-hydroxy-ent-kaur-16-en-19-oic acid, 15-oxo-ent-kaur-16-en-19-oic acid and two new selective trypanocidal stereoisomers of 15-acetoxy-16,17-ent-epoxy-kauran-19-oic acid, respectively. All the compounds except the synthetic epoxides displayed cytotoxic effects on the mammalian fibroblast cell line MRC-5 as well as inhibitory effects on the growth of the bloodstream forms of Trypanosoma brucei brucei cells (strain 241).

Methanolic Extract of Xylopia aethiopica Ameliorates Acetaminophen-Induced Liver Damage in Male Wistar Rats.

Aims: To examine the ameliorative effect of the methanolic extract of Xylopia aethiopica in acetaminophen-induced hepatic damage male Wistar rats. Study Design: Twelve male rats were randomly grouped into four. “A” = Control, “B” = Paracetamol-induced hepatotoxic (PCM-IHT), “C” = 200 mg/kg b.w treated and “D” = 400 mg/kg b.w treated. Place and Duration of Study: Department of Biochemistry, Lagos State University, Ojo Lagos, Nigeria between November 2011 and March 2012. Methodology: “A” received 3.0 ml of distilled water, “B” received 350 mg/kg b.w/day of Paracetamol, “C” after been induced (B) was treated with 200 mg/kg b.w/day and “D” after been induced (B) was treated with 400 mg/kg b.w/day of the plant extract. Two days after the last treatment, the serum was used to assay for alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP) and acid phosphatase (ACP) using Randox commercial enzyme kits. Results: The activities of ALT and AST reduced from 85.83±3.4 U/L and 148.2±9.75 U/L in the induced groups to 39.33±1.67 U/L and 68.84±5.72 U/L when treated with 200mg/kg and 35.67±2.46 U/L and 38.26±3.0 U/L when treated with 400 mg/kg respectively. There was no significant difference when 200 and 400 mg/kg b.w treatments were compared with the control (ALT = 38.0±0.40 U/L and AST = 53.71±2.70 U/L) (P>.05). Similarly, the activities of ALP and ACP reduced from 240.8±3.98 U/L and 152.2±7.91 U/L in the induced groups to 126.0±7.62 U/L and 56.17±1.55 U/L when treated with 200 mg/kg and 188.5±4.71 U/L and 93.55±2.18 U/L when treated with 400mg/kg respectively. The 200 and 400 mg/kg b.w treatments appeared to be significantly different from each other but with former being positively correlated with the control (ALP = 135.8±6.74 U/L and ACP = 61.96±4.12 U/L). Conclusion: The methanolic extract of Xylopia aethiopica possessed hepatoreparative property especially in acetaminophen-induced hepatotoxicity; however, its toxicity needs to be examined.

Antihemolytic Properties of Extracts of Six Plants Used in the Traditional Treatment of Sickle Cell Disease in Benin.

This study is focused on the in vitro evaluation of the hemolysis inhibitory activity of aqueous extracts of six plants used in the traditional treatment of sickle cell disease in Benin: Morinda lucida, Uvaria chamae, Lonchocarpus cyanescens, Croton zambesicus, Raphiostylis beninensis and Xylopia aethiopica. AS and SS red blood cells are subjected to hyposmotic impact with decreasing concentrations of NaCl solution. All the aqueous extracts of the six plants showed a better contribution in erythrocyte osmotic resistance from the concentration of 5 mg/mL to 1 mg/mL, except the extract at 5 mg/mL of Raphiostylis beninensis that caused hemolysis of both red blood cells AS and SS. The extract at 1 mg/mL of Raphiostylis beninensis and the extracts at 5mg/mL of Xylopia aethiopica and Croton zambesicus showed a high hemolysis inhibition of red blood cells AS and SS. The extracts of Lonchocarpus cyanescens showed moderate hemolysis inhibition of SS red blood cells while extracts of Uvaria chamae inhibited highly the hemolysis of AS red blood cells. As for the roots of Morinda lucida, only the extract at 5mg/mL highly inhibited the hemolysis of the AS red blood cells. This protocol seems appropriate to work with both AS and SS blood because the comparative effects of each tested extract on hemolysis of AS and SS blood showed a good correlation coefficient of Pearson (1 or -1). All the plants tested in this work showed, at different doses, an in vitro antisickling effect and this explains partially their use in the traditional treatment of sickle cell disease.

Xylodiol from Xylopia langsdorfiana induces apoptosis in HL60 cells

An atisane diterpene was isolated from Xylopia langsdorfiana St. Hilaire & Tulasne, Annonaceae, leaves, ent-atisane-7α,16α-diol (xylodiol). Preliminary study showed that xylodiol was cytotoxic and induced differentiation on human leukemia cell lines. However, the molecular mechanisms of xylodiol-mediated cytotoxicity have not been fully defined. Thus, we investigated the anti-tumor effect of xylodiol in human leukemia HL60 cell line. Xylodiol induced apoptosis and necrosis. HL60 cells treated with xylodiol showed biochemical changes characteristic of apoptosis, including caspases-8, -9 and -3 activation and loss of mitochondrial transmembrane potential (∆ Ψm). However, there was a condensation rather than swelling of mitochondria. Moreover, the formation of condensed mitochondria and the loss of ∆ Ψm occurred downstream of caspase activation. Cyclosporine A did not protect HL60 cells from the cytotoxic effects of xylodiol, suggesting that the loss of ∆ Ψm is a late event in xylodiol-induced apoptosis. Oxidative stress was involved in xylodiol-induced apoptosis. Thus, we conclude that activated caspases cleave cellular proteins resulting in mitochondrial damage leading to mitochondrial condensation, loss of ∆ Ψm and ROS release from the mitochondria. ROS can further induce and maintain a collapse of ∆ Ψm leading to cellular damage through oxidation of lipids and proteins resulting in apoptotic cell death.

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.

Xymarginatin: a new acetogenin inhibitor of mitochondrial electron transport from Xylopia emarginata Mart., Annonaceae / Xymarginatin: uma nova acetogenina inibidora do transporte mitocondrial eletrônico de Xylopia emarginata Mart., Annonaceae

A new Annonaceous acetogenin, xymarginatin (1), was isolated from the twigs of Xyliopia emarginata Mart. (Annonaceae) by bioactivity-directed fractionation using lethality to brine shrimp. The compound 1 represents a linear C-35 Annonaceous acetogenin, lacking either tetrahydrofuran (THF) or epoxide rings, bearing a keto group at C-10, and possessing two cis-double bonds separated by two methylenes units. The structure of 1 was elucidated by ¹H and 13C-NMR, COSY, HMBC, HMQC and HRMS. The ability to inhibit the mitochondrial respiratory chain of Xymarginatin (1) was tested in a rat liver mitochondrial oxygen uptake assay, with IC50 value of 1720 nM; Rotenone as a positive control gave IC50 34.8 nM. The toxicity of compound 1 against Artemia salina Leach gave LC50 of 127 μg/mL.

Uma nova acetogenina de Anonaceae, xymarginatin (1), foi isolada dos caules de Xyliopia emarginata Mart. (Annonaceae) por fracionamento biodirecionado usando o teste de letalidade em Artemia salina. A substância 1 representa uma acetogenina linear C-35, sema neis tetrahidrofureano ou epóxidos, mas com um grupo cetônico em C-10 e com uma dupla ligação cis separada por duas unidades metilênicas. A estrutura de 1 foi elucidada por ¹H e 13C-RNM, COSY, HMBC, HMQC e HRMS. A habilidade de inibir a cadeia respiratória mitocondrial de 1 foi testada em ensaios de produção de oxigênio mitocondrial em fígado de ratos, com IC50 de 1720 nM; rotenona, controle positivo, apresentou IC50 de 34,8 nM. A toxicidade da substância 1 contra Artemia salina Leach foi de LC50 127 μg/mL.

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.

Cardiovascular effects induced by the hydroalcoholic extract of the stem of Xylopia cayennensis in rats / Efeitos cardiovasculares induzidos pelo extrato hidroalcoólico das cascas de Xylopia cayennensis em ratos

The cardiovascular effects induced by the hydroalcoholic extract of the stem of Xylopia cayennensis (HEXC) were studied in rats using a combined in vivo and in vitro approach. In non-anesthetized rats, HEXC injections produced a significant and dose-dependent hypotension associated with an increase in heart rate. The hypotensive response was not attenuated after nitric oxide (NO) synthase blockade, L-NAME (20 mg/Kg, i.v.). In isolated rat superior aortic rings, HEXC was able to relax the tonus induced by phenylephrine (1 µM) and KCl (80 mM), (EC50 = 85±13 and 62±5 µg/mL, respectively). The smooth muscle-relaxant activity of HEXC was not inhibited by removal of vascular endothelium (EC50 = 58±6 µg/mL). HEXC antagonized CaCl2-induced contractions in depolarizing medium nominally without Ca2+. HEXC inhibited the intracellular calcium-dependent transient contractions induced by caffeine (20 mM) in Ca2+-free solution, but not those induced by norepinephrine (1 µM). In isolated rat atrial preparations, HEXC produced negative inotropic and chronotropic responses (IC50= 534±42 and 259±22 µg/mL, respectively). The results obtained suggest that the hypotensive effect of HEXC is probably due to a peripheral vasodilatation, at least, secondary to an interference with the Ca2+ mobilization as a consequence of voltage-dependent Ca2+ channel blockade and the inhibition of Ca2+ release from caffeine-sensitive intracellular stores. Finally, HEXC acts directly on the heart decreasing contractility and heart rate, these effects are of little importance to the expression of the hypotensive response induced by HEXC.

Os efeitos cardiovasculares induzidos pelo extrato hidroalcoólico do caule de Xylopia cayennensis (EHXC) foram estudados em ratos, utilizando uma abordagem combinada in vivo e in vitro. Em ratos não anestesiados, EHXC induziu uma hipotensão não dependente de dose associada com um aumento da freqüência cardíaca. Esta resposta hipontesora não foi atenuada depois do bloqueio com L-NAME (20 mg/Kg, i.v.). Em anéis de aorta isolados de rato, EHXC foi capaz de relaxar o tônus induzido por fenilefrina (1 µM) e KCl (80 mM), (CE50 = 85±13 e 62±5 µg/mL, respectivamente). A atividade vasorelaxante do HEXC não foi inibida pela remoção do endotélio vascular (CE50 = 58±6 µg/mL). HEXC antagonizou as contrações induzidas por CaCl2 em meio despolarizante nominalmente sem Ca+2. EHXC antagonizou de maneira dependente de concentração as contrações transientes induzidas por cafeína (20 mM), em meio livre de Ca2+, contudo não alterou aquelas induzidas por noradrenalina (1 µM). Em átrio isolado de rato, EHXC induziu um efeito inotrópico e cronotrópico negativo (CI50= 534±42 µg/mL e 259±22 µg/mL; respectivamente). Os resultados obtidos demonstram que EHXC apresenta um potente efeito hipotensor, provavelmente conseqüência da diminuição da resistência periférica total que parece ser, em parte, devido a uma ação inibitória sobre o influxo de Ca+2 através de canais de cálcio dependentes de voltagem e também através da inibição da liberação de Ca+2 dos estoques intracelulares sensíveis à cafeína. HEXC atua diretamente no coração diminuindo a contratilidade e a freqüência cardíaca, estes efeitos têm importância pequena na expressão da resposta hipotensiva induzida por HEXC.

Building of Leaf Shelters by Stenoma scitiorella Walker (Lepidoptera: Elachistidae): Manipulation of Host Plant Quality? / Construção de Abrigos Foliares por Stenoma scitiorella Walker (Lepidoptera: Elachistidae): Manipulação da Qualidade da Planta Hospedeira?

A construção de abrigos foliares é um comportamento comum entre lagartas de microlepidópteros e, ao que parece, tais abrigos proporcionam um refúgio contra as intempéries e o ataque de predadores e parasitóides. Estudos recentes sobre a ecologia nutricional de insetos têm sugerido que tal comportamento seria, na realidade, uma estratégia evolutivamente selecionada para maximizar a qualidade da planta hospedeira que consomem. As lagartas de Stenoma scitiorella Walker unem as folhas jovens de Xylopia aromatica (Lam.) Mart. (Annonaceae) para a construção de um abrigo no qual se refugiam alimentando-se exclusivamente das folhas internas. Por proporcionar as melhores condições para o desenvolvimento larval, a maioria dos abrigos foliares (53,4 por cento) é ocupada por apenas uma lagarta. Os resultados revelaram que, apesar de alterar os teores de água e carboidratos solúveis, a construção dos abrigos foliares não afeta a concentração de taninos nem a preferência das lagartas por folhas externas ou internas. Assim, tal comportamento não representa uma estratégia adaptativa do inseto para superar as defesas químicas da planta hospedeira. Dessa forma, é provável que os abrigos foliares de S. scitiorella sejam construídos para outros fins como, por exemplo, proteção das lagartas contra dessecação ou predação.

Building of leaf shelters is a widespread behavior among microlepidopteran larvae. Apparently, these shelters provide refuge to caterpillars against bad weather and reduce the risks of predation and parasitism. Recent studies about nutritional ecology of insects have suggested that such behavior would actually be an strategy evolutionarily selected to maximize the quality of the host plant consumed by them. Stenoma scitiorella Walker caterpillars tie together young Xylopia aromatica (Lam.) Mart. (Annonaceae) leaves to build a shelter in which they retreat, feeding exclusively on inner leaves. The accumulation of damage and excrement in leaf shelters with several caterpillars may lead to a decline in larval development and survivorship. For providing the best conditions for larval development most leaf shelters (53,4 percent) are occupied by only one caterpillar. Although altering the water and soluble carbohydrates contents, the building of shelters did not affect either the tannins concentrations or the preference of caterpillars for external or internal leaves. Hence, probably this behavior does not denote an adaptative strategy of the insect to overcome the host plant chemical defenses. Thus, it is possible that the leaf shelters of S. scitiorella caterpillars are built for other purposes as, for example, to protect caterpillars from desiccation and predation.