Anti-Tumor and Anti-Inflammatory Activity In Vivo of Apodanthera congestiflora Cogn. (Cucurbitaceae).

This work aimed to carry out a study of Apodanthera congestiflora by investigating its chemical composition and pharmacological potential. From the dichloromethane phase (Dic-Ac) of the A. congestiflora stems, three compounds were identified: cayaponoside C5b (Ac-1), cabenoside C (Ac-2) and fevicordin C2 glucoside (Ac-3), being last identified for the first time as a natural product. These compounds were obtained by chromatographic methods and their structures were elucidated by means of spectroscopic analysis of IR, MS and NMR. In the quantification of Dic-Ac, it was possible to observe the presence of 7% of cayaponoside C5b. Dic-Ac showed significant toxicity for in vivo tests, with macroscopic and biochemical changes. The anti-inflammatory activity of Dic-Ac was investigated using the paw edema model. A decrease in inflammatory signs was observed in the first 5 h and the most effective dose in reducing edema with was 7.5 mg kg-1 (66.6%). Anti-tumor activity of Dic-Ac was evaluated by Ehrlich's carcinoma model, which showed inhibition rate of 78.46% at 15 mg kg-1 dosage. The phytochemical investigation, together with the biological tests carried out in this study, demonstrated that A. congestiflora is a promising species in the search for therapeutics, since it contains substances with high pharmacological potential in its composition.

Purified anacardic acids exert multiple neuroprotective effects in pesticide model of Parkinson's disease: in vivo and in silico analysis.

Parkinson's disease (PD) induced by environmental toxins involves a multifactorial cascade of harmful factors, thus motivating the search for therapeutic agents able to act on the greatest number of molecular targets. This study evaluated the efficacy of 50 mg/kg purified anacardic acids (AAs), isolated from cashew nut shell liquid, on multiple steps of oxidative stress and inflammation induced by rotenone in the substantia nigra (SN) and striatum. Adult mice were divided into four groups: Control, rotenone, AAs + rotenone, and AAs alone. Lipoperoxidation, nitric oxide (NO) levels, and reduced glutathione (GSH)/oxidized gluthatione (GSSG) ratio were evaluated. NF-kB-p65, pro-IL-1ß, cleaved IL-1ß, metalloproteinase-9, Tissue Inhibitory Factor-1 (TIMP-1), tyrosine hydroxylase (TH), and glial fibrillary acidic protein (GFAP) levels were assessed by Western blot. In silico studies were also made using the SwissADME web tool. Rotenone increased lipoperoxidation and NO production and reduced TH levels and GSH/GSSG ratio in both SN and striatum. It also enhanced NF-kB-p65, pro, and cleaved IL-1ß, MMP-9, GFAP levels compared to control and AAs groups. The AAs alone reduced pro-IL-1ß in the striatum while they augmented TIMP1 and reduced MMP-9 amounts in both regions. AAs reversed rotenone-induced effects on lipoperoxidation, NO production, and GSH/GSSG ratio, as well as increased TH and attenuated pro-IL-1ß and MMP-9 levels in both regions, NF-kB-p65 in the SN and GFAP in the striatum. Altogether, the in vivo and in silico analysis reinforced multiple and defined molecular targets of AAs, identifying that they are promising neuroprotective drug candidates for PD, acting against oxidative and inflammatory conditions induced by rotenone.

Evaluation of cytotoxicity and wound healing activity of Avicennia schaueriana in cream.

Avicennia schaueriana is found in Brazilian mangrove coast. The cytotoxicity in vitro of the Aqueous Extract of Leaves of Avicennia schaueriana (AELAs) and the healing activity of the plant in cream on mice skin wounds were evaluated in this study. The cytotoxic evaluation was performed on Vero cells. The healing activity was evaluated on mice treated during 5, 10 and 15 days with cream at 5%, solution of sodium chloride at 0.9% and dexpanthenol in cream at 5%. The extract did not show cytotoxicity, but showed mitogenic activity (100µg/ml). In morphometric analysis, the percentage of wound contraction after 10 days was higher in dexpanthenol group (93.41%). In 15 days, the lowest percentage of contraction was observed in the dexpanthenol group (94.41%) and the highest in the AELAs cream group (98.50%). In histomorphometry the dexpanthenol showed the lowest length of re-epithelialization in 10 days. In 15 days, the AELAs cream group showed 100% of re-epithelialization. The number of fibroblasts found in AELAs cream group was higher than the saline solution in 10 days. In 15 days, AELAs cream group maintained a higher amount of fibroblasts when compared to the others. A. schaueriana did not show cytotoxicity. Furthermore, topical application of AELAs cream decreased the wound area, stimulated the re-epithelialization and increased the number of fibroblasts. The species A. schaueriana could become a topical treatment in tissue repair process.

Phytochemical Screening and Acute Toxicity of Aqueous Extract of Leaves of Conocarpus erectus Linnaeus in Swiss Albino Mice.

Mangroves represent areas of high biological productivity and it is a region rich in bioactive substances used in medicine production. Conocarpus erectus (Combretaceae) known as button mangrove is one of the species found in mangroves and it is used in folk medicine in the treatment of anemia, catarrh, conjunctivitis, diabetes, diarrhea, fever, gonorrhea, headache, hemorrhage, orchitis, rash, bumps and syphilis. The present study aimed to investigate the acute toxicity of aqueous extract of leaves of C. erectus in Swiss albino mice. The plant material was collected in Vila Velha mangroves, located in Itamaracá (PE). The material was subjected to a phytochemical screening where extractive protocols to identify majority molecules present in leaves were used. The evaluation of acute toxicity of aqueous extract of C. erectus followed the model of Acute Toxicity Class based on OECD 423 Guideline, 2001. The majority molecules were identified: flavonoids, tannins and saponins. The LD50 was estimated at 2,000 mg/kg bw. Therefore, the aqueous extract showed low acute toxicity classified in category 5.

A Comparative Study of the effects of Vitamins C and E in the Development of Sarcoma 180 in Mice.

In this work we have investigated the effects of vitamins C and E on tumors via the mice xenotransplant model of sarcoma 180 (S180) in vivo. The experimental results suggest that dosages of 100 mg/kg vitamin C and 400 mg/kg vitamin E yields a great inhibitory behavior on tumors.

Antineoplasic effect of aqueous extract of plectranthus amboinicus in ehrlich ascites carcinoma.

There are 46,000 new cases of peritoneal carcinomatosis per year in the USA and 17,700 in Brazil. New media, including plant derivatives, are being tested in its treatment. Plectranthus amboinicus is a medicinal plant widely used in Brazil, especially in the northeast region, for the treatment of various diseases, including cancer. This present study evaluates the intraperitoneal use of aqueous extracts of Plectranthus amboinicus (AEPa) at a dose of 200 mg / kg for the treatment of the ascitic form of Ehrlich carcinoma. It is concluded also the AEPa produced antineoplastic effect in ascitic form of Ehrlich carcinoma.

Pharmacological screening and acute toxicity of bark roots of Guettarda platypoda

Due to its folk use, scientific reports and phytochemical screening, the purpose of this work was to study the phytochemical and the biological properties of the methanol extract and to evaluate the anti-inflammatory activity as well as determine the acute toxicity, antitumor and cytotoxic activity of the root barks of Guettarda platypoda DC., Rubiaceae. In this analysis the presence of flavonoids and therpenoids were identified. These data and the ones in the literature indicated it as a potential antioxidant and motivated the cytotoxic analysis related with three tumoral cell strains as well as to evaluate its antitumoral activity (sarcoma 180 and Ehrlich carcinoma) in female mice. Due to the presence of esteroids and the previous study of the ethanolic extract, its anti-inflammatory activity and toxicity were also evaluated. Absence or low toxicity in 2000 mg/kg doses was verified and the attention to their phytochemical and pharmacological properties is constantly increasing.

Avaliação dos parâmetros hematológicos e bioquímicos de ratas no segundo terço da gestação submetidas à ação do extrato metanólico de Cereus jamacaru DC., Cactaceae / Evaluation hematological and biochemical parameters of rats in the second thirds of the gestation submitted to the action of the extract methanol of Cereus jamacaru DC., Cactaceae

Os efeitos da administração oral do extrato metanólico (EM) de Cereus jamacaru DC., Cactaceae, foram investigados sobre os parâmetros hematológicos e bioquímicos em ratas Wistar adultas grávidas. Vinte ratas (n = 5 por grupo) foram tratadas durante quatro dias consecutivos com EM por via oral nas doses de 100, 250 e 500 mg/kg de peso e, em seguida, determinados os perfis bioquímico e hematológico. Os resultados mostraram que durante o período do tratamento não foi observado efeitos nocivos ou óbitos. Os parâmetros hematológicos e bioquímicos não foram modificados pela administração oral do EM, excetuando-se o aumento significativo de 45,7 por cento e de 41,9 por cento para alanina transferase (ALT) nas doses de 250 e 500 mg/kg além do aumento significativo, respectivo de 48,2 por cento, 39,8 por cento e 41,8 por cento para aspartato aminotransferase (AST). Em relação aos valores hematológicos, registrou-se flutuação dentro dos valores de referência na contagem diferencial de hemoglobina, de neutrófilo e de linfócito. Dessa forma, a administração do extrato metanólico de C. jamacaru não apresentou reações tóxicas sobre a maioria dos parâmetros hematológicos e bioquímicos estudados em ratas Wistar adultas grávidas. Entretanto, o aumento dos níveis séricos de AST e ALT em doses elevadas sugere uma sobrecargas hepática, as quais devem ser investigadas em maiores detalhes.

The effects of oral administration of methanol extract (ME) prepared from stems of Cereus jamacaru DC., Cactaceae were investigated on the biochemical and hematological parameters in pregnant adult Wistar rats. Twenty rats (n = 5 per group) have been treated orally for four consecutive days with ME in doses of 100, 250 and 500 mg/kg weight, and then, it was determined the biochemical and hematological profiles. The results showed that during the period of treatment there was no signs of toxicity or death. The hematological and biochemical parameters were not modified by oral administration of ME, except for a significant increase of 45.7 percent and 41.9 percent for alanine transaminase (ALT) in doses of 250 and 500 mg/kg in addition to the significant increase, of to 48.2 percent, 39.8 percent and 41.8 percent for aspartate transaminase (AST). In hematology, it was registered a fluctuation within the reference values of hemoglobin in the differential count of neutrophil and lymphocyte. In this way the administration of methanol extract of C. jamacaru does not produce toxic effects or alters the majority of biochemical and hematological studies in pregnant adult Wistar rats. However, the increase of serum ALT and AST in high doses suggests a liver overload, which must be investigated in more detail.

Atividade inibitória das folhas e caule de Kalanchoe brasiliensis Cambess frente a microrganismos com diferentes perfis de resistência a antibióticos / Inhibitory activity of aerial parts of Kalanchoe brasiliensis Cambess against microorganisms with variation profile antibiotic-resistant

A avaliação antimicrobiana das partes aéreas de Kalanchoe brasiliensis Cambess, Crassulaceae, a qual é comumente utilizada para o tratamento de inflamações da mucosa oral, bronquites e congestão nasal, é relatada. Esta atividade foi avaliada em discos de Petri usando o método de difusão para a determinação da Concentração Inibitória Mínima (MIC) e cinética bactericida. Foram usadas amostras bacterianas gram-positivas, gram-negativas e cepas de fungos leveduriformes do gênero Cândida. Apenas o óleo essencial demonstrou ser efetivo, apresentando atividade frente amostras gram-positivas de Staphylococcus aureus (MRSA) meticilina resistente. A ação observada foi considerada bacteriostática por reduzir um log10 UFC/mL a partir da sexta hora de exposição da amostra ao óleo essencial nas concentrações de 4 por cento e 8 por cento. Compostos fenólicos estão presentes em óleo essencial, sugerindo que o efeito foi devido à presença dos mesmos. Por este motivo à planta Kalanchoe brasiliensis Cambess pode representar uma alternativa terapêutica para infecções provocadas por Staphylococcus aureus.

This study reports the antimicrobial evaluation of the aerial parts of Kalanchoe brasiliensis Cambess, Crassulaceae, commonly used for the treatment of the oral mucosa inflammation, bronchitis and nasal congestion. The antimicrobial activity was assayed in petri dishes using the diffusion method for determination of the minimal inhibitory concentration (MIC) and the kill curve kinetic methods. It were used gram-positive and gram-negative strain, leveduriforms fungi strain classified in genus Cândida. Only the essential oil showed activity against methicilin resistant Staphylococcus aureus (MRSA). This action was considered bacteriostatic with the reduction to one log10 CFU/ml after six hour of exhibition at the concentration of 4 percent and 8 percent. There are studies accounts that polyphenols are present in the essential oil and are active against bacteria. K. brasiliensis is rich in polyphenols suggering that the antimicrobial effect showed is due to this. For this reason, the plant Kalanchoe brasiliensis, can represent a therapeutic alternative against infections caused for Staphylococcus aureus.

In vivo study of the anti-inflammatory and antitumor activities of leaves from Plectranthus amboinicus (Lour.) Spreng (Lamiaceae).

ETHNOPHARMACOLOGICAL RELEVANCE: Plectranthus amboinicus (Lour.) Spreng is a medicinal specie often used in Brazil, especially in Northeast Region, for the treatment of several diseases including inflammations and cancer. AIM OF THE STUDY: To evaluate the anti-inflammatory and antitumor activities of the hydroalcoholic extract from leaves of P. amboinicus in an attempt to determine whether the medicinal uses are supported by pharmacological effects. MATERIALS AND METHODS: Anti-inflammatory activity was determined by carrageenan-induced paw edema method. The antitumor effect was evaluated in an in vivo experimental study, using the following tumors: Sarcoma-180 and Erlich ascite carcinoma. RESULTS: There were statistically significant decreases (p<.05) of edema paw in at the doses of 150, 250 and 350 mg/kg (i.p.) of the hydroalcoholic extract of P. amboinicus. Similarly, the administration of P. amboinicus at the doses of 100, 150, 250 and 350 mg/kg (i.p.) inhibited the growth of sarcoma-180 and Ehrlich ascite carcinoma tumors in mice. CONCLUSION: The results suggest that the hydroalcoholic extract of P. amboinicus possesses anti-inflammatory and antitumor activities, supporting the folk use of this medicinal specie.

Avaliação do controle radioquímico do Ricinus communis L. e Tc-99m na marcação de hemácias / Assessment of the radiochemical control of Ricinus communis L. and Tc-99m with the labeling of red blood cells

O Ricinus communis L. pertence à família das Euforbiáceas, possui frutos típicos de onde é extraído o óleo de rícino, altamente tóxico. Neste estudo foi analisado o efeito do extrato de Ricinus communis L na marcação de hemácias com Tc-99m através do controle radioquímico. Os resultados mostraram que no controle radioquímico por meio da cromatografia, foi observado que o extrato marcado com Tc-99m mostrou duas frações com 130.007 e 494.592 cpm, e na marcação de hemácias, com por centoATI de 61.88 e 41.32 por cento nas frações 1 e 2. Foi concluído que o extrato de R. communis L. altera a captação do Tc-99m in vitro, competindo com o material radioativo em possíveis sítios de ligação nas células vermelhas do sangue, como a capacidade de oxidação do íon estanoso ou por competição com o íon pertecnetato.

Ricinus communis L. belongs to the Euphorbiaceae family, from whose fruits the ricin oil is extracted, highly toxic. In this study it was analyzed the effect of the extract of Ricinus communis L. in the labeling of red blood cells with Tc-99m through the radiochemical control. The results showed that in the radiochemical control through chromatography, it was observed that the extract labeled with Tc-99m showed two fractions with 130.007 and 494.592 cpm, and in the labeling of red blood cells, with percentATI of 61.88 and 41.32 percent in the fractions 1 and 2. It has been concluded that the extract of Ricinus communis alters the captivating of Tc-99m in vitro, competing with the radioactive material in the possible binding sites of the red blood cells, as well in the capacity of oxidation of the stannous ion or by competition with the pertechnetate ion.

Estudo toxicológico pré-clínico (agudo) do extrato do Syzygium aromaticum (L) em roedores / Preclinical (acute) toxicologic study of the extract of Syzygium aromaticum (L) in rodents

O objetivo desta pesquisa foi estimar a toxicidade aguda do extrato do cravo-da-índia (Syzygium aromaticum Linné) em roedores. O extrato hidro-alcoólico a 80 por cento foi concentrado em evaporador rotativo obtendo-se uma mistura final de extrato pilular. Camundongos albinos (Mus musculus) fêmeas, divididos em 13 lotes de seis animais foram observados por 24 horas a partir da administração do extrato diluído em solução fisiológica a 0,9 por cento nas dosagens de 137,5; 180; 187,5; 250; 375; 437,5; 500 e 1.000 mg/kg para via intraperitoneal e 1.000; 2.400; 2.880; 4.000 e 5.000 mg/kg para via oral. O cálculo proporcional foi realizado a fim de se obter a mesma dose para todos os animais de cada grupo. As punções foram por via intraperitoneal sendo respeitados intervalos de cinco minutos entre as administrações individuais. Nos ensaios de toxicidade por via oral a solução foi introduzida no trato digestório dos animais através de cânula metálica acoplada a seringa (gavagem). Os animais apresentaram alguns sinais de toxicidade, porém não letais até a dose de 5.000 mg/kg. A DL50 para via intraperitoneal foi calculada pelo método de Karber e Behrens (1964), sendo estabelecida em 255 mg/kg (muito tóxico, grau 4). Conclui-se que sob condições agudas de exposição, o extrato do cravo-da-índia é um agente tóxico, devendo ser considerado como tal, dependendo da dose administrada ou absorvida, tempo e freqüência de exposição e vias de administração.

The objective of this research was to estimate the acute toxicity of the extract of clove (Syzygium aromaticum Linné) in rodents. The 80 percent hidro-alcoholic extract was concentrated in rotary evaporator until a final resinous mixture extract was obtained. Albino female mice (Mus musculus), divided in 13 lots of six animals were observed for 24 hours. The extract diluted in 0.9 percent physiologic solution was administrated at the dosages of 137.5; 180.0; 187.5; 250.0; 375.0; 437.5; 500.0 and 1,000 mg/kg through intraperitoneal route and 1000; 2,400; 2,880; 4,000 and 5,000 mg/kg through oral route. A proportional calculation was carried out in order to have the same dose for the animals in each group. The punctures were gotten by intraperitoneal route in intervals of five minutes among the individual doses. For the oral toxicity the solution was introduced in the digestive system of the animals through coupled metallic stem syringe (gavage). The animals presented non lethal toxic signs up to 5,000 mg/kg. DL50 was established by the method of Karber and Behrens (1964). LD50 was estimated in 255 mg/kg (highly poisonous, degree 4). It can be concluded that under acute conditions of exposure, the extract of clove is a poisonous agent and it should be considered as such, depending on the administered or absorbed dose, time and frequency exhibition and administration routes.

Atividade antimicrobiana do extrato de Anacardium occidentale Linn. em amostras multiresistentes de Staphylococcus aureus / Antimicrobial activity of the hydroalcoholic extract of Anacardium occidentale Linn. against multi-drug resistant strains of Staphylococcus aureus

Plantas medicinais com propriedades terapêuticas são de grande relevância em todo o mundo, principalmente em países em desenvolvimento. A planta Anacardium occidentale Linn. é largamente usada na medicina tradicional na nossa região, como antidiarréico, para amigdalite, bronquites, artrites, e antiiflamatório. No presente estudo avaliou-se a ação antimicrobiana do extrato hidroalcóolico da casca do caule do cajueiro frente a amostras de Staphylococcus aureus resistentes e sensíveis à meticilina, obtidas a partir de pacientes internados do Hospital Universitário/Universidade Federal da Paraíba. A atividade antimicrobiana foi determinada pelo método de difusão em meio sólido para a determinação da Concentração Inibitória Mínima do extrato, e foi observada no total de 30 amostras, pela presença ou não do halo de inibição. Todas as amostras ensaiadas mostraram-se sensíveis à ação do extrato do cajueiro, com diâmetros dos halos de inibição variando de 10 a 20 mm, demonstrando grande eficácia do cajueiro. Assim, o uso desta planta na nossa região pode inferir uma alternativa terapêutica eficiente e de baixo custo, contra infecções bacterianas causadas por Staphylococcus aureus.

Medicinal plants with therapeutical properties are of great significance in the whole world, especially in developing countries. Anacardium occidentale Linn. is a plant widely used in the traditional medicine in our region against diarrhea, tonsillitis, bronchitis, arthritis, and inflammation. In this paper, the antimicrobial activity of the hydroalcoholic extract of the cashew tree stem was evaluated against samples of meticillin-resistant and meticillin-sensible Staphylococcus aureus, attained from patients interned at Hospital Universitário/Universidade Federal da Paraíba. The antimicrobial activity was determined by the diffusion method in solid milieu to determine the Minimum Inhibitory Concentration (MIC) of the extract, and it was observed in 30 samples the presence or not of inhibition zone. All the assayed samples proved to be sensible to the activity of the extract of the cashew tree, with inhibition zones diameter of 10 to 20 mm, displaying consequently great effectiveness of the extract of the cashew tree stem. Thus, the use of this plant in our region can infer a low cost and efficient therapeutical alternative against bacterial infections caused by Staphylococcus aureus.

Synthesis, antitumour and antimicrobial activities of new peptidyl derivatives containing the 1,3-benzodioxole system.

Two series of 5 and 6-substituted 1,3-benzodioxole peptidyl derivatives were synthesized and evaluated as antitumour and antimicrobial agents. The compounds that could be conveniently prepared in a few steps processes from natural safrole have been characterised by IR and 1H-NMR spectroscopy. In vivo antitumor activity tests showed that some of the compounds were able to inhibit carcinoma S-180 tumour growth in mice. The in vitro antimicrobial activity of all compounds revealed that they are able to promote the growth of some organisms, including Bacillus subtilis.