Evaluation of Strychnos pseudoquina St. Hil. leaves extract on gastrointestinal activity in mice

Strychnos pseudoquina St. Hil. (Loganiaceae) was investigated for its ability to protect the gastric mucosa against injuries caused by non-steroidal anti-inflammatory drugs (piroxicam) and a necrotizing agent (HCl/EtOH) in mice. The MeOH extract and enriched alkaloidic fraction (EAF) provided significant protection in experimental models wheer used at doses of 250 and 1000 mg/kg. In vivo tests were carried out to evaluate for possible toxic effects and no mortality was observed up to the 5 g/kg dose level. Phytochemical investigation led to the isolation of a new indole alkaloid, which elucidated the observed pharmacological effects. © 2005 Pharmaceutical Society of Japan.

Benzopyrans from Curvularia sp., an endophytic fungus associated with Ocotea corymbosa (Lauraceae)

An isolate of Curvularia sp. was obtained from the leaves of Ocotea corymbosa, a native plant of the Brazilian Cerrado. The ethyl acetate extract from culture of this fungus afforded two benzopyran derivatives: (2′S)-2-(propan-2′-ol)-5-hydroxy-benzopyran-4-one (2) and 2,3-dihydro-2-methyl-benzopyran-4,5-diol (4); and two known benzopyrans: 2-methyl-5-methoxy-benzopyran-4-one (1) and (2R)-2,3-dihydro-2-methyl-5-methoxy- benzopyran-4-one (3). The structures of 2 and 4 were established on the basis of comprehensive spectroscopic analysis, mainly using 1D and 2D NMR experiments. The benzopyrans 1 and 2 showed weak in vitro antifungal activity against Cladosporium sphaerospermum and C. cladosporioides. Analyses of the biological activities were also carried out on HeLa (human cervix tumor) and CHO (Chinese hamster ovary) cells, aiming to evaluate their potential effects on mammalian cell line proliferation. Results from both cell lines indicated that compound 2 was able to induce cell proliferation: 70% on HeLa cells and 25% on CHO cells. © 2005 Elsevier Ltd. All rights reserved.

Advances in prodrug design

The background of prodrug design is presented herein as the basis for introducing new and advanced latent systems, taking into account mainly the versatility of polymers and other macromolecules as carriers. PDEPT (Polymer-Directed Enzyme Prodrug Therapy); PELT (Polymer-Enzyme Liposome Therapy); CDS (Chemical Delivery System); ADEPT(Antibody-Directed Enzyme Prodrug Therapy); GDEPT/VDEPT (Gene-Directed Enzyme Prodrug Therapy/Virus-Directed Enzyme Prodrug Therapy); ODDS (Osteotropic Drug Delivery System) and LEAPT (Lectin-directed enzyme-activated prodrug therapy) are briefly described and some examples are given. © 2005 Bentham Science Publishers Ltd.

Action of anti-bothropic factor isolated from Didelphis marsupialis on renal effects of Bothrops erythromelas venom

Acute renal failure is the most common complication in the lethal cases caused by snakebites in Brazil. Among the Brazilian venom snakes, Bothrops erythromelas is responsible for the majority of accidents in Northeastern Brazil. Didelphis marsupialis serum could inhibit myonecrotic, hemorrhagic, edematogenic hyperalgesic and lethal effects of envenomation determined by ophidian bites. In the present study, we evaluated the action of the anti-bothropic factor isolated from D. marsupialis on the renal effects promoted by B. erythromelas venom without systemic interference. Isolated kidneys from Wistar rats were perfused with Krebs-Henseleit solution containing 6% bovine serum albumin. We analyzed renal perfusion pressure (PP), renal vascular resistance (RVR), glomerular filtration rate (GFR), urinary flow (UF), and the percentages of sodium and potassium tubular transport (%TNa +, %TK +). The B. erythromelas venom (10 μg mL -1) decreased the PP (ct=108.71±5.09 mmHg; BE=65.21±5.6 mmHg*) and RVR (ct=5.76±0.65 mmHg mL -1 g -1 min -1; BE=3.10±0.45 mmHg mL -1 g -1 min -1*) . On the other hand, the GFR decreased at 60 min (ct 60=0.76±0. 07 mL g -1 min -1; BE 60=0.42±0.12 mL g -1 min -1*) and increased at 120 min (ct 120=0.72±0.01 mL g -1 min -1; BE 120=1.24±0.26 mL g -1 min -1*). The UF increased significantly when compared with the control group (ct=0.14±0.01 mL g -1 min -1; BE=0.47±0.08 mL g -1 min -1*). The venom reduced the %TNa + (ct 90=79.18±0.88%; BE 90=58.35±4.86%*) and %TK + (ct 90=67.20±4.04%; BE 90=57. 32±5.26%*) The anti-bothropic factor from D. marsupialis (10 μg mL -1) incubated with B. erythromelas venom (10 μg mL -1) blocked the effects on PP, RVR, %TNa +, and %TK +, but was not able to reverse the effects in UF and GFR promoted by venom alone. However, the highest concentration of D. marsupialis serum (30 μg mL -1) reversed all the renal effects induced by the venom. In conclusion, B. erythromelas venom altered all the renal functional parameters evaluated and the anti-bothropic factor from D. marsupialis was able to inhibit the effects induced by the venom in isolated kidney. © 2005 Elsevier Ltd. All rights reserved.

Effects of acetylsalicylic acid and acetic acid solutions in VX2 carcinoma cells. In vitro analysis

Purpose: To analyze, in vitro, the effects of acetylsalicylic acid (aspirin) and acetic acid solutions on VX2 carcinoma cells in suspension and to examine the correlation between these effects and neoplastic cell death. Methods: The VX2 tumor cells (107 cells/ml) were incubated in solutions containing differing concentrations (2.5% and 5%) of either acetylsalicylic acid or acetic acid, or in saline solution (controls). Every five minutes, cell viability was tested (using the trypan blue test) and analyzed under light microscopy. Results: Tumor cell viability (in %) decreased progressively and, by 30 minutes, neoplastic cell death had occurred in all solutions. Conclusion: Based on this experimental model and the methodology employed, we conclude that these solutions cause neoplastic cell death in vitro.

Antimicrobial activity of Uncaria tomentosa against oral human pathogens

Uncaria tomentosa is considered a medicinal plant used over centuries by the peruvian population as an alternative treatment for several diseases. Many microorganisms usually inhabit the human oral cavity and under certain conditions can become etiologic agents of diseases. The aim of the present study was to evaluate the antimicrobial activity of different concentrations of Uncaria tomentosa on different strains of microorganisms isolated from the human oral cavity. Micropulverized Uncaria tomentosa was tested in vitro to determine the minimum inhibitory concentration (MIC) on selected microbial strains. The tested strains were oral clinical isolates of Streptococcus mutans, Staphylococcus spp., Candida albicans, Enterobacteriaceae and Pseudomonas aeruginosa. The tested concentrations of Uncaria tomentosa ranged from 0.25-5% in Müeller-Hinton agat. Three percent Uncaria tomentosa inhibited 8% of Enterobacteriaceae isolates, 52% of S. mutans and 96% of Staphylococcus spp. The tested concentrations did not present inhibitory effect on P. aeruginosa and C. albicans. It could be concluded that micropulverized Uncaria tomentosa presented antimicrobial activity on Enterobacteriaceae, S. mutans and Staphylococcus spp. isolates.

Effects of fibrin sealer and resorbable gelatin on the repair of osseous defects in rat tibia

Gelfoam® - a biologically resorbable gelatin sponge - has the function of restricting hemorrhage, providing platelet rupture, and supporting fibrin threads. Beriplast® - a fibrinogen-thrombin compound - is used to adhere tissues, to consolidate sutures and in hemostasis. The objective of this study was to perform a histological analysis of the effects of haemostatic agents on osseous repair. These materials were inserted into surgical sites in young rat right and left tibiae. After the observation periods of 7, 14, 30 and 45 days, according to the bioethic protocol, the animals were killed, the tibiae were removed and fixed in 10% formalin and decalcified in equal parts of formic acid and sodium citrate solutions. After routine processing, the specimens were embedded in paraffin for microtomy. Analysis of the results demonstrated that the haemostatic agents are effective in controlling hemorrhage; they stimulate osteogenesis, featuring a pattern of osseous tissue formation similar to the control pattern, although the amount of osseous trabeculae was superior, especially in the Gelfoam group in the periods of 7 and 14 days; 30 days after surgery, the delay in tissue healing in the control group in relation to the experimental groups started to decrease, and the control and experimental groups exhibited similar tissue repair after 45 days, when all the groups exhibited secondary osseous tissue.

The influence of ovariectomy, simvastatin and sodium alendronate on alveolar bone in rats

Bisphosphonates are currently used in the treatment of many diseases involving increased bone resorption such as osteoporosis. Statins have been widely used for the treatment of hypercholesterolemia and recent studies have shown that these drugs are also capable of stimulating bone formation. The purpose of this study was to evaluate thel influence of an estrogen deficient state and the effects of simvastatin and sodium alendronate therapies on alveolar bone in female rats. Fifty-four rats were either ovariectomized (OVX) or sham operated. A month later, the animals began to receive a daily dose of simvastatin (SIN - 25 mg/kg), sodium alendronate (ALN - 2 mg/kg) or water (control) orally. Thirty-five days after the beginning of the treatment, the rats were sacrificed and their left hemimandibles were removed and radiographed using digital X-ray equipment. The alveolar radiographic density under the first molar was determined with gray-level scaling and the values were submitted to analysis of variance (α = 5%). Ovariectomized rats gained more weight (mean ± standard deviation: 20.06 ± 6.68%) than did the sham operated animals (12.13 ± 5.63%). Alveolar radiographic density values, expressed as gray levels, were lowest in the OVX-water group (183.49 ± 6.47), and differed significantly from those observed for the groups receiving alendronate (sham-ALN: 193.85 ± 3.81; OVX-ALN: 196.06 ± 5.11) and from those of the sham-water group (193.66 ± 4.36). Other comparisons between groups did not show significant differences. It was concluded that the ovariectomy reduced alveolar bone density and that alendronate was efficient for the treatment of this condition.

Bioprospecção de atividade antioxidante e antimicrobiana da casca de Stryphnodendron adstringens (Mart.) Coville (Leguminosae-Mimosoidae)

The aim of this work was to evaluate the class of secondary metabolites responsible for the antioxidant and antimicrobial activities of bark extracts of Stryphnodendron adstringens (Mart.) Coville (Leguminosae-Mimosoidae), a plant widely used in folk medicine in Brazil. Extracts of the bark were prepared with 50% ethanol, 70% ethanol, acetone:water (7:3, v/v) and chloroform. Antioxidant activity was prospected by spraying thin-layer chromatographs of the extracts with 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and measuring the DPPH radical scavenging capacity by spectrophotometry. Antibacterial activity was revealed by the agar diffusion method and bioautography. TLC spots assigned to tannins in the polar extracts showed antioxidant activity by DPPH radical scavenging and the chloroform extract showed the least scavenging activity. Antimicrobial activity was indicated by the bacterial growth inhibition haloes around polar extracts and bioautography showed activity in the TLC spots assigned to tannins. It was concluded that polar extracts of the bark of S. adstringens possessed antioxidant and antimicrobial activities which were due to secondary metabolite derived from the tannin class, which are the main constituent of these bark extracts, according to the literature.

Comparative study of disk diffusion and microdilution methods for evaluation of antifungal activity of natural compounds against medical yeasts Candida spp and Cryptococcus sp

Antifungal activity of natural products has been tested by adapting methods designed for synthetic drugs. In this study, two methods for the determination of antifungal activity of natural products, agar diffusion and broth microdilution, the CLSI reference methods for synthetic drugs, are compared and discussed. The microdilution method was more sensitive. The minimal inhibitory concentrations (MIC) of crude extracts, fractions and pure substances from different species of the plant families Piperaceae, Rubiaceae, Clusiaceae, Fabaceae and Lauraceae, from the Biota project, were determined. Antifungal activities against Candida albicans, C.krusei, C.parapsilosis and Cryptococcus neoformans were produced by several samples.

rastreamento histoquímico, fitoquímico e biológico de folhas de Plinia cauliflora (DC.) Kausel (Myrtaceae)

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Pharmacognostical evaluation of fruits of Solanum lycocarpum A. St.-Hill. (Solanaceae)

This study describes the chemical and physical-chemical profile of plant drug and ethanolic extract obtained from fruits of Solanum lycocarpum A. St.-Hill. (Solanaceae). The physical and chemical analysis involved the granulometry determination, non-compacted apparent density, loss on drying in oven and in infrared scale, pH, ash values and extractive values. The results determined the physical-chemical characteristics of the drug plant. It was also carried out the microbiological control of the plant drug. The preliminary phytochemical screening featured the presence of tannins, flavonoids and saponins in the plant drug and alkaloids and steroids in the ethanolic exctract. The solamargine and solasonine glycoalkaloids were identified through TLC and GC/ MS. The levels of total phenols and tannins were quantified in the extract (8.90% and 6,85% respectively). Such studies contribute to the chemical identification and quality control of S. lycocarpum fruits. © 2010 Phcog.net.

Mutagenicidade de duas espécies do gěnero Alchornea avaliadas através de ensaios com Salmonella microssomo e teste do micronúcleo

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Estudo clínico randomizado e aberto para avaliação de eficácia e superioridade dos medicamentos EF028 aerossol, EF028 creme e Andolba® frente ao tratamento controle e comparativo de não inferioridade entre os medicamentos EF028 aerossol, EF028 creme e Andolba® para avaliação de eficácia na redução da sintomatologia dolorosa

Aim: This study aimed to evaluate the efficacy of a new topical drug (EF028) in two separate presentations (aerosol and cream) in a comparative way with the already registered medication, Andolba® (benzocaine, benzoxiquina chloride benzeconio, menthol) and the negative control (hygiene), in the analgesic efficacy after episiotomy wound, reducing the requirement for systemic medication. Methods: 60 patients were voluntary post normal vaginal childbirth with episiotomy, were divided into four groups to comparatively assess the action of the product EF028 (cream and aerosol), Andolba® and soap, the efficacy of decreasing painful symptoms from daily use for 2 times a day for seven days. Clinical assessments and subjective pain occurred daily until the third postoperative day and on the 7th postoperative day. Results: The results showed that the drugs promoted a reduction of painful symptoms and there was no statistically significant difference (p <0.05) between presentations of drug EF028 (cream and aerosol) and Andolba® and the three products were significantly higher (p <0.05) to the control. Conclusions: The evaluated drugs EF028 aerosol, EF028 cream and Andolba® had similar efficacy in relieving the painful symptoms of the perineal region in postoperative episiotomy can be considered as indication for postoperative episiotomies. © Copyright Moreira Jr. Editora.