Evaluation of estrogenic, antiestrogenic and genotoxic activity of nemorosone, the major compound found in brown Cuban propolis

Background: Brown propolis is the major type of propolis found in Cuba; its principal component is nemorosone, the major constituent of Clusia rosea floral resins. Nemorosone has received increasing attention due to its strong in vitro anti-cancer action. The citotoxicity of nemorosone in several human cancer cell lines has been reported and correlated to the direct action it has on the estrogen receptor (ER). Breast cancer can be treated with agents that target estrogen-mediated signaling, such as antiestrogens. Phytoestrogen can mimic or modulate the actions of endogenous estrogens and the treatment of breast cancer with phytoestrogens may be a valid strategy, since they have shown anti-cancer activity.Methods: The aim of the present investigation was to assess the capacity of nemorosone to interact with ERs, by Recombinant Yeast Assay (RYA) and E-screen assays, and to determine by comet assay, if the compound causes DNA-damaging in tumoral and non-tumoral breast cells.Results: Nemorosone did not present estrogenic activity, however, it inhibited the 17-β-estradiol (E2) action when either of both methods was used, showing their antiestrogenicity. The DNA damage induced by the benzophenone in cancer and normal breast cells presented negative results.Conclusion: These findings suggest that nemorosone may have therapeutic application in the treatment of breast cancer. © 2013 Camargo et al.; licensee BioMed Central Ltd.

Effect of muscle fatigue and physical activity level in motor control of the gait of young adults

The aim of this study was to analyze the effect of muscle fatigue in active and inactive young adults on the kinematic and kinetic parameters of normal gait and obstacle crossing. Twenty male subjects were divided into active (10) and inactive (10), based on self-reported physical activity. Participants performed three trials of two tasks (normal gait and obstacle crossing) before and after a fatigue protocol, consisting of repeated sit-to-stand transfers until the instructed pace could no longer be maintained. MANOVAs were used to compare dependent variables with the following factors: physical activity level, fatigue and task. The endurance time in the fatigue protocol was lower for the inactive group. Changes of gait parameters with fatigue, among which increased step width and increased stride speed were the most consistent, were independent of task and physical activity level. These findings indicate that the kinematic and kinetic parameters of gait are affected by muscle fatigue irrespective of the physical activity level of the subjects and type of gait. Inactive individuals used a slightly different strategy than active individuals when crossing an obstacle, independently of muscle fatigue. © 2013.

Degradation, residual determination, and cholinesterase activity of triclorfon in Piaractus mesopotamicus Holmberg (Pacu) 1887

The aim of this study was to determine the no-observable-adverse-effect concentration (NOAEC) for trichlorfon, an antiparasitic agent used in aquaculture, in Piractus mesopotamicus (pacu) using acetylcholinesterase (AChE) activity as an end point. Fish were exposed 24 h/d for 15 d to different concentrations of trichlorfon in tanks of water for which a curve of dissipation was previously determined. Analysis of trichlorfon in water and fish plasma using gas chromatography with electron capture detection (GC-ECD) enabled measurement of limit of detection (LOD) and limit of quantification (LOQ), respectively, to be 3 and 10 ppb. Thirty-six hours after trichlorfon dilution in water, the concentration was below the LOD, and data showed that plasma concentrations did not exceed the LOQ. Apart from the 6.25 g/L, all concentrations of trichlorfon significantly inhibited plasma and brain AChE activity compared to controls. The AChE activity levels returned to control values in 7 d. These data may be useful to determine the concentration of trichlorfon that destroys parasites without producing adverse effects in fish.

Uterine Involution, Fluid Accumulation and Ovarian Activity after Injection of Prostaglandin at Different Periods of Buffalo Puerperium

This study aimed to evaluate the effect of chloprostenol administration, at early or intermediary puerperium, under uterine involution, intrauterine fluid accumulation and ovarian activity return. 30 Murrah postpartum buffaloes were randomly divided into three groups: CONT (saline, n = 10); CLO2 (chloprostenol at days 2 and 5 postpartum, n = 10) and; CLO15 (chloprostenol at days 15 and 20 postpartum, n = 10). Gynecological exams were performed at days 2, 7, 14, 21 and 28 postpartum, when uterine involution degree (1 to 3 scale, by transrectal palpation), intrauterine fluid accumulation (0 to 3 scale, by ultrasound exam) and ovarian activity (B-mode ultrasound exam) were evaluated. CLO2 group presented higher uterine involution (2.00 +/- 0.23, 1.66 +/- 0.23, 1.58 +/- 0.23 for groups CLO2, CONT and CLO15, respectively) and faster ovarian activity return in relation to groups CONT and CLO15 (P < 0.05). Groups CLO2 and CLO15 showed lower intrauterine fluid accumulation compared to CONT group (2.04 +/- 0.20, 1.58 +/- 0.20, 1.92 +/- 0.20 for groups CONT, CLO2 and CLO15, respectively; P < 0.05). Prostaglandin analogue administration in postpartum buffalo benefited uterine involution, lochia expulsion and ovarian activity return, improving reproductive efficiency in this specie.

Natural Products from Cyanobacteria with Antimicrobial and Antitumor Activity

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

Chemical composition and lipoxygenase activity in soybeans (Glycine max L. Merr.) submitted to gamma irradiation

Soybeans are an important food due to their functional and nutritional characteristics. However, consumption by western populations is limited by the astringent taste of soybeans and their derivatives which results from the action of lipoxygenase, an enzyme activated during product processing. The aim of this study was to evaluate the effect of gamma irradiation on the chemical composition and specific activity of lipoxygenase in different soybean cultivars. Soybeans were stored in plastic bags and irradiated with doses of 2.5, 5 and 10 kGy. The chemical composition (moisture, protein, lipids, ashes, crude fiber, and carbohydrates) and lipoxygenase specific activity were determined for each sample. Gamma irradiation induced a small increase of protein and lipid content in some soybean cultivars, which did not exceed the highest content of 5% and 26%, respectively, when compared to control. Lipoxygenase specific activity decreased in the three cultivars with increasing gamma irradiation dose. In conclusion, the gamma irradiation doses used are suitable to inactivate part of lipoxygenase while not causing expressive changes in the chemical composition of the cultivars studied. (C) 2014 Elsevier Ltd. All rights reserved.

Type 2 Diabetes Elicits Lower Nitric Oxide, Bradykinin Concentration and Kallikrein Activity Together with Higher DesArg(9)-BK and Reduced Post-Exercise Hypotension Compared to Non-Diabetic Condition

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Effects of maternal diabetes on male offspring: high cell proliferation and increased activity of MMP-2 in the ventral prostate

This study presents a comprehensive view of the histological and functional status of the prostate of adult rat offspring of mothers subjected to gestational diabetes induced by alloxan. The ventral prostate of male adult offspring of diabetic (DP) or normal (CP) mothers was evaluated for collagen fibres, cell death, fibroblasts, smooth muscle cells, cell proliferation, matrix metalloproteinases (MMPs), androgen receptors (AR), transforming growth factor beta 1 (TGF beta-1), catalase and total antioxidant activity. The prostates of DP animals were lower in weight than those of the CP group. The DP group also exhibited hyperglycaemia and hypotestosteronemia, higher cell proliferation and AR expression, a reduction in alpha-actin (possibly interfering with the reproductive function of the prostate), and enhanced activity of MMP-2, although the absolute content of MMP-2 was lower in this group. These findings were associated with increased TGF beta-1 and decreased collagen distribution. The prostates of DP rats additionally exhibited reductions in catalase and total antioxidant activity. Thus, rats developing in a diabetic intrauterine environment have glycaemic and hormonal changes that impact on the structure and physiology of the prostate in adulthood. The increased AR expression possibly leads to elevated cell proliferation. Stromal remodelling was characterized by enhanced activity of MMP-2 and collagen degradation, even with increased TGF beta-1 activation. These changes associated with increased oxidative stress might interfere with tissue architecture and glandular homeostasis.

Hancornia speciosa latex for biomedical applications: physical and chemical properties, biocompatibility assessment and angiogenic activity

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Radiopacity, pH and antimicrobial activity of Portland cement associated with micro- and nanoparticles of zirconium oxide and niobium oxide

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

Long-range and short-range structures of cube-like shape SrTiO3 powders: microwave-assisted hydrothermal synthesis and photocatalytic activity

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Composition and antifungal activity against Candida albicans, C. parapsilopisis, Candida krusei and Cryptococcus neoformans of essential oils from leaves of Piper and Peperomia species

This study was addressed to investigate the composition and antifungal activity of essential oils from leaves of Piperaceae species (Piper aduncum, Piper amalago, Piper cernuum, Piper diospyrifolium, Piper crassinervium, Piper gaudichaudianum, Piper solmsianum, Piper regnellii, Piper tuberculatum, Piper umbelata and Peperomia obtusifolia) against Candida albicans, C. parapsilosis, C. krusei and Cryptococcus neoformans. The essential oils from P. aduncum, P. gaudichaudianum and P. solmsianum showed the highest antifungal activity against Cryptococcus neoformans with the MIC of 62.5, 62.5 and 3.9 mg.mL-1, respectively. The oil from P. gaudichaudianum showed activity against C. krusei with MIC of 31.25 mg.mL-1.

Antitumor and cytotoxic activity of Kielmeyera coriacea mart. Zucc. and Pyrostegia venusta (ker-gawl.) Miers extracts

This study aimed to investigate the antitumor and cytotoxicity activities of Kielmeyera coriacea and Pyrostegia venusta extracts. Therefore, the hydroalcoholic extracts of P. venusta flowers and K. coriacea leaves were prepared. The extracts were evaporated and the dry extracts were diluted at concentrations of 1.0, 0.1, 0.01 and 0.001 mg/ml for carrying out the bioassays. Artemia salina eggs were incubated in saline solution at 28°C for 24 h. The larvae were treated with different extracts concentrations and the mortality was evaluated after 24 and 48 h. Five discs of potato were placed in Petri dishes and 50 μl of inoculum of Agrobacterium tumefaciens were added to it at 28°C for 24 h incubation. So, 50 μl of the extracts in different concentrations were added. Positive and negative controls were made. The P. venusta and K. coriacea extracts did not show statistically significant acute toxicity. K. coriacea extract showed (mean% of tumor ± standard deviation) 15.30 ± 3.24, 6.34 ± 3.82, 7.57 ± 2.92 and 5.77 ± 2.85 and P. venusta showed 25.82 ± 5.15, 38.40 ± 8.28, 15.75 ± 4.44 and 13.38 ± 7.92, with their concentrations for the antitumor bioassay, and the positive control showed 25.80 ± 6.14. According to the obtained results it was established that the K. coriacea and P. venusta extracts showed antitumor activity but did not show significant cytotoxic activity in A. salina test.

Effect of zirconium oxide and zinc oxide nanoparticles on physicochemical properties and antibiofilm activity of a calcium silicate-based material

The aim of the present study was to evaluate the antibiofilm activity against Enterococcus faecalis, compressive strength. and radiopacity of Portland cement (PC) added to zirconium oxide (ZrO2), as radiopacifier, with or without nanoparticulated zinc oxide (ZnO).The following experimental materials were evaluated: PC, PC + ZrO2, PC + ZrO2 + ZnO (5%), and PC + ZrO2 + ZnO (10%). Antibiofilm activity was analyzed by using direct contact test (DCT) on Enterococcus faecalis biofilm, for 5 h or 15 h. The analysis was conducted by using the number of colony-forming units (CFU/mL). The compressive strength was performed in a mechanical testing machine. For the radiopacity tests, the specimens were radiographed together with an aluminium stepwedge. The results were submitted to ANOVA and Tukey tests, with level of significance at 5%. The results showed that all materials presented similar antibiofilm activity (

Ph and antimicrobial activity of portland cement associated with different radiopacifying agents

The aim of this study was to evaluate the antimicrobial activity and pH changes induced by Portland cement (PC) alone and in association with radiopacifiers. Methods. The materials tested were pure PC, PC + bismuth oxide, PC + zirconium oxide, PC + calcium tungstate, and zinc oxide and eugenol cement (ZOE). Antimicrobial activity was evaluated by agar diffusion test using the following strains: Micrococcus luteus, Streptococcus mutans, Enterococcus faecalis, Pseudomonas aeruginosa, and Candida albicans. After 24 hours of incubation at 37°C, inhibition of bacterial growth was observed and measured. For pH analysis, material samples (n=10) were placed in polyethylene tubes and immersed in 10 mL of distilled water. After 12, 24, 48, and 72 hours, the pH of the solutions was determined using a pH meter. Results. All microbial species were inhibited by the cements evaluated. All materials composed of PC with radiopacifying agents promoted pH increase similar to pure Portland cement. ZOE had the lowest pH values throughout all experimental periods. Conclusions. All Portland cement-based materials with the addition of different radiopacifiers (bismuth oxide, calcium tungstate, and zirconium oxide) presented antimicrobial activity and pH similar to pure Portland cement.