Potential of Ginkgo biloba L. leaves in the management of hyperglycemia and hypertension using in vitro models

Leaves from four different Ginkgo biloba L. trees (1 and 2 - females; 3 and 4 - males), grown at the same conditions, were collected during a period of 5 months (from June to October, 2007). Water and 12% ethanol extracts were analyzed for total phenolics content, antioxidant activity, phenolic profile, and the potential in vitro inhibitory effects on alpha-amylase, alpha-glucosidase, and Angiotensin I-Converting Enzyme (ACE) enzymes related to the management of diabetes and hypertension. The results indicated a significant difference among the trees in all functional benefits evaluated in the leaf extracts and also found important seasonal variation related to the same functional parameters. In general, the aqueous extracts had higher total phenolic content than the ethanolic extracts. Also, no correlation was found between total phenolics and antioxidant activity. In relation to the ACE inhibition, only ethanolic extracts had inhibitory activity. (C) 2009 Elsevier Ltd. All rights reserved.

Microbial Decontamination Study of Medicinal Plants by Plasma Treatment

In the present work the microbial decontamination of some medicinal plants by plasma treatment using oxygen gas or a mixture of oxygen and hydrogen peroxide was investigated. The efficiency of the decontamination process was analyzed by the count of heterotropic microorganisms and pathogenic research. The results showed a reduction in the microorganism number such as 3 and 4 logarithmic cycles for ginkgo and artichoke, while it was not efficient for samples containing hard and thick cells, and mucilage, such as guarana and chamomile.

Novel benzofuroxan derivatives against multidrug-resistant Staphylococcus aureus strains: Design using Topliss` decision tree, synthesis and biological assay

The aim of this study was the design of a set of benzofuroxan derivatives as antimicrobial agents exploring the physicochemical properties of the related substituents. Topliss` decision tree approach was applied to select the substituent groups. Hierarchical cluster analysis was also performed to emphasize natural clusters and patterns. The compounds were obtained using two synthetic approaches for reducing the synthetic steps as well as improving the yield. The minimal inhibitory concentration method was employed to evaluate the activity against multidrug-resistant Staphylococcus aureus strains. The most active compound was 4-nitro-3-(trifluoromethyl)[N`-(benzofuroxan-5-yl) methylene] benzhydrazide (MIC range 12.7-11.4 mu g/mL), pointing out that the antimicrobial activity was indeed influenced by the hydrophobic and electron-withdrawing property of the substituent groups 3-CF(3) and 4-NO(2), respectively. (C) 2011 Elsevier Ltd. All rights reserved.

The intake of caffeine does not improve the performance of judo

The objective of this study was to investigate the ergogenic effects of caffeine on motor performance of judo female athletes. Thirteen female athletes (17.6 +/- 1.6 years, 58.3 +/- 11.4 kg, 162 +/- 4.1 cm, 22.5 +/- 4 kg/m(2)), registered in the State Federation of Judo for at least two years, participated in this study. The motor performance was assessed using the Special Judo Fitness Test (SJFT), from which was considered the number of throws in each block, the total number of throws, recovery and final heart rate (HR) and final score in SJFT. The subjects were tested in two different conditions, after ingestion of gelatin capsules of caffeine (6 mg.kg(-1)) or placebo (dextrose) 60 minutes before testing in a randomized double-blind, crossover study. The number of throws in each block did not differs between the caffeine (CAF) and placebo (PL) conditions (Block A: 4.53 +/- 0.51 CAF and 4.46 +/- 0.51 PL; Block B: 8.3 +/- 0.63 CAF and 8.23 +/- 0.72 PL; Block C: 7.23 +/- 0.59 CAF and 7.46 +/- 0.77 PL), as well as the total number of throws (20.07 +/- 1.18 CAF and 20.15 +/- 1.67 PL), HR (Final: 190.3 +/- 9.63 bpm CAF and 190.69 +/- 9.19 bpm PL; Recovery 162.07 +/- 13.78 bpm CAF and 164.3 +/- 9.64 bpm PL) and final score in SJFT (17.59 +/- 1.4 CAF and 17.75 +/- 1.98 PL). Ingestion of caffeine did not improve performance during high intensity and short duration exercise in judo fighters

Antileishmanial Sesquiterpenes from the Brazilian Red Alga Laurencia dendroidea

Investigation of the bioactive crude extracts from two populations of the red alga Laurencia dendroidea from the southeastern Brazilian coast led to the identification of five sesquiterpenes: (+)-obtusane (1), a triquinane derivative (2), (-)-elatol (3), obtusol (4), and cartilagineol (5). An antileishmanial bioassay against Leishmania amazonensis was conducted for crude lipophilic extracts and for sesquiterpenes 2, 3, and 4. Compounds 3 and 4 displayed in vitro and in vivo leishmanicidal activity and very low cytotoxicity.

Endogenous cannabinoids induce fever through the activation of CB(1) receptors

Background and purpose: The effects of centrally administered cannabinoids on body core temperature (Tc) and the contribution of endogenous cannabinoids to thermoregulation and fever induced by lipopolysaccharide (LPS) (Sigma Chem. Co., St. Louis, MO, USA) were investigated. Experimental approach: Drug-induced changes in Tc of male Wistar rats were recorded over 6 h using a thermistor probe (Yellow Springs Instruments 402, Dayton, OH, USA) inserted into the rectum. Key results: Injection of anandamide [(arachidonoylethanolamide (AEA); Tocris, Ellisville, MO, USA], 0.01-1 mu g i.c.v. or 0.1-100 ng intra-hypothalamic (i.h.), induced graded increases in Tc (peaks 1.5 and 1.6 degrees C at 4 h after 1 mu g i.c.v. or 10 ng i.h.). The effect of AEA (1 mu g, i.c.v.) was preceded by decreases in tail skin temperature and heat loss index (values at 1.5 h: vehicle 0.62, AEA 0.48). Bell-shaped curves were obtained for the increase in Tc induced by the fatty acid amide hydrolase inhibitor [3-(3-carbamoylphenyl)phenyl] N-cyclohexylcarbamate (Cayman Chemical Co., Ann Arbor, MI, USA) (0.001-1 ng i.c.v.; peak 1.9 degrees C at 5 h after 0.1 ng) and arachidonyl-2-chloroethylamide (ACEA; Tocris) (selective CB(1) agonist; 0.001-1 mu g i.c.v.; peak 1.4 degrees C 5 h after 0.01 mu g), but (R,S)-(+)-(2-Iodo-5-nitrobenzoyl)-[1-(1-methyl-piperidin-2-ylmethyl)-1H-indole-3-yl] methanone (Tocris) (selective CB(2) agonist) had no effect on Tc. AEA-induced fever was unaffected by i.c.v. pretreatment with 6-Iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indole-3-yl](4-methoxyphenyl) methanone (Tocris) (selective CB(2) antagonist), but reduced by i.c.v. pretreatment with N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (AM251; Tocris) (selective CB(1) antagonist). AM251 also reduced the fever induced by ACEA or LPS. Conclusions and implications: The endogenous cannabinoid AEA induces an integrated febrile response through activation of CB(1) receptors. Endocannabinoids participate in the development of the febrile response to LPS constituting a target for antipyretic therapy.

Purification and characterization of Ts15, the first member of a new alpha-KTX subfamily from the venom of the Brazilian scorpion Tityus serrulatus

Voltage-gated potassium channel toxins (KTxs) are basic short chain peptides comprising 23-43 amino acid residues that can be cross-linked by 3 or 4 disulfide bridges. KTxs are classified into four large families: alpha-, beta-, gamma- and kappa-KTx. These peptides display varying selectivity and affinity for K(v) channel subtypes. In this work, a novel toxin from the Tityus serrulatus venom was isolated, characterized and submitted to a wide electrophysiological screening on 5 different subtypes of Nay channels (Na(V)1.4; Na(V)1.5; Na(V)1.6; Na(V)1.8 and DmNa(V)1) and 12 different subtypes of Kv channels (K(V)1.1 - K(V)1.6; K(V)2.1; K(V)3.1; K(V)4.2; K(V)4.3; Shaker IR and ERG). This novel peptide, named Ts15, has 36 amino acids, is crosslinked by 3 disulfide bridges, has a molecular mass of 3956 Da and pI around 9. Electrophysiological experiments using patch clamp and the two-electrode voltage clamp techniques show that Ts15 preferentially blocks K(V)1.2 and K(V)1.3 channels with an IC(50) value of 196 +/- 25 and 508 +/- 67 nM, respectively. No effect on Na(V) channels was observed, at all tested concentrations. Since Ts15 shows low amino acid identity with other known KTxs, it was considered a bona fide novel type of scorpion toxin. Ts15 is the unique member of the new alpha-Ktx21 subfamily and therefore was classified as alpha-Ktx21.1. (C) 2011 Elsevier Ltd. All rights reserved.

Brazilian Propolis: Seasonal Variation of the Prenylated p-Coumaric Acids and Antimicrobial Activity

Brazilian green propolis, which is used in food and beverages to improve health and to prevent diseases, demostrates antioxidant, antimutagenic, and antimicrobial activities. Most biological activities are thought to be related to the high levels of drupanin, artepillin C, and baccharin, which are compounds also present in Baccharis dracunculifolia D.C. (Asteraceae). Since propolis chemical composition depends on the region and the period of collection, as well as its plant origin, the effect of seasonal variation on the both content of prenylated p-coumaric acids and in vitro antimicrobial activity of Brazilian propolis from four different sites, was performed. The results showed that MIC values ranged from 100 to 300 mu g/mL against both Staphylococcus aureus and Kocuria rhizophila, while none of the propolis samples was active against Pseudomonas aeruginosa, Escherichia coli, and Candida albicans. HPLC analysis showed that the content of drupanin, artepillin C, and baccharin varied throughout the year, as well as among the different study sites. Also, it is suggested that Baccharis dracunculifolia is the main botanical source of Brazilian propolis in sites I and 2, while in sites 3 and 4, other plant species are also used by bees to produce propolis. All the evaluated propolis samples exhibited similar antibacterial activity, but different contents of prenylated p-coumaric acids throughout the year.

Antimicrobial activity of the extract and isolated compounds from Baccharis dracunculifolia D. C. (Asteraceae)

Baccharis dracunculifolia D. C. (Asteraceae) is the most important plant source of the Brazilian green propolis. Since propolis is known for its antimicrobial activity, the aim of this work was to evaluate the showed that the leaves extract of B. dracunculifolia (BdE) presents antifungal and antibacterial activities, especially against Candida krusei and Cryptococcus neoformans, for which the BdE showed IC50 values of 65 mu g mL(-1) and 40 mu g mL(-1), respectively In comparison to the BdE, it was observed that the green propolis extract (GPE) showed better antimicrobial activity, displaying an IC50 value of 9 mu g mL(-1) against C krusei. Also, a phytochemical study of the BdE was carried out, affording the isolation of ursolic acid (1), 2 alpha-hydroxy-ursolic acid (2), isosakuranetin (3), aromadendrin-4`-methylether (4), baccharin (5), viscidone (6), hautriwaic acid lactone (7), and the clerodane diterpene 8. This is the first time that the presence of compounds 1, 2, and 8 in B. dracunculifolia has been reported. Among the isolated compounds, 1 and 2 showed antibacterial activity against methicillin-resistant Staphylococcus aureus, displaying IC50 values of 65 mu g mL(-1) and 40 mu g mL(-1), respectively. 3 was active against C neoformans, showing an IC50 value of 15 mu g mL(-1) and a MIC value of 40 mu g mL(-1), while compounds 4-8 were inactive against all tested microorganisms. The results showed that the BdE, similar to the GPE, displays antimicrobial activity, which may be related to the effect of several compounds present in the crude extract.

In vitro evaluation of the antioxidant activity of liposomal flavonols by the HRP--H(2)O(2)--luminol system

Considering that antioxidant flavonols have been reported to be beneficial to human health, but that their low water solubility and bioavailability limit their administration through systemic route, the development of suitable flavonol-carriers is of great importance for clinical therapeutics. The aim of this study was to prepare liposomes containing flavonols or not and evaluate their antioxidant activity. Vesicles were obtained by ethanol injection method and characterized in terms of entrapment efficiency, size and zeta potential. Inhibitory activity of liposomal flavonols on reactive oxygen species generation was assessed in vitro using luminol--H(2)O(2)--horseradish peroxidase technique. Antioxidant activity of liposomal flavonols is dependent on concentration and chemical structure of active compound. Quercetin and myricetin are the most active flavonols (IC(50) == 0.6--0.9 mu A mu mol/L), followed by kaempferol (IC(50) == 3.0--4.5 mu A mu mol/L) and galangin (IC(50) == 4.0--7.0 mu A mu mol/L). Our results suggest that antioxidant-loaded liposomes may be promising tools for therapy of diseases where oxidative stress is involved.

In Vivo Antigenotoxicity of Baccharin, an Important Constituent of Baccharis dracunculifolia DC (Asteraceae)

Baccharin (3-prenyl-4-(dihydrocinnamoyloxy)cinnamic acid) is an important chemical compound isolated from the aerial parts of Baccharis dracunculifolia DC (Asteraceae), a native plant of South America, and the most important plant source of Brazilian green propolis. The present study was designed to investigate the ability of baccharin to modulate the genotoxic effects induced by doxorubicin and methyl methanesulphonate in male Swiss mice using the micronucleus and comet assays, respectively. The different doses of baccharin [0.12, 0.24 and 0.48 mg/kg body-weight (b.w.)] were administered simultaneously to doxorubicin (micronucleus test; 15 mg/kg b.w.) and to methyl methanesulphonate (comet assay; 40 mg/kg b.w.). The results showed a significant decrease in the frequency of micronucleated polychromatic erythrocytes in animals treated with baccharin and doxorubicin compared to animals that received only doxorubicin. This reduction ranged from 39.8% to 50.7% in the micronucleus test. The extent of DNA damage in liver cells was significantly lower in animals treated with different concentrations of baccharin combined with methyl methanesulphonate in comparison with the damage observed for animals treated only with methyl methanesulphonate. These differences resulted in a significant reduction in the extent of DNA damage, which ranged from 47.8% to 60.6%.

Lactobacillus sakei 1 and its bacteriocin influence adhesion of Listeria monocytogenes on stainless steel surface

Listeria monocytogenes is of particular concern for the food industry due to its psychrotolerant and ubiquitous nature. In this work, the ability of L monocytogenes culturable cells to adhere to stainless steel coupons was studied in co-culture with the bacteriocin-producing food isolate Lactobacillus sakei 1 as well as in the presence of the cell-free neutralized supernatant of L sakei 1 (CFSN-S1) containing sakacin 1. Results were compared with counts obtained using a non bacteriocin-producing strain (L sakei ATCC 15521) and its bacteriocin free supernatant (CFSN-SA). Culturable adherent L monocytogenes and lactobacilli cells were enumerated respectively on PALCAM and MRS agars at 3-h intervals for up to 12 h and after 24 and 48 h of incubation. Bacteriocin activity was evaluated by critical dilution method. After 6 h of incubation, the number of adhered L monocytogenes cells in pure culture increased from 3.8 to 5.3 log CFU/cm(2) (48h). Co-culture with L sakei 1 decreased the number of adhered L monocytogenes cells (P < 0.001) during all sampling times with counts lower than 3.0 log CFU/cm(2). The CFNS-S1 also led to a significant and similar reduction in culturable adhered L. monocytogenes counts for up to 24 h of incubation, however after 48 h of incubation, re-growth of L monocytogenes number of adhered cells was observed, likely due to lack of competition for nutrients. L sakei ATCC 15521 or its supernatant (CFNS-SA) did not reduce the number of adhered L monocytogenes cells on stainless steel surface and from 6 h of incubation, listerial counts were between 4.3 and 4.5 log CFU/cm(2). These results indicate that L sakei 1 and its bacteriocin sakacin 1 may be useful to inhibit early stages of L monocytogenes adherence to abiotic surface. (C) 2011 Elsevier Ltd. All rights reserved.

Dexamethasone Effects in the Strongyloides venezuelensis Infection in A Murine Model

The aim of this study was to investigate the immunomodulatory effects of glucocorticoids on the immune response to Strongyloides venezuelensis in mice. Balb/c mice were infected with S. venezuelensis and treated with Dexamethasone (Dexa) or vehicle. Dexa treatment increased circulating blood neutrophil numbers and inhibited eosinophil and mononuclear cell accumulation in the blood, bronchoalveolar, and peritoneal fluid compared with control animals. Moreover, Dexa decreased tumor necrosis factor-alpha (TNF-alpha), interferon-gamma (IFN-gamma), interleukin-3 (IL-3), IL-4, IL-5, IL-10, and IL-12 production in the lungs and circulating immunoglobulin G1. (IgG1), IgG2a, and IgE antibody levels while increasing the overall parasite burden in the feces and intestine. Dexa treatment enhanced the fertility of female nematodes relative to untreated and infected mice. In summary, the alterations in the immune response induced by Dexa resulted in a blunted, aberrant immune response associated with increased parasite burden. This phenomenon is similar to that observed in S. stercoralis-infected humans who are taking immunosuppressive or antiinflammatory drugs, including corticosteroids.

Synthesis of (2S)-isopropyl-5-alkynylpyrimidin-2-ones: precursors of beta-aminoacids

The efficient palladium-catalyzed Suzuki-Miyaura cross-coupling reaction of (2S)-isopropyl-5-iodo-2,3-dihydro-4(H)-pyrimidin-4-one with, arylethynyl-, heteroarylethynyl-, and alkylethynyltrifluoroborate salts is reported. The standard protocol was evaluated and optimized in order to gain access to suitable precursors of enantiopure 2-substituted beta-amino acids. The scope and limitations of this methodology are discussed. (C) 2010 Elsevier Ltd. All rights reserved.

Solid-State Experimental and Theoretical Investigation of the Ammonium Salt of Croconate Violet, a Pseudo-Oxocarbon Ion

The present work describes the crystal structure, vibrational spectra, and theoretical calculations of ammonium salts of 3,5-bis-(dicyanomethylene)cyclopentane-1,2,4-trionate, (NH(4))(2)(C(11)N(4)O(3)) [(NH(4))(2)CV], also known as ammonium croconate violet. This compound crystallizes in triclinic P (1) over bar and contains two water molecules per unit formula. The crystal packing is stabilized by hydrogen bonds involving water molecules and ammonium cations, giving rise to a 3D polymeric arrangement. In this structure, a pi-stacking interaction is not observed, as the smaller centroid-centroid distance is 4.35 angstrom. Ab initio electronic structure calculations under periodic boundary conditions were performed to predict vibrational and electronic properties. The vibrational analysis was used to assist the assignments of the Raman and infrared bands. The solid structure was optimized and characterized as a minimum in the potential-energy surface. The stabilizing intermolecular hydrogen bonds in the crystal Structure were characterized by difference charge-density analysis. The analysis of the density of states of (NH(4))(2)CV gives an energy gap of 1.4 eV with a significant contribution of carbon and nitrogen 2p states for valence and conduction bands.