RESUMEN

Chia (Salvia hispanica L.) is an herbaceous plant used as omega-3 polyunsaturated fatty acid (ω-3 PUFA) source that presents a range of beneficial effects on human health. Herein, it was used a chia oil containing over than 62% of α-linolenic acid (ALA), a compound widely related to anti-inflammatory actions. Chia oil effect was tested using paw edema and mechanical hyperalgesia induced by carrageenan, and ear edema induced by croton oil, histamine, and capsaicin. Croton oil was used in both preventive and therapeutic treatment schedules of chia oil while histamine and capsaicin were used only in preventive treatment schedule. Chia oil mechanism of action was investigated using nociception and paw edema response induced by intraplantar injection of acidified saline (ASIC activator), PGE2 (prostaglandin pathway), cinnamaldehyde (TRPA1 activator), bradykinin (BK pathway), menthol (TRPM8 activator), and capsaicin (TRPV1 activator). Further, RT-PCR for inflammatory mediators (TRPA1, NF-κB, PPAR-γ, COX-2, IL-6, TNF, FPR2, FAAH, MAGL, and IL-12A) induced by carrageenan, NLRP3 inflammasome activation, and the cell viability were then accessed. Later, chia oil actions were evaluated in the experimental autoimmune encephalomyelitis (EAE), a multiple sclerosis (MS) model. Chia oil showed anti-edematogenic and anti-hyperalgesic effects when administered 1 h before pro-inflammatory stimulus - particularly carrageenan and croton oil. Moreover, chia oil upregulated the mRNA levels of COX-2 and formyl peptide receptor 2 (FPR2) while reduced IL-6 expression in the spinal cord of mice submitted to i.pl. injection of carrageenan. Interestingly, chia oil mediates antinociceptive effects in mice decreasing the nociceptive response induced by acidified saline, PGE2, and cinnamaldehyde, but not by bradykinin, menthol, and capsaicin. On the EAE model, chia oil preventively administered attenuated EAE-induced motor deficits and mechanical hyperalgesia in mice, suggesting a valuable effect of chia oil supplementation in regulating inflammatory responses and some immune functions during immune-mediated inflammatory disorders (IMID). Nonetheless, additional reports will need to assess the effect of chia oil in well-controlled clinical trials performed in MS patients.

Asunto(s)

Antiinflamatorios , Extractos Vegetales , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Carragenina , Edema/inducido químicamente , Edema/tratamiento farmacológico , Edema/prevención & control , Humanos , Mediadores de Inflamación , Ratones , Extractos Vegetales/uso terapéutico

RESUMEN

Depression has a multifactorial etiology that arises from environmental, psychological, genetic, and biological factors. Environmental stress and genetic factors acting through immunological and endocrine responses generate structural and functional changes in the brain, inducing neurogenesis and neurotransmission dysfunction. Terpineol, monoterpenoid alcohol, has shown immunomodulatory and neuroprotective effects, but there is no report about its antidepressant potential. Herein, we used a single lipopolysaccharide (LPS) injection to induce a depressive-like effect in the tail suspension test (TST) and the splash test (ST) for a preventive and therapeutic experimental schedule. Furthermore, we investigated the antidepressant-like mechanism of action of terpineol while using molecular and pharmacological approaches. Terpineol showed a coherent predicted binding mode mainly against CB1 and CB2 receptors and also against the D2 receptor during docking modeling analyses. The acute administration of terpineol produced the antidepressant-like effect, since it significantly reduced the immobility time in TST (100-200 mg/kg, p.o.) as compared to the control group. Moreover, terpineol showed an antidepressant-like effect in the preventive treatment that was blocked by a nonselective dopaminergic receptor antagonist (haloperidol), a selective dopamine D2 receptor antagonist (sulpiride), a selective CB1 cannabinoid receptor antagonist/inverse agonist (AM281), and a potent and selective CB2 cannabinoid receptor inverse agonist (AM630), but it was not blocked by a nonselective adenosine receptor antagonist (caffeine) or a ß-adrenoceptor antagonist (propranolol). In summary, molecular docking suggests that CB1 and CB2 receptors are the most promising targets of terpineol action. Our data showed terpineol antidepressant-like modulation by CB1 and CB2 cannabinoid receptors and D2-dopaminergic receptors to further corroborate our molecular evidence.

Asunto(s)

Antiinflamatorios/uso terapéutico , Antidepresivos/uso terapéutico , Moduladores de Receptores de Cannabinoides/uso terapéutico , Depresión/tratamiento farmacológico , Dopaminérgicos/uso terapéutico , Monoterpenos/uso terapéutico , Animales , Sitios de Unión , Depresión/etiología , Suspensión Trasera/efectos adversos , Lipopolisacáridos/toxicidad , Masculino , Ratones , Simulación del Acoplamiento Molecular , Unión Proteica , Receptores de Cannabinoides/química , Receptores de Cannabinoides/metabolismo , Receptores de Dopamina D2/química , Receptores de Dopamina D2/metabolismo

RESUMEN

Cellulose nanofibers have mechanical properties that make them very attractive in a myriad of fields such as biomedicine, tissue engineering, biosensors, cosmetics and food packet products. To evaluate the potential health risks of airborne cellulose nanofibers, the cellulose nanofiber was prepared and characterized and then its pulmonary potential toxicity to a mouse model was studied. Cellulose nanofiber has been prepared by acid hydrolysis of cotton cellulose and characterized by transmission electron microscopy, zeta potential and X-ray diffraction analysis. Then, using a short-term inhalation test, the pulmonary biocompatibility of cotton cellulose nanofibers at different concentrations (0.5 mg/mL, 1 mg/mL and 2 mg/mL) were evaluated. Transmission electron images showed needle-shaped particle with a diameter of about 6-18 nm and a length of 85-225 µm. Zeta potential was -25.3±7.80 mV and the X-ray diffraction patterns indicate that cotton cellulose nanofiber has pure structural characteristics. The In Vivo results revealed that the exposure to cotton cellulose nanofiber did not alter the number of inflammatory cells or cytokine secretion by lung cells (p > 0.05). The results demonstrate that the cotton cellulose nanofiber is biocompatible and it is an environment-friendly nanomaterial with promise in various industrial sectors.

Asunto(s)

Nanofibras , Animales , Celulosa , Ratones , Microscopía Electrónica de Transmisión , Nanofibras/toxicidad , Textiles , Difracción de Rayos X

RESUMEN

Citral ((2E)-3,7-dimethylocta-2,6-dienal), a bioactive component of lemongrass, inhibits oxidant activity, nuclear factor kappa B (NF-κB) activation, and cyclooxygenase-2 (COX-2) expression, even as it activates peroxisome proliferator-activated receptor (PPAR)-α and γ. Additionally, citral produces long-lasting inhibition of transient receptor potential (TRP) channels that are found in sensory neurons, such as TRPV1-3 and TRPM8, while it transiently blocks TRPV4 and TRPA1. Here, the effect of citral in experimental models of acute inflammation and hyperalgesia in mice, and the underlying citral mechanisms of action were investigated. ADMET properties and molecular targets were predicted using the online server. The immunomodulatory and antihyperalgesic effects of citral were evaluated, using mechanical and thermal stimuli, at different time-points on carrageenan, lipopolysaccharides (LPS), and zymosan-induced paw edema and hyperalgesia in mice. ADMET analysis ensures that the citral has not violated Lipinski's rule of five, indicating its safety consumption, and molecular target prediction software identified that citral is a potential fatty acid amide hydrolase (FAAH) inhibitor. Oral treatment with citral (50-300 mg/kg) significantly inhibited carrageenan-induced paw edema and thermal allodynia. Furthermore, citral modulated the inflammation induced by LPS and zymosan, toll-like receptor (TLR) 4, and TLR2/dectin-1 ligands, respectively. Moreover, pretreatment with cannabinoid receptor type 2 (CB2R) antagonists and ATP-sensitive K+ channel inhibitor, but not with a cannabinoid receptor type 1 (CB1R) antagonist, significantly reversed the anti-inflammatory effect of citral. Intriguingly, citral did not cause any relevant action in the central nervous system, and it was safe when assessed in a 14 day toxicity assay in male mice. Therefore, citral constitutes a promising, innovative, and safe molecule for the management of immunoinflammatory conditions and pain states.

Asunto(s)

Monoterpenos Acíclicos/farmacología , Adenosina Trifosfato/química , Amidohidrolasas/química , Analgésicos/farmacología , Inflamación/metabolismo , Lectinas Tipo C/química , Monoterpenos/farmacología , Receptor Cannabinoide CB2/química , Receptor Toll-Like 4/química , Amidohidrolasas/metabolismo , Animales , Hiperalgesia/tratamiento farmacológico , Hiperalgesia/metabolismo , Inflamación/tratamiento farmacológico , Lectinas Tipo C/metabolismo , Ratones , Estructura Molecular , Monoterpenos/química , Receptor Cannabinoide CB2/uso terapéutico , Canales Catiónicos TRPV/química , Canales Catiónicos TRPV/metabolismo , Receptor Toll-Like 2

RESUMEN

BACKGROUND: Transdermal delivery is an alternative route for the administration of drugs. However, it requires the development of vehicles that allow the drugs to cross the layers of the skin and reach the systemic circulation. OBJECTIVE: In this study, a new transdermal vehicle was evaluated using progesterone, estradiol, estradiol + estriol (Biest) and ketoprofen administered as model drugs. METHODS: To evaluate the ex vivo permeation of the drugs, the Franz vertical diffusion cell with human skin was used. RESULTS: After 24 h, the vehicle was able to deliver 18.32 µg/cm2 of progesterone and 92.07 µg/cm2 of ketoprofen through the skin to the receptor medium. The permeation percentages were 91%, 78.8%, 48.5%, 73.2%, and 63.6%, respectively, for estradiol, estradiol (Biest), estriol (Biest), progesterone and ketoprofen. For all drugs, sufficient amounts were delivered to achieve a systemic effect, and it was also possible to decrease the amount of emulsion applied. CONCLUSION: Thus, the vehicle demonstrated a high performance and the possibility of it being used for drugs that present difficulties in regards to administration by the transdermal route.

Asunto(s)

Sistemas de Liberación de Medicamentos , Absorción Cutánea , Piel/metabolismo , Administración Cutánea , Adulto , Antiinflamatorios no Esteroideos/administración & dosificación , Combinación de Medicamentos , Estradiol/administración & dosificación , Estriol/administración & dosificación , Femenino , Humanos , Técnicas In Vitro , Cetoprofeno/administración & dosificación , Progesterona/administración & dosificación

RESUMEN

Gold nanoparticles (AuNP) were synthesized and modified with anti-folate receptor antibody (AB), folic acid (FA), crystal violet (CV), poly (ethyleneglycol) methyl ether thiol and the antineoplastic drug tamoxifen (TAM). Such a preparation was incubated in vitro with MCF-7 human breast cancer cells, showing a decrease in the TAM dosage for the reduction of cell viability. The adsorption of TAM on gold surface was investigated by surface-enhanced Raman scattering (SERS) spectroscopy and the assignment based on Density Functional Theory calculations showed that the ether moiety was involved in the interactions with the metal. Such a chemical affinity was correlated with the carrying of TAM in the biological media. CV was included in the preparation as a molecular probe for SERS spectroscopy, whose signal was monitored to analyse the efficiency of the modified AuNP in the target of neoplastic cells. The results showed AB, FA and TAM components had complementary roles in the cell recognition and, therefore, in the efficiency of the drug carrier nanosystem.

Asunto(s)

Antineoplásicos Hormonales/farmacología , Oro/química , Nanopartículas del Metal/química , Tamoxifeno/farmacología , Antineoplásicos Hormonales/química , Antineoplásicos Hormonales/metabolismo , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Células MCF-7 , Teoría Cuántica , Programas Informáticos , Espectrometría Raman , Propiedades de Superficie , Tamoxifeno/química , Tamoxifeno/metabolismo

RESUMEN

BACKGROUND: Green synthesis is an ecological technique for the production of well characterized metallic nanoparticles using plants. This study investigated the synthesis of silver nanoparticles (AgNPs) using a Caesalpinia ferrea seed extract as a reducing agent. METHODS: The formation of AgNPs was identified by instrumental analysis, including ultraviolet-visible (UV-Vis) spectroscopy, scanning electron microscopy (SEM), X-ray diffraction (XRD) of the AgNPs, and surface-enhanced Raman scattering (SERS) spectra of rhodamine-6G (R6G). We studied the physicochemical characterization of AgNPs, evaluated them as an antifungal agent against Candida albicans, Candida kruzei, Candida glabrata and Candida guilliermondii, and estimated their minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) values. Lastly, this study evaluated the cytotoxicity of the AgNPs in murine L929 fibroblasts cells using an MTT assay. RESULTS: The UV-Vis spectroscopy, SERS, SEM and XRD results confirmed the rapid formation of spheroidal 30-50 nm AgNPs. The MIC and MFC values indicated the antifungal potential of AgNPs against most of the fungi studied and high cell viability in murine L929 fibroblasts. In addition, this study demonstrated that C. ferrea seed extracts may be used for the green synthesis of AgNPs at room temperature for the treatment of candidiasis.

RESUMEN

BACKGROUND: Taxifolin (TAX) is a flavonoid that has numerous pharmacological properties, including an antioxidant ability superior to that of other flavonoids due to its particular structure. Nevertheless, it has low oral bioavailability, which limits its therapeutic application. In this context, potentially important approaches for systemic drug delivery could be by alternative routes such as skin and vaginal mucosa, once both routes have a variety of advantages compared with the oral route, including the ability to bypass both first-pass hepatic metabolism and the consequent degradation in the gastrointestinal tract. Vaginal delivery could also account for a local effect, or an effect on circumvent microregion. OBJECTIVE: The major objective of this study was to develop and validate a high-performance liquid chromatography (HPLC) method for the determination of TAX in a semisolid dosage forms and then to evaluate ex vivo permeations across porcine vaginal mucosa and human skin. METHODS: TAX was incorporated into an oil-in-water emulsion developed previously by our group. Method for quantification was developed and validated using HPLC. Permeation through human skin and vaginal porcine mucosa were conducted in Franz-type cells. RESULTS: The method was precise (CV < 5%), accurate (recovery between 98% and 102%), linear (R2> 0.99), specific, and robust. Permeation experiments through porcine vaginal mucosa and human skin presented permeated percentages equal to 87.43% and 48.09% (per dose), respectively. CONCLUSION: The results suggest that, in the matrixes studied, TAX may be able to exert its biological activities systemically when applied by these routes. Furthermore, it exhibits greater permeability potential when administered by intravaginal route.

Asunto(s)

Antiinflamatorios no Esteroideos/administración & dosificación , Membrana Mucosa/metabolismo , Quercetina/análogos & derivados , Crema para la Piel/administración & dosificación , Piel/metabolismo , Administración Tópica , Adulto , Animales , Antiinflamatorios no Esteroideos/farmacocinética , Cromatografía Líquida de Alta Presión/métodos , Emulsiones , Femenino , Humanos , Técnicas In Vitro , Permeabilidad , Quercetina/administración & dosificación , Quercetina/farmacocinética , Absorción Cutánea , Crema para la Piel/farmacocinética , Porcinos , Vagina

RESUMEN

Nitrogenated heterocyclic compounds are present in both natural and synthetic drugs, and hexahydropyrimidine derivatives may prove to be efficient in treating dermatomycosis causing fungi. This study evaluated the antifungal activity of four hexahydropyrimidine derivatives against the dermatomycosis causing fungi. These derivatives were synthesized, characterized, and assessed in terms of their activity against Trichophyton mentagrophytes, Microsporum canis, Microsporum gypseum, Trichophyton rubrum, Fusarium oxysporum, and Epidermophyton floccosum between concentrations 7.8 and 1,000 µg mL-1. Scanning electron micrographs were assessed for the active derivatives and reference drugs, and these micrographs revealed that new agents cause morphological changes in fungi. The derivatives HHP1, HHP3, and HHP4 revealed poor activity against the four fungal strains (MICs range 500-1000 µg mL-1). Compound HHP3 was found to be the best potential antifungal agent among those tested and was the most effective among all the active derivatives that caused morphological changes in the susceptible strains.

Asunto(s)

Antifúngicos/farmacología , Dermatomicosis/microbiología , Hongos/efectos de los fármacos , Pirimidinas/farmacología , Antifúngicos/síntesis química , Antifúngicos/química , Dermatomicosis/tratamiento farmacológico , Hongos/ultraestructura , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Pirimidinas/síntesis química , Pirimidinas/química

RESUMEN

Multi-walled carbon nanotubes (MWCNTs) have potential applications in the industrial, agricultural, pharmaceutical, medical, and environmental remediation fields. However, many uncertainties exist regarding the environmental implications of engineered nanomaterials. This study examined the effect of the MWCNTs on metabolic status and morphology of filamentous green microalgae Klebsormidium flaccidum. Appropriate concentrations of MWCNT (1, 50, and 100 µg mL-1) were added to a microalgal culture in the exponential growth phase and incubated for 24, 48, 72, and 96 h. Exposure to MWCNT led to reductions in algal growth after 48 h and decreased on cell viability for all experimental endpoints except for 1 µg mL-1 at 24 h and 100 µg mL-1 after 72 h. At 100 µg mL-1, MWCNTs induced reactive oxygen species (ROS) production and had an effect on intracellular adenosine triphosphate (ATP) content depending on concentration and time. No photosynthetic activity variation was observed. Observations by scanning transmission electron microscopy showed cell damage. In conclusion, we have demonstrated that exposure to MWCNTs affects cell metabolism and microalgal cell morphology. To our best knowledge, this is the first case in which MWCNTs exhibit adverse effects on filamentous green microalgae K. flaccidum. These results contribute to elucidate the mechanism of MWCNT nanotoxicity in the bioindicator organism of terrestrial and freshwater habitats.

Asunto(s)

Microalgas/fisiología , Nanotubos de Carbono/toxicidad , Contaminantes Químicos del Agua/toxicidad , Supervivencia Celular/efectos de los fármacos , Especies Reactivas de Oxígeno/metabolismo

RESUMEN

The pellucid zone (PZ) is a protective embryonic cells barrier against chemical, physical or biological substances. This put, usual transfection methods are not efficient for mammal oocytes and embryos as they are exclusively for somatic cells. Carbon nanotubes have emerged as a new method for gene delivery, and they can be an alternative for embryos transfection, however its ability to cross the PZ and mediated gene transfer is unknown. Our data confirm that multiwall carbon nanotubes (MWNTs) can cross the PZ and delivery of pDNA into in vitro-fertilized bovine embryos. The degeneration rate and the expression of genes associated to cell viability were not affected in embryos exposed to MWNTs. Those embryos, however, had lower cell number and higher apoptotic cell index, but this did not impair the embryonic development. This study shows the potential utility of the MWNT for the development of new method for delivery of DNA into bovine embryos.

Asunto(s)

Blastocisto/metabolismo , ADN/administración & dosificación , Técnicas de Transferencia de Gen , Nanotubos de Carbono , Animales , Bovinos , Técnicas de Cultivo de Célula , Células Cultivadas , Femenino , Genes Reporteros , Nanotubos de Carbono/química , Nanotubos de Carbono/ultraestructura , Técnicas de Transferencia Nuclear , Plásmidos/administración & dosificación , Plásmidos/genética , Embarazo

RESUMEN

Plant species are sources of active compounds that can fight and/or prevent damage caused by reactive oxygen species, which enables the development of natural products that can help to prevent premature aging caused by exposure to solar radiation. This study assessed the antioxidant and photoprotective activities of six dried extracts of plants from the Brazilian Amazon biome. Plant extracts were prepared in 70% (v/v) ethanol by dynamic maceration for 72h in the dark, and then filtered, concentrated and lyophilized. The extracts were subjected to a phytochemical screening. The antioxidant activity was measured using a 2,2-diphenyl-1-picrylhydrazyl assay and the photoprotection assay was performed using the diffuse transmittance technique. The data obtained from the antioxidant activity assay was evaluated by Student's t-test for independent samples, with the aid of Statistical Package for Social Sciences v.14.0 for Windows software. The flavonoids represent a special metabolites class present in all analyzed extracts. The antioxidant activity (µgmL(-1)) decreased in the following order: Aniba canelilla (1.80±0.16), Brosimum acutifolium (2.84±0.38), Dalbergia monetaria (5.46±0.17) or Caesalpinia pyramidalis (6.45±1.18), Arrabidaea chica (15.35±0.86), and Aspidosperma nitidum (99.14±2.3). Only D. monetaria showed a considerable sun protection factor allowing for labeling (6.0±0.3). The D. monetaria extract was considered the most promising sample because it had optimal antioxidant and photoprotective activities against solar radiation, considering the limit established by regulatory agencies. These extracts with antioxidant potential can be used in photoprotective formulations, providing synergistic photoprotective effect or elevating the adeed value of the product. Additionally, these formulations are attractive to a population who searchs for products made with natural ingredients.

Asunto(s)

Antioxidantes/química , Bignoniaceae/química , Extractos Vegetales/química , Protectores Solares/química , Bignoniaceae/metabolismo , Brasil , Hojas de la Planta/química , Hojas de la Planta/metabolismo , Factor de Protección Solar , Rayos Ultravioleta

RESUMEN

The objective of this study was to evaluate the feasibility of 10 commonly used active pharmaceutical ingredients (APIs) compounded in oral suspensions using an internationally used suspending vehicle (SyrSpend(®) SF PH4 liquid): (i) amlodipine, (as besylate) 1.0mg/mL; (ii) chloroquine phosphate,15.0 mg/mL; (iii) dapsone, 2.0 mg/mL; (iv) phenytoin, 15.0 mg/mL; (v) pyridoxine hydrochloride, 50.0 mg/mL; (vi) sulfadiazine, 100.0 mg/mL; (vii) sulfasalazine, 100.0 mg/mL; (viii) tetracycline hydrochloride, 25.0 mg/mL; (ix) trimethoprim, 10.0 mg/mL; and (x) zonisamide, 10.0 mg/mL. All suspensions were stored both at controlled refrigeration (2-8 °C) and controlled room temperature (20-25 °C). Feasibility was assessed by measuring the percent recovery at varying time points throughout a 90-day period. API quantification was performed by high-performance liquid chromatography (HPLC-UV), via a stability-indicating method. Given the percentage of recovery of the APIs within the suspensions, the expiration date of the final products (API+vehicle) was at least 90 days for all suspensions with regard to both the controlled temperatures. This suggests that the vehicle is stable for compounding APIs from different pharmacological classes.

Asunto(s)

Estabilidad de Medicamentos , Almacenaje de Medicamentos/métodos , Suspensiones/análisis , Suspensiones/normas , Administración Oral , Amlodipino/análisis , Amlodipino/normas , Cloroquina/análogos & derivados , Cloroquina/análisis , Cloroquina/normas , Cromatografía Líquida de Alta Presión/métodos , Dapsona/análisis , Dapsona/normas , Almacenaje de Medicamentos/normas , Estudios de Factibilidad , Concentración de Iones de Hidrógeno , Isoxazoles/análisis , Isoxazoles/normas , Fenitoína/análisis , Fenitoína/normas , Piridoxina/análisis , Piridoxina/normas , Sulfadiazina/análisis , Sulfadiazina/normas , Sulfasalazina/análisis , Sulfasalazina/normas , Tetraciclina/análisis , Tetraciclina/normas , Trimetoprim/análisis , Trimetoprim/normas , Zonisamida

RESUMEN

Reduced phospholipase A2 (PLA2) activity has been reported in blood cells and in postmortem brains of patients with Alzheimer disease (AD), and there is evidence that conjugated linoleic acid (CLA) modulates the activity of PLA2 groups in non-brain tissues. As CLA isomers were shown to be actively incorporated and metabolized in the brains of rats, we hypothesized that feeding a diet naturally enriched in CLA would affect the activity and expression of Pla 2 -encoding genes in rat brain tissue, with possible implications for memory. To test this hypothesis, Wistar rats were trained for the inhibitory avoidance task and fed a commercial diet (control) or experimental diets containing either low CLA- or CLA-enriched butter for 4 weeks. After this period, the rats were tested for memory retrieval and killed for tissue collection. Hippocampal expression of 19 Pla 2 genes was evaluated by qPCR, and activities of PLA2 groups (cPLA2, iPLA2, and sPLA2) were determined by radioenzymatic assay. Rats fed the high CLA diet had increased hippocampal mRNA levels for specific PLA2 isoforms (iPla 2 g6γ; cPla 2 g4a, sPla 2 g3, sPla 2 g1b, and sPla 2 g12a) and higher enzymatic activity of all PLA2 groups as compared to those fed the control and the low CLA diet. The increment in PLA2 activities correlated significantly with memory enhancement, as assessed by increased latency in the step-down inhibitory avoidance task after 4 weeks of treatment (rs = 0.69 for iPLA2, P < 0.001; rs = 0.81 for cPLA2, P < 0.001; and rs = 0.69 for sPLA2, P < 0.001). In face of the previous reports showing reduced PLA2 activity in AD brains, the present findings suggest that dairy products enriched in cis-9, trans-11 CLA may be useful in the treatment of this disease.

Asunto(s)

Mantequilla , Dieta , Hipocampo/metabolismo , Ácidos Linoleicos Conjugados , Memoria/fisiología , Fosfolipasas A2/genética , Enfermedad de Alzheimer/dietoterapia , Alimentación Animal , Animales , Reacción de Prevención/fisiología , Masculino , Fosfolipasas A2/metabolismo , Reacción en Cadena de la Polimerasa , Pruebas Psicológicas , ARN Mensajero/genética , ARN Mensajero/metabolismo , Radioinmunoensayo , Ratas Wistar , Regulación hacia Arriba

RESUMEN

Studies have been demonstrating that smaller particles can lead to unexpected and diverse ecotoxicological effects when compared to those caused by the bulk material. In this study, the chemical composition, size and shape, state of dispersion, and surface's charge, area and physicochemistry of micro (BT MP) and nano barium titanate (BT NP) were determined. Green algae Chlorella vulgaris grown in Bold's Basal (BB) medium or Seine River water (SRW) was used as biological indicator to assess their aquatic toxicology. Responses such as growth inhibition, cell viability, superoxide dismutase (SOD) activity, adenosine-5-triphosphate (ATP) content and photosynthetic activity were evaluated. Tetragonal BT (~170 nm, 3.24 m(2) g(-1) surface area) and cubic BT (~60 nm, 16.60 m(2) g(-1)) particles were negative, poorly dispersed, and readily aggregated. BT has a statistically significant effect on C. vulgaris growth since the lower concentration tested (1 ppm), what seems to be mediated by induced oxidative stress caused by the particles (increased SOD activity and decreased photosynthetic efficiency and intracellular ATP content). The toxic effects were more pronounced when the algae was grown in SRW. Size does not seem to be an issue influencing the toxicity in BT particles toxicity since micro- and nano-particles produced significant effects on algae growth.

Asunto(s)

Compuestos de Bario/toxicidad , Chlorella vulgaris/efectos de los fármacos , Chlorella vulgaris/fisiología , Nanopartículas del Metal/toxicidad , Titanio/toxicidad , Contaminantes Químicos del Agua/toxicidad , Francia

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Pterodon emarginatus Vogel is a medicinal plant commonly used in Brazilian traditional medicine as a folk therapy due to its immunosuppressive, anti-inflammatory, anti-rheumatic, healing, tonic and depurative activities. The essential oil (EO) of Pterodon emarginatus is composed of volatile aromatic terpenes and phenyl propanoids, mainly, ß-elemene and ß-caryophyllene sesquiterpenes. Here we reported the effects and some underlying mechanisms of action of EO during murine model of MS, the experimental autoimmune encephalomyelitis (EAE). MATERIALS AND METHODS: EO (50 and 100 mg/kg) was orally administered during the entire period of development of EAE (preventive treatment, day 0-25). In vitro and in vivo immunological responses were evaluated by ELISA, immunohistochemistry, immunofluorescence and flow cytometry. RESULTS: We provide evidence that EO of Pterodon emarginatus (100 mg/kg, p.o.) significantly attenuates neurological signs and also the development of EAE. Furthermore, at the same dose EO consistently inhibited Th1 cell-mediated immune response and upregulated Treg response in vitro. Moreover, the EO inhibited both microglial activation and expression of iNOS, associated with inhibition of axonal demyelization and neuronal death during the development of the disease. CONCLUSION: This is the first experimental evidence showing that oral administration of EO consistently reduces and limits the severity and development of EAE, mainly, through the modulation of Th1/Treg immune balance, and might represent a helpful new tool for control immunoinflammatory conditions, such as MS.

Asunto(s)

Encefalomielitis Autoinmune Experimental/tratamiento farmacológico , Fabaceae/química , Aceites Volátiles/farmacología , Células TH1/inmunología , Animales , Brasil , Relación Dosis-Respuesta a Droga , Encefalomielitis Autoinmune Experimental/inmunología , Encefalomielitis Autoinmune Experimental/fisiopatología , Ensayo de Inmunoadsorción Enzimática , Femenino , Citometría de Flujo , Medicina Tradicional , Ratones , Ratones Endogámicos C57BL , Aceites Volátiles/administración & dosificación , Aceites Volátiles/aislamiento & purificación , Semillas , Índice de Severidad de la Enfermedad , Linfocitos T Reguladores/inmunología

RESUMEN

Dermatophytoses are mycoses that affect keratinized tissues in both humans and animals. The aim of this study was to investigate the antifungal activity of the oleoresin extracted from Copaifera langsdorffii Desf. against the strains Microsporum canis ATCC 32903, Microsporum gypseum ATCC 14683, Trichophyton mentagrophytes ATCC 11481 and Trichophyton rubrum CCT 5507. The antimicrobial activity was determined by minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) values. Ketoconazole and terbinafine were used as reference drugs. The copaiba oleoresin showed moderate fungicidal activity against T. mentagrophytes ATCC 11481 (MIC and MFC = 170 µg mL-1) and weak fungicidal activity against T. rubrum CCT 5507 (MIC = 1,360 µg mL-1 and MFC = 2,720 µg mL-1). There was no activity against M. canis ATCC 32903 and M. gypseum ATCC 14683. SEM analysis revealed physical damage and morphological alterations such as compression and hyphae clustering in the structure of the fungi exposed to the action of the oleoresin. The results stimulate the achievement of in vivo assays to confirm the benefits of the application of oleoresin extracted from copaiba in the treatment of dermatophytosis, both in humans and in animals.

Asunto(s)

Antifúngicos/farmacología , Arthrodermataceae/efectos de los fármacos , Fabaceae/química , Extractos Vegetales/farmacología , Antifúngicos/química , Arthrodermataceae/ultraestructura , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química

RESUMEN

Currently, the research and development of sunscreens play an important role on the synthesis of actives that are stable in various kinds of formulations-in addition to their efficiency and broad spectrum of protection against ultraviolet radiation. Our objective here was to synthesize new sunscreening chemical agents using quinoline as a base molecule. Twelve quinoline derivatives were synthesized, four of them novel molecules, and their photoprotective activity was determined in vitro using diffuse transmittance spectrophotometry. We determined their SPF, UVAPF, UVA/UVB ratio, critical wavelength and Boots Star Rating. The quinolines derivatives presented a varied profile of photoprotection, their SPF ranging from 2 to 11 and their UVAPF from 2 to 7. In terms of the critical wavelength, all molecules were considered of broad-spectrum by different classifications. Regarding the Boots Star Rating, one compound received no rating, seven of them received a three stars rating, three received a four stars rating and three were given a five stars rating. The molecules showed in the present work have a wide range of possibilities for creating new sunscreen products, once they have good SPF or UVAPF for single molecules, and they also possess other different qualities that can act synergistically.

Asunto(s)

Quinolinas/síntesis química , Protectores Solares/síntesis química , Química Farmacéutica , Estructura Molecular , Quinolinas/química , Espectrofotometría , Protectores Solares/química

RESUMEN

Resveratrol has been extensively researched for its powerful antioxidant capacity and other biological effects. The number of patents involving this compound has been growing in recent years. However, the biggest problem associated with this molecule, a limited bioavailability due to its fast metabolism in the liver, has led to obtaining its analogues or derivatives. In this work, we selected patents which describe the application of the antioxidant activity of resveratrol and its analogues as food for the human segment.

Asunto(s)

Antioxidantes/farmacología , Dieta , Suplementos Dietéticos , Patentes como Asunto , Extractos Vegetales/farmacología , Estilbenos/farmacología , Disponibilidad Biológica , Humanos , Resveratrol

RESUMEN

Pterodon emarginatus Vogel, Fabaceae, is a native aromatic tree distributed by central region of Brazil. Hydroalcoholic infusions of the seeds are used in folk medicine for their anti-rheumatic and anti-inflammatory properties. The objective of this work was identified the chemical components and verify the cytotoxic effect of the essential oil (EO) from P. emarginatus seeds. Thus, the EO of P. emarginatus seeds was analyzed by GC/MS analysis followed by brine shrimp lethality test and cytotoxic activity against tumor cell lines and human peripheral mononuclear blood cells (PBMC). The cancer cell lines tested were C6 (rat glioma), MeWo (human melanoma), CT26.WT (mouse colon carcinoma), MDA (human breast cancer), A549 (human lung carcinoma), B16-F1 (mouse melanoma), CHO-K1 (hamster ovary cell) and BHK-21 (hamster kidney fibroblast). Eleven compounds were identified by GC and CG/MS analyses. The main compounds with concentrations higher than 5% were β-elemene (15.3%), trans-caryophyllene (35.9%), α-humulene (6.8%), germacrene-D (9.8%), bicyclo germacrene (5.5%) and spathulenol (5.9%). The EO of P. emarginatus seeds showed toxicity to Artemia salina (LC50 1.63 µg/mL) and was active against all the cell lines tested. The potent cytotoxic activity had IC50 values ranging from 24.9 to 47 µg/mL. However, EO (1-100 µg/mL) had less cytotoxicity in PBMCs isolated from a healthy subject. In summary, the present study showed the potential antiproliferative of the EO of P. emarginatus seeds.