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1.
Neurochem Res ; 47(7): 1888-1903, 2022 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-35426598

RESUMEN

This study aimed to evaluate the effect of Cynara cardunculus leaf ethanol extract on inflammatory and oxidative stress parameters in the hypothalamus, prefrontal cortex, hippocampus, striatum, cerebral cortex and liver of high-fat diet-induced obese mice. Food intake, body weight, visceral fat weight, and liver weight were also evaluated. Male Swiss mice were divided into control (low-fat purified diet) and obese (high-fat purified diet) groups. After 6 weeks, mice were divided into control + saline, control + C. cardunculus leaf ethanol extract, obese + saline, obese + C. cardunculus leaf ethanol extract. Cynara cardunculus leaf ethanol extract (1600 mg/kg/day) or saline was administered orally for 4 weeks. Brain structures (hypothalamus, hippocampus, prefrontal cortex, striatum and cerebral cortex) and liver were removed. Treatment with C. cardunculus leaf ethanol extract did not affect body weight but did reduce visceral fat. Obesity can cause inflammation and oxidative stress and increase the activity of antioxidant enzymes in brain structures. Treatment with ethanolic extract of C. cardunculus leaves partially reversed the changes in inflammatory damage parameters and oxidative damage parameters and attenuated changes in the antioxidant defense. The C. cardunculus leaf ethanol extract benefited from the brains of obese animals by partially reversing the changes caused by the consumption of a high-fat diet and the consequent obesity. These results corroborate those of studies indicating that the C. cardunculus leaf ethanol extract can contribute to the treatment of obesity.


Asunto(s)
Cynara scolymus , Cynara , Animales , Antioxidantes/farmacología , Cynara/química , Cynara scolymus/química , Dieta Alta en Grasa/efectos adversos , Modelos Animales de Enfermedad , Etanol/efectos adversos , Masculino , Ratones , Obesidad/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Hojas de la Planta/química
2.
Acta Trop ; 230: 106395, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35278367

RESUMEN

Piperine is an alkaloid extracted from the seed of Piper spp., which has demonstrated a larvicidal effect against Ae. aegypti. The incorporation of piperine into nanostructured systems can increase the effectiveness of this natural product in the control of Ae. aegypti larvae. In this study, we evaluated the effectiveness of piperine loaded or not into two nanostructured systems (named NS-A and NS-B) prepared by the nanoprecipitation method. The Ae. aegypti larvae were exposed to different concentrations of piperine loaded or not (2 to 16 ppm) and the mortality was investigated after 24, 48, and 72 hours. The nanostructures prepared were spherical in shape with narrow size distribution and great encapsulation efficiency. The lethal concentration 50 (LC50) for non-loaded piperine were 13.015 ppm (24 hours), 8.098 ppm (48 hours), and 7.248 ppm (72 hours). The LC50 values found for NS-A were 35.378 ppm (24 hours), 12.091 ppm (48 hours), and 8.011 ppm (72 hours), whereas the values found for NS-B were 21.267 ppm (24 hours), 12.091 ppm (48 hours), and 8.011 ppm (72 hours). Collectively, these findings suggested that non-loaded piperine caused higher larval mortality in the first hours of exposure while the nanostructured systems promoted the slow release of piperine and thereby increased the larvicidal activity over time. Therefore, loading piperine into nanostructured systems might be an effective tool to improve the larval control of vector Ae. aegypti.


Asunto(s)
Aedes , Alcaloides , Insecticidas , Nanoestructuras , Alcaloides/farmacología , Animales , Benzodioxoles , Insecticidas/farmacología , Larva , Mosquitos Vectores , Piperidinas , Extractos Vegetales/química , Polímeros , Alcamidas Poliinsaturadas
3.
Drug Dev Ind Pharm ; 47(10): 1556-1567, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-34821528

RESUMEN

The use of polymeric blends is a potential strategy to obtain novel nanotechnological formulations aiming at drug delivery systems. Saquinavir, an antiretroviral drug, was chosen as a model drug for the development of new stable liquid formulations with unpleasant taste masking properties. Three formulations containing different polymeric ratios (1:3, 1:1 and 3:1) were prepared and properly characterized by particle size distribution, zeta potential, pH, drug content and encapsulation efficiency measurements. The stability was verified by monitoring the zeta potential, particle size distribution, polydispersity index and drug content by 90 days. The light backscattering analysis was used to early identify possible phenomena of instability in the formulations. The in vitro drug release and saquinavir cytotoxicity were evaluated. The in vitro and in vivo taste masking properties were studied using an electronic tongue and a human sensory panel. All formulations presented nanometric sizes around 200 nm and encapsulation efficiency above 99%. The parameters evaluated for stability remained constant throughout 90 days. The in vitro tests showed a controlled drug release and absence of toxic effects on human T lymphocytes. The electronic tongue experiment showed taste differences for all formulations in comparison to drug solutions, with a more pronounced difference for the formulation with higher polycaprolactone content (3:1). This formulation was chosen for in vivo sensory panel evaluation which results corroborated the electronic tongue experiments. In conclusion, the polymer blend nanoformulation developed herein showed the promising application to incorporate drugs aiming at pharmaceutical taste-masking properties.


Asunto(s)
Saquinavir , Gusto , Humanos , Preparaciones Farmacéuticas/química , Poliésteres , Polímeros , Saquinavir/farmacología
4.
Mater Sci Eng C Mater Biol Appl ; 120: 111392, 2021 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-33545808

RESUMEN

In this study, we performed two experiments. In the first experiment, the objective was to link gold nanoparticles (GNPs) with sodium diclofenac and/or soy lecithin and to determine their concentration in tissues and their toxicity using hepatic and renal analyzes in mice to evaluate their safety as therapeutic agents in the subsequent treatment of obesity. In the second experiment, we evaluated the effect of GNPs on inflammatory and biochemical parameters in obese mice. In the first experiment, we synthesized and characterized 18 nm GNPs that were administered intraperitoneally in isolation or in association with sodium diclofenac and/or soy lecithin in mice once daily for 1 or 14 days. Twenty-four hours after the single or final administration, the animals were euthanized, following which the tissues were removed for evaluating the concentration of GNPs, and serum samples were collected for hepatic and renal analysis. Hepatic damage was evaluated based on the levels of alanine aminotransferase (ALT), whereas renal damage was evaluated based on creatinine levels. A higher concentration of GNPs was detected in the tissues upon administration for 14 days, and there were no signs of hepatic or renal damage. In the second experiment, the mice were used as animal models of obesity and were fed a high-fat diet (obese group) and control diet (control group). After eight weeks of high-fat diet administration, the mice were treated with saline or with GNPs (average size of 18 nm) at a concentration of 70 mg/L (70 mg/kg) once a day, for 14 days, for 10 weeks. Body weight and food intake were measured frequently. After the experiment ended, the animals were euthanized, serum samples were collected for glucose and lipid profile analysis, the mesenteric fat content was weighed, and the brains were removed for inflammatory and biochemical analysis. In obese mice, although GNP administration did not reduce body and mesenteric fat weight, it reduced food intake. The glucose levels were reversed upon administration of GNPs, whereas the lipid profile was not altered in any of the groups. GNPs exerted a beneficial effect on inflammation and oxidative stress parameters, without reverting mitochondrial dysfunction. Our results indicate that the intraperitoneal administration of GNPs for 14 days results in a significant GNP concentration in adipose tissues, which could be an interesting finding for the treatment of inflammation associated with obesity. Based on the efficacy of GNPs in reducing dietary intake, inflammation, and oxidative stress, they can be considered potential alternative agents for the treatment of obesity.


Asunto(s)
Oro , Nanopartículas del Metal , Animales , Encéfalo , Oro/metabolismo , Hígado/metabolismo , Nanopartículas del Metal/toxicidad , Ratones , Obesidad/tratamiento farmacológico , Estrés Oxidativo
5.
An Acad Bras Cienc ; 92(1): e20180793, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32401835

RESUMEN

The therapeutic effects from Citrus reticulata on painful inflammatory ailments are associated to its flavonoids constituent and phytochemical studies with Citrus genus affirm that the peels have important amounts of it. These bioactive compounds have been a considerable therapeutic source and evaluate potential application of the peel extract is significant. This research aims to investigate the influence of ethanolic crude extract from the peels of Citrus reticulata and its possible mechanism of action in different animal models of pain. The extract reduced hyperalgesia in the second phase of formalin test (vehicle: 501.5 ± 40.0 s; C. reticulata extract 300 mg/kg: 161.8 ± 41.1 s), in the carrageenan model (vehicle at 4th h: 82.5 ± 9.6 %; C. reticulata extract 300 mg/kg at 4th h: 47.5 ± 6.5 %) and in Complete Freund's Adjuvant model (vehicle: 501.5 ± 40.0 s; C. reticulata extract 300 mg/kg: 161.8 ± 41.1 s). The possible contribution of opioidergic and adenosinergic systems in the anti-hyperalgesic effect of C. reticulata extract was observed after treatment, with non-selective antagonists for both systems, which produced reversal effects. In conclusion, these properties of C. reticulata extract suggest a potential therapeutic benefit in treating painful conditions.


Asunto(s)
Analgésicos/farmacología , Citrus/química , Hiperalgesia/tratamiento farmacológico , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Carragenina , Evaluación Preclínica de Medicamentos , Etanol , Masculino , Ratones , Dimensión del Dolor , Fitoquímicos/análisis , Fitoquímicos/uso terapéutico , Extractos Vegetales/uso terapéutico
6.
J Parasit Dis ; 44(1): 79-87, 2020 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-32174708

RESUMEN

Cutaneous leishmaniasis (CL), a clinical condition caused mainly by Leishmania amazonensis in Brazil, is characterized by topical, painless ulcers. The current treatment, based on intravenous administration of pentavalent antimonials, presents low adherence by patients and may cause serious adverse effects, leading to the need for searching new therapeutic options. Thus, this study aimed at evaluating a topical administration of "intelligent dressings" as an alternative treatment for CL. BALB/c mice were infected with L. amazonensis promastigotes. Afterward, lesions were treated with hydrophobic dressings incorporated with clinically used drugs. After lesion development, the following analyses were carried out: measurement of lesion diameters, biochemical analyses of serum, evaluation of the recovery of amastigote forms and histological analyses. No significant clinical changes in serum parameters were observed. The group that was treated with dressings impregnated with Glucantime® displayed the lowest number of amastigotes recovered from tissues (parasite load). Conventional treatment with Glucantime® (i.p.) was also able to reduce parasite load. After 6 weeks from the measurement of the lesions mice treated with dressings impregnated with Pentamidine displayed the smallest values. Representative histological aspects of the lesions showed the absence or few amastigotes inside the macrophages when mice were treated with dressings impregnated with Glucantime® and Pentamidine, respectively. The findings presented here indicate that the topical treatments may constitute an alternative treatment option for CL.

7.
J Drug Target ; 28(4): 428-436, 2020 04.
Artículo en Inglés | MEDLINE | ID: mdl-31594390

RESUMEN

Herein, we report the effect of gold nanoparticles (AuNP) and n-acetylcysteine (NAC) isolated or in association as important anti-inflammatory and antioxidant compounds on brain dysfunction in septic rats. Male Wistar rats after sham operation or caecal ligation and perforation (CLP) were treated with subcutaneously injection of AuNP (50 mg/kg) and/or NAC (20 mg/kg) or saline immediately and 12 h after surgery. Twenty-four hours after CLP, hippocampus and prefrontal cortex were obtained and assayed for myeloperoxidase (MPO) activity, cytokines, lipid peroxidation, protein carbonyls formation, mitochondrial respiratory chain, and CK activity. AuNP + NAC association decreased MPO activity and pro-inflammatory cytokines production, being more effective than NAC or AuNP isolated treatment. AuNP + NAC association and NAC isolated treatment decreased oxidative stress to lipids in both brain structures, while protein oxidation decreased only in the hippocampus of AuNP + NAC association-treated animals. Complex I activity was increased with AuNP + NAC association and NAC isolated in the hippocampus. Regarding CK activity, AuNP and AuNP + NAC association increased this marker in both brain structures after CLP. Our data provide the first experimental demonstration that AuNP and NAC association was able to reduce sepsis-induced brain dysfunction in rats by decreasing neuroinflammation, oxidative stress parameters, mitochondrial dysfunction and CK activity.


Asunto(s)
Acetilcisteína/metabolismo , Oro/farmacología , Nanopartículas del Metal/administración & dosificación , Sepsis/tratamiento farmacológico , Animales , Antioxidantes/metabolismo , Citocinas/metabolismo , Modelos Animales de Enfermedad , Hipocampo/efectos de los fármacos , Hipocampo/metabolismo , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Masculino , Mitocondrias/efectos de los fármacos , Mitocondrias/metabolismo , Oxidación-Reducción/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Peroxidasa/metabolismo , Ratas , Ratas Wistar , Sepsis/metabolismo
8.
PLoS One ; 14(5): e0217718, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31150479

RESUMEN

This study aimed to evaluate the potential adverse effects of the dermal administration of Dillenia indica Linnaeus (D. indica) fruit extract in healthy rodents; the extract was standardized to betulinic acid. In the initial phase, the acute effects were evaluated on the skin application site of a single extract dose. A skin irritation test was performed in male Wistar rats (n = 8/group) receiving the extract (50-150 mg/mL) with betulinic acid (0.5-1.5%, respectively). A photosensitivity test was performed in male BALB/c mice (n = 6/group) receiving the extract (150 mg/mL). Afterwards, other BALB/c mice (n = 20, male:female, 1:1) were used to assess the systemic alterations caused by 14 daily repeated doses (150 mg/mL) by monitoring the effects on mortality, body morphology, behavior, nutrition status, neuromotor reactions, organ morphology and weight, and blood tests. At this time, 0.5 mg/mL clobetasol was used as the positive control. The skin irritation index suggested that negligible skin irritation had occurred, even when the extract was applied to the rat skin at 150 mg/mL. However, the extract acted as a photosensitizer on mouse skin, showing a photosensitizing activity close to that of 10 mg/mL 5-methoxypsoralen. Repeated doses caused no mouse mortality, aggressiveness, piloerection, diarrhea, convulsions, neuromotor alterations or nutrition status changes. The mouse organ weights did not change, and the mice did not have alterations in their blood compositions. Clobetasol caused a reduction in the mononuclear leukocyte numbers. In general, the data suggest that the extract was safe in healthy rodents but indicate that caution should be taken with the photosensitizing activity; in addition, this activity should be further explored as it may be useful for phototherapeutic drug development.


Asunto(s)
Clobetasol/farmacología , Dilleniaceae/química , Fármacos Fotosensibilizantes/farmacología , Piel/efectos de los fármacos , Administración Cutánea , Animales , Frutas/química , Humanos , Leucocitos Mononucleares/efectos de los fármacos , Ratones , Triterpenos Pentacíclicos , Fármacos Fotosensibilizantes/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Ratas , Pruebas de Irritación de la Piel , Triterpenos/química , Triterpenos/farmacología , Ácido Betulínico
9.
Carbohydr Polym ; 206: 362-370, 2019 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-30553333

RESUMEN

A smart wound dressing based on carrageenan (κC), locust bean gum (LBG), and cranberry extract (CB) for monitoring bacterial wound infections was developed and characterized using UV-vis spectroscopy, FT-IR, and SEM. The mechanical, swelling, cytotoxic and pH sensor properties were also investigated. UV-vis spectra demonstrated that the obtained κC:LBG:CB hydrogel film exhibited a visible change of colors as it was immersed in PBS solution pH 5.0, 7.3 and 9.0. The spectra of FT-IR suggested that chemical interactions had occurred between κC and CB extract. The obtained κC:LBG:CB hydrogel film exhibited adequate mechanical properties and a swelling behavior dependent on pH. Cytotoxicity tests indicated that κC:LBG:CB hydrogel film had dose-dependent cytotoxicity against NIH 3T3 fibroblast cells. The in vitro studies using Staphylococcus aureus and Pseudomonas aeruginosa demonstrated that the color changes of the κC:LBG:CB hydrogel film could be observed by naked eyes, confirming the potential use of the obtained hydrogel film as a visual system for monitoring bacterial wound infections.


Asunto(s)
Infecciones Bacterianas/diagnóstico , Vendajes , Hidrogeles/química , Indicadores y Reactivos/farmacología , Extractos Vegetales/farmacología , Infección de Heridas/diagnóstico , Animales , Antocianinas/química , Antocianinas/farmacología , Antocianinas/toxicidad , Antibacterianos/química , Antibacterianos/farmacología , Antibacterianos/toxicidad , Carragenina/química , Carragenina/toxicidad , Color , Módulo de Elasticidad , Galactanos/química , Galactanos/toxicidad , Hidrogeles/toxicidad , Concentración de Iones de Hidrógeno , Indicadores y Reactivos/química , Indicadores y Reactivos/toxicidad , Mananos/química , Mananos/toxicidad , Ratones , Células 3T3 NIH , Extractos Vegetales/química , Extractos Vegetales/toxicidad , Gomas de Plantas/química , Gomas de Plantas/toxicidad , Pseudomonas aeruginosa/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Resistencia a la Tracción , Vaccinium macrocarpon/química
10.
An Acad Bras Cienc ; 90(4): 3249-3264, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30517213

RESUMEN

Stevia (stevia rebaudiana Bertoni) is a species characterized by producing non-caloric substances with high sweetening potential. Among these substances, rebaudioside A and stevioside are produced in greater quantity. Plant density and harvesting time are factors that affects biomass and sweetening compounds yield in this species. The objective of this research was to evaluate the effect of plant densities and harvesting times on the productive and physiological characteristics of stevia in southern Brazil. The experimental design was in randomized blocks, in a split-plot scheme, with 9 treatments comparing the effect of three planting densities (166 667, 83 333 and 33 333 plants ha-1) in the plots and three harvesting periods (before, in the beginning and in full flowering) in the subplots. Harvesting at the beginning of flowering promoted higher dry leaf biomass yield and, when associated with the lowest planting density, promoted higher levels of rebaudioside A and stevioside. The lowest planting density resulted in greater leaves biomass accumulation, whereas the highest density promoted higher yields per area. Interaction between density of 166 667 plants ha-1 and the harvest at the onset of flowering promoted higher yields of rebaudioside A (43.22 kg ha-1) as well as higher rebaudioside A/stevioside ratio (0.60).


Asunto(s)
Agricultura/métodos , Biomasa , Diterpenos de Tipo Kaurano/análisis , Glucósidos/análisis , Hojas de la Planta/crecimiento & desarrollo , Stevia/química , Stevia/crecimiento & desarrollo , Brasil , Estaciones del Año
11.
Int J Biol Macromol ; 113: 51-58, 2018 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-29471089

RESUMEN

This manuscript was focused on introducing a facile, green and scalable method to produce kappa-carrageenan (κC) hydrogel membranes containing in situ synthesized silver nanoparticles (AgNPs). In a typical protocol, κC hydrogels were obtained by heating (sol phase), followed by cooling (gel phase) the polysaccharide solution, which enabled the simultaneous synthesis of AgNPs during the heating time. The as synthesized AgNPs were characterized spectrophotometrically, and by dynamic light scattering and transmission electron microscopy. The swelling properties at different pH and the antimicrobial activity of κC-AgNP hydrogel were investigated. AgNPs were mostly spherical in shape, crystalline in nature and measuring ca. 27nm in diameter. The in situ synthesis of AgNPs changed the swelling properties of κC hydrogel and also reduces its viscosity and gelling temperature. The AgNPs were continuously released from κC hydrogel for up to 48h in a concentration sufficient to prevent the bacterial growth as confirmed by antimicrobial tests. The simplicity involved in the AgNPs synthesis combined to the good spreadability of κC hydrogel makes this method suitable for scale-up to manufacturing quantities of wound dressing.


Asunto(s)
Vendajes , Carragenina/química , Hidrogeles/química , Nanopartículas del Metal/química , Plata/química , Cicatrización de Heridas , Antibacterianos/química , Antibacterianos/farmacología , Vendajes/microbiología , Tecnología Química Verde , Concentración de Iones de Hidrógeno , Pruebas de Sensibilidad Microbiana , Tamaño de la Partícula
12.
Mater Sci Eng C Mater Biol Appl ; 76: 365-373, 2017 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-28482539

RESUMEN

This paper discusses the feasibility of using membranes based on cellulose acetate butyrate/poly(caprolactone)triol loaded with doxycycline for guided bone regeneration. Those membranes were obtained by solvent casting varying the cellulose acetate butyrate: poly(caprolactone)triol:doxycycline (CAB:PCL-T:DOX) mass ratios and characterized by scanning electron microscopy, differential scanning calorimetry, dynamical mechanical analysis, swelling and weight loss, drug release, in vitro antimicrobial activity and in vivo inflammatory response. Neat CAB and CAB:PCL-T:DOX membranes exhibited inner porous structure, which has a pore-size reduced with increasing of the PCL-T ratio. DSC results demonstrated that the molecular dispersion of the DOX into the CAB:PCL-T membrane was conditioned by PCL-T amount. Elastic modulus reduced noticeably with increased of the PCL-T ratio in the membrane from 2 to 3, while the strain at failure showed an increase of ca. 10-fold on the same condition. The DOX release mechanism from the membranes was found to be Fickian or quasi-Fickian diffusion. Membranes assessed immediately after the preparation, and even as the membranes immersed in synthetic saliva during 7 days, demonstrated significant inhibition in the growth of Staphylococcus aureus and Escherichia coli. Subcutaneous implant test on rat in vivo showed that the CAB:PCL-T:DOX membrane (7:3:1) did not trigger chronic inflammatory responses. These results suggest the feasibility in applying the CAB:PCL-T:DOX membrane as a barrier for guided bone regeneration.


Asunto(s)
Regeneración Ósea , Animales , Butiratos , Caproatos , Celulosa/análogos & derivados , Doxiciclina , Lactonas , Poliésteres , Ratas , Staphylococcus aureus
13.
J Ethnopharmacol ; 204: 179-188, 2017 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-28412216

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Casearia sylvestris Sw. is widely used in popular medicine to treat conditions associated with pain. AIM OF THE STUDY: The present study investigated the influence of hydroalcoholic crude extract of Casearia sylvestris (HCE-CS) and contribution of pro-resolving mediators on mechanical hyperalgesia in a mouse model of chronic post-ischemia pain (CPIP). METHODS AND RESULTS: Male Swiss mice were subjected to ischemia of the right hind paw (3h), then reperfusion was allowed. At 10min, 24h or 48h post-ischemia/reperfusion (I/R), different groups of animals were treated with HCE-CS (30mg/Kg, orally [p.o]), selected agonists at the pro-resolving receptor ALX/FPR2 (natural molecules like resolvin D1 and lipoxin A4 or the synthetic compound BML-111; 0.1-1µg/animal) or vehicle (saline, 10mL/Kg, s.c.), in the absence or presence of the antagonist WRW4 (10µg, s.c.). Mechanical hyperalgesia (paw withdrawal to von Frey filament) was asseseed together with histological and immunostainning analyses. In these settings, pro-resolving mediators reduced mechanical hyperalgesia and HCE-CS or BML-111 displayed anti-hyperalgesic effects which was markedly attenuated in animals treated with WRW4. ALX/FPR2 expression was raised in skeletal muscle or neutrophils after treatment with HCE-CS or BML-111. CONCLUSION: These results reveal significant antihyperalgesic effect of HCE-CS on CPIP, mediated at least in part, by the pathway of resolution of inflammation centred on the axis modulated by ALX/FPR2.


Asunto(s)
Analgésicos/uso terapéutico , Casearia , Dolor Crónico/tratamiento farmacológico , Hiperalgesia/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Daño por Reperfusión/tratamiento farmacológico , Proteínas Adaptadoras Transductoras de Señales/metabolismo , Analgésicos/farmacología , Animales , Anexina A1/genética , Dolor Crónico/metabolismo , Hiperalgesia/metabolismo , Masculino , Ratones Endogámicos C57BL , Ratones Noqueados , Músculo Esquelético/efectos de los fármacos , Músculo Esquelético/metabolismo , Neutrófilos/efectos de los fármacos , Neutrófilos/metabolismo , Extractos Vegetales/farmacología , Hojas de la Planta , Receptores de Formil Péptido/metabolismo , Daño por Reperfusión/metabolismo
14.
Pharm Biol ; 55(1): 641-648, 2017 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-27951742

RESUMEN

CONTEXT: Dillenia indica Linn. (Dilleniaceae) is traditionally used to treat skin inflammation. OBJECTIVE: This study evaluated the healing effect of Dillenia indica fruit extracts on induced psoriasis-like wounds in Wistar rats. MATERIALS AND METHODS: Extracts were standardized to betulinic acid, including an aqueous ethanolic extract (AEE), ethyl acetate extract (EAE) and petroleum ether extract. Effects against lipid peroxidation were assessed in vitro. Wounds were created at rat tails (n = 12). Topical treatments were applied once daily for 7 days (1 mL of AEE or EAE at 5 or 50 mg/mL). Maximal dose was defined by the extract solubility. A 10-fold lower dose was also tested. Positive and negative controls were treated with clobetasol (0.5 mg/mL) or excipient. Half of each group was euthanized for histology. The remaining animals were observed for 20 days for wound measurements. RESULTS: Yields of AEE and EAE were 4.3 and 0.7%, respectively. Betulinic acid concentrations in AEE and EAE were 4.6 and 107.6 mg/g. Extracts neutralized lipid peroxidation in vitro at 0.02 µg/mL, accelerating healing at 50 mg/mL. Complete healing in mice treated with AEE occurred 16 days after wound induction. This time was 14 and 12 days in mice treated with EAE and clobetasol. Compared to orthokeratosis, parakeratosis was reduced by AEE (25%), EAE (45%) and clobetasol (55%). EAE caused superior protection against biomolecules oxidation of skin compared to AEE. DISCUSSION AND CONCLUSION: EAE exhibited activity closer to that of clobetasol. Betulinic acid may be an active constituent, which should be assessed in future studies.


Asunto(s)
Antiinflamatorios/farmacología , Antioxidantes/farmacología , Fármacos Dermatológicos/farmacología , Dilleniaceae/química , Frutas/química , Extractos Vegetales/farmacología , Psoriasis/tratamiento farmacológico , Piel/efectos de los fármacos , Triterpenos/farmacología , Rayos Ultravioleta , Cicatrización de Heridas/efectos de los fármacos , Animales , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/normas , Antioxidantes/aislamiento & purificación , Antioxidantes/normas , Biomarcadores/metabolismo , Clobetasol/farmacología , Fármacos Dermatológicos/aislamiento & purificación , Fármacos Dermatológicos/normas , Modelos Animales de Enfermedad , Peroxidación de Lípido/efectos de los fármacos , Masculino , Malondialdehído/metabolismo , Estrés Oxidativo/efectos de los fármacos , Triterpenos Pentacíclicos , Fitoterapia , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/normas , Plantas Medicinales , Carbonilación Proteica/efectos de los fármacos , Psoriasis/etiología , Psoriasis/metabolismo , Psoriasis/patología , Ratas Wistar , Piel/metabolismo , Piel/patología , Solventes/química , Factores de Tiempo , Triterpenos/aislamiento & purificación , Triterpenos/normas , Ácido Betulínico
15.
Rev Soc Bras Med Trop ; 49(6): 687-692, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-28001214

RESUMEN

INTRODUCTION:: The significant increase in dengue, Zika, and chikungunya and the resistance of the Aedes aegypti mosquito to major insecticides emphasize the importance of studying alternatives to control this vector. The aim of this study was to develop a controlled-release device containing Piper nigrum extract and to study its larvicidal activity against Aedes aegypti. METHODS:: Piper nigrum extract was produced by maceration, standardized in piperine, and incorporated into cotton threads, which were inserted into hydrogel cylinders manufactured by the extrusion of carrageenan and carob. The piperine content of the extract and thread reservoirs was quantified by chromatography. The release profile from the device was assessed in aqueous medium and the larvicidal and residual activities of the standardized extract as well as of the controlled-release device were examined in Aedes aegypti larvae. RESULTS: The standardized extract contained 580mg/g of piperine and an LC50 value of 5.35ppm (24h) and the 3 cm thread reservoirs contained 13.83 ± 1.81mg of piperine. The device showed zero-order release of piperine for 16 days. The P. nigrum extract (25ppm) showed maximum residual larvicidal activity for 10 days, decreasing progressively thereafter. The device had a residual larvicidal activity for up to 37 days. CONCLUSIONS:: The device provided controlled release of Piper nigrum extract with residual activity for 37 days. The device is easy to manufacture and may represent an effective alternative for the control of Aedes aegypti larvae in small water containers.


Asunto(s)
Aedes/efectos de los fármacos , Insectos Vectores/efectos de los fármacos , Insecticidas/administración & dosificación , Piper nigrum/química , Extractos Vegetales/administración & dosificación , Animales , Preparaciones de Acción Retardada , Dengue/transmisión , Sistemas de Liberación de Medicamentos , Insecticidas/aislamiento & purificación , Larva/efectos de los fármacos , Dosificación Letal Mediana
16.
Rev. Soc. Bras. Med. Trop ; 49(6): 687-692, Dec. 2016. tab, graf
Artículo en Inglés | LILACS | ID: biblio-829677

RESUMEN

Abstract: INTRODUCTION: The significant increase in dengue, Zika, and chikungunya and the resistance of the Aedes aegypti mosquito to major insecticides emphasize the importance of studying alternatives to control this vector. The aim of this study was to develop a controlled-release device containing Piper nigrum extract and to study its larvicidal activity against Aedes aegypti. METHODS: Piper nigrum extract was produced by maceration, standardized in piperine, and incorporated into cotton threads, which were inserted into hydrogel cylinders manufactured by the extrusion of carrageenan and carob. The piperine content of the extract and thread reservoirs was quantified by chromatography. The release profile from the device was assessed in aqueous medium and the larvicidal and residual activities of the standardized extract as well as of the controlled-release device were examined in Aedes aegypti larvae. RESULTS The standardized extract contained 580mg/g of piperine and an LC50 value of 5.35ppm (24h) and the 3 cm thread reservoirs contained 13.83 ± 1.81mg of piperine. The device showed zero-order release of piperine for 16 days. The P. nigrum extract (25ppm) showed maximum residual larvicidal activity for 10 days, decreasing progressively thereafter. The device had a residual larvicidal activity for up to 37 days. CONCLUSIONS: The device provided controlled release of Piper nigrum extract with residual activity for 37 days. The device is easy to manufacture and may represent an effective alternative for the control of Aedes aegypti larvae in small water containers.


Asunto(s)
Animales , Extractos Vegetales/administración & dosificación , Aedes/efectos de los fármacos , Piper nigrum/química , Insectos Vectores/efectos de los fármacos , Insecticidas/administración & dosificación , Sistemas de Liberación de Medicamentos , Preparaciones de Acción Retardada , Dengue/transmisión , Insecticidas/aislamiento & purificación , Larva/efectos de los fármacos , Dosificación Letal Mediana
17.
Int J Colorectal Dis ; 31(11): 1759-1766, 2016 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-27614446

RESUMEN

PURPOSES: The objective of this study was to evaluate the effect of supplementation with vitamin C on intestinal anastomosis healing in malnourished rats. METHODS: Male Wistar rats were divided into three groups: (1) sham, well-nourished rats that received vehicle; (2) FR+Veh, rats that were subjected to food restriction and received vehicle; and (3) FR+VC, rats that were subjected to food restriction and received vitamin C. Four days before surgery, the animals received vitamin C (100 mg/kg/day) via gavage and underwent colon resection with anastomosis in a single plane. The survival rate of rats was monitored until day 7 after surgery. Regarding anastomosis tissues, we examined intra-abdominal adhesion index, hydroxyproline content, collagen density, inflammatory parameters, and oxidative damage to proteins and lipids. RESULTS: Malnutrition decreases body weight and increases mortality; the survival rate was 90 % in group 1, 60 % in group 2, and 80 % in group 3. Vitamin C was able to increase hydroxyproline concentration and density of collagen and decrease the intra-abdominal adhesion index, as well as the infiltration of neutrophils and oxidative damage to proteins in malnourished rats compared to group treated with vehicle. CONCLUSIONS: Preoperative vitamin C supplementation can improve the intestinal anastomosis healing, biochemical alterations, and prolong survival in rats subjected to food restriction.


Asunto(s)
Ácido Ascórbico/uso terapéutico , Colon/cirugía , Suplementos Dietéticos , Desnutrición/tratamiento farmacológico , Cuidados Preoperatorios , Recto/cirugía , Cicatrización de Heridas/efectos de los fármacos , Anastomosis Quirúrgica , Animales , Ácido Ascórbico/administración & dosificación , Ácido Ascórbico/farmacología , Peso Corporal/efectos de los fármacos , Colágeno/metabolismo , Colon/efectos de los fármacos , Colon/patología , Hidroxiprolina/metabolismo , Masculino , Desnutrición/complicaciones , Nitratos/metabolismo , Nitritos/metabolismo , Estrés Oxidativo/efectos de los fármacos , Peroxidasa/metabolismo , Ratas Wistar , Recto/efectos de los fármacos , Recto/patología , Adherencias Tisulares/complicaciones , Adherencias Tisulares/tratamiento farmacológico , Factor de Necrosis Tumoral alfa/metabolismo
18.
J. res. dent ; 3(6): 859-868, nov.-dec2015.
Artículo en Inglés | LILACS-Express | LILACS | ID: biblio-1363233

RESUMEN

The aim of this study was to do a literature review on herbal medicines used in dentistry. For that purpose, an electronic search of papers in Portuguese, Spanish, and English was performed in the following databases: PubMed, MEDLINE, SciELO, Science Direct, LILACS, and BBO, supplemented by hand search in books, theses, and journals. For the search, the following keywords were used: phytotherapy, Copaifera, and Baccharis dracunculifolia. Medicinal plants have been used since ancient times and some of them such as the Copaifera multijuga Hayne and Baccharis dracunculifolia DC have shown medicinal properties. Different ways to obtain extracts from those plants have been described, as well as their many important properties, such as antimicrobial, anti-inflammatory, and antiseptic effects. However, studies on their medicinal properties are still scarce, which indicates the need for further studies to unravel their effects and possible side effects, as well as implications of improper use of these plants.

19.
Inflammation ; 38(4): 1394-400, 2015 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-25616904

RESUMEN

The study evaluates the role of Ebselen (Eb), an organoselenium compound in animal model of acute lung injury induced by carrageenan (CG). Wistar rats received saline or 2 % λ-carrageenan in the pleural cavity, and treatment with Eb (50 mg/kg intragastrically) or dexamethasone (Dx) (0.5 mg/kg intraperitoneal) after CG administration. After 4 h, rats were euthanized and the pleural exudate removed for analysis of the total cell count, total protein, lactate dehydrogenase, and nitrite/nitrate. Moreover, lung tissue were removed to verify the myeloperoxidase activity and oxidative damage. Eb showed anti-inflammatory activity by inhibiting leukocyte influx, myeloperoxidase activity, and nitrite/nitrate concentration. Eb presented with an anti-inflammatory activity similar to Dx and an antioxidant activity better than Dx. This study suggests that Eb plays an important role against the oxidative damage associated with anti-inflammatory activity in animal model of acute lung injury, proving to be similar or potentially more effective than Dx.


Asunto(s)
Antiinflamatorios no Esteroideos/uso terapéutico , Azoles/uso terapéutico , Carragenina/toxicidad , Modelos Animales de Enfermedad , Lesión Pulmonar/prevención & control , Compuestos de Organoselenio/uso terapéutico , Pleuresia/tratamiento farmacológico , Animales , Antiinflamatorios no Esteroideos/farmacología , Isoindoles , Lesión Pulmonar/inducido químicamente , Lesión Pulmonar/metabolismo , Masculino , Pleuresia/inducido químicamente , Pleuresia/metabolismo , Ratas , Ratas Wistar
20.
Mater Sci Eng C Mater Biol Appl ; 44: 225-33, 2014 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-25280700

RESUMEN

The production and evaluation of cornstarch/cellulose acetate/silver sulfadiazine extrudate matrices are reported herein. The matrices were melt extruded under nine different conditions, altering the temperature and the screw speed values. The surface morphology of the matrices was examined by scanning electron microscopy. The micrographs revealed the presence of non-melted silver sulfadiazine microparticles in the matrices extruded at lower temperature and screw speed values. The thermal properties were evaluated and the results for both the biopolymer and the drug indicated no thermal degradation during the melt extrusion process. The differential scanning analysis of the extrudate matrices showed a shift to lower temperatures for the silver sulfadiazine melting point compared with the non-extruded drug. The starch/cellulose acetate matrices containing silver sulfadiazine demonstrated significant inhibition of the growth of Pseudomonas aeruginosa and Staphylococcus aureus. In vivo inflammatory response tests showed that the extrudate matrices, with or without silver sulfadiazine, did not trigger chronic inflammatory processes.


Asunto(s)
Celulosa/análogos & derivados , Sulfadiazina de Plata/química , Almidón/química , Animales , Antibacterianos/química , Antibacterianos/farmacología , Celulosa/química , Cromatografía Líquida de Alta Presión , Interleucina-10/sangre , Interleucina-6/sangre , Pseudomonas aeruginosa/efectos de los fármacos , Ratas , Ratas Wistar , Sulfadiazina de Plata/farmacología , Espectroscopía Infrarroja por Transformada de Fourier , Staphylococcus aureus/efectos de los fármacos
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