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1.
Ther Deliv ; 2024 Mar 12.
Artículo en Inglés | MEDLINE | ID: mdl-38469701

RESUMEN

Aim: This study explores chia oil, rich in ω-3 fatty acids and nutraceutical components, as a potential remedy for diseases, especially those linked to inflammation and cancer. Methods/materials: A chia oil-based nanoemulsion, developed through single emulsification, underwent comprehensive analysis using various techniques. In vitro and in vivo assays, including macrophage polarization, nitrite and cytokine production, cellular uptake and biodistribution, were conducted to assess the anti-inflammatory efficacy. Results & conclusion: Results reveal that the chia nanoemulsion significantly inhibits inflammation, outperforming pure oil with twice the efficacy. Enhanced uptake by macrophage-like cells and substantial accumulation in key organs indicate its potential as an economical and effective anti-inflammatory nanodrug, addressing global economic and health impacts of inflammation-related diseases.

2.
Curr Med Chem ; 2024 Jan 23.
Artículo en Inglés | MEDLINE | ID: mdl-38265391

RESUMEN

INTRODUCTION: Nanoceria is a well-known nanomaterial with various properties, including antioxidant, proangiogenic, and therapeutic effects. Despite its potential, there are still aspects that require further exploration, particularly its anti-inflammatory and antimicrobial activities. METHOD: The global demand for novel anti-inflammatory and antimicrobial drugs underscores the significance of understanding nanoceria in both contexts. In this study, we evaluated the effect of nanoceria on macrophage polarization to better understand its anti-inflammatory effects. Additionally, we investigated the mechanism of action of nanoceria against Cryptococcus neoformans (ATCC 32045), Candida parapsilosis (ATCC 22019), Candida krusei (ATCC 6258), and Candida albicans. RESULT: The results demonstrated that nanoceria can polarize macrophages toward an anti-inflammatory profile, revealing the cellular mechanisms involved in the anti-inflammatory response. Concerning the antimicrobial effect, it was observed that nanoceria have a more pronounced impact on Candida parapsilosis, leading to the formation of pronounced pores on the surface of this species. CONCLUSION: Finally, biochemical analysis revealed transitory alterations, mainly in liver enzymes. The data support the use of nanoceria as a potential anti-inflammatory and antimicrobial drug and elucidate some of the mechanisms involved, shedding light on the properties of this nanodrug.

3.
Colloids Surf B Biointerfaces ; 227: 113351, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37244202

RESUMEN

Arthritis is a chronic disease that affects, approximately, 1 % of the total global population. It is characterized by chronic inflammation, accompanied in most of the cases of motor disability and sever pain. The main therapies available have high risk of failure and advanced treatments are scarce and highly cost. In this scenario, search for effective, safe and low-cost treatments is quite desirable. Methyl gallate (MG) is a plant-derived phenolic compound described to present remarkable anti-inflammatory effect in experimental models of arthritis. Thus, in this study we formulated nanomicelles of MG using Pluronic (F-127) as matrix and evaluated in vivo the pharmacokinetic, biodistribution and its effect in the mice model of zymosan-induced arthritis. The nanomicelles were formed with a size 126 nm. The biodistribution showed a ubiquitous tissue deposition with a renal excretion. The pharmacokinetics showed elimination half-life of 1.72 h and a clearance of 0.006 L/h. The oral pretreatment with nanomicelles containing MG (3.5 or 7 mg/kg) demonstrated a reduction in total leukocytes, neutrophils, and mononuclear cells from the inflammation site. The data supports the use of methyl gallate nanomicelles as an alternative drug for arthritis. DATA AVAILABILITY: All the data of this study are transparent.


Asunto(s)
Artritis Experimental , Personas con Discapacidad , Trastornos Motores , Ratones , Animales , Humanos , Neutrófilos , Zimosan/efectos adversos , Artritis Experimental/inducido químicamente , Artritis Experimental/tratamiento farmacológico , Distribución Tisular , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico
4.
Artículo en Inglés | MEDLINE | ID: mdl-38650740

RESUMEN

Graphene quantum dots (GQDs), are biocompatible materials, with mechanical strength and stability. Chitosan, has antibacterial and anti-inflammatory properties, and biocompatibility. Wound healing is a challenging process especially in chronic diseases and infection. In this study, films consisting of chitosan and graphene quantum dots were developed for application in infected wounds. The chitosan-graphene films were prepared in the acidic solution followed by slow solvent evaporation and drying. The chitosan-graphene films were characterized by the scanning electron microscopy, x-ray diffraction, atomic force microscopy, Raman spectroscopy and thermogravimetric analysis. The films' was evaluated by the wound healing assays, hemolytic potential, and nitrite production, cytokine production and swelling potential. The obtained films were flexible and well-structured, promoting cell migration, greater antibacterial activity, lower hemolytic activity, and maintaining wound moisture. Our data suggested that the use of graphene quantum dot-containing chitosan films would be an efficient and promising way in combating wounds.

5.
Inflammopharmacology ; 30(1): 251-266, 2022 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-35112275

RESUMEN

Methyl gallate (MG) is a plant-derived phenolic compound known to present remarkable anti-inflammatory effect in different experimental models, such as paw oedema, pleurisy, zymosan-induced arthritis and colitis. Herein we investigated the effect of MG in the mice model of antigen-induced arthritis (AIA), a model with complex inflammatory response, driven primally by immune process and that cause bone and cartilage erosion similarly found in rheumatoid arthritis. Arthritis was induced by intra-articular injection of albumin methylated from bovine serum (mBSA) in C57BL/6 male mice previously immunized. The dose-response analysis of MG (0.7-70 mg/kg; p.o) showed that maximum inhibition was reached with the dose of 7 mg/kg on paw oedema and cell infiltration induced by AIA at 7 h. Treatment with MG (7 mg/kg; p.o) or with the positive control, dexamethasone (Dexa, 10 mg/kg, ip) reduced AIA oedema formation, leukocyte infiltration, release of extracellular DNA and cytokine production 7 and 24 h (acute response). Mice treated daily with MG for 7 days showed no significant weight loss or liver and kidney toxicity contrary to dexamethasone that induced some degree of toxicity. Prolonged treatment with MG inhibited the late inflammatory response (28 days) reducing oedema formation, cell infiltration, synovial hyperplasia, pannus formation and cartilage degradation as observed in histopathological analyses. Ultimately, MG reduced bone resorption as evidenced by a decrease in tartrate-resistant acid phosphate (TRAP)-positive cells number in femur histology. Altogether, we demonstrate that MG ameliorates the inflammatory reaction driven primarily by the immune process, suggesting a potential therapeutic application in arthritis treatment.


Asunto(s)
Artritis Experimental , Artritis Reumatoide , Animales , Artritis Experimental/patología , Artritis Reumatoide/tratamiento farmacológico , Ácido Gálico/análogos & derivados , Ácido Gálico/uso terapéutico , Masculino , Ratones , Ratones Endogámicos C57BL
6.
Colloids Surf B Biointerfaces ; 211: 112280, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-34902784

RESUMEN

Aptamers may form well-defined three-dimensional structures binding with high affinity and stability to a specific receptor. The aptamer anti-MUC1 isoform Y is one the most used due the affinity to MUC1, which is overexpressed in several types of cancer and inflammation process. In this study we have developed, characterized, in vitro as in vivo evaluated a nanoaptamer (anti-MUC1/Y) as a nanoagent for rheumatoid arthritis treatment. The results showed that a nanoaptamer with a size range of 241 nm was produced. The entrapment efficacy was 90% with a biodistribution showing a high hepatic uptake (>98%). The results in vivo showed a potent effect in arthritis experimental model, especially in low doses. The results corroborate the applicability of this nanosystem for RA treatment.


Asunto(s)
Aptámeros de Nucleótidos , Artritis , Nanopartículas , Aptámeros de Nucleótidos/química , Humanos , Mucina-1/química , Nanopartículas/química , Distribución Tisular
7.
Oxid Med Cell Longev ; 2021: 7612380, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34745422

RESUMEN

Solidago chilensis Meyen (Compositae) is a species native to South America (Brazil) popularly known as arnica. In Brazilian popular medicine, inflorescences and rhizomes of this plant have been used since the end of the 19th century to replace the exogenous and hepatotoxic Arnica montana L. in the treatment of edema and inflammatory pathologies. Although the anti-inflammatory activity of S. chilensis is evidenced in the literature, there is a lack of studies with enriched fractions or compounds isolated from it. The objective of the current study was to characterize phytochemically and to evaluate the pharmacological action in vivo and in vitro of the crude extract and the different fractions (hexane, dichloromethane, acetal, butanolic, and aqueous) isolated from the inflorescence of S. chilensis. The inflorescence crude extract (ScIE) and fractions were administered by intraperitoneal route to mice at different doses. In an LPS-induced pleurisy model, inhibition of leukocyte influx was observed for the ScIE and all fractions tested, as compared to controls. Dichloromethane (ScDicF), butanolic (ScButF), and aqueous (ScAquF) were selected for further analysis as they showed the best inhibitory effects in leukocyte migration and inflammatory cytokine and chemokine production: TNF-α, CXCL1/KC, CXCL2/MIP-2, and CCL11/eotaxin-1. In LPS-stimulated J774A.1 cell line, ScIE and the ScDicF exhibited an inhibitory effect on nitric oxide (NO) production and downmodulated the COX-2 expression; ScAquF failed to modulate NO production and COX-2 expression. In phytochemical analysis, HPLC-UV-DAD chromatograms of ScDicF and ScAquF showed the main peaks with UV spectrum characteristics of flavonoids; chlorogenic acid and isoquercetin were the most present phytochemicals identified in the ScAquF, and a high number of n-alkanes was found in ScHexF. Our study was the first to address biological effects and correlate them to phytochemically characterized fractions from inflorescences of S. chilensis.


Asunto(s)
Antiinflamatorios/farmacología , Inflamación/tratamiento farmacológico , Inflorescencia/química , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta/química , Solidago/química , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Inflamación/patología , Masculino , Ratones , Fitoquímicos/química , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación
8.
Eur J Nucl Med Mol Imaging ; 49(1): 336-344, 2021 12.
Artículo en Inglés | MEDLINE | ID: mdl-34370060

RESUMEN

Rheumatoid arthritis (RA) is an inflammatory chronic autoimmune disease. The treatment of RA is difficult and, in many cases, ineffective, and the arsenal of drugs is limited. Due the longevity of the disease, RA may cause extreme musculoskeletal disorders with a high impact on quality of life. Also, RA is related with severe comorbidities decreasing the life expectancy. Finally, RA has been reported to impact in economy and healthy public. In this direction, the necessity to discover new strategies to efficiently treat RA is immediate. In this direction, we have reported the use of low doses of [223Ra] RaCl2 (radium dichloride) as intra-articular injection to treat RA. Mice were post-treated with [223Ra] RaCl2 (1.48 µCi; i.a.) 24 h after zymosan stimulus. Zymosan-induced arthrithis is responsible for leucocyte recruitment (total leukocytes, neutrophils, and mononuclear cells), which were inhibited by intra-articular injection of [223Ra] RaCl2 (69%, 77%, and 66%, respectively).


Asunto(s)
Artritis , Radio (Elemento) , Animales , Antiinflamatorios , Artritis/inducido químicamente , Artritis/tratamiento farmacológico , Inyecciones Intraarticulares , Ratones , Calidad de Vida
9.
Colloids Surf B Biointerfaces ; 206: 111952, 2021 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-34273810

RESUMEN

Rheumatoid arthritis (RA) is the most common inflammatory rheumatic disease, affecting almost 1% of the world population. It is a long-lasting autoimmune disease, which mainly affects the joints causing inflammation and swelling of the synovial joint. RA has a significant impact on the ability to perform daily activities including simple work and household chores. Nonetheless, due to the long periods of pain and the continuous use of anti-inflammatory drugs, RA can debilitate the quality of life and increases mortality. Current therapeutic approaches to treat RA aim to achieve prolonged activity and early and persistent remission of the disease, with the gradual adoption of different drugs available. In this study, we developed a novel hydroxychloroquine and methotrexate co-loaded Pluronic® F-127 nanomicelle and evaluated its therapeutic effects against RA. Our results showed that drug-loaded nanomicelles were capable of modulating the inflammatory process of RA and reducing osteoclastogenesis, edema, and cell migration to the joint. Overall, compared to the free drugs, the drug-loaded nanomicelles showed a 2-fold higher therapeutic effect.


Asunto(s)
Artritis Reumatoide , Metotrexato , Artritis Reumatoide/tratamiento farmacológico , Humanos , Hidroxicloroquina/farmacología , Articulaciones , Metotrexato/farmacología , Calidad de Vida
10.
Inflamm Res ; 69(12): 1257-1270, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33037469

RESUMEN

OBJECTIVE AND DESIGN: Methyl gallate (MG) is a prevalent polyphenol in the plant kingdom, which may be related to the effects of several medicinal plants. Although it is widely reported that polyphenols have therapeutic effects, there are few studies demonstrating that MG has anti-inflammatory action. This study aimed to investigate the molecular mechanism behind the anti-inflammatory activity of MG and its effect on hyperalgesia. METHODS: Swiss mice were pretreated orally with different doses of MG and subjected to i.pl. injection of zymosan to induce paw edema. RAW264.7 macrophages and BMDMs stimulated with different TLR agonists such as zymosan, LPS, or Pam3CSK4 were used to investigate the molecular mechanisms of MG RESULTS: MG inhibits zymosan-induced paw edema and hyperalgesia and modulates molecular pathways crucial for inflammation development. Pretreatment with MG inhibited cytokines production and NF-κB activity by RAW 264.7 cells stimulated with zymosan, Pam3CSK4 or LPS, but not with PMA. Moreover, pretreatment with MG decreased IκB degradation, nuclear translocation of NF-κBp65, c-jun and c-fos and ERK1/2, p38 and JNK phosphorylation. CONCLUSION: Thus, the results of this study demonstrate that MG has a promising anti-inflammatory effect and suggests an explanation of its mechanism of action through the inhibition of NF-κB signaling and the MAPK pathway.


Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Ácido Gálico/análogos & derivados , Inflamación/tratamiento farmacológico , Proteínas Quinasas Activadas por Mitógenos/antagonistas & inhibidores , FN-kappa B/antagonistas & inhibidores , Transducción de Señal/efectos de los fármacos , Receptores Toll-Like/efectos de los fármacos , Animales , Antiinflamatorios no Esteroideos/uso terapéutico , Citocinas/metabolismo , Edema/inducido químicamente , Edema/tratamiento farmacológico , Ácido Gálico/farmacología , Ácido Gálico/uso terapéutico , Hiperalgesia/tratamiento farmacológico , Masculino , Ratones , Células RAW 264.7 , Zimosan
11.
J Biomed Nanotechnol ; 16(8): 1254-1266, 2020 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-33397555

RESUMEN

Rheumatoid arthritis, a chronic disease, affects from 0.5% to 1% of the world population. The main consequences include loss of joint functionality and severe pain, with lost in life quality and increased risk of morbidity and mortality. The main strategy for RA treatment relies in early diagnosis as targeted therapy. In this regard, the development and application of designed/engineered nanoparticles may represent an innovative approach and the key to success, since is a personalized nanodrug. Thus, we have synthetized, characterized, and in vivo evaluated a tri-loaded monoclonal antibody nanoparticle. For the production we used a mix of monoclonal antibodies: adalimumab, rituximab and trastuzumab to surround all RA metabolic pathways. The characterization included atomic force microscopy, dynamic light scattering analysis and entrapment efficacy using BCA analysis. The in vivo evaluation was done in mice. At this stage we used animals to assess the pharmacokinetics, the tissue distribution as the proof of concept (therapeutic efficacy) of the nanoparticles developed in inducted animals with rheumatoid arthritis. The interpretation of our results revealed that a spherical shaped nanoparticle has been produced with a mean size of 229.7 nm, and a polydispersity index of 0.191. This data has been corroborated by DLS and AFM analysis. The pre-clinical (in vivo) evaluation demonstrated a low elimination rate of 2,34 L/hour, with a purge of 0,42 h. The therapeutic efficacy showed that the nanoparticles have an increased therapeutic effect than the conventional drug with a reduction in all main parameters including the interleukins.


Asunto(s)
Antirreumáticos , Artritis Reumatoide , Nanopartículas , Adalimumab/uso terapéutico , Animales , Anticuerpos Monoclonales/uso terapéutico , Anticuerpos Monoclonales Humanizados/uso terapéutico , Artritis Reumatoide/tratamiento farmacológico , Ratones , Rituximab/uso terapéutico , Trastuzumab/uso terapéutico
12.
J Pharm Pharmacol ; 70(7): 964-975, 2018 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-29600536

RESUMEN

OBJECTIVES: The aim of this article was to use copaiba oil (C.O) to improve skin permeability and topical anti-inflammatory activity of celecoxib (Cxb). METHODS: Formulations containing C.O (1-50%) were associated with Cxb (2%). In vitro skin permeability studies were conducted using porcine ear skin. Histological analysis of the hairless mice skin samples after application of formulations was achieved with the routine haematoxylin/eosin technique. The anti-inflammatory activity was assessed using the AA-induced ear oedema mice model. KEY FINDINGS: The formulation containing 25% C.O promoted the highest levels of in vitro Cxb permeation through pig ear skin, retention in the stratum corneum (SC) and epidermis/dermis of pig ear skin in vitro (~5-fold) and hairless mice skin in vivo (~2.0-fold), as compared with the control formulation. At 25%, C.O caused SC disorganization and increased cell infiltration and induced angiogenesis without clear signs of skin irritation. The formulation added to 25% C.O as adjuvant inhibited ear oedema and protein extravasation by 77.51 and 89.7%, respectively, and that it was, respectively, 2.0- and 3.4-fold more efficient than the commercial diethylammonium diclofenac cream gel to suppress these inflammatory parameters. CONCLUSIONS: 25% C.O is a potential penetration enhancer for lipophilic drugs like Cxb that can improve cutaneous drug penetration and its anti-inflammatory activity.


Asunto(s)
Celecoxib/farmacología , Celecoxib/farmacocinética , Fabaceae , Aceites Volátiles/farmacología , Absorción Cutánea/efectos de los fármacos , Animales , Antiinflamatorios/farmacología , Diclofenaco/análogos & derivados , Diclofenaco/farmacología , Dietilaminas/farmacología , Sinergismo Farmacológico , Edema/prevención & control , Masculino , Ratones , Porcinos
13.
Curr Drug Deliv ; 14(7): 992-1004, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28124617

RESUMEN

BACKGROUND: Celecoxib (CXB) has been explored as an anti-inflammatory or chemopreventive drug for topical treatment of skin diseases and cancer. OBJECTIVE: The main aim of this work was to investigate the potential of dimethylsufoxide (DMSO) and Azone (AZ) as penetration enhancers (P.Es) for topical delivery of CXB. METHOD: The in vitro studies, drug release, skin permeability and potential cytotoxicity/genotoxicity were carried out with formulations containing or not DMSO or AZ (5% and 10%). Skin irritation in rabbits and topical anti-inflammatory activity in mice were assayed in vivo. RESULTS: Skin permeation was minimal while higher retention in stratum corneum (SC) and epidermis plus dermis was found (28.0 and 3-fold respectively) from 10.0% AZ compared to the control indicating a localized CXB effect. CXB associated to 5% or 10% DMSO has shown high drug permeation through skin with low retention. Associations of CXB with both enhancers were not cytotoxic or genotoxic, suggesting safety for cutaneous application. In vivo skin irritation assays of all formulations indicated mild irritation effects and, thus, possible use for longer periods. In vivo anti-inflammatory tests showed that ear edema could be inhibited by CXB associated with 5.0% DMSO (53.0%) or 10.0% AZ (40.0%). These inhibition values were almost 2-fold higher when compared to a commercial formula. CONCLUSION: Although DMSO- associated CXB is an efficient edema inhibitor its high skin permeation suggests risks of systemic effects, whereas association to 10% AZ may improve topical delivery of the drug with good anti-inflammatory activity and no cytotoxic/genotoxic or significant skin irritation effects.


Asunto(s)
Azepinas/administración & dosificación , Celecoxib/administración & dosificación , Inhibidores de la Ciclooxigenasa 2/administración & dosificación , Dimetilsulfóxido/administración & dosificación , Absorción Cutánea/efectos de los fármacos , Administración Cutánea , Animales , Azepinas/química , Azepinas/uso terapéutico , Celecoxib/química , Celecoxib/uso terapéutico , Inhibidores de la Ciclooxigenasa 2/química , Inhibidores de la Ciclooxigenasa 2/uso terapéutico , Dimetilsulfóxido/química , Dimetilsulfóxido/uso terapéutico , Edema/tratamiento farmacológico , Escherichia coli/efectos de los fármacos , Escherichia coli/genética , Masculino , Ratones , Pruebas de Mutagenicidad , Conejos , Saccharomyces cerevisiae/efectos de los fármacos , Saccharomyces cerevisiae/genética , Piel/efectos de los fármacos , Piel/metabolismo , Pruebas de Irritación de la Piel , Porcinos
14.
Inflamm Res ; 65(11): 869-879, 2016 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-27379721

RESUMEN

OBJECTIVE AND DESIGN: ß-Caryophyllene (BCP) is a sesquiterpene that binds to the cannabinoid 2 (CB2) receptor and exerts anti-inflammatory effects. In this study, we investigated the anti-inflammatory effect of BCP and another CB2 agonist, GP1a in inflammatory experimental model induced by Mycobacterium bovis (BCG). METHODS: C57Bl/6 mice were pretreated orally with BCP (0.5-50 mg/kg) or intraperitonealy with GP1a (10 mg/kg) 1 h before the induction of pleurisy or pulmonary inflammation by BCG. The direct action of CB2 agonists on neutrophils function was evaluated in vitro. RESULTS: ß-Caryophyllene (50 mg/kg) impaired BCG-induced neutrophil accumulation in pleurisy without affecting mononuclear cells or the production of TNF-α and CCL2/MCP-1. However, BCP inhibited CXCL1/KC, leukotriene B4 (LTB4), IL-12, and nitric oxide production. GP1a had a similar effect to BCP. Preincubation of neutrophils with BCP (10 µM) impaired chemotaxis toward LTB4 and adhesion to endothelial cells stimulated with TNF-α, and both, BCP and GP1a, impaired LTB4-induced actin polymerization. CONCLUSION: These results suggest that the CB2 receptor may represent a new target for modulating the inflammatory reaction induced by mycobacteria.


Asunto(s)
Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Receptor Cannabinoide CB2/agonistas , Sesquiterpenos/farmacología , Sesquiterpenos/uso terapéutico , Tuberculosis Pulmonar/tratamiento farmacológico , Actinas/metabolismo , Animales , Adhesión Celular/efectos de los fármacos , Línea Celular , Movimiento Celular/efectos de los fármacos , Citocinas/inmunología , Dinoprostona/metabolismo , Macrófagos/efectos de los fármacos , Masculino , Ratones Endogámicos C57BL , Mycobacterium bovis , Neutrófilos/efectos de los fármacos , Neutrófilos/metabolismo , Neutrófilos/fisiología , Óxido Nítrico/metabolismo , Pleuresia/tratamiento farmacológico , Pleuresia/inmunología , Neumonía/tratamiento farmacológico , Neumonía/inmunología , Sesquiterpenos Policíclicos , Tuberculosis Pulmonar/inmunología
15.
J Nat Prod ; 79(6): 1554-66, 2016 06 24.
Artículo en Inglés | MEDLINE | ID: mdl-27227459

RESUMEN

Methyl gallate (MG) is a prevalent phenolic acid in the plant kingdom, and its presence in herbal medicines might be related to its remarkable biological effects, such as its antioxidant, antitumor, and antimicrobial activities. Although some indirect evidence suggests anti-inflammatory activity for MG, there are no studies demonstrating this effect in animal models. Herein, we demonstrated that MG (0.7-70 mg/kg) inhibited zymosan-induced experimental arthritis in a dose-dependent manner. The oral administration of MG (7 mg/kg) attenuates arthritis induced by zymosan, affecting edema formation, leukocyte migration, and the production of inflammatory mediators (IL-1ß, IL-6, TNF-α, CXCL-1, LTB4, and PGE2). Pretreatment with MG inhibited in vitro neutrophil chemotaxis elicited by CXCL-1, as well as the adhesion of these cells to TNF-α-primed endothelial cells. MG also impaired zymosan-stimulated macrophages by inhibiting IL-6 and NO production, COX-2 and iNOS expression, and intracellular calcium mobilization. Thus, MG is likely to present an anti-inflammatory effect by targeting multiple cellular events such as the production of various inflammatory mediators, as well as leukocyte activation and migration.


Asunto(s)
Ácido Gálico/análogos & derivados , Mediadores de Inflamación/farmacología , Macrófagos/efectos de los fármacos , Infiltración Neutrófila/efectos de los fármacos , Plantas Medicinales/química , Administración Oral , Animales , Artritis Experimental , Brasil , Ciclooxigenasa 2/metabolismo , Citocinas/metabolismo , Relación Dosis-Respuesta a Droga , Edema/inducido químicamente , Edema/tratamiento farmacológico , Ácido Gálico/química , Ácido Gálico/farmacología , Inflamación/inducido químicamente , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Ratones Endogámicos C57BL , Estructura Molecular , Óxido Nítrico Sintasa de Tipo II , Factor de Necrosis Tumoral alfa/farmacología , Zimosan/farmacología
16.
J Ethnopharmacol ; 175: 490-8, 2015 Dec 04.
Artículo en Inglés | MEDLINE | ID: mdl-26453933

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Schinus terebinthifolius is a species of plant from the Anacardiaceae family, which can be found in different regions of Brazil. Schinus is popularly known as aroeirinha, aroeira-vermelha, or Brazilian pepper. In folk medicine, S. terebinthifolius is used for several disorders, including inflammatory conditions, skin wounds, mucosal membrane ulcers, respiratory problems, gout, tumors, diarrhea and arthritis. According to chemical analyses, gallic acid, methyl gallate and pentagalloylglucose are the main components of hydroalcoholic extracts from S. terebinthifolius leaves. In the present study, we demonstrated the ability of a hydroalcoholic extract to inhibit cell migration in arthritis and investigated the mechanisms underlying this phenomenon. MATERIALS AND METHODS: The anti-inflammatory effect of S. terebinthifolius hydroalcoholic leaf extract (ST-70) was investigated in a zymosan-induced experimental model of inflammation. Male Swiss and C57Bl/6 mice received zymosan (100 µg/cavity) via intra-thoracic (i.t.) or intra-articular (i.a.) injection after oral pre-treatment with ST-70. The direct action of ST-70 on neutrophils was evaluated via chemotaxis. RESULTS: ST-70 exhibited a dose-dependent effect in the pleurisy model. The median effective dose (ED50) was 100mg/kg, which inhibited 70% of neutrophil accumulation when compared with the control group. ST-70 reduced joint diameter and neutrophil influx for synovial tissues at 6h and 24h in zymosan-induced arthritis. Additionally, ST-70 inhibited synovial interleukin (IL)-6, IL-1ß, keratinocyte-derived chemokine (CXCL1/KC) and Tumor Necrosis Factor (TNF)-α production at 6h and CXCL1/KC and IL-1ß production at 24h. The direct activity of ST-70 on neutrophils was observed via the impairment of CXCL1/KC-induced chemotaxis in neutrophils. Oral administration of ST-70 did not induce gastric damage. Daily administration for twenty days did not kill any animals. In contrast, similar administrations of diclofenac induced gastric damage and killed all animals by the fifth day. CONCLUSIONS: Our results demonstrated significant anti-inflammatory effects of ST-70, suggesting a putative use of this herb for the development of phytomedicines to treat inflammatory diseases, such as joint inflammation.


Asunto(s)
Anacardiaceae , Antiinflamatorios/uso terapéutico , Artritis Experimental/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Pleuresia/tratamiento farmacológico , Animales , Antiinflamatorios/farmacología , Artritis Experimental/inmunología , Células Cultivadas , Quimiotaxis de Leucocito/efectos de los fármacos , Citocinas/inmunología , Etanol/química , Ácido Gálico/farmacología , Humanos , Articulación de la Rodilla/inmunología , Recuento de Leucocitos , Masculino , Ratones Endogámicos C57BL , Neutrófilos/efectos de los fármacos , Neutrófilos/fisiología , Fitoterapia , Extractos Vegetales/farmacología , Hojas de la Planta/química , Pleuresia/inmunología , Solventes/química , Zimosan
17.
Drug Dev Ind Pharm ; 40(9): 1180-9, 2014 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-23826859

RESUMEN

OBJECTIVE: We investigated the potential effects of oleic acid (OA) and glycerol monooleate (GMO) on the skin delivery of CXB. METHODS: The influence of both OA and GMO (5.0% or 10.0%) on the in vitro skin permeability of CXB (2.0%) was evaluated using propylene glycol (PG) as a vehicle. Also the in vitro potential cytotoxicity and genotoxicity and in vivo assays (skin irritation in rabbits and topical anti-inflammatory activity by in mice) were conducted. RESULTS: As expected, the amount of CXB that permeated through the skin was minimal, but drug retention on the viable skin (epidermis plus dermis) was higher in association with treatment with 5.0% OA or GMO compared to the control treatment, meaning that there was a localized effect of CXB in the skin. No formulation presented cytotoxic or genotoxic potential, suggesting safety for cutaneous application. In vivo skin irritation assays indicated that no formulation was irritating to the skin becomes its use possible for a prolonged time. In vivo anti-inflammatory experiments indicated that both edema and protein extravasation were inhibited with a maximum % inhibition of 53.5.0% and 61.0% for 5.0 % GMO, respectively, and 48.0% and 35.5% for 5.0% OA, respectively. Such formulations were able to inhibit around twofold the percentage of ear edema in mice compared to a commercial product reference diclofenac commercial formula. CONCLUSION: There is no topical formulation currently available that contains both CXB and 5.0% GMO or OA, suggesting them as potential adjuvants that improve the skin delivery of CXB.


Asunto(s)
Pirazoles/administración & dosificación , Pirazoles/química , Piel/metabolismo , Sulfonamidas/administración & dosificación , Sulfonamidas/química , Administración Cutánea , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/química , Celecoxib , Química Farmacéutica/métodos , Edema/tratamiento farmacológico , Glicéridos/química , Masculino , Ratones , Ácido Oléico/química , Permeabilidad , Propilenglicol/química , Conejos , Absorción Cutánea/fisiología , Porcinos
18.
Int Immunopharmacol ; 8(11): 1552-60, 2008 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-18672096

RESUMEN

Schinus is a genus of the Anacardiaceae family and contains Schinus terebinthifolius, the Brazilian pepper tree that is widely used in folk medicine. We investigate the anti-allergic activity of the ethyl acetate fraction of S. terebinthifolius Raddi (ST fraction). HPLC analysis reveled that gallic acid, methyl gallate and 1,2,3,4,6-pentagalloylglucose are the major aromatic components of the fraction. Oral pre-treatment with the ST fraction (100 mg/kg) significantly inhibited paw edema induced by compound 48/80 (100 ng/paw) and to a lesser extent, the allergic paw edema (OVA, 3 microg/paw). The ST fraction (100 and 200 mg/kg) also inhibited the edema induced by histamine (100 microg/paw), preventing mast cell degranulation and, consequently, histamine release in Wistar rat peritoneal mast cells induced by C 48/80 (5 microg/mL). This histamine inhibition was also observed after mast cell pre-treatment with both methyl gallate and 1,2,3,4,6-pentagalloylglucose (100 microg/mL), the isolated compounds from the ethyl acetate fraction. Pre-treatment with the ST fraction (100 mg/kg) significantly inhibited total leukocyte and eosinophil accumulation in pleural cavities 24 h after the intrathoracic injection of OVA (12.5 microg/cavity). This effect was related to the inhibition of CCL11/eotaxin and CCL5/RANTES in pleural lavage fluid. Pre-treatment with this fraction (100 mg/kg) failed to reduce the cell influx that was observed after LPS-injection into pleural cavity (250 ng/cavity). These findings demonstrate the anti-allergic effect of the ST fraction, which includes the inhibition of edema formation and histamine release caused by mast cell degranulation and eosinophil influx into the pleural cavity probably reflected by the decreased levels of chemokines in recovered pleural lavage fluid.


Asunto(s)
Anacardiaceae/química , Antialérgicos/uso terapéutico , Edema/tratamiento farmacológico , Hipersensibilidad/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Hojas de la Planta/química , Pleuresia/tratamiento farmacológico , Animales , Antialérgicos/farmacología , Quimiocinas/efectos de los fármacos , Quimiocinas/inmunología , Edema/inmunología , Histamina/administración & dosificación , Histamina/farmacología , Liberación de Histamina/efectos de los fármacos , Liberación de Histamina/inmunología , Hipersensibilidad/inmunología , Inmunoglobulina E/efectos de los fármacos , Inmunoglobulina E/inmunología , Lipopolisacáridos/farmacología , Masculino , Mastocitos/inmunología , Mastocitos/metabolismo , Ratones , Ratones Endogámicos BALB C , Ovalbúmina/administración & dosificación , Ovalbúmina/farmacología , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Pleuresia/inmunología , Prometazina/administración & dosificación , Prometazina/farmacología , Ratas , Ratas Wistar
19.
Rio de Janeiro; s.n; 2004. 110 p. tab, graf.
Tesis en Portugués | LILACS | ID: lil-398652

RESUMEN

O envolvimento de linfócitos Tgd nas reações inflamatórias induzidas por bactéria, produtos bacterianos e antígeno, assim como seu papel no acúmulo de eosinófilos tem sido descrito. Neste trabalho tivemos como objetivo caracterizar os linfócitos Tgd presentes na pleurisia induzida por LPS, Mycobacterium bovis - BCG e antígeno. A pleurisia foi induzida em camundongos Balb-c machos, através da injeção i.t. de LPS (250 ng/cav.), M. bovis - BCG (3x 105 UFC/cav.) e ovoalbumina (Ova 12,5 mg/cav - em animais previamente sensibilizados depletados ou não de linfócitos Tgd, CD4 e CD8). Após diferentes intervalos de tempo, células recolhidas da cavidade torácica foram adquiridas por citometria de fluxo para posterior análise dos subtipos de linfócitos e citocinas intracelulares. Observamos um aumento no número de linfócitos T gd na cavidade torácica de animais estimulados com LPS (24h), BCG (24h e 15 dias) ou Ova (72h) em relação aos animais controles. Ocorreu um aumento dos subtipos de linfócitos T gd Td4, Tg2 e Tg3 24 h após o estímulo com LPS e BCG, e 72h na pleurisia alérgica. Já 15 e 30 dias após a indução da pleurisia por BCG, os subtipos de linfócitos T gd estatisticamente significativos foram Tg2 (15d) e Td4 (30d). Os camundongos alérgicos depletados de linfócitos T gd apresentaram uma inibição no acúmulo de leucócitos totais e principalmente eosinófilos. A análise da expressão de citocinas intracelulares por linfócitos Tgd obtidos da cavidade torácica de camundongos estimulados com LPS, demonstrou uma queda na expressão de IL-4, IL-5, IL-10 e IFN-g. Por outro lado, a expressão destas citocinas aumentou nos linfócitos Tgd obtidos dos animais estimulados com M. bovis - BCG. Na pleurisia alérgica, nós observamos um aumento na expressão de IL-4 e IL-5 por linfócitos Tgd. Nossos resultados demonstram que na reação inflamatória aguda ou tardia, há um aumento no número dos linfócitos Tgd. Além disso, sugere um papel destas células no acúmulo de eosinófilos na pleurisia alérgica.


Asunto(s)
Animales , Ratones , Anticuerpos Monoclonales , Eosinófilos , Inmunofenotipificación , Recuento de Leucocitos , Mycobacterium bovis , Pleuresia , Linfocitos T , Tuberculosis
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