Your browser doesn't support javascript.
Show: 20 | 50 | 100
Results 1 - 19 de 19
J. venom. anim. toxins incl. trop. dis ; 27: e20200152, 2021. tab, graf
Article in English | LILACS, VETINDEX | ID: biblio-1346435


Peptides obtained from different animal species have gained importance recently due to research that aims to develop biopharmaceuticals with therapeutic potential. In this sense, arthropod venoms have drawn attention, not only because of their toxicity but mainly for the search for molecules with various bioactivities, including anti-inflammatory activity. The purpose of the present study is to gather data available in the literature on new peptides derived from arthropod species with anti-inflammatory potential. This systematic review followed the Preferred Reporting Items for Systematic Reviews and Meta-Analysis (PRISMA) guidelines. Studies on peptides from arthropods that display anti-inflammatory activity were retrieved from PubMed, Scopus, Web of Science, and Google Scholar databases. The bibliographic research started in 2020 and searched papers without a limit on the publication date. The articles were analyzed using a search string containing the following terms: "Peptides" and "Anti-inflammatory", in combinations such as "Ant", "Bee", "Wasp", "Crab", "Shrimp", "Scorpion", "Spider", "Tick" and "Centipedes". Besides, a search was carried out in the databases with the terms: "Peptides", "Antitumor", or "Anticancer", and "Arthropods". Articles that met the inclusion and exclusion criteria totalized 171, and these served for data extraction. Additionally, the present review included anti-inflammatory peptides with anticancer properties. Peptides with confirmed anti-inflammatory activity were from insects (ants, bees, and wasps), crustaceans (shrimp and crabs), arachnids (scorpions, spiders, and ticks), and centipedes. These arthropod peptides act mainly by decreasing pro-inflammatory cytokines as analyzed in vitro and in vivo. Some showed significant antineoplastic activity, working in essential cellular pathways against malignant neoplasms.(AU)

Animals , Peptides , Arthropod Venoms , Arthropods , Biological Products , Anti-Inflammatory Agents/analysis , Cytokines , Literature
Braz. J. Pharm. Sci. (Online) ; 54(1): e17320, 2018. tab, graf
Article in English | LILACS | ID: biblio-951910


This study aimed to determine whether the anti-inflammatory drugs that are most commonly consumed in Brazil, including diclofenac, ketoprofen, naproxen, indomethacin, ibuprofen and acetaminophen, are present in drinking water and to derive guideline values to characterize the human risk. These pharmaceuticals were quantified in surface waters by LC-MS/MS with solid phase extraction, both before and after conventional treatment on a laboratory scale, using a jar test assay. The methods used to quantify these drugs showed good results: the chromatographic analysis obtained correlation coefficients between 0.9952 and 0.9991, with limits of quantification of 0.5 ng.mL-1 - 50 ng.mL-1 and precision standard deviations (0.08 - 2.08). Only ketoprofen and ibuprofen were not completely removed through the jar test. Environmental samples were collected and handled by the same method; the values |for ketoprofen and ibuprofen after treatment were 18.67 - 19.65 ng.L-1 (±17%) and 166.70 - 244.73 ng.L-1 (±14%), respectively. Human risk was assessed by comparing the guideline values for each compound to the concentrations obtained in the environmental samples, considering the toxicological backgrounds, following WHO (2011) method. The results suggest that the concentrations of ketoprofen and ibuprofen found in drinking water do not pose a risk to human health, even with chronic consumption

Water Pollution/analysis , Drinking Water/microbiology , Anti-Inflammatory Agents/analysis , Mass Spectrometry/instrumentation , Chromatography, Liquid/instrumentation
Braz. J. Pharm. Sci. (Online) ; 54(2): e17183, 2018. tab, graf, ilus
Article in English | LILACS | ID: biblio-951934


ABSTRACT Interpolyelectrolyte complexes, which constitute a type of polymeric material obtained through the self-assembly of oppositely charged polymers, exhibit interesting properties for use in the design of smart matrices for drug delivery. In the present study, a stoichiometric interpolyelectrolyte complex (SIPEC) composed of Eudragit E® and Eudragit® L100 was obtained at pH 6.0 and characterized and evaluated as a hydrophilic matrix for dexibuprofen. The formation of a SIPEC was monitored by ζ-potential measurements and characterized using infrared spectroscopy, thermal analysis, and scanning electron microscopy. The results indicated that a SIPEC obtained under these conditions can be used as a matrix for controlling the release of dexibuprofen and exhibit a pH-triggered release

Drug Liberation , Hydrogen-Ion Concentration , Technology, Pharmaceutical/instrumentation , Anti-Inflammatory Agents/analysis
Rev. biol. trop ; 64(1): 247-257, ene.-mar. 2016. tab, ilus
Article in English | LILACS | ID: biblio-843275


AbstractThe biodiversity rich state of Meghalaya, India located in the realms of mega-biodiversity hotspots, is home to numerous species of wild edible macrofungi that are used extensively by the mycophillic ethnic population, as a part of their traditional cuisine and medicine systems. However, habitat loss, due to deforestation and climate change, is destroying the natural population of these mushrooms, depleting their availability to the local communities. In the present investigation, a GIS guided habitat search, using Lentinula edodes as a representative species, was used in mapping the habitats of wild edible macrofungi of the study region. Sampling of around 4 000 specimens per distinct morphological type available in the traditional markets and "sacred grove" forests indicated presence of ten common genera, belonging to nine different families of wild edible mushrooms. Nutritional profiling of the representative species Lentinula edodes was carried out by evaluation of its moisture, total fat, crude protein and carbohydrates contents by standard methods. Similarly, bioactive components determination was performed by estimation of total phenols, flavonoids, ascorbic acid, β-carotene and lycopenes. Bioactivity of the mushrooms extracts was studied using the DPPH radical scavenging and Human Red Blood Cell (HRBC) membrane stabilization assays. The present investigation successfully attempted to explore remote sensing technologies and GIS (Geographic Information System) based system to predict the natural habitats of wild edible mushrooms of Meghalaya, India which we believe will lead to the generation of a mushroom specific non-wood forest resource mapping system in the near future. Results of nutritional profiling and biological activity studies on the representative species of wild edible mushrooms from the studied region revealed that it is a rich source of essential nutrients and antioxidants.

ResumenLa rica biodiversidad del estado de Meghalaya, India situado en los reinos de los hotspots mega-biodiversidad es el hogar de numerosas especies de macro hongos silvestres comestibles que se utilizan ampliamente por la población étnica micofílica como parte de su alimentación y medicina tradicional. Sin embargo, la pérdida de hábitat debido a la deforestación y el cambio climático está destruyendo la población natural de estos hongos, que agotan su disponibilidad para las poblaciones locales. En la presente investigación, se utilizó el SIG para la búsqueda guiada de hábitat usando Lentinula edodes como especie representativa en la cartografía de los hábitats de macrohongos silvestres comestibles de la región de estudio. Alrededor de cuatro mil ejemplares de distinto tipo morfológico fueron muestreados según su disponibilidad en los mercados tradicionales y los "sacred grove" (bosques sagrados) lo que indicó la presencia de diez géneros comunes pertenecientes a nueve familias de setas silvestres comestibles. Perfiles nutricionales de las especies representativas Lentinula edodes se llevaron a cabo mediante la evaluación de su humedad, grasa total, proteína cruda y contenido de carbohidratos. Del mismo modo, la determinación de componentes bioactivos se realizó por estimación de fenoles totales, flavonoides, ácido ascórbico, β-caroteno y licopeno. La bioactividad de los extractos de setas se estudió mediante la captación de radicales DPPH y el ensayo de estabilización de la membrana de glóbulos rojos de la sangre humana (hRBC). Los resultados de estudios de perfiles nutricionales y actividad biológica en hongos comestibles revelan que es una fuente rica en nutrientes esenciales y antioxidantes. La presente investigación ha intentado con éxito explorar las tecnologías de teledetección y SIG (Sistema de Información Geográfica) para predecir el hábitat natural de los hongos silvestres comestibles de Meghalaya, India que creemos dará lugar a la generación de un mapeo de los recursos forestales no madereros, específicamente de hongos, en el futuro cercano.

Plants, Edible/chemistry , Shiitake Mushrooms/chemistry , Anti-Inflammatory Agents/analysis , Nutritive Value , Plants, Edible/classification , Forests , Shiitake Mushrooms/classification , Geographic Information Systems , Biodiversity , India
Article in English | IMSEAR | ID: sea-158242


Context: C‑reactive protein (CRP) estimation for quantitative analysis to assess anti‑inflammatory action of nonsteroidal anti‑inflammatory drugs (NSAIDs) after surgery in maxillofacial surgery. Aims: This study was to evaluate the efficacy of CRP as a quantitative analysis for objective assessment of efficacy of three NSAIDs in postoperative inflammation and pain control. Settings and Design: The parallel study group design of randomization was done. Totally 60 patients were divided into three groups. CRP was evaluated at baseline and postoperatively (immediate and 72 h) after surgical removal of impacted lower third molar. The respective group received the drugs by random coding postoperatively. Subjects and Methods: The assessment of pain control and inflammation using NSAIDs postoperatively after surgical removal of impacted lower third molar was qualitatively and quantitatively assessed with CRP levels. The blood sample of the patient was assessed immediate postoperatively and after 72 h. The visual analog scale (VAS) was used for assessment of pain and its correlation with CRP levels. Statistical Analysis: Comparison of difference in levels of CRP levels had P < 0.05 with immediate postoperative and baseline levels. The duration of surgery with association of CRP levels P = 0.425 which was nonsignificant. The pain score was increased with mefenamic acid (P = 0.003), which was significant on VAS. Results: Diclofenac had the best anti‑inflammatory action. There was a significant increase in CRP levels in immediate postoperative values and 72 h. CRP test proved to be a useful indicator as a quantitative assessment tool for monitoring postsurgical inflammation and therapeutic effects of various anti‑inflammatory drugs. Conclusions: CRP test is a useful indicator for quantitative assessment for comparative evaluation of NSAIDs.

Anti-Inflammatory Agents/analysis , /analysis , Female , Humans , Inflammation/drug therapy , Male , Mandible/surgery , Molar, Third/surgery , Pain, Postoperative/drug therapy , Young Adult
Biol. Res ; 48: 1-9, 2015. ilus, graf, tab
Article in English | LILACS | ID: biblio-950776


BACKGROUND: In the present study, we examined the inhibitory effects of a methanolic extract, dichloromethane fraction, water layer, and polyhydroxylated sterols (1-4) isolated from the Vietnamese starfish Protoreaster nodosus on pro-inflammatory cytokine (IL-12 p40, IL-6, and TNF-α) production in LPS-stimulated bone marrow-derived dendritic cells (BMDCs) using enzyme-linked immunosorbent assays (ELISA). RESULTS: The methanolic extract and dichloromethane fraction exerted potent inhibitory effects on the production of all three pro-inflammatory cytokines, with IC50 values ranging from 0.60 ± 0.01 to 26.19 ± 0.64 µg/mL. Four highly pure steroid derivatives (1-4) were isolated from the dichloromethane fraction and water layer of P. nodosus. Potent inhibitory activities were also observed for (25S)5α-cholestane-3ß,4ß,6α,7α,8ß,15α,16ß,26-octol (3) on the production of IL-12 p40 and IL-6 (IC50s = 3.11 ± 0.08 and 1.35 ± 0.03 µM), and for (25S) 5α-cholestane-3ß,6α,8ß,15α,16ß,26-hexol (1) and (25S)5α-cholestane-3ß,6α,7α,8ß,15α,16ß,26-heptol (2) on the production of IL-12 p40 (IC50s = 0.01 ± 0.00 and and 1.02 ± 0.01 µM). Moreover, nodososide (4) exhibited moderate inhibitory effects on IL-12 p40 and IL-6 production. CONCLUSION: This is the first report of the anti-inflammatory activity from the starfish P. nodosus. The main finding of this study is the identification oxygenated steroid derivatives from P. nodosus with potent anti-inflammatory activities that may be developed as therapeutic agents for inflammatory diseases.

Animals , Mice , Starfish/chemistry , Dendritic Cells/drug effects , Interleukin-6/pharmacology , Tumor Necrosis Factor-alpha/pharmacology , Interleukin-12 Subunit p40/pharmacology , Anti-Inflammatory Agents/analysis , Steroids/administration & dosage , Vietnam , Enzyme-Linked Immunosorbent Assay , Cell Survival/drug effects , Lipopolysaccharides , Interleukin-6/analysis , Tumor Necrosis Factor-alpha/analysis , Inhibitory Concentration 50 , Interleukin-12 Subunit p40/analysis , Primary Cell Culture , Mice, Inbred C57BL
Braz. j. pharm. sci ; 50(4): 885-893, Oct-Dec/2014. tab, graf
Article in English | LILACS | ID: lil-741363


Curcuma longa is a ginger family aromatic herb (Zingiberaceae) whose rhizomes contain curcuminoid pigments, including curcumin, a compound known for its anti-inflammatory effects. The objective of this study was to obtain curcuminoid-rich extracts, develop topical formulations thereof, and assess the stability and skin permeation of these formulations. Curcuma longa extracts were obtained and used to develop formulations. Skin permeation studies were conducted in a modified Franz diffusion cell system, and skin retention of curcuminoid pigments was quantified in pig ear membrane. Prepared urea-containing gel-cream formulations were unstable, whereas all others had satisfactory stability and pseudoplastic rheological behavior. The amount of curcuminoid pigments recovered from the receptor solution was negligible. The skin concentration of curcuminoid pigments retained was positive (>20 µg/g of skin, mostly in the stratum corneum), considering the low skin permeability of curcumin. We conclude that development of topical formulations containing curcumin or Curcuma longa extract is feasible, as long as adjuvants are added to improve preservation and durability. The formulations developed in this study enabled penetration of curcumin limited to the superficial layers of the skin and then possibly without a risk of systemic action, thus permitting local use as a topical anti-inflammatory.

Curcuma longa é uma erva aromática, pertencente à família Zingiberaceae e seus rizomas contêm pigmentos curcuminoides, dentre eles a curcumina, conhecida por seu efeito anti-inflamatório. O objetivo deste trabalho foi obter extratos ricos nestes pigmentos, desenvolver e avaliar a estabilidade de formulações tópicas e realizar o estudo da penetração cutânea. Extratos de Curcuma longa foram obtidos e utilizados no desenvolvimento de formulações. A penetração e retenção cutâneas de pigmentos curcuminoides foi avaliada em pele de orelha de porco, utilizando célula de difusão de Franz modificada. As formulações de gel creme preparadas que continham ureia foram instáveis e as demais apresentaram estabilidade satisfatória e comportamento reológico pseudoplástico. A quantidade de pigmentos curcuminoides encontrada na solução receptora foi insignificante, enquanto que a quantidade retida na pele foi superior a 20 µg/g de pele. Concluiu-se como possível o desenvolvimento de formulações tópicas contendo curcumina ou extrato de Curcuma longa, conciliando a adição de adjuvantes para a preservação e maior durabilidade da mesma. As formulações promoveram a penetração da curcumina limitada às camadas superiores da pele, possivelmente sem o risco de ocorrência de ação sistêmica sendo possível a sua utilização para ação local com atividade anti-inflamatória.

Animals , Chemistry, Pharmaceutical , Curcuma/classification , Pigments, Biological , Additives in Cosmetics , Anti-Inflammatory Agents/analysis , Biological Products/classification
Braz. j. pharm. sci ; 49(4): 903-909, Oct.-Dec. 2013. ilus, tab
Article in English | LILACS | ID: lil-704122


Several 6-aryl-4-substituted benzylidene/furfurylidene pyridazin(2H)-3-one derivatives (4a-f) were synthesized and evaluated as analgesic and anti-inflammatory agents in mice and rats, respectively. All compounds were tested by using Eddy's hot plate and the carrageenan-induced hind paw oedema method for the evaluation of analgesic and anti-inflammatory activities, respectively. Results showed that compounds 4f, 4b, 4d, and 4e exhibited higher analgesic and anti-inflammatory activities than other remaining compounds. All title compounds (4a-f) were characterized by IR, NMR and Mass spectroscopy.

Diversos derivados benzilideno/furfurilideno piridazin(2H)-3-ona 6-aril-4-substituídos (4a-f) foram sintetizados e avaliados como analgésicos e anti-inflamatórios em camundongos e ratos, respectivamente. Todos os compostos foram testados utilizando-se o método de placa quente de Eddy e o de edema de pata induzido por carragenana para a avaliação das atividades analgésica e anti-inflamatória, respectivamente. Os resultados mostraram que os compostos 4f, 4b, 4d e 4e exibiram atividade analgésica e anti-inflamatória mais alta do que os compostos restantes. Todos os compostos (4a-f) foram caracterizados por IV, RMN e espectrometria de massas.

Rats , Analgesics/analysis , Anti-Inflammatory Agents/analysis , Pyridazines/classification , Analgesics/classification
Arq. ciênc. vet. zool. UNIPAR ; 16(1)jan-jun. 2013. tab
Article in Portuguese | LILACS | ID: lil-718760


A produção de embrião in vitro (PIV) associada à aspiração folicular transvaginal guiada O número médio de folículos a serem aspirados (imagem ultrassom) foi semelhante em todos os tratamentos (p>0,05). O Grupo III apresentou menor média de COC’s viáveis (p<0,05), enquanto o grupo Controle e o tratado com flunixin meglumine apresentaram média de COC’s viáveis semelhante (p>0,05). O número médio de COC’s aspirados no Grupo Controle foi 19,52 ± 11,00 COC’s e o de COC’s viáveis de 14,09 ± 8,53 por sessão de aspiração folicular. O número médio de ovócitos Grau I e II foi semelhante entre os grupos experimentais (p>0,05). No entanto, o número médio de ovócitos Grau III foi menor nos animais tratados com meloxicam (p<0,05). O número de ovócitos sem cumulus foi semelhante entre os grupos experimentais (p>0,05), enquanto o número de ovócitos atrésicos apresentou diferença somente entre os grupos tratados com anti-inflamatório (p<0,05), onde os animais tratados com meloxicam, apresentaram menor número médio de ovócitos atrésicos.

The production of bovine embryo in vitro (PIV) associated to the ultrasound-guided transvaginal folicularaspiration (OPU - Ovum pick-up) provided an increment in the reproduction productivity of cows, being of great importancefor the fast multiplication of these animals. However, it can cause morphologic and functional alterations in the ovaries. Thisstudy aims to evaluate the anti-inflammatory effects on the quantity and quality of cumulus oophorus complexes (COC’s)aspirated from the ovaries of crossbred heifers treated with anti-inflammatory. In order to do so, 18 heifers were divided inthree treatment groups, being Group I Control, II treated with Flunixin Meglumine (1.1 mg/Kg - Banamine®) and III treatedwith Meloxican (0,5 mg/kg - Maxicam®). The animals were submitted to ten OPU’s, being the collected oocytes quantifiedand evaluated. The average number of follicles to be aspirated was similar in all the treatments (p> 0.05). Group III showeda smaller average number of viable COC’s (p<0.05), whereas the Control group and the one treated with flunixin meglumineshowed a similar average number of viable COC’s (p>0.05). In the Control Group the average number of aspirated COC’swas 19.52 ± 11.00 COC’s and the average number of viable COC’s was 14.09 ±8.53 per folicular aspiration session. Theaverage number of oocytes of Degree I and II was similar among the experimental groups (p> 0.05). However, the averagenumber of oocytes of Degree III was smaller in the animals treated with meloxicam (p<0.05). The number of oocytes withoutcumulus was similar among the groups (p> 0.05), whereas the number of atresic oocytes showed difference among the groupstreated with anti-inflammatory, where that one treated with meloxicam showed a smaller average number of atresic oocytes.

Animals , Anti-Inflammatory Agents/analysis , Oocytes , Ovarian Follicle , Ovary/anatomy & histology , Cattle/classification
Rev. bras. plantas med ; 15(2): 264-272, 2013. graf, tab
Article in Portuguese | LILACS | ID: lil-677036


A espécie Mucuna pruriens (L.) DC. (Fabaceae) é popularmente conhecida no Brasil como "café berão" e "pó de mico". Suas sementes são bastante estudadas sendo empregadas na medicina popular para o tratamento de desordens nervosas e do aparelho reprodutor, porém poucas informações sobre a composição química e atividade farmacológica das folhas dessa espécie são descritas na literatura. Assim, os objetivos desse estudo foram: a determinação do perfil fitoquímico, a avaliação da atividade antioxidante in vitro, e a avaliação das atividades anti-inflamatória e antinociceptiva in vivo do extrato metanólico das folhas de M. pruriens nas concentrações de 100 e 300 mg/kg. O estudo fitoquímico foi realizado por meio da pesquisa qualitativa dos constituintes químicos e determinação quantitativa do teor de fenóis totais e flavonoides. O potencial antioxidante foi avaliado pelos métodos do DPPH e poder de redução. As atividades anti-inflamatória e antinociceptiva foram a ante foi promissor, com CI50 de 13,2∝g/mL pelo método do DPPH, e CE50 de 47,9∝g/mL pelo método que avalia o poder de redução. Em relação à atividade anti-inflamatória, o extrato foi capaz de inibir o edema de orelha em 63% (100mg/kg) e 28% (300mg/kg). Quanto à atividade antinociceptiva, houve redução do número de contorções abdominais de 64% (100 mg/kg) e 69% (300 mg/kg). Estes resultados indicam que M. pruriens apresenta um potencial farmacológico promissor e reforçam o conceito de que a pesquisa de plantas com usos etnofarmacológicos pode revelar um número substancial de respostas em ensaios in vitro e in vivo.

The species Mucuna pruriens (L.) DC. (Fabaceae) is popularly known in Brazil as "café berão" and "pó de mico". Its seeds have been widely studied and used in folk medicine for the treatment of nervous and reproductive system disorders; however, few studies are related to the chemical composition and pharmacological activity of its leaves. Therefore, the aims of this study were: investigation of the phytochemical profile, in vitro assessment of the antioxidant activity, and in vivo evaluation of the anti-inflammatory and antinociceptive activities of methanol extract of M. pruriens leaves at the concentrations of 100 and 300mg/kg. The phytochemical study was performed by means of qualitative identification of chemical constituents and quantitative determination of total phenols and flavonoids. The antioxidant potential was assayed by DPPH and reducing power methods. Anti-inflammatory and antinociceptive activities were evaluated by croton oil-induced ear edema and acetic acid-induced writhing tests, respectively. Alkaloids, coumarins, flavonoids, triterpenes and saponins were identified in the extract. Total phenol and flavonoid levels were 112 and 18.3mg/g extract, respectively. The antioxidant potential was promising, with IC50 of 13.2∝g/mL by DPPH assay and EC50 of 47.9∝g/mL by the method that evaluates the reducing power. Regarding the anti-inflammatory activity, the extract was capable of inhibiting by 63% (100mg/kg) and 28% (300mg / kg) the ear edema. As to the antinociceptive activity, there was a reduction in the number of writhings by 64% (100mg/kg) and 69% (300mg/kg). Results indicate that M. pruriens presents a promising pharmacological potential and reinforce the concept that the investigation of ethnopharmacologically used plants may reveal a substantial number of positive responses in in vitro and in vivo assays.

Antioxidants/analysis , Analgesics/analysis , Anti-Inflammatory Agents/analysis , Dolichos pruriens/pharmacology , Plant Leaves/adverse effects
Rev. bras. plantas med ; 15(3): 415-422, 2013. ilus, tab
Article in Portuguese | LILACS | ID: lil-684159


Foram avaliados os efeitos antiinflamatório, antibacteriano e mutagênico do extrato aquoso das sementes de Amburana cearensis. A atividade antiinflamatória foi avaliada em modelo de edema de pata induzido por carragenina, utilizando o extrato em concentrações de 10 % e 20 % nos grupos experimentais; AAS 10 mg/kg (v.o) no grupo padrão e água destilada no grupo controle. A atividade antimicrobiana foi determinada através do método de diluição em Agar, utilizando concentrações de extrato de 10 %, 7,5 %, 5 %, 2,5 % e 1 % em cepas de Sthaphylococcus aureus ATCC 27853, Escherichia coli ATCC 25922 e Pseudomonas aeruginosas ATCC 25923) e a atividade mutagênica foi determinada pelo teste de Allium cepa, utilizando extrato em concentrações de 0,02 mg/mL, 0,1 mg/mL e 0,5 mg/mL. O extrato aquoso das sementes de Amburana cearensis nas concentrações de 10 % e 20 % apresentou efeito antiedematogênico, estatisticamente significativo a partir de duas horas após administração do flogógeno, e tal efeito persistiu até 24 horas após a indução da resposta inflamatória. Quanto à atividade antibacteriana, o extrato não apresentou ação contra as cepas bacterianas de Sthaphylococcus aureus, Escherichia coli e Pseudomonas aeruginosas nas concentrações testadas. A análise dos resultados do teste de Allium cepa evidenciou ação tóxica (em concentração de 0,5 mg/mL) e mutagênica (micronúcleo 0,1 mg/mL e aberrações cromossômicas 0,1 mg/mL e 0,5 mg/mL) do extrato de Amburana cearensis em células meristemáticas de Allium cepa. Tais resultados sugerem potencial aplicação terapêutica no tratamento da inflamação. Contudo, também demonstram a necessidade de estudar para comprovar a segurança na utilização dessa espécie.

The anti-inflammatory, antibacterial and mutagenic effects of the aqueous extract of Amburana cearensis seeds were evaluated. The anti-inflammatory activity was evaluated by a paw edema model induced by carrageenan, using the extract at 10 % and 20 % concentrations in the experimental groups: AAS 10 mg/kg (orally administrated) in the standard group and distilled water in the control group. The antimicrobial activity was determined by the agar dilution method, using extract concentrations of 10 %, 7.5 %, 5 %, 2.5 % and 1% in strains of Staphylococcus aureus ATCC 27853, Escherichia coli ATCC 25922 and Pseudomonas aeruginosas ATCC 25923), and the mutagenic activity was determined by the Allium cepa test using extract concentrations of 0,02 mg/mL, 0,1 mg/mL and 0,5 mg/mL. The aqueous extract of Amburana cearensis seeds at 10 % and 20 % concentrations had an statistically significant antiedematogenic effect two hours after administering the flogogen, and this effect persisted for up to 24 hours after inducing the inflammatory response. Regarding the antibacterial activity, the extract showed no action against the bacterial strains of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosas at the concentrations tested. The results of the Allium cepa test showed the toxic (at a concentration of 0,5 mg/mL) and mutagenicity (0.1 mg/mL micronucleus and 0.1 mg/mL and 0.5 mg/mL chromosomal aberrations) actions of the Amburana cearensis extract on meristematic cells of Allium cepa. These results suggest potential therapeutic applications to treat inflammations. However, they also show the need for further studies to demonstrate the safe use of this species.

Animals , Female , Rats , Anti-Infective Agents/analysis , Anti-Inflammatory Agents/analysis , Bursera/classification , Mutagens/analysis , Carrageenan , Edema , Plant Extracts/therapeutic use , Seeds
Rev. bras. plantas med ; 15(3): 449-466, 2013. ilus, tab
Article in Portuguese | LILACS | ID: lil-684163


O processo inflamatório é o elo entre a síndrome metabólica e as doenças cardiovasculares. Para verificar a presença e o grau da inflamação, vários biomarcadores têm sido propostos e investigados. Este trabalho tem como objetivo revisar as recentes pesquisas que associam alguns marcadores expressos no tecido adiposo, enfatizando, dentre eles, a adiponectina, a resistina, a leptina e o transportador de glicose GLUT-4 na síndrome metabólica, a relação da inflamação decorrente desse conjunto de desordens metabólicas sob os receptores proliferadores peroxissomais (PPARs), bem como o efeito de diferentes extratos vegetais e produtos naturais bioativos na ativação desses receptores.

The inflammatory process is the link between metabolic syndrome and cardiovascular diseases. To verify the presence and degree of inflammation, several biomarkers have been proposed and different receptors have been investigated. This study aims to review recent researches involving some markers expressed in the adipose tissue, emphasizing, among them, adiponectin, resistin, leptin and glucose transporter GLUT-4 in the metabolic syndrome, the relationship of inflammation arising from this set of metabolic disorders on the peroxisome proliferator receptors (PPARs) and the effect of different bioactive compounds in the activation of these receptors.

Peroxisome Proliferator-Activated Receptors/pharmacology , Adipokines , Adipose Tissue , Anti-Inflammatory Agents/analysis , Biological Products/therapeutic use , Metabolic Syndrome/diagnosis
Braz. j. pharm. sci ; 49(spe): 57-65, 2013. ilus
Article in English | LILACS | ID: lil-686586


Dendrimers constitute an intriguing class of macromolecules which find applications in a variety of areas including biology. These hyperbranched macromolecules with tailored backbone and surface groups have been extensively investigated as nanocarriers for gene and drug delivery, by molecular encapsulation or covalent conjugation. Dendrimers have provided an excellent platform to develop multivalent and multifunctional nanoconjugates incorporating a variety of functional groups including drugs which are known to be anti-inflammatory agents. Recently, dendrimers have been shown to possess anti-inflammatory properties themselves. This unexpected and intriguing discovery has provided an additional impetus in designing novel active pharmaceutical agents. In this review, we highlight some of the recent developments in the field of dendrimers as nanoscale anti-inflammatory agents.

Dendrímeros constituem uma classe intrigante de macromoléculas que apresentam aplicações em diversas áreas incluindo biologia. Essas macromoléculas extremamente ramificadas com esqueleto planejado e grupos de superfície foram extensivamente investigadas como nanotransportadores de genes e de fármacos, por encapsulamento molecular ou conjugação covalente. Dendrímeros têm proporcionado uma plataforma excelente de desenvolvimento nanoconjugados multivalentes e multifuncionais incorporando uma variedade de grupos funcionais, incluindo fármacos que são conhecidos por atuarem agentes antiinflamatórios. Recentemente, os dendrímeros mostraram propriedades antiinflamatórias. Esta inesperada e intrigante descoberta tem proporcionado um impulso adicional no planejamento de novos agente farmacêuticos ativos. Nesta revisão, nós destacamos alguns dos desenvolvimentos recentes no campo dos dendrímeros como agentes antiinflamatórios em nanoescala.

Anti-Inflammatory Agents/analysis , Dendrimers/analysis , Cytokines , Nitric Oxide Synthase/metabolism
Braz. j. pharm. sci ; 47(4): 861-872, Oct.-Dec. 2011. ilus, graf, tab
Article in English | LILACS | ID: lil-618080


Atranorin (ATR) is the main compound from the lichen Cladina kalbii Ahti, which grows in the arid regions of northeastern Brazil. This study was conducted to evaluate the anti-inflammatory and toxicological properties of ATR. To evaluate anti-inflammatory properties, paw edema was induced by injecting 0.1 mL of carrageenan into the subplantar region of the right hind paw of rats, and leukocyte migration was induced by injection of 500 µL of carrageenan into the peritoneal cavity of mice. In addition, we determined ATR cytotoxicity in L929 cells by MTT assay and acute (5 g/kg-single dose) and subchronic (50 mg/kg-30 days) toxicity tests in Wistar rats. The results showed that ATR (100 mg/kg and 200 mg/kg) exhibited significant anti-inflammatory activity (paw edema and leukocyte migration). In the acute toxicity test, the animals showed hypoactivity and lethargy during the initial period (first 6 hours) and increase in total protein, total and indirect bilirubin, and alkaline phosphatase after 14 days in ATR-treated male rats. The subchronic toxicity test revealed increases in total protein, globulin, gamma-glutamyl transferase, alkaline phosphatase, and total and direct bilirubin in ATR-treated female rats. Histological analysis revealed no changes in the architecture and morphology of the organs. These results suggest that ATR has significant anti-inflammatory activity, with no significant acute and subchronic toxicity or cytotoxicity.

Atranorina (ATR) é o principal composto do líquen Cladina kalbii Ahti, que cresce em terras áridas do nordeste brasileiro. Este estudo foi realizado para avaliar as propriedades antiinflamatórias e toxicológicas da ATR. Para avaliar as propriedades antiinflamatórias, o edema de pata foi induzido, administrando-se 0,1 mL de carragenina na região subplantar da pata traseira direita e a migração leucocitária foi induzida pela injeção de 500 µL de carragenina no peritônio. Além disso, determinou-se a citotoxicidade da ATR, utilizando-se a linhagem celular L929, através do teste de MTT e dos testes de toxicidade aguda (5 g/kg - dose única) e subcrônica (50 mg/kg-30 dias) em ratos Wistar. Os resultados mostraram que nas doses de (100 mg/kg e 200 mg/kg) a ATR exibiu atividade antiinflamatória significativa nos ensaios de edema de pata e migração leucocitária. Nos testes de toxicidade aguda, os animais apresentaram hipoatividade e letargia no período inicial (primeiras 6 horas) e aumento das proteínas totais, bilirrubinas total e indireta e fosfatase alcalina depois de 14 dias nos machos tratados. Para o ensaio subcrônico, houve aumento das proteínas totais, gama-glutamil-transferase, fosfatase alcalina e bilirrubina total e direta nas fêmeas tratadas com ATR. Não foram encontradas alterações na arquitetura e morfologia das lâminas histológicas observadas. Esses resultados sugerem que a ATR apresenta atividade antiinflamatória significativa, sem apresentar significativa toxicidade aguda, subcrônica e citotoxicidade.

Anti-Inflammatory Agents/analysis , Parmeliaceae , Pharmacognosy/classification , Plants, Medicinal
Rev. Inst. Nac. Hig ; 42(2): 50-55, jul. 2011. tab
Article in Spanish | LILACS, LIVECS | ID: lil-631804


Introducción: El nimesulide es un analgésico antiinflamatorio no esteroideo, asociado en reportes de casos clínicos con hepatotoxicidad. Sin embargo, se han publicado pocos estudios controlados en animales. Objetivo: Determinar si la administración de dosis terapéuticas de nimesulide, durante diferentes periodos, altera el funcionalismo hepático en ratas Wistar machos y hembras. Materiales y métodos: Cuarenta ratas Wistar fueron distribuidas en 4 grupos de 10 cada uno (5 hembras y 5 machos). Grupo I (control): recibió 0.1 mL de solución salina durante 7 días, los animales de los grupos II, III y IV fueron tratados con nimesulide (3 mg/kg) durante 7, 21 y 35 días, respectivamente. Se determinaron niveles séricos de bilirrubina, fosfatasa alcalina y transaminasas. Resultados: La actividad de la enzima alanino-amino-transferasa (ALT) aumentó en machos (p< 0.01) y hembras (p < 0.02) de los grupos III y IV respecto a los controles. En los machos de los grupos II y IV aumentó la fosfatasa alcalina en comparación con las hembras de los mismos grupos (p < 0.05). Las bilirrubinas di - recta y total disminuyeron en las hembras del grupo IV respecto al control (p < 0.03). Conclusiones: Los resultados sugieren que a dosis terapéuticas el nimesulide altera el funcionalismo hepático en ratas Wistar.

Introduction: Nimesulide is a non-steroidal antiinfflamatory drug associated with hepatotoxicity. Nevertheless, there have few published controlled studies with animals. Objec - tive: Determine whether the administration of therapeutic doses of nimesulide during differents periods alters hepatic function in male and female rats. Materials and me - thods: Forty Wistar rats were classified into 4 groups of 10 rats each. Group I received 0,1 ml of saline for 7 days, whe reas the animals from groups II, III and IV were treated with Ni mesulide (3 mg/kg) during 7, 21 and 35 days, respectively. It has determined serum levels of bilirubin, alkaline phos pha tase and transaminases. Results: Alanino-amino-transferase (ALT) enzyme was increased in males (p<0.01) and females (p<0.02) from groups III and IV in com parison with the control group. Alkalin phosphate increased in males from groups II and IV in comparison with the females from these same groups (p< 0.05). Direct and total bilirubins decreased in group IV females (p< 0.03) in comparison with the control group. Conclusions: The administration of therapeutic doses of nimesulide affects hepatic function on Wistar rats.

Humans , Animals , Male , Female , Rats , Pharmaceutical Preparations/classification , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Liver Function Tests/methods , Anti-Inflammatory Agents/analysis , Rats/metabolism , Public Health
Bauru; s.n; 1996. 209 p. tab, graf.
Thesis in Portuguese | LILACS, BBO | ID: lil-222716


Aprofundamos o estudo dos efeitos farmacológicos da dexametasona, indometacina e tenoxicam e de uma droga citostática (metotrexano), assim como a análise dos mecanismos envolvidos na estimulaçäo flogógena causada por agentes de intensidades fraca, média e forte. Para isso, empregamos o teste edemogênico, que demonstrou serem os fármacos antiinflamatórios näo esteróides (tenoxicam e indometacina), os de maior potência na inibiçäo da exsudaçäo plasmática induzida pela paracoccidioidina. Todavia, com agentes flogógenos de intensidade média (carragenina), o metotrexano foi o medicamento mais potente, enquanto que com a placa microbiana dental (agente forte), a dexametasona e a indometacina foram os de maior potência antiinflamatória. Por meio da análise histomorfométrica relativa dos granulomas induzidos por esse último agente, verificamos até 14 dias, a maior potência antiinflamatória apresentada pelo tenoxicam, comparativamente a indometacina, pois inibiu mais acentuadamente a regiäo central de necrose supurativa, demonstrando efeito semelhante ao da dexametasona, näo obstante, em relaçäo à inibiçäo da densidade do volume do tecido granulomatoso, os fármacos mais potentes terem sido a indometacina e a dexametasona. Após os 14 dias näo foi constatada diferença significativa entre o efeito apresentado pelo tenoxicam e o da indometacina. O acentuado efeito apresentado pelos NSAIDs em relaçäo à inibiçäo da densidade de volume dos macrófagos, semelhante ao efeito do metotrexato, sugeriu que os NSATDs inibiram a proliferaçäo das células progenitoras mielóides dos monócitos/macrófagos. Também agiram tanto aumentando (21 dias) como inibindo (28 dias) a densidade de volume ocupada pelas fibras colágenas, enquanto que a dexametasona apresentou efeito contrário. Tais resultados indicaram que no processo inflamatório induzido por agentes flogógenos de intensidade forte (PMD) estimulores da acentuada produçäo Lts e PGs, o emprego de antiinflamatórios esteróides e näo esteróides foi vantajosa em relaçäo ao fármaco citostático

Animals , Male , Female , Adult , Rats , Anti-Inflammatory Agents, Non-Steroidal/analysis , Anti-Inflammatory Agents/analysis , Inflammation/pathology , Dexamethasone/adverse effects , Dexamethasone/analysis , Dexamethasone/pharmacology , Indomethacin/adverse effects , Indomethacin/analysis , Indomethacin/pharmacology , Methotrexate/adverse effects , Methotrexate/analysis , Methotrexate/pharmacology , Pathology, Oral
Article in English | WPRIM | ID: wpr-92429


Dexamethasone sodium phosphate (DSP) is increasingly used in the treatment of ocular inflammatory diseases by systemic, periocular, and recently, intravitreal injection. We have developed a method for the determination of vitreous levels of DSP by reverse phase HPLC. In this method, co-elution of vitreous proteins with DSP is resolved by a prior sample clean-up procedure using Waters Sep-Pak C18 cartridge; the protein is separated and eluted with water while DSP, paraben and prednisone are eluted with methanol. DSP in the resulting sample is then separated by reverse phase HPLC and quantified by UV absorption at 254 nm. The recovery of DSP through the sample clean-up is 68.9 +/- 3.0%. DSP quantitation is linear from 0.1 mg to 1.0 mg per 1.0 ml vitreous. This method provides a simple, sensitive and reliable technique for determining the vitreous levels of DSP.

Animals , Anti-Inflammatory Agents/analysis , Chromatography, High Pressure Liquid/methods , Dexamethasone/analogs & derivatives , Rabbits , Reproducibility of Results , Sensitivity and Specificity , Vitreous Body/chemistry
Indian J Exp Biol ; 1991 Feb; 29(2): 120-2
Article in English | IMSEAR | ID: sea-58533


Carrageenin (2%) was used to produce edema and hyperalgesia; indomethacin, phenylbutazone, aspirin, ibuprofen, analgin, paracetamol and phenacetin were tested at different doses for anti-inflammatory and analgesic activity in the same rats as the peak for the edema reached at the end of 3rd hr and for the hyperalgesia at the end of 4th hr. Indomethacin, phenylbutazone and ibuprofen reduced edema and increased the pain threshold. Analgin and aspirin increased the pain threshold relatively at a low dose. Paracetamol and phenacetin were inactive in the doses tested. Carrageenin (2%) was observed to possess both phlogistic and allogenic properties.

Analgesics/analysis , Animals , Anti-Inflammatory Agents/analysis , Drug Evaluation, Preclinical/methods , Edema/chemically induced , Hyperalgesia/chemically induced , Male , Rats , Rats, Inbred Strains