Assuntos
Educação de Pós-Graduação , Pesquisadores , Apoio à Pesquisa como Assunto , Justiça Social , Brasil , Pesquisadores/economia , Pesquisadores/educação , Bolsas de Estudo/economia , Bolsas de Estudo/tendências , Apoio à Pesquisa como Assunto/economia , Apoio à Pesquisa como Assunto/tendências , Justiça Social/economia , Justiça Social/tendênciasRESUMO
Pain is one of the most prevalent and difficult to manage symptoms in cancer patients, and conventional drugs present a range of adverse reactions. The development of ß-cyclodextrins (ß-CD) complexes has been used to avoid physicochemical and pharmacological limitations due to the lipophilicity of compounds such as p-Cymene (PC), a monoterpene with antinociceptive effects. Our aim was to obtain, characterize, and measure the effect of the complex of p-cymene and ß-cyclodextrin (PC/ß-CD) in a cancer pain model. Initially, molecular docking was performed to predict the viability of complex formation. Afterward, PC/ß-CD was obtained by slurry complexation, characterized by HPLC and NMR. Finally, PC/ß-CD was tested in a Sarcoma 180 (S180)-induced pain model. Molecular docking indicated that the occurrence of interaction between PC and ß-CD is favorable. PC/ß-CD showed complexation efficiency of 82.61%, and NMR demonstrated PC complexation in the ß-CD cavity. In the S180 cancer pain model, PC/ß-CD significantly reduced the mechanical hyperalgesia, spontaneous nociception, and nociception induced by non-noxious palpation at the doses tested (p < 0.05) when compared to vehicle differently from free PC (p > 0.05). Therefore, the complexation of PC in ß-CD was shown to improve the pharmacological effect of the drug as well as reducing the required dose.
Assuntos
Dor do Câncer , Ciclodextrinas , Neoplasias , beta-Ciclodextrinas , Humanos , Camundongos , Animais , Simulação de Acoplamento Molecular , beta-Ciclodextrinas/química , Dor/tratamento farmacológico , Dor/etiologia , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Analgésicos/química , SolubilidadeRESUMO
Obesity is a major public health problem, and there is increasing scientific interest in its mechanisms, as well as a search for new compounds with antioxidant and anti-inflammatory properties that can minimize the metabolic complications associated with its pathology. One potential source of these compounds is natural products; Among these, flavonoids are a promising group of natural substances. Flavonoids are active constituents with diverse biological activities and are widely found in plants kingdom. Numerous studies have shown that flavonoids can effectively inhibit obesity and related metabolic disorders. The review synthesizes recent evidence in respect of progress in the understanding of the anti-obesity effects of flavonoids. Such effects which occurs through the modulation of proteins, genes and transcriptional factors involved in decreasing lipogenesis, increasing lipolysis, expenditure energy, stimulating fatty acids B-oxidation, digestion and metabolism of carbohydrates. In addition to mitigating inflammatory responses and suppress oxidative stress. A better understanding of the modulating effects and mechanisms of flavonoids in relation to obesity will allow us to better use these compounds to treat or even prevent obesity and its associated comorbidities.
Assuntos
Fármacos Antiobesidade , Flavonoides , Obesidade , Fármacos Antiobesidade/farmacologia , Produtos Biológicos/farmacologia , Flavonoides/farmacologia , Humanos , Obesidade/prevenção & controleRESUMO
Parkinson's disease (PD) is identified by the loss of dopaminergic neurons in the Substantia Nigra pars compacta (SNpc), and is correlated to aggregates of proteins such as α-synuclein, Lewy's bodies. Although the PD etiology remains poorly understood, evidence suggests a main role of oxidative stress on this process. Lippia grata Schauer, known as "alecrim-do-mato", "alecrim-de-vaqueiro", "alecrim-da-chapada", is a native bush from tropical areas mainly distributed throughout the Central and South America. This plant species is commonly used in traditional medicine for relief of pain and inflammation conditions, and that has proven antioxidant effects. We evaluated the effects of essential oil of the L. grata after its complexed with ß-cyclodextrin (LIP) on PD animal model induced by reserpine (RES). Behavioral assessments were performed across the treatment. Upon completion the treatment, the animals were euthanized, afterwards their brains were isolated and processed for immunohistochemical and oxidative stress analysis. The LIP treatment delayed the onset of the behavior of catalepsy, decreased the number of oral movements and prevented the memory impairment on the novel object recognition task. In addition, the treatment with LIP protected against dopaminergic depletion in the SNpc and dorsal striatum (STRd), and decreased the α-syn immunoreactivity in the SNpc and hippocampus (HIP). Moreover, there was reduction of the oxidative stability index. These findings demonstrated that the LIP treatment has neuroprotective effect in a progressive parkinsonism model, suggesting that LIP could be an important source for novel treatment approaches in PD.
Assuntos
Lippia , Fármacos Neuroprotetores , Óleos Voláteis , Doença de Parkinson , Transtornos Parkinsonianos , beta-Ciclodextrinas , Animais , alfa-Sinucleína/metabolismo , Lippia/metabolismo , Reserpina , Óleos Voláteis/efeitos adversos , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Antioxidantes/metabolismo , Transtornos Parkinsonianos/induzido quimicamente , Transtornos Parkinsonianos/tratamento farmacológico , Transtornos Parkinsonianos/metabolismo , Doença de Parkinson/metabolismo , Neurônios Dopaminérgicos/metabolismo , Modelos Animais de Doenças , beta-Ciclodextrinas/efeitos adversos , Substância Negra/metabolismoRESUMO
Limonene (LIM) is a monoterpene, which is abundant in essential oils of Citrus fruits peels (Rutaceae). More recently, LIM, as a potential natural anticancer compound, has attracted major attention and exerted a chemopreventive activity, stimulating the detoxification of carcinogenic compounds and limiting tumor growth and angiogenesis in various cancer models. Twenty-six (26) articles were selected based on previously established criteria. Anticancer activity of LIM was related to the inhibition of tumor initiation, growth, and angiogenesis and the induction of cancer cells apoptosis. LIM was able to increase Bax expression, release cytochrome c, and activate the caspase pathway. In addition, LIM increased the expression of p53 and decreased the activity of Ras/Raf/MEK/ERK and PI3K/Akt pathways. LIM also decreased the expression of VEGF and increased the activities of the Man-6-P / IGF2R and TGF-ßIIR receptors. These results highlight LIM as an abundant natural molecule with low toxicity and pleiotropic pharmacological activity in cancer cells, targeting various cell-signaling pathways critically involved in the initiation, growth, and chemoresistance of cancer cells.
Assuntos
Limoneno/farmacologia , Neoplasias , Transdução de Sinais/efeitos dos fármacos , Apoptose , Humanos , Neoplasias/tratamento farmacológicoRESUMO
Phytol is a diterpene constituent of chlorophyll and has been shown to have several pharmacological properties, particularly in relation to the management of painful inflammatory diseases. Arthritis is one of the most common of these inflammatory diseases, mainly affecting the synovial membrane, cartilage, and bone in joints. Proinflammatory cytokines, such as TNF-α and IL-6, and the NFκB signaling pathway play a pivotal role in arthritis. However, as the mechanisms of action of phytol and its ability to reduce the levels of these cytokines are poorly understood, we decided to investigate its pharmacological effects using a mouse model of complete Freund's adjuvant (CFA)-induced arthritis. Our results showed that phytol was able to inhibit joint swelling and hyperalgesia throughout the whole treatment period. Moreover, phytol reduced myeloperoxidase (MPO) activity and proinflammatory cytokine release in synovial fluid and decreased IL-6 production as well as the COX-2 immunocontent in the spinal cord. It also downregulated the p38MAPK and NFκB signaling pathways. Therefore, our findings demonstrated that phytol can be an innovative antiarthritic agent due to its capacity to attenuate inflammatory reactions in joints and the spinal cord, mainly through the modulation of mediators that are key to the establishment of arthritic pain.
Assuntos
Anti-Inflamatórios/farmacologia , Citocinas/metabolismo , Adjuvante de Freund/química , Interleucina-6/metabolismo , Fitol/farmacologia , Fitol/uso terapêutico , Fator de Necrose Tumoral alfa/farmacologia , Animais , Anti-Inflamatórios/química , Clorofila/metabolismo , Clorofila/farmacologia , Clorofila/uso terapêutico , Citocinas/química , Modelos Animais de Doenças , Edema/tratamento farmacológico , Adjuvante de Freund/farmacologia , Hiperalgesia/tratamento farmacológico , Inflamação/metabolismo , Interleucina-6/química , Camundongos , Estrutura Molecular , NF-kappa B/metabolismo , Dor/tratamento farmacológico , Fitol/metabolismo , Membrana Sinovial/efeitos dos fármacos , Membrana Sinovial/metabolismo , Fator de Necrose Tumoral alfa/químicaRESUMO
This study evaluated whether resistance training (RT) could prevent glucocorticoid-induced vascular changes. Wistar rats were divided into groups: control (CO), dexamethasone (DEX), and Dexamethasone+RT (DEX+RT). On the eighth week, dexamethasone was administered in the DEX and DEX+RT groups. Thereafter, the animals were sacrificed and blood samples were used to assess the lipid profile, glucose and insulin. Vascular reactivity to insulin and phenylephrine (Phe) were evaluated. The DEX+RT group presented an improvement in the lipid profile, fasting glucose, and insulin levels compared to the DEX group. In addition, vasodilation was reduced in the DEX group compared to the CO group, and was increased in the DEX+RT group. After inhibition of phosphatidylinositol 3-kinase, DEX group showed contraction, in which it was in the DEX + RT group. When nitric oxide synthase (NOS) participation was evaluated, the DEX group presented a contraction compared to the CO group, with no contractile effect in the DEX+RT group. Moreover, vasoconstriction caused by NOS inhibition was abolished by BQ123 (endothelin receptor antagonist). In respect Phe response, there was an increase in tension in the DEX group compared to the CO group, being reduced in the DEX+RT group. The results suggest that RT prevented damage to vascular reactivity.
Assuntos
Treinamento Resistido , Vasodilatação , Animais , Dexametasona/farmacologia , Humanos , Insulina , Artérias Mesentéricas , Ratos , Ratos WistarRESUMO
The present study aimed to perform a systematic literature review to determine if there is a non-steroidal anti-inflammatory drug (NSAID) that interferes less within tooth movement. This research was performed according to the PRISMA statement. Articles were searched in eight electronic databases (PubMed, Scopus, Embase, Web of Science, LILACS, SciELO, Google Scholar, and Open Grey). Only experimental studies on male Wistar rats were selected, which included experiments related to the influence of NSAIDs on orthodontic movement. Studies in animals with pathological conditions, literature review articles, letters to the editor and/or editorials, case reports, abstracts, books, and book chapters were excluded. Each of the steps of this systematic literature review was performed by two examiners independently. RESULTS: the total sample consisted of 505 articles, from which 6 studies were eligible after a qualitative analysis. From the drugs assessed, paracetamol was unanimous for not interfering within orthodontic movement when compared to the control group. However, drugs such as aspirin, ibuprofen, sodium diclofenac, and selective cyclooxygenase-2 inhibitors caused a reduction in tooth movement when compared to the control group. CONCLUSION: paracetamol could be considered the drug of choice for pain relief because it interferes less within tooth movement.
Assuntos
Acetaminofen/farmacologia , Analgésicos não Narcóticos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Ibuprofeno/farmacologia , Dor Processual/tratamento farmacológico , Técnicas de Movimentação Dentária/efeitos adversos , Animais , Modelos Animais de Doenças , Ratos , Ratos WistarRESUMO
Peripheral nerve injury (PNI) is a serious public health problem that is linked with motor, sensory and autonomic deficits. Given the fact that this type of disorder leads to a decreased quality of life in most patients and adherence of available drugs is limited and have adverse effects, we investigated the efficacy of natural products in a PNI model. The search terms plants, medicinal, nerve regeneration, nerve crush, sciatic nerve as well as MeSH terms or free-text words were used to retrieve English language articles in PubMed, Scopus, Web of Science and LILACS published until July 2015. After sciatic nerve crush, natural products have improved significantly motor performance, sensory function and electrical conductance measured over weeks. Among the pharmacological targets suggested by the action of natural products, there were citations on the activation of the antiapoptotic signaling pathway, modulation in the expression of pro-inflammatory cytokines and neurotrophic factors. The systematic review provides scientific evidence that natural products are pharmacologically effective in the treatment of PNI such as sciatic nerve crush.
Assuntos
Produtos Biológicos/uso terapêutico , Regeneração Nervosa/efeitos dos fármacos , Doenças Neurodegenerativas/tratamento farmacológico , Doenças do Sistema Nervoso Periférico/tratamento farmacológico , Animais , Humanos , Doenças Neurodegenerativas/metabolismo , Doenças Neurodegenerativas/patologia , Traumatismos dos Nervos Periféricos/tratamento farmacológico , Traumatismos dos Nervos Periféricos/metabolismo , Traumatismos dos Nervos Periféricos/patologia , Doenças do Sistema Nervoso Periférico/metabolismo , Doenças do Sistema Nervoso Periférico/patologia , Extratos Vegetais/uso terapêuticoRESUMO
Annona vepretorum Mart. (Annonaceae) is a species popularly known in Brazil as "araticum" and "pinha da Caatinga". We have evaluated the antinociceptive effects of A. vepretorum in formalin-, capsaicin-, and glutamate-induced orofacial nociception in mice. Male Swiss mice were pretreated with either saline (p.o.), A. vepretorum ethanol extract (Av-EtOH 25, 50 and 100 mg/kg, p.o.), or morphine (10 mg/kg, i.p.), before formalin, capsaicin, or glutamate was injected into the right upper lip. Pre-treatment with Av-EtOH at all doses produced a reduction in face-rubbing behavior induced by formalin in both phases, and these pre-treatments also produced a significant antinociceptive effect in the capsaicin and glutamate tests. Pre-treatment with naloxone (1.5 mg/kg, i.p.) did not reverse the antinociceptive activity of the extract at the dose of 100 mg/kg in the first phase of this test. Our results suggest that Av-EtOH might be useful in the treatment of orofacial pain.
Assuntos
Analgésicos/farmacologia , Annona/química , Dor Facial/prevenção & controle , Extratos Vegetais/farmacologia , Folhas de Planta/química , Analgésicos/química , Animais , Capsaicina , Relação Dose-Resposta a Droga , Antagonismo de Drogas , Etanol/química , Dor Facial/induzido quimicamente , Formaldeído , Ácido Glutâmico , Masculino , Camundongos , Naloxona/farmacologia , Antagonistas de Entorpecentes/farmacologia , Medição da Dor/métodos , Fitoterapia , Extratos Vegetais/químicaRESUMO
The aim of this study was to investigate the wound-healing activity of (-)-borneol (BOR) incorporated in chitosan film on healing protocol in rodents. To assess the BOR wound-healing potential, male Wistar rats were subjected to a full-thickness excisional wound. The animals were divided into three groups: dressed with chitosan-based film (QUIN); dressed with chitosan-based film containing 0·5% BOR (QUIBO05); or dressed with chitosan-based film containing 1% BOR (QUIBO1). Dressing the wound areas and histological analysis were performed on the 3rd, 7th, 14th, and 21st days. The myeloperoxidase (MPO) activity was assessed on the third and seventh days after surgical procedures. Wounds dressed with chitosan-based film containing BOR reduced significantly the MPO activity (P < 0·001), showed significantly larger wound retraction rates (7 days, P < 0·05), improved the granulation reaction, and also provided better collagenisation density and arrangement during wound healing. It is suggested that BOR modulates the wound-healing process and is a promising compound to be used in wound care. This product may be quite useful in improving wound healing and could be a new biotechnological product with healing properties and clinical application. Further ongoing studies will enable us to understand the precise mechanisms whereby BOR improves the wound-healing process.
Assuntos
Canfanos/uso terapêutico , Quitosana/uso terapêutico , Monoterpenos/uso terapêutico , Pele/efeitos dos fármacos , Pele/patologia , Cicatrização/efeitos dos fármacos , Ferimentos e Lesões/tratamento farmacológico , Animais , Bandagens , Masculino , Ratos , Ratos Wistar , Cicatrização/fisiologiaRESUMO
CONTEXT: Chrysobalanus icaco L. (Chrysobalanaceae) has been used for the treatment of abdominal pain and cramps. OBJECTIVE: Assess the chemical and pharmacological profile of the lyophilized aqueous extract from C. icaco leaves (AEC). MATERIALS AND METHODS: Chromatographic methods were used to assess compounds from AEC. Mice were treated with vehicle (control group) or AEC (100, 200 or 400 mg/kg, p.o.) (group with 7-8 mice) and the analgesic profile was assessed employing the acetic acid-induced writhing, formalin, hot plate tests and hyperalgesia induced by carrageenan (CG) or tumour necrosis factor-alpha. The animal motor performance was assessed using rota-rod and grip strength tests. RESULTS: The chromatographic profile of AEC demonstrated the presence of terpenoid compounds. The acute pretreatment with AEC, at all doses, produced a significant (p < 0.01) inhibition of painful bahaviour (11.4 ± 3.6; 10.3 ± 2.8; 11.3 ± 2.2) when compared to the control group (24.7 ± 4.7) in acetic acid-induced writhing test. In the formalin test, AEC were effective in the second phase (p < 0.01) (57.2 ± 10.3; 56.3 ± 9.2; 54.7 ± 8.9) when compared to control group (121.9 ± 18.5). No response was observed in the hot plate test. The higher dose of AEC produced a significant (p < 0.01 or p < 0.05) inhibitory effect on the mechanical hyperalgesia test. AEC did not affect the motor performance of the mice. DISCUSSION: The terpenoids from AEC are known for its analgesic and anti-inflammatory properties. So, these results corroborate the experiments using the AEC in inflammatory pain protocols. CONCLUSION: Our results suggest that AEC act against inflammatory pain.
Assuntos
Analgésicos/farmacologia , Chrysobalanaceae , Medição da Dor/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta , Analgésicos/isolamento & purificação , Animais , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos/métodos , Liofilização , Masculino , Camundongos , Medição da Dor/métodos , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Água/farmacologiaRESUMO
BACKGROUND: Annona vepretorum Mart. (Annonaceae) is a native tree from Caatinga (Brazilian Northeastern savanna biome), popularly known as "araticum" and "pinha da Caatinga". In this study, we investigated the effects of the crude ethanolic extract (Av-EtOH) in models of pain and inflammation in rodents. METHODS: The evaluation of antinociceptive activity was carried out by the acetic acid-induced writhing, formalin, hot plate and tail flick tests, while paw edema induced by carrageenan or histamine, and leukocyte migration to the peritoneal cavity were used for anti-inflammatory profile. Histological analyses also were carried out. RESULTS: Av-EtOH (25, 50 and 100 mg/kg, p.o) significantly reduced the number of writhing (P < 0.01) and decreased (P < 0.01) the paw licking time in both phases of the formalin test. In the hot plate and tail flick tests, this extract increased the reaction time, consequently reduced painful behavior. The effects in the formalin and hot plate tests were antagonized by naloxone. Av-EtOH inhibited significantly (P < 0.01) the increase in the edema volume after administration of carrageenan and histamine. In the peritonitis test, acute pre-treatment with Av-EtOH inhibited leukocyte migration. Histological analysis showed less inflammation in the groups treated with the extract when the inflammation was induced by carrageenan or histamine. CONCLUSION: Thus, Av-EtOH has significant antinociceptive and anti-inflammatory properties, which are related probably with the activation of opioid receptors and inhibition of release of mediators of the inflammatory process. This specie is a potential target for drug discovery.
Assuntos
Analgésicos , Annona/química , Anti-Inflamatórios , Edema/tratamento farmacológico , Inflamação/tratamento farmacológico , Extratos Vegetais , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Comportamento Animal/efeitos dos fármacos , Dor , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , RatosRESUMO
The monoterpenes are the main constituents of most essential oils and p-cymene is a monoterpene commonly found in various species of aromatic herbs, which has been reported for anti-inflammatory, antinociceptive, and antimicrobial activities. However, there is no report concerning its pharmacological activity on the vascular smooth muscle. The aim of current work was to investigate the effects of p-cymene in isolated rat aorta and also study its mechanism of action. In this work, we show that p-cymene has a relaxant effect, in a dose-dependent way, on the vascular smooth muscle, regardless of the presence of the endothelium. Using a nonselective potassium channel blocker, the CsCl, the relaxant effect of p-cymene was attenuated. In the presence of more selective potassium channels blockers, such as TEA or 4-AP, no change in the relaxant effect of p-cymene was evidenced, indicating that BKCa and KV channels are not involved in that relaxant effect. However, in the presence of glibenclamide or BaCl2, KATP and Kir blockers, respectively, the relaxant effect of p-cymene was attenuated. The data presented indicate that p-cymene has a relaxing effect on rat aorta, regardless of the endothelium, but with the participation of the KATP and Kir channels.
Assuntos
Monoterpenos/farmacologia , Canais de Potássio/efeitos dos fármacos , Vasodilatação/efeitos dos fármacos , Vasodilatadores/farmacologia , 4-Aminopiridina/farmacologia , Animais , Aorta/efeitos dos fármacos , Césio/farmacologia , Cloretos/farmacologia , Cimenos , Dimetil Sulfóxido/farmacologia , Glibureto/farmacologia , Masculino , Músculo Liso Vascular/efeitos dos fármacos , Fenilefrina/farmacologia , Bloqueadores dos Canais de Potássio/farmacologia , Canais de Potássio/fisiologia , Ratos , Ratos Wistar , Tetraetilamônio/farmacologiaRESUMO
Remirea maritima is a tropical plant with a reticulated root system belonging to the family Cyperaceae, also known to have biologically active secondary metabolites. However, very few data on R. maritima's biological actions are available and there are no reports regarding the redox-active profile of this plant. In this study, we examined the total phenolic content of Remirea maritima hydroalcoholic (RMHA) extracts, redox properties against different reactive species generated in vitro and their cytotoxic effect against fibroblasts (L929) and melanoma (B16F10) cells. Total reactive antioxidant potential index (TRAP) and total antioxidant reactivity (TAR) results revealed that RMHA at all concentrations tested showed significant antioxidant capacity. RMHA was also effective against hydroxyl radical formation, reduction of Fe3+ to Fe2+ and in scavenging nitric oxide (NO) radicals. In vitro, the level of lipid peroxidation was reduced by RMHA extract and the data showed significant oxidative damage protection. The RMHA cytotoxicity was evaluated by a neutral red assay in fibroblast (L929) and melanome (B16F10) cells. The obtained results showed that the RMHA (40 and 80 µg/mL, respectively) reduced 70% of the viable cells. In conclusion, this study represents the first report regarding the antioxidant and anti-proliferative potential of R. maritima against B16F10 melanoma cells.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Cyperaceae/química , Fibroblastos/efeitos dos fármacos , Melanoma Experimental/metabolismo , Extratos Vegetais/farmacologia , Animais , Linhagem Celular , Linhagem Celular Tumoral , Fibroblastos/citologia , Fibroblastos/metabolismo , Melanoma Experimental/patologia , Camundongos , OxirreduçãoRESUMO
Xylopia laevigata (Annonaceae) is a medicinal plant used in folk medicine to treat pain and inflammation. Thus, we investigated the possible antioxidant, antinociceptive, and anti-inflammatory effects of X. laevigata leaf essential oil (EOX) in animal models. Our EOX sample showed the presence of γ-muurolene (17.78%), δ-cadinene (12.23%), bicyclogermacrene (7.77%), and α-copaene (7.17%) as main compounds. EOX presented a strong antioxidant potential according to the DPPH, TBARS, and nitrite production tests. Additionally, pretreatment with EOX, in mice, also significantly produced (P < 0.05 or P < 0.001) antinociceptive effect by reduction of nociceptive behavior (in formalin and writhing tests). The EOX showed c-Fos label in the olfactory bulb, piriform cortex, and periaqueductal gray. Acute administration of EOX exhibited a significant (P < 0.01 or P < 0.001) anti-inflammatory profile in the carrageenan-induced peritonitis and by the carrageenan-induced hindpaw edema tests in mice. Our results provide evidence for the use of X. laevigata by traditional medicine practitioners in the management of pain and inflammatory disorders.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Xylopia/química , Analgésicos/química , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Edema/tratamento farmacológico , Inflamação/tratamento farmacológico , Masculino , Camundongos , Nociceptividade/efeitos dos fármacos , Óleos Voláteis/química , Óleos Voláteis/uso terapêutico , Peritonite/tratamento farmacológico , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Proteínas Proto-Oncogênicas c-fos/genética , Proteínas Proto-Oncogênicas c-fos/metabolismo , Sesquiterpenos/análiseRESUMO
Chronic diseases such as cancer, diabetes, neurodegenerative and cardiovascular diseases are characterized by an enhanced state of oxidative stress, which may result from the overproduction of reactive species and/or a decrease in antioxidant defenses. The search for new chemical entities with antioxidant profile is still thus an emerging field on ongoing interest. Due to the lack of reviews concerning the antioxidant activity of lichen-derived natural compounds, we performed a review of the antioxidant potential and mechanisms of action of natural compounds isolated from lichens. The search terms "lichens", "antioxidants" and "antioxidant response elements" were used to retrieve articles in LILACS, PubMed and Web of Science published until February 2014. From a total of 319 articles surveyed, 32 met the established inclusion and exclusion criteria. It was observed that the most common isolated compound studied was usnic acid, cited in 14 out of the 32 articles. The most often described antioxidant assays for the study of in vitro antioxidant activity were mainly DPPH, LPO and SOD. The most suggested mechanisms of action were scavenging of reactive species, enzymatic activation and inhibition of iNOS. Thus, compounds isolated from lichens are possible candidates for the management of oxidative stress, and may be useful in the treatment of chronic diseases.
Assuntos
Elementos de Resposta Antioxidante , Antioxidantes/química , Líquens/química , Neoplasias/tratamento farmacológico , Antioxidantes/farmacologia , Benzofuranos/metabolismo , Compostos de Bifenilo/administração & dosagem , Compostos de Bifenilo/química , Sequestradores de Radicais Livres/metabolismo , Humanos , Oxirredução , Estresse Oxidativo , Picratos/administração & dosagem , Picratos/químicaRESUMO
The search for more effective and lower cost therapeutic approaches for wound healing remains a challenge for modern medicine. In the search for new therapeutic options, plants and their metabolites are a great source of novel biomolecules. Among their constituents, the monoterpenes represent 90% of essential oils, and have a variety of structures with several activities such as antimicrobial, anti-inflammatory, antioxidant and wound healing. Based on that, and also due to the lack of reviews concerning the wound-healing activity of monoterpenes, we performed this systematic review-which provides an overview of their characteristics and mechanisms of action. In this search, the terms "terpenes", "monoterpenes", "wound healing" and "wound closure techniques" were used to retrieve articles published in LILACS, PUBMED and EMBASE until May 2013. Seven papers were found concerning the potential wound healing effect of five compouds (three monoterpenes and two iridoid derivatives) in preclinical studies. Among the products used for wound care, the films were the most studied pharmaceutical form. Monoterpenes are a class of compounds of great diversity of biological activities and therapeutic potential. The data reviewed here suggest that monoterpenes, although poorly studied in this context, are promising compounds for the treatment of chronic wound conditions.
Assuntos
Iridoides/farmacologia , Monoterpenos/farmacologia , Extratos Vegetais/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Avaliação Pré-Clínica de Medicamentos , Humanos , Iridoides/uso terapêutico , Monoterpenos/uso terapêutico , Extratos Vegetais/uso terapêutico , Plantas Medicinais/químicaRESUMO
CONTEXT: Syzygium cumini (L.) Skeels (Myrtaceae) is a tree with dark purple fruits, popularly known as "jambolão" or "jambolan". In folk medicine, this plant is used for the treatment of diabetes and inflammatory conditions. OBJECTIVE: We investigated the antinociceptive effect of ethanol extract (EE) from S. cumini leaves on orofacial nociception. MATERIAL AND METHODS: The antinociceptive effects of the EE obtained from the leaves of S. cumini were evaluated in mice using formalin- and glutamate-induced orofacial nociception. RESULTS: ESI-MS/MS analyses demonstrated that major constituents in the analyzed samples coincided with the mass of the phenolic acids and flavonoids. In pharmacological approach, pre-treatment with EE (100, 200, or 400 mg/kg, p.o.) significantly reduced (p<0.05 or p<0.01) the percentage of paw licks time during phase 2 (43.2, 47.1, and 57.4%, respectively) of a formalin pain test when compared to control group animals. This effect was prevented by pretreatment with glibenclamide and N(G)-nitro-l-arginine (l-NOARG). The extract, all doses, also caused a marked inhibition (p<0.01 or p<0.001) of glutamate-induced orofacial nociception (38.8, 51.7, and 54.7%) when compared with the control group. No effect was observed with the rota-rod model. CONCLUSIONS: We can suggest that the antinociceptive effect of the EE is mediated by peripheral mechanisms, possibly involving KATP channels and the nitric oxide pathways. These effects appear to be related to the presence of flavonoids compounds, such as quercetin.
Assuntos
Analgésicos/uso terapêutico , Dor Facial/tratamento farmacológico , Medição da Dor/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Folhas de Planta , Syzygium , Analgésicos/isolamento & purificação , Animais , Método Duplo-Cego , Dor Facial/patologia , Masculino , Camundongos , Nociceptividade/efeitos dos fármacos , Nociceptividade/fisiologia , Medição da Dor/métodos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologiaRESUMO
Neuropathic pain is a high-intensity pain that can be caused by compression, transection, injury, nerve infiltration and drug treatment of cancer. Furthermore, drug therapy has low clinical efficacy, many adverse effects and remission of painful symptoms. In this way, natural products derived from plants constitute a promising therapeutic alternative. Therefore, the aim of this study was to evaluate the antihyperalgesic effect of γ-terpinene (γ-TPN) e γ-terpinene in ß-cyclodextrin inclusion complexes (TPN/CD) on neuropathic pain induced by tumor cells. Complexation extended the effect time for another 5 h and daily treatment for six days with γ-TPN (50 mg/kg, p.o.) and γ-TPN/ß-CD (50 mg/kg, p.o.) significantly reduced (p < 0.001) the mechanical hyperalgesia induced by the administration of 2x106 sarcoma cells 180 in the around the sciatic nerve. In addition, the Grip and Rota-rod techniques demonstrated that there was no interference on the muscle strength and motor coordination of the animals, suggesting that the compound under study does not have central nervous system depressant effects at the doses used. Molecular docking studies demonstrate favorable binding energies between γ-TPN and ß-CD, and alpha-2 adrenergic, glutamatergic, opioid and cholinergic receptors. Thus, this study demonstrates the potential of terpinene complexation in controlling neuropathic pain induced by tumor cells.