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1.
Med Chem ; 17(9): 983-993, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32885758

RESUMO

BACKGROUND: Inflammation involves a dynamic network that is highly regulated by signals that initiate the inflammation process as well as signals that downregulate it. However, an imbalance between the two leads to tissue damage. Throughout the world, inflammatory disease becomes common in the aging society. The drugs which are used clinically have serious side effects. Natural products or compounds derived from natural products show diversity in structure and play an important role in drug discovery and development. OBJECTIVE: Oreganum Vulgare is used in traditional medicine for various ailments including respiratory and rheumatic disorders, severe cold, suppression of tumors. The current study aims to evaluate the anti-inflammatory potential by evaluating various in vitro parameters. METHODS: Inflammation-induced in macrophages via LPS is the most accepted model for evaluating the antiinflammatory activity of various plant extracts and lead compounds. RESULTS: The extracts (OVEE, OVEAF) as well as the isolated compound(OVRA)of Oreganum Vulgare inhibit the pro-inflammatory cytokines (IL-6 and TNF-α) and NO without affecting cell viability. CONCLUSION: Our study established that the leaf extracts of Oreganum vulgare L. exhibit anti-inflammatory activity and thus confirm its importance in traditional medicine.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Origanum/química , Animais , Anti-Inflamatórios/química , Antioxidantes/química , Sobrevivência Celular/efeitos dos fármacos , Cinamatos/química , Cinamatos/metabolismo , Citocinas/metabolismo , Depsídeos/química , Depsídeos/metabolismo , Dexametasona/química , Dexametasona/metabolismo , Avaliação Pré-Clínica de Medicamentos , Interleucina-1beta/química , Interleucina-1beta/metabolismo , Lipopolissacarídeos/farmacologia , Camundongos , Simulação de Acoplamento Molecular , Óxido Nítrico/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Células RAW 264.7 , Fator de Necrose Tumoral alfa/química , Fator de Necrose Tumoral alfa/metabolismo , Ácido Rosmarínico
2.
Brain Behav Immun ; 81: 560-573, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31310797

RESUMO

A reduction in food intake is commonly observed after bacterial infection, a phenomenon that can be reproduced by peripheral administration of Gram-negative bacterial lipopolysaccharide (LPS) or interleukin-1beta (IL-1ß), a pro-inflammatory cytokine released by LPS-activated macrophages. The arcuate nucleus of the hypothalamus (ARH) plays a major role in food intake regulation and expresses IL-1 type 1 receptor (IL-1R1) mRNA. In the present work, we tested the hypothesis that IL-1R1 expressing cells in the ARH mediate IL-1ß and/or LPS-induced hypophagia in the rat. To do so, we developed an IL-1ß-saporin conjugate, which eliminated IL-R1-expressing neurons in the hippocampus, and micro-injected it into the ARH prior to systemic IL-1ß and LPS administration. ARH IL-1ß-saporin injection resulted in loss of neuropeptide Y-containing cells and attenuated hypophagia and weight loss after intraperitoneal IL-1ß, but not LPS, administration. In conclusion, the present study shows that ARH NPY-containing neurons express functional IL-1R1s that mediate peripheral IL-1ß-, but not LPS-, induced hypophagia. Our present and previous findings indicate that the reduction of food intake after IL-1ß and LPS are mediated by different neural pathways.


Assuntos
Peso Corporal/efeitos dos fármacos , Ingestão de Alimentos/efeitos dos fármacos , Interleucina-1beta/farmacologia , Saporinas/farmacologia , Animais , Núcleo Arqueado do Hipotálamo/efeitos dos fármacos , Núcleo Arqueado do Hipotálamo/metabolismo , Citocinas/metabolismo , Hipotálamo/efeitos dos fármacos , Hipotálamo/metabolismo , Proteína Antagonista do Receptor de Interleucina 1/metabolismo , Interleucina-1/metabolismo , Interleucina-1beta/química , Lipopolissacarídeos/farmacologia , Masculino , Vias Neurais/metabolismo , Neurônios/metabolismo , Neuropeptídeo Y/metabolismo , Ratos , Ratos Sprague-Dawley , Proteínas Recombinantes/farmacologia
3.
Drug Des Devel Ther ; 10: 1935-45, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27354767

RESUMO

Standardized extract of Phyllanthus amarus has previously been shown to have a strong inhibitory effect on phagocytic activity of human neutrophils. The current study was carried out to evaluate the effects of constituents of the extract of P. amarus on nitric oxide (NO) production as well as lymphocyte proliferation and cytokine release from phagocytes. Three compounds, ethyl 8-hydroxy-8-methyl-tridecanoate, 7ß,19α dihydroxy-urs-12-ene, and 1,7,8-trihydroxy-2-naphtaldehyde, together with seven known compounds were isolated from the whole plant of P. amarus. The isolated compounds and reference standards, ie, gallic acid, ellagic acid, corilagin, and geraniin, which were quantitatively analyzed in the extracts, were evaluated for their effects on immune cells. Among the compounds tested, the lignans, especially phyltetralin and phyllanthin, showed strong inhibition on lymphocyte proliferation with half maximal inhibitory concentration (IC50) values of 1.07 µM and 1.82 µM, respectively. Ethyl 8-hydroxy-8-methyl-tridecanoate and 1,7,8-trihydroxy-2-naphtaldehyde exhibited strong inhibition on nitric oxide production with IC50 values of 0.91 µM and 1.07 µM, respectively. Of all the compounds, corilagin was the strongest inhibitor of tumor necrosis factor-α release with an IC50 value of 7.39 µM, whereas geraniin depicted the strongest inhibitory activity on interleukin-1ß release with an IC50 value of 16.41 µM. The compounds constituting the extract of P. amarus were able to inhibit the innate immune response of phagocytes at different steps.


Assuntos
Interleucina-1beta/antagonistas & inibidores , Lignanas/química , Lignanas/farmacologia , Linfócitos/efeitos dos fármacos , Óxido Nítrico/química , Fagócitos/efeitos dos fármacos , Phyllanthus/química , Triterpenos/química , Triterpenos/farmacologia , Humanos , Interleucina-1beta/química , Lignanas/isolamento & purificação , Ativação Linfocitária , Linfócitos/química , Extratos Vegetais/farmacologia , Triterpenos/isolamento & purificação
4.
Animal ; 6(11): 1821-9, 2012 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-22717081

RESUMO

The experiment was conducted to evaluate the effects of dietary threonine (Thr) supplement on reproductive performance and immune function of the male mice challenged with pseudorabies virus (PRV). Kun-Ming male mice were assigned randomly to four groups with different Thr levels (0.70%, 0.88%, 1.10% and 1.30%). Half of the mice in each group were injected with PRV or phosphate-buffered saline (PBS) after 5 weeks' adaptation to diets. The second experiment examined the effects of dietary Thr level on copulation rate, pregnancy rate and average number per litter of PRV- or PBS-challenged male mice that copulated with adult female mice on the 9th day post PRV challenge. Sperm quality and testosterone of mice were decreased after PRV infection, but this effect was attenuated by increasing Thr levels. Copulation and conception rates were increased with increasing Thr levels (P = 0.14), but litter size was not affected (P > 0.05). In the PBS and PRV groups, mice fed higher levels of Thr had increased immunoglobulin (Ig)G, IgA and IgM concentrations. The PRV-specific antibody level, interleukin (IL)-1ß and tumor necrosis factor (TNF)-α concentration in PRV groups enhanced with increasing Thr levels; however, there was no difference in PBS groups. Furthermore, higher toll-like receptor (TLR)2 and TLR9 expressions in testis were observed by PRV challenge compared with PBS groups, and higher Thr supplement attenuated PRV-challenged induced the upregulation effect of TLR2 and TLR9 mRNA expression in testis (P < 0.05). These data suggest that higher Thr consumption was recommended in order to counteract the deleterious effects of virus invasion, possibly through the downregulated expression of TLRs, and thus to improve immunity and reproduction performance of male mice challenged with PRV.


Assuntos
Herpesvirus Suídeo 1 , Imunidade/efeitos dos fármacos , Pseudorraiva/tratamento farmacológico , Treonina/uso terapêutico , Animais , Anticorpos Antivirais/sangue , Suplementos Nutricionais , Imunoglobulina G/sangue , Interleucina-1beta/química , Masculino , Camundongos , Pseudorraiva/imunologia , Pseudorraiva/fisiopatologia , Reação em Cadeia da Polimerase em Tempo Real , Reprodução/efeitos dos fármacos , Reprodução/fisiologia , Espermatozoides/efeitos dos fármacos , Testículo/química , Testosterona/química , Testosterona/fisiologia , Treonina/administração & dosagem , Treonina/farmacologia , Fator de Necrose Tumoral alfa/química
5.
Photomed Laser Surg ; 25(6): 467-73, 2007 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-18158747

RESUMO

OBJECTIVE: This study evaluated the action of low-level laser therapy (LLLT) on the modulation of inflammatory reactions during wound healing in comparison with meloxicam. BACKGROUND DATA: LLLT has been recommended for the postoperative period because of its ability to speed healing of wounds. However, data in the literature are in disagreement about its anti-inflammatory action. METHODS: Standardized circular wounds were made on the backs of 64 Wistar rats. The animals were divided into four groups according to the selected postoperative therapy: group A-control; group B-administration of meloxicam; and groups C and D-irradiation with red (lambda = 685 nm) and infrared (lambda = 830 nm) laser energy, respectively. The animals were killed at 12, 36, and 72 h and 7 days after the procedure. RESULTS: Microscopic analysis revealed significant vascular activation of irradiated sites in the first 36 h. Only group B showed decreases in the intensity of polymorphonuclear infiltrates and edema. Group D showed a higher degree of organization and maturation of collagen fibers than the other groups at 72 h. The animals in group C showed the best healing pattern at 7 days. The anti-inflammatory action of meloxicam was confirmed by the results obtained in this research. The quantification of interleukin-1beta (IL-1beta) mRNA by real-time polymerase chain reaction (PCR) did not show any reduction in the inflammatory process in the irradiated groups when compared to the other groups. CONCLUSIONS: LLLT improves the quality of histologic repair and is useful during wound healing. However, with the methods used in this study the laser energy did not minimize tissue inflammatory reactions.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Inflamação/radioterapia , Terapia com Luz de Baixa Intensidade , Tiazinas/uso terapêutico , Tiazóis/uso terapêutico , Cicatrização/efeitos da radiação , Animais , Colágeno , Imuno-Histoquímica , Inflamação/tratamento farmacológico , Interleucina-1beta/química , Masculino , Meloxicam , Fotomicrografia , Reação em Cadeia da Polimerase , RNA Mensageiro/análise , Ratos , Ratos Wistar
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