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1.
J Sci Food Agric ; 100(2): 614-622, 2020 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-31597198

RESUMO

BACKGROUND: Lonicera japonica Thunb is a common herb in East Asia. The flower buds are usually regarded as the traditional medicinal part, while leaves and stems are considered less valuable and receive little attention. This study compared the chemical constituents and anti-inflammatory effects of the different tissues in L. japonica Thunb for the first time. RESULTS: Thirty compounds were identified by ultra-performance liquid chromatography-photodiode detector-quadrupole / time of flight-mass spectrometry (UPLC-PDA-Q/TOF-MS/MS) analysis. Hydroxycinnamic acids, flavonoids, and iridoids were identified as the major components. The flower buds (FLJ), leaves (LLJ), and stems (SLJ) of L. japonica Thunb showed strong similarities in chemical components. The LLJ contained higher levels of hydroxycinnamic acids and flavonoids than the FLJ and SLJ. Furthermore, FLJ, LLJ, and SLJ exhibited potent anti-inflammatory activity in croton oil-induced ear edema and carrageenan-induced paw edema assays in mice. Moreover, FLJ, LLJ, and SLJ showed a cytoprotective effect on lipopolysaccharide- (LPS-) stimulated RAW 264.7 macrophages. Lipopolysaccharide-induced increases in nitric oxide (NO), tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß), and interleukin-6 (IL-6) were suppressed by treatments of FLJ, LLJ, and SLJ, respectively. The LLJ possessed a stronger anti-inflammatory effect than the FLJ. CONCLUSION: Leaves and stems of L. japonica Thunb have chemical components and anti-inflammatory properties similar to flower buds, and may become alternative or supplementary sources of flower buds. © 2019 Society of Chemical Industry.


Assuntos
Anti-Inflamatórios/química , Edema/tratamento farmacológico , Lonicera/química , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Animais , Anti-Inflamatórios/administração & dosagem , Carragenina/efeitos adversos , Cromatografia Líquida de Alta Pressão , Edema/induzido quimicamente , Edema/genética , Edema/imunologia , Flavonoides/administração & dosagem , Flavonoides/química , Flores/química , Interleucina-1beta/genética , Interleucina-1beta/imunologia , Interleucina-6/genética , Interleucina-6/imunologia , Camundongos , Folhas de Planta/química , Caules de Planta/química , Espectrometria de Massas em Tandem , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/imunologia
2.
Planta Med ; 85(16): 1216-1224, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31546267

RESUMO

Bixin is the main natural apocarotenoid extracted from the seeds of Bixa orellana, widely used as a cosmetic and textile colorant. Despite the description of several pharmacological properties of B. orellana extracts, little has been studied regarding the pharmacological properties of bixin. Then we aimed to investigate the potential anti-inflammatory and antinociceptive effect of bixin in preclinical models of inflammation and acute pain. The anti-inflammatory activity of bixin (15 or 30 mg/kg, orally) was determined using carrageenan-induced paw edema and the myeloperoxidase (MPO) activity in male Wistar rats. The antinociceptive effect of bixin was assessed in the formalin and hot plate tests in rats (at same doses) and in the acetic acid-induced writhing test in Swiss albino male mice (at doses of 27 or 53 mg/kg). General locomotor activity was evaluated in the open field test. Only the higher dose of bixin significantly decreased the carrageenan-induced paw edema and the MPO activity and increased the latency time in the hot plate. Both doses of bixin significantly reduced the number of flinches in both phases of the formalin test and the number of acetic acid-induced writhings without changing the locomotor performance in the open field test. This study validates the use of bixin as an anti-inflammatory trough mechanism related to the reduction of neutrophil migration. Furthermore, this is the first report showing the antinociceptive property of bixin, which does not appear to be related to the sedative effect. Further studies are necessary to characterize the mechanisms involved in these effects.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Bixaceae/química , Carotenoides/farmacologia , Edema/tratamento farmacológico , Ácido Acético/efeitos adversos , Analgésicos/química , Animais , Anti-Inflamatórios/química , Carotenoides/química , Carragenina/efeitos adversos , Modelos Animais de Doenças , Inflamação/tratamento farmacológico , Masculino , Camundongos , Medição da Dor , Ratos , Ratos Wistar
3.
BMC Complement Altern Med ; 19(1): 214, 2019 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-31412852

RESUMO

BACKGROUND: The present study evaluated the antinociceptive effect of the bark of Artocarpus lacucha, which is used for the treatment of stomachache, headache and boils in the traditional system of medicine. METHODS: The antinociceptive activity was investigated by the tail immersion, hot plate, acetic acid- & formalin-induced nociception and carrageenan-induced paw edema tests using a hydro-methanolic extract of A. lacucha bark. The plant extract was found to contain a substantial amount of phenolic compounds according to the total phenolic and flavonoid content assay. A phenolic metabolite, (+)-catechin, has been isolated using different chromatographic techniques. The compound was characterized with 1D and 2D NMR spectroscopic data. (+)-catechin, isolated from A. lacucha was assessed for antinociceptive effects swiss albino mice. Furthermore, the possible involvement of opioid receptors and ATP-sensitive K+ channel for the effect of the plant extract and (+)-catechin has been justified using naloxone and glibenclamide, respectively. RESULTS: Oral administration (p.o) of the plant extract (50-200 mg/Kg b.w.) resulted in significant thermal pain protection in the hot plate and tail immersion tests. The action of the plant extract was significantly antagonized by naloxone, a non-selective opioid antagonist, in the hot plate and tail immersion tests, which supports the involvement of opioid receptors. Both the plant extract and (+)-catechin, (50-200 mg/Kg b.w., p.o.) significantly diminished the acetic acid- & formalin-induced nociception, and carrageenan-induced paw edema. Glibenclamide, an ATP-sensitive K+ channel blocker, significantly reversed their effect in the acetic acid-induced writhing test which indicates the participation of ATP-sensitive K+ channel system. CONCLUSIONS: The investigation revealed potential central and peripheral antinociceptive effects of A. lacucha bark supports its applications in the traditional system of medicine.


Assuntos
Analgésicos/administração & dosagem , Artocarpus/química , Catequina/administração & dosagem , Edema/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Analgésicos/química , Analgésicos/isolamento & purificação , Animais , Carragenina/efeitos adversos , Catequina/análise , Catequina/isolamento & purificação , Edema/induzido quimicamente , Humanos , Masculino , Camundongos , Nociceptividade/efeitos dos fármacos , Dor/tratamento farmacológico , Extratos Vegetais/química
4.
Phytomedicine ; 60: 152987, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31257118

RESUMO

BACKGROUND: Urinary tract infections are among the most common types of infections and give rise to inflammation with pain as one of the main symptoms. The herbal medicinal product Canephron® N contains BNO 2103, a defined mixture of pulverized rosemary leaves, centaury herb, and lovage root, and has been used in the treatment of urinary tract infections for more than 25 years. PURPOSE: To test the hypothesis that BNO 2103 reduces pain in cystitis and prostatitis by virtue of anti-inflammatory properties, and to reveal potential mechanisms underlying the anti-inflammatory features. STUDY DESIGN: BNO 2103 was studied for anti-inflammatory and analgesic properties in three animal models in vivo, and the mode of action underlying the anti-inflammatory features was investigated in human leukocytes and cell-free assays in vitro. METHODS: To assess the anti-inflammatory and analgesic efficacy of BNO 2103 we employed cyclophosphamide-induced cystitis and carrageenan-induced prostatitis in rats, and zymosan-induced peritonitis in mice. Human neutrophils and monocytes as well as isolated human 5-lipoxygenase and microsomal prostaglandin E2 synthase-1-containing microsomes were utilized to assess inhibition of leukotriene and/or prostaglandin E2 production by HPLC and/or ELISA. RESULTS: When given orally, BNO 2103 reduced inflammation and hyperalgesia in experimental cystitis in rats, while individual components of BNO 2103 also reduced hyperalgesia. Furthermore, BNO 2103 reduced hyperalgesia in rats with carrageenan-induced prostatitis. Cell-based and cell-free studies implicate inhibition of prostaglandin E2 and leukotriene B4 biosynthesis as potential mechanisms underlying the analgesic and anti-inflammatory effects. CONCLUSION: Our data support the hypothesis that BNO 2103 reduces pain by virtue of its anti-inflammatory properties, possibly related to suppression of prostaglandin E2 and leukotriene B4 formation, and suggest that this combination has the potential to treat clinical symptoms such as inflammatory pain. Thus BNO 2103 may represent an alternative to reduce the use of antibiotics in urinary tract infections.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Cistite/complicações , Dor/tratamento farmacológico , Extratos Vegetais/farmacologia , Prostatite/complicações , Analgésicos/química , Animais , Anti-Inflamatórios/química , Carragenina/efeitos adversos , Ciclofosfamida/efeitos adversos , Cistite/induzido quimicamente , Medicamentos de Ervas Chinesas , Feminino , Humanos , Hiperalgesia/tratamento farmacológico , Hiperalgesia/etiologia , Inflamação/tratamento farmacológico , Inflamação/etiologia , Masculino , Camundongos , Monócitos/efeitos dos fármacos , Neutrófilos/efeitos dos fármacos , Dor/etiologia , Extratos Vegetais/química , Prostatite/induzido quimicamente , Ratos , Ratos Sprague-Dawley
5.
Drug Dev Res ; 80(5): 666-679, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-31112325

RESUMO

Inflammation is the response of the body to noxious stimuli such as infections, trauma, or injury. Experimental studies have shown that vanillic acid has anti-inflammatory effects. The objective of this study was to investigate the anti-inflammatory and antipyretic properties of the derivative of vanillic acid, isopropyl vanillate (ISP-VT), in mice. The results of this study indicated that ISP-VT reduced paw edema induced by carrageenan, dextran sulfate (DEX), compound 48/80, serotonin, bradykinin (BK), histamine (HIST), and prostaglandin E2 (PGE2). Furthermore, ISP-VT reduced recruitment of leukocytes and neutrophils and reduced its adhesion and rolling, and decreased myeloperoxidase enzyme activity (MPO), cytokine levels (tumor necrosis factor-α and interleukin-6), and vascular permeability. ISP-VT also significantly reduced the expression of cyclooxygenase-2 (COX-2) in subplantar tissue of mice. ISP-VT inhibited COX-2 selectively compared to the standard drug. Our results showed that although ISP-VT binds to COX-1, it is less toxic than indomethacin, as evidenced by MPO analysis of gastric tissue. Treatment with the ISP-VT significantly reduced rectal temperature in yeast-induced hyperthermia in mice. Our results showed that the main mechanism ISP-VT-induced anti-inflammatory activity is by inhibition of COX-2. In conclusion, our results indicate that ISP-VT has potential as an anti-inflammatory and antipyretic therapeutic compound.


Assuntos
Anti-Inflamatórios/administração & dosagem , Carragenina/efeitos adversos , Inibidores de Ciclo-Oxigenase/administração & dosagem , Inflamação/tratamento farmacológico , Fenóis/efeitos adversos , Ácido Vanílico/química , Animais , Anti-Inflamatórios/síntese química , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Anticorpos Monoclonais/efeitos dos fármacos , Inibidores de Ciclo-Oxigenase/síntese química , Inibidores de Ciclo-Oxigenase/química , Inibidores de Ciclo-Oxigenase/farmacologia , Modelos Animais de Doenças , Feminino , Inflamação/induzido quimicamente , Inflamação/metabolismo , Injeções Intraperitoneais , Masculino , Camundongos , Modelos Moleculares , Fenóis/síntese química , Fenóis/química , Fenóis/farmacologia , Bibliotecas de Moléculas Pequenas/administração & dosagem , Bibliotecas de Moléculas Pequenas/síntese química , Bibliotecas de Moléculas Pequenas/química , Bibliotecas de Moléculas Pequenas/farmacologia
6.
Molecules ; 24(6)2019 Mar 26.
Artigo em Inglês | MEDLINE | ID: mdl-30917586

RESUMO

The purpose of this research was to extract and separate the compounds from frankincense, and then evaluate their anti-inflammatory effects. The isolated compound was a representative tetracyclic triterpenes of glycine structure according to ¹H-NMR and 13C-NMR spectra, which is ß-elemonic acid (ß-EA). We determined the content of six different localities of frankincense; the average content of ß-EA was 41.96 mg/g. The toxic effects of ß-EA administration (400, 200, 100 mg/kg) for four weeks in Kunming (KM) mice were observed. Compared with the control group, the body weight of mice, the visceral coefficients and serum indicators in the ß-EA groups showed no systematic variations. The anti-inflammatory effects of ß-EA were evaluated in LPS-induced RAW264.7 cells, xylene-induced induced ear inflammation in mice, carrageenin-induced paw edema in mice, and cotton pellet induced granuloma formation in rats. ß-EA inhibited overproduction of tumor necrosis factor-α(TNF-α), interleukin-6 (IL-6), monocyte chemotactic protein 1 (MCP-1), soluble TNF receptor 1 (sTNF R1), Eotaxin-2, Interleukin 10 (IL-10) and granulocyte colony-stimulating factor (GCSF) in the RAW264.7 cells. Intragastric administration with ß-EA (300, 200, and 100 mg/kg in mice, and 210, 140, and 70 mg/kg in rats) all produced distinct anti-inflammatory effects in vivo in a dose-dependent manner. Following treatment with ß-EA (300 mg/kg, i.g.), the NO level in mice ears and PGE2 in mice paws both decreased (p < 0.01). In conclusion, our study indicates that ß-EA could be a potential anti-inflammatory agent for the treatment of inflammatory diseases.


Assuntos
Anti-Inflamatórios/administração & dosagem , Dinoprostona/metabolismo , Franquincenso/química , Inflamação/tratamento farmacológico , Triterpenos/administração & dosagem , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Carragenina/efeitos adversos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Técnicas In Vitro , Inflamação/induzido quimicamente , Lipopolissacarídeos/efeitos adversos , Camundongos , Óxido Nítrico/metabolismo , Células RAW 264.7 , Ratos , Triterpenos/química , Triterpenos/farmacologia , Xilenos/efeitos adversos
7.
Food Funct ; 10(3): 1760-1762, 2019 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-30794268

RESUMO

Carrageenan (CGN) is a polysaccharide that is found in various types of sea weed. It is a common food additive used for its gelling and thickening properties and has been used safely throughout the world for decades. CGN is approved as Generally Recognized as Safe (GRAS) by the United States Food and Drug Administration and is also considered safe for the general population by the World Health Organizations Joint Expert Committee on Food Additive (JECFA) and the European Food Safety Authority. CGN has been tested for safety in various animal models for many years and more recently in an array of in vitro or cell-based models. A recent review published by this journal entitled "Revisiting the Carrageenan controversy: Do we really understand the digestive fate and safety of carrageenan in our foods?" has provided the impetus for this commentary (S. David, et al., Food Funct., 2018, 9(3), 1344-1352). It is important that our food is safe, and clearly there are examples of food additives that were found to be unsafe after years of use, but the issue is the need for accurate interpretation of previously published studies and the need for designing and conducting experiments that can be used to make decisions on safety. It is our hope that this commentary brings to light some of the important physical and chemical properties of CGN and how information can be easily misinterpreted.


Assuntos
Carragenina/efeitos adversos , Carragenina/química , Aditivos Alimentares/efeitos adversos , Aditivos Alimentares/química , Carragenina/metabolismo , Digestão , Aditivos Alimentares/metabolismo , Análise de Alimentos , Humanos
8.
Food Funct ; 10(3): 1763-1766, 2019 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-30794278

RESUMO

This commentary re-emphasizes the aim of our recent review (David et al., 2018) and addresses some of the points raised in the adjacent commentary by M. Weiner and J. McKim, Food Funct., 2019, 10, DOI: 10.1039/C8FO01282B. In agreement with the commentary, the discussed review highlights the need to adequately understand the complex physicochemistry of the food additive carrageenan (CGN) and its fate in the alimentary canal. In fact, there is a realm of scientific findings that justify the continuation of an open discussion of CGN safety. This response emphasizes that there is sparse information on [i] the physicochemical properties of commercial CGN, [ii] human levels of exposure to CGN from foods, [iii] the role of CGN in gut microbiome dysbiosis and inflammation, and [iv] the effects of CGN on susceptible populations. As long as the determinants of the increased prevalence of chronic and autoimmune diseases are not identified, we must continue to explore the possible beneficial or deleterious effects that may arise from extrinsic factors, including food additives, and do so in meticulous independent studies.


Assuntos
Carragenina/efeitos adversos , Carragenina/química , Aditivos Alimentares/efeitos adversos , Aditivos Alimentares/química , Carragenina/metabolismo , Digestão , Aditivos Alimentares/metabolismo , Análise de Alimentos , Humanos
9.
Daru ; 27(1): 59-70, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30701460

RESUMO

OBJECTIVE: Clinical utility of lornoxicam in oral therapy is primarily restricted by the low solubility and gastric adverse effects. This study evaluated the prospective of optimized proniosomal gel to improve the clinical efficacy of lornoxicam and compare with oral therapy. METHODS: Proniosomes were formulated by coacervation phase separation technique using span 60, lecithin and cholesterol. A four-factor three-level Box-Behnken design was used to evaluate the effect of amount of four independent variables; span 60 (X1), cholesterol (X2), lecithin (X3) and lornoxicam (X4) on response variables; vesicle size (Y1), entrapment efficiency (Y2) and transdermal flux (Y3). The selected proniosomal gel (F19) was characterized, and evaluated for the transdermal efficacy by ex vivo and in vivo experiments. RESULTS: Optimization study signifies that amount of formulation components (span 60, cholesterol, lecithin and lornoxicam) influence the vesicle size, entrapment efficiency and/or transdermal flux. Optimized formulation F19 exhibited nano size with high entrapment efficiency, adequate zeta potential, greater transdermal flux and better stability (at refrigerated conditions). The entrapment of lornoxicam in the bilayers of proniosome vesicles was confirmed by differential scanning calorimeter. Release profile of F19 was distinct (p < 0.001) from gel prepared using hydroxypropyl methylcellulose (control) and displayed steady lornoxicam release by Fickian diffusion. Transdermal administration of F19 significantly inhibited the carrageenan induced hind-paw edema in rats as compared to oral lornoxicam group. CONCLUSIONS: The data observed in this study demonstrated that the developed proniosomal gel (F19) improved the clinical efficacy of lornoxicam as compared to oral therapy. Graphical Abstract Proniosomal gel for transdermal delivery of lornoxicam: optimization using factorial design and in vivo evaluation in rats.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Carragenina/efeitos adversos , Inflamação/tratamento farmacológico , Piroxicam/análogos & derivados , Administração Cutânea , Administração Oral , Animais , Anti-Inflamatórios não Esteroides/química , Varredura Diferencial de Calorimetria , Composição de Medicamentos , Géis , Inflamação/induzido quimicamente , Lipossomos , Piroxicam/administração & dosagem , Piroxicam/química , Ratos
10.
Int J Food Sci Nutr ; 70(6): 725-737, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30775939

RESUMO

This study sought to determine the possible detrimental effects of several low- or non-caloric sweeteners on endothelial progenitor cells (EPCs), inflammation and behavioural changes in mice. C57BL/6 male mice received low and high dose of natural and artificial sweeteners for 4 weeks. EPCs, physical and biochemical variables, inflammation and behavioural changes were evaluated. A significant reduction of about 25% of EPCs was found when mice received a moderate amount of all sweeteners (p < .05). This reduction was more strongly significant when a double dose of glucose, aspartame, rebaudioside A and cyclamate (p < .005) in comparison to fructose and sucrose (p < .05) was administered. During inflammation carrageenan-induced, all sweeteners produced a significant increase of EPCs compared to the control group (p < .05). Consumption of glucose and sugar substitutes affect mouse EPC number according to the absence or presence of an inflammatory status, but does not induce detrimental effects on inflammation and behavioural changes.


Assuntos
Comportamento Animal/efeitos dos fármacos , Células Progenitoras Endoteliais/efeitos dos fármacos , Inflamação/tratamento farmacológico , Edulcorantes/farmacologia , Animais , Ansiedade , Pressão Sanguínea/efeitos dos fármacos , Peso Corporal , Carragenina/efeitos adversos , Comportamento Compulsivo , Diterpenos de Caurano/farmacologia , Frutose , Glucose , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Modelos Animais , Comportamento Obsessivo , Soro/química , Memória Espacial/efeitos dos fármacos , Sacarose
11.
Phytomedicine ; 52: 272-283, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30599908

RESUMO

BACKGROUND: Berberine (BBR) is the most abundant and major active constituent of Rhizoma Coptidis (RC), which has been widely used to treat inflammatory diseases in traditional oriental medicine. Despite BBR has been found to exhibit pronounced anti-inflammatory effect, the anti-inflammatory activities of its natural derivatives were sparsely dissected out. PURPOSE: To comparatively investigate the anti-inflammatory potential of BBR, and its natural oxoderivative (oxyberberine, OBB) and reduced derivative (dihydroberberine, DHBB) in vitro and in vivo, and delineate the possible underlying mechanism. METHODS: LC-MS/MS was used to identify the natural derivatives of BBR in RC. The potential anti-inflammatory properties of BBR and its natural derivatives were comparatively evaluated in vitro by lipopolysaccharide (LPS)-induced RAW264.7 macrophages cells, and in vivo via three typical acute inflammation murine models. Some important inflammation-related molecules were analyzed by ELISA, qRT-PCR and Western blotting. RESULTS: LC-MS/MS led to the identification of BBR, OBB and DHBB in RC ethyl acetate extract. The in vitro assay indicated that BBR, OBB and DHBB (1.25, 2.5 and 5 µM) pretreatment significantly decreased the levels of pro-inflammatory cytokines tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß), interleukin-6 (IL-6), prostaglandinE2 (PGE2) and nitricoxide (NO), and inhibited the mRNA expressions of cyclooxygenase-2 (COX-2) and inducible nitricoxide synthase (iNOS) in a dose-dependent manner, with relative efficiency of OBB > BBR > DHBB. Furthermore, OBB, BBR and DHBB remarkably inhibited the phosphorylation of nuclear factor-κB (NF-κB) p65 and inhibitory kappa Bα (IκBα). In vivo, BBR (20 mg/kg) and OBB (5, 10, and 20 mg/kg) pretreatment significantly ameliorated the xylene-induced ear edema, carrageenan-stimulated paw edema, and acetic acid-elicited vascular permeability in mice in a dose-dependent manner, with OBB exhibiting superior anti-inflammatory effect at the same dose (20 mg/kg). Histopathological analysis indicated that OBB and BBR could markedly attenuate the inflammatory deterioration and decrease the cellular infiltration in paw tissues. Additionally, the carrageenan-induced increases in TNF-α, IL-6, IL-1ß, PGE2 and NO productions, and COX-2 and iNOS mRNA expressions were effectually and concentration-dependently suppressed by OBB and BBR pretreatment. CONCLUSION: The anti-inflammatory activity of BBR and its natural derivatives was in the order of OBB > BBR > DHBB. OBB was for the first time found to be endowed with pronounced anti-inflammatory property, which was probably associated with suppressing the activation of NF-κB signaling pathway, and the subsequent gene expressions and productions of pro-inflammatory mediators. The results might contribute to illuminating the pharmacodynamic underpinnings of RC and provide evidence for developing OBB as a safe and promising natural lead compound in inflammation treatment.


Assuntos
Anti-Inflamatórios/farmacologia , Berberina/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Animais , Berberina/análogos & derivados , Carragenina/efeitos adversos , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/metabolismo , Edema/induzido quimicamente , Edema/tratamento farmacológico , Feminino , Inflamação/tratamento farmacológico , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Lipopolissacarídeos , Macrófagos/efeitos dos fármacos , Masculino , Camundongos , Inibidor de NF-kappaB alfa/metabolismo , Óxido Nítrico/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Células RAW 264.7 , Transdução de Sinais/efeitos dos fármacos , Fator de Transcrição RelA/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
12.
Phytomedicine ; 47: 58-68, 2018 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-30166109

RESUMO

BACKGROUND: Passiflora cincinnata Mast. is described as a native species from the Caatinga biome, and used by traditional medicine for several pharmacological purposes, such as inflammatory disorders. However, studies that prove its biological activities are scarce. HYPOTHESIS/PURPOSE: This paper aims to evaluate the antinociceptive and anti-inflammatory activities of the aerial parts of Passiflora cincinnata (Pc-EtOH) in mice. METHODS: The chemical composition of Pc-EtOH was assessed by high-performance liquid chromatography coupled to diode array detector (HPLC-DAD). The antinociceptive profile of the extract (given orally: 100, 200 and 400 mg/kg) was established using the in vivo chemical models (acetic acid-induced abdominal constriction and formalin-induced paw licking test) and thermal (hot plate test) of nociception. The role of opioid, potassium channels, TRPV-1, muscarinic, serotoninergic (5-HT3) receptors and the participation of the nitric oxide pathway also was determined. The rota-rod test was used to verify the possible interference of the extract treatment in motor performance. Paw edema induced by carrageenan or histamine, and leukocyte migration, determination of total protein and nitric oxide to the peritoneal cavity were used for anti-inflammatory profile. RESULTS: The presence of flavonoids in the extract was confirmed using HPLC-DAD. At all doses tested the Pc-EtOH significantly reduced the number of writhing and decreased the paw licking time in both phases of the formalin test (p < 0.05). In the hot plate test, the extract increased the reaction time, reducing painful behavior. The antinociceptive mechanism probably involves central and peripheral pathways, involving the pathway of opioid and muscarinic receptors with influence of potassium channels and the nitric oxide pathway. However, the motor coordination test indicated that in the time of 120 min the extract decreases the stay time of the animal in the rota-rod. Pc-EtOH inhibited significantly (p < 0.05) the increase of the edema volume after administration of carrageenan and histamine. In the peritonitis test, acute pre-treatment with Pc-EtOH inhibited leukocyte migration, with a reduction in the number of neutrophils and concentration of total proteins and nitric oxide. CONCLUSION: The present study suggests that Pc-EtOH possesses peripheral and central antinociceptive action, and showed potential in inhibition of release of mediators of the inflammatory process.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Passiflora/química , Extratos Vegetais/farmacologia , Animais , Carragenina/efeitos adversos , Edema/tratamento farmacológico , Etanol/efeitos adversos , Flavonoides/uso terapêutico , Masculino , Camundongos , Nociceptividade/efeitos dos fármacos , Dor/tratamento farmacológico , Medição da Dor , Componentes Aéreos da Planta/química
13.
Molecules ; 23(10)2018 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-30248903

RESUMO

Non-steroidal anti-inflammatory drugs (NSAIDs) are an important pharmacological class of drugs used for the treatment of inflammatory diseases. They are also characterized by severe side effects, such as gastrointestinal damage, increased cardiovascular risk and renal function abnormalities. In order to synthesize new anti-inflammatory and analgesic compounds with a safer profile of side effects, a series of 2,6-diaryl-imidazo[2,1-b][1,3,4]thiadiazole derivatives 5a⁻l were synthesized and evaluated in vivo for their anti-inflammatory and analgesic activities in carrageenan-induced rat paw edema. Among all compounds, 5c showed better anti-inflammatory activity compared to diclofenac, the standard drug, and compounds 5g, 5i, 5j presented a comparable antinociceptive activity to diclofenac. None of the compounds showed ulcerogenic activity. Molecular docking studies were carried out to investigate the theoretical bond interactions between the compounds and target, the cyclooxygenases (COX-1/COX-2). The compound 5c exhibited a higher inhibition of COX-2 compared to diclofenac.


Assuntos
Analgésicos/síntese química , Anti-Inflamatórios não Esteroides/síntese química , Edema/tratamento farmacológico , Imidazóis/síntese química , Tiadiazóis/síntese química , Analgésicos/administração & dosagem , Analgésicos/química , Analgésicos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Carragenina/efeitos adversos , Ciclo-Oxigenase 1/química , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/química , Ciclo-Oxigenase 2/metabolismo , Diclofenaco/administração & dosagem , Diclofenaco/uso terapêutico , Edema/induzido quimicamente , Feminino , Imidazóis/administração & dosagem , Imidazóis/química , Imidazóis/farmacologia , Proteínas de Membrana/química , Proteínas de Membrana/metabolismo , Conformação Molecular , Simulação de Acoplamento Molecular , Estrutura Molecular , Ratos , Relação Estrutura-Atividade , Tiadiazóis/administração & dosagem , Tiadiazóis/química , Tiadiazóis/farmacologia
14.
Eur J Pharmacol ; 836: 83-88, 2018 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-30118661

RESUMO

Chrysin, a natural polyphenol plentifully contained in honey, propolis, vegetables and fruits, it has been reported to exert a variety of pharmacological activities. In the present study, we mainly investigated the protective effects and underlying molecular mechanisms of chrysin on carrageenan-induced lung injury in rats. The results showed that chrysin inhibited the neutrophils infiltration, attenuated histological injury of lung tissues, decreased PMNs markers level and oxidative stress markers levels of lungs in rats. Further studies showed chrysin can inhibit the NF-кB activation in neutrophils cells, activate SIRT1/NRF2 pathway and reduce the expression of adhesion molecule in lung tissues. Taken together, these results suggested that chrysin can attenuate carrageenan-induced lung injury via inhibition of neutrophils activation and oxidative stress response, and that this attenuation is, at least partially, related to up-regulation of SIRT1/NRF2 signaling pathway. This study also validates SIRT1/NRF2 is an effective pharmacological target to protect against carrageenan-induced lung injury.


Assuntos
Carragenina/efeitos adversos , Flavonoides/farmacologia , Lesão Pulmonar/tratamento farmacológico , Fator 2 Relacionado a NF-E2/metabolismo , Pleurisia/tratamento farmacológico , Transdução de Sinais/efeitos dos fármacos , Sirtuína 1/metabolismo , Animais , Biomarcadores/metabolismo , Citocinas/metabolismo , Flavonoides/uso terapêutico , Lesão Pulmonar/induzido quimicamente , Lesão Pulmonar/metabolismo , Lesão Pulmonar/patologia , Masculino , Infiltração de Neutrófilos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Fosforilação/efeitos dos fármacos , Pleurisia/induzido quimicamente , Pleurisia/metabolismo , Pleurisia/patologia , Ratos , Ratos Sprague-Dawley , Fator de Transcrição RelA/metabolismo
15.
Med Glas (Zenica) ; 15(2): 87-92, 2018 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-29790482

RESUMO

Aim To investigate the lipid membranes of rat enterocytes in chronic carrageenan-induced gastroenterocolitis accompanied by the activation of apoptotic processes. Methods Steady-state fluorescence spectroscopy: a study by fluorescent probes - by ortho-hydroxy derivatives of 2,5-diaryl-1,3- oxazole. Activity of apoptosis signal-regulating kinase 1 and poly (ADP-ribose) polymerase in small intestinal homogenates, blood serum levels of matrix metalloproteinase-2 and caspase-3 and the level of DNA fragmentation in small intestinal homogenates were determined. Results Biochemical analysis revealed that an activation of apoptotic processes occurred in the intestinal epithelium of rats during chronic carrageenan-induced gastroenterocolitis. The fluorescence probes showed that activation of apoptotic processes in carrageenan-induced gastroenterocolitis was accompanied by changes in polar regions of rat enterocyte membranes, while no changes were revealed in more hydrophobic regions of the membranes. Conclusion The increase in hydration of membranes was attributed to the activation of the apoptosis of enterocytes. It has been shown that a fluorescent probe (2-(2'-hydroxyphenyl)-5-phenyl-1,3-oxazole) can be used for the detection of apoptosis of enterocytes.


Assuntos
Apoptose , Carragenina/efeitos adversos , Membrana Celular/efeitos dos fármacos , Enterocolite/fisiopatologia , Enterócitos/efeitos dos fármacos , Intestinos/efeitos dos fármacos , Animais , Caspase 3/sangue , Membrana Celular/química , Fragmentação do DNA , Enterocolite/induzido quimicamente , Enterocolite/metabolismo , Enterócitos/citologia , Enterócitos/metabolismo , Feminino , Corantes Fluorescentes , Inflamação/induzido quimicamente , Inflamação/metabolismo , Inflamação/fisiopatologia , Mucosa Intestinal/metabolismo , Intestinos/citologia , MAP Quinase Quinase Quinase 5/metabolismo , Metaloproteinase 2 da Matriz/sangue , Poli(ADP-Ribose) Polimerases/metabolismo , Ratos
16.
Phytomedicine ; 41: 82-95, 2018 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-29519324

RESUMO

BACKGROUND: Inflammation makes up a set of vascularized tissue reactions acting in the defense of the body against harmful stimuli. Natural products are a lower cost alternative with better benefit, often used in popular medicine in the treatment of inflammatory processes. Several species from the genus Croton have scientifically proven anti-inflammatory action. PURPOSE: This study aims to analyze the chemical composition of the Croton campestris A. St.-Hil essential oil (EOCC), derived from fresh leaves, as well as to evaluate the anti-inflammatory potential and the possible mechanisms of action of the EOCC and its constituent ß-caryophyllene. METHODS: The assays were performed in in vivo models of acute and chronic inflammation. Initially, the chemical composition of the EOCC was determined and its oral toxicity was evaluated, followed by the evaluation of its topical antiedematogenic effect through acute and chronic ear edema induced by Croton oil. For the systemic verification of an anti-inflammatory action, the abdominal contortions, formalin test, paw edema induced by carrageenan, dextran, histamine and arachidonic acid models, as well as a peritonitis test, vascular permeability and granuloma assays were performed. RESULTS: The evaluation of the essential oil chemical composition revealed the presence of ß-caryophyllene (15.91%), 1,8-cineol (16.98%) and germacrene-D (14.51%) as its main constituents. The EOCC had no relevant clinical toxicity on oral administration, with an LD50 of more than 5000 mg/kg. The tested substances showed anti-inflammatory action in the abdominal contortions, paw edema induced by carrageenan, dextran, histamine and arachidonic acid models, the formalin test, peritonitis test and vascular permeability; however, ß-caryophyllene had no significant effect on the granuloma assay. This suggests as a hypothesis that both substances tested showed significant influence on the arachidonic acid and histamine pathway reducing edema in these models. CONCLUSION: The tested substances have a clinically safe profile, additionally the EOCC and ß-caryophyllene presented relevant anti-inflammatory activity. This study supports the hypothesis that ß-caryophyllene, in association with other constituents present in the EOCC such as 1,8-cineole, contributed to the anti-inflammatory effect observed, in addition to suggesting that one of the mechanisms of action probably involves the inhibition of cytokines with the involvement of the arachidonic acid and histamine pathways.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Croton/química , Óleos Voláteis/química , Sesquiterpenos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/química , Ácido Araquidônico/toxicidade , Carragenina/efeitos adversos , Cicloexanóis/análise , Dextranos/toxicidade , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos/métodos , Edema/induzido quimicamente , Edema/tratamento farmacológico , Eucaliptol , Inflamação/tratamento farmacológico , Masculino , Camundongos , Monoterpenos/análise , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Sesquiterpenos/análise , Testes de Toxicidade Aguda
17.
Food Funct ; 9(3): 1344-1352, 2018 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-29469913

RESUMO

Carrageenan (CGN), a family of marine polysaccharides isolated from seaweeds, has been at the heart of considerable debate in recent years. To date, CGN is generally recognized as safe based on a history of safe use, various acute toxicology studies and some recent chronic toxicology tests. This review offers readers an overview of evidence on CGN characteristics and digestive fate that highlight various gaps in our understanding. Specifically, three unresolved gaps are identified. Firstly, little information can be found on the current levels of public exposure to CGN. Secondly, the link between CGN physicochemical properties, its impact on digestive proteolysis, the colon microbiome and inflammation are yet to be fully resolved. Thirdly, scant scientific evidence exists on the differential digestive fate of CGN in the gut of liable and predisposed populations, such as elderly people or IBD patients. Altogether, revisiting the scientific evidence indicates that more research is needed to elucidate the possibility that continued exposure to increasing levels of CGN in the human diet may compromise human health and well-being.


Assuntos
Carragenina/efeitos adversos , Carragenina/metabolismo , Extratos Vegetais/efeitos adversos , Extratos Vegetais/metabolismo , Alga Marinha/metabolismo , Animais , Carragenina/química , Digestão , Aditivos Alimentares/efeitos adversos , Aditivos Alimentares/química , Aditivos Alimentares/metabolismo , Humanos , Extratos Vegetais/química , Alga Marinha/química
18.
Nat Prod Res ; 32(23): 2861-2864, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29034741

RESUMO

Gmelina arborea has been traditionally used for treatment of abdominal pain, burning sensation and as stomachic. The anti-inflammatory effect of aqueous and methanol extract of this plant has been studied but detailed investigations on anti-inflammatory activity of G. arborea stem bark are still not available. Therefore, the present study was designed to evaluate the anti-inflammatory activity of methanol extract and its fractions using carrageenan induced paw oedema model. Methanol extract at the dose of 500 mg/kg and its ethyl acetate fraction at 50 mg/kg showed significant reduction in paw oedema in comparison with standard drug. Ethyl acetate fraction was subjected to column chromatography which resulted in isolation of a new flavonoid (GM-01). Anti-inflammatory effect of methanol extract and its fractions can be attributed to the presence of the flavonoid GM-01. Further studies are underway for evaluation of anti-inflammatory effect of GM-01 and identification of active constituents present in ethyl acetate fraction.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Casca de Planta/química , Verbenaceae/química , Animais , Anti-Inflamatórios/farmacologia , Carragenina/efeitos adversos , Edema/induzido quimicamente , Edema/tratamento farmacológico , Flavonoides/análise , Flavonoides/farmacologia , Masculino , Metanol , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar
19.
J Pharmacol Exp Ther ; 364(2): 221-228, 2018 02.
Artigo em Inglês | MEDLINE | ID: mdl-29212832

RESUMO

Adenosine is the final product of ATP metabolism, mainly derived from the action of 5'-nucleotidase cleavage of AMP. Cellular production of adenosine is greatly enhanced in inflamed tissues, ischemic tissues, and under hypoxia, where ATP is released from damaged cells. Much evidence has been accumulated on adenosine anti-inflammatory effects mediated through A2A receptor activation; A2A adenosine receptor has also been shown to play a role in matrix deposition and wound healing in a damaged tissue, contributing to dermal tissue protection and repair. Fibroblast growth factor-2 (FGF-2) is a powerful mitogen for fibroblast; it is expressed by several inflammatory cell types and plays a pivotal role in angiogenesis, wound healing, gastric ulcer protection. Human recombinant FGF-2 has been shown to have anti-inflammatory effects. The purpose of the present work was to investigate on the anti-inflammatory effect of systemic administration of the adenosine A2A agonist 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamidoadenosine hydrochloride hydrate (CGS21680) in the rat model of carrageenan-induced paw edema. We found that CGS21680 inhibits inflammation induced by carrageenan injection into the rat paw, and this effect is associated to the local reduction of cytokine levels and dermal increase of FGF-2 expression. Our results suggest that FGF-2 might be involved in the anti-inflammatory and tissue protective effect due to A2A receptor activation.


Assuntos
Agonistas do Receptor A2 de Adenosina/farmacologia , Adenosina/análogos & derivados , Edema/tratamento farmacológico , Fator 2 de Crescimento de Fibroblastos/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Membro Posterior , Fenetilaminas/farmacologia , Receptor A2A de Adenosina/metabolismo , Adenosina/farmacologia , Adenosina/uso terapêutico , Agonistas do Receptor A2 de Adenosina/uso terapêutico , Animais , Carragenina/efeitos adversos , Citocinas/metabolismo , Edema/induzido quimicamente , Edema/metabolismo , Inflamação/tratamento farmacológico , Masculino , Fenetilaminas/uso terapêutico , Ratos , Ratos Wistar
20.
Phytother Res ; 32(3): 480-487, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29243291

RESUMO

This study investigated the antiinflammatory properties of betulinic acid (BA) and xylopic acid (XA) extracted from Margaritaria discoidea and Xylopia aethiopica, respectively. M. discoidea and X. aethiopica are plants native in Ghana and the West-African region and used traditionally to treat different pathologies including inflammatory conditions. The antiinflammatory effect of BA and XA was established by an in vivo assay using the carrageenan-induced pleural inflammation model in mice. Also, the ability of BA and XA to increase catalase, superoxide dismutase, glutathione levels and decrease lipid peroxidation level in reactive oxidative assays was assessed. In addition, the ability of XA and BA to prevent potential lung tissue damage was quantified. Pretreatment with BA and XA reduced significantly, signs of inflammation: neutrophil infiltration, oedema, and alveoli septal thickening in carrageenan-treated lung tissue. Additionally, BA or XA pretreatment lowered the degree of lipid peroxidation in the lung tissue while increasing the levels of catalase, superoxide dismutase, and glutathione in vivo. Comparatively, XA was more efficacious than BA in the prevention of lung tissue damage. BA and XA derived from X. aethiopica and M. discoidea possess antiinflammatory and in vivo antioxidant activities in mice pleurisy model. The effect of these compounds gives credence to the traditional use in the management of inflammatory conditions of the airway.


Assuntos
Anti-Inflamatórios/uso terapêutico , Carragenina/efeitos adversos , Pleurisia/tratamento farmacológico , Pneumonia/tratamento farmacológico , Triterpenos/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Masculino , Camundongos , Pleurisia/patologia , Pneumonia/patologia
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