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1.
Carbohydr Polym ; 220: 43-52, 2019 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-31196549

RESUMO

An environmentally friendly and low-cost material based on cellulose filter paper modified with ß-cyclodextrin (ß-CD) was designed to uptake and elute drugs for water purification. To carry out the work, a ß-CD derivative was first obtained through reaction of ß-CD with N-(hydroxymethyl) acrylamide (NMA), and then ß-CD-NMA was grafted on cellulose by means of the Fenton's reaction. The CD-grafted cellulose paper was characterized by ATR-FTIR analysis, SEM images, and mechanical properties. CD-functionalized (F1) and non-functionalized (NF) papers were tested in aqueous media containing an antibiotic (ciprofloxacin) or a non-steroidal anti-inflammatory drug (diclofenac) covering a wide range of salinity levels. Ciprofloxacin was similarly adsorbed by both papers through ionic interactions, while diclofenac was selectively and remarkably captured by the CD-functionalized filter (up to 25 mg g-1 from saline medium under biorelevant conditions; ca. 60 mg g-1 Langmuir isotherm model). Effects of diclofenac concentration, volume of medium, and incubation time on the amount adsorbed were investigated in detail. Elution tests involved the combination of several organic solvents and alkaline solutions and revealed that acetonitrile:NaOH 10 mM aq. solution (50:50, v/v) allows for an effective recovery of the previously trapped diclofenac. Application of ultrasounds shortened the process to 10 min. Reusability of F1 papers was also evaluated. Overall, the CD-grafted cellulose paper appears as a suitable material for bioremediation and analytical purposes.


Assuntos
Anti-Inflamatórios não Esteroides/isolamento & purificação , Celulose/análogos & derivados , Ciclodextrinas/química , Diclofenaco/isolamento & purificação , Filtração/instrumentação , Poluentes Químicos da Água/isolamento & purificação , Purificação da Água/instrumentação , Água/análise , Anti-Inflamatórios não Esteroides/química , Biodegradação Ambiental , Ciprofloxacino/química , Ciprofloxacino/isolamento & purificação , Diclofenaco/química , Salinidade , Poluentes Químicos da Água/química
2.
Phytochemistry ; 164: 206-214, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31177053

RESUMO

Eight undescribed cholestane glycosides named osaundersioside A-H, along with three previously known compounds named osaundersioside I-K were isolated from Ornithogalum saundersiae Baker bulbs (Asparagaceae). Their structures were elucidated by extensive spectroscopic analysis and chemical methods. All isolates were evaluated for their cytotoxic activity and inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production. Osaundersioside C was thus determined to exhibit specific cytotoxicity towards MCF-7 cell line with an IC50 value of 0.20 µM, Osaundersioside H exhibited inhibitory effect on NO production in macrophages at the concentration of 10-5 M, with inhibition rate of 56.81%.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Asparagaceae/química , Colestanos/farmacologia , Glicosídeos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Colestanos/química , Colestanos/isolamento & purificação , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Glicosídeos/química , Glicosídeos/isolamento & purificação , Humanos , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Células MCF-7 , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Casca de Planta/química , Raízes de Plantas/química , Relação Estrutura-Atividade
3.
Phytochemistry ; 164: 228-235, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31181354

RESUMO

Terminthia paniculata (Sanyeqi) is widely used for treating inflammation and rheumatic arthritis in the folk areas of Yunnan province, China. Its total extract was first revealed with xanthine oxidase (XO) inhibitory activity in vitro and anti-hyperuricemic effect in vivo. Bioassay-guided separation on Fr. A5 yielded six chalcone-flavonone heterodimers, termipaniculatones A-F. Their structures were elucidated based on extensive spectroscopic analyses involving HRESIMS, 1D and 2D NMR, UV, IR and [α]D, and the absolute configuration of termipaniculatone F was verified by ECD calculation. Termipaniculatones A and E showed obvious XO inhibitory activity with IC50 values of 55.6 and 89.5 µM, respectively, which took effects via a mix-type mode. A molecular modeling study revealed that termipaniculatone A was well located into the active site of XO by interacting with Glu802, Arg880, Thr1010 and Val1011 residues. Termipaniculatone A showed anti-hyperuricemic effects by decreasing serum uric acid levels and inhibiting XO activity in both serum and liver on potassium oxonate (PO)-induced hyperuricemia mice, and anti-inflammatory activity through alleviating paw swelling on monosodium urate (MSU)-induced mice, at the concentration of 20 mg/kg. This is the first time to reveal the anti-hyperuricemic and anti-acute gouty arthritis potency of T. paniculata and the characteristic biflavonoids as active constituents, which provides valuable information for searching new XO inhibitors from natural sources.


Assuntos
Anacardiaceae/química , Anti-Inflamatórios não Esteroides/farmacologia , Artrite Gotosa/tratamento farmacológico , Inibidores Enzimáticos/farmacologia , Hiperuricemia/tratamento farmacológico , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Artrite Gotosa/induzido quimicamente , Artrite Gotosa/metabolismo , Chalcona/química , Chalcona/isolamento & purificação , Chalcona/farmacologia , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Edema/tratamento farmacológico , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Flavanonas/química , Flavanonas/isolamento & purificação , Flavanonas/farmacologia , Hiperuricemia/induzido quimicamente , Hiperuricemia/metabolismo , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos , Estrutura Molecular , Ácido Oxônico/antagonistas & inibidores , Relação Estrutura-Atividade , Ácido Úrico/antagonistas & inibidores , Xantina Oxidase/antagonistas & inibidores , Xantina Oxidase/metabolismo
4.
Phytochemistry ; 164: 236-242, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31185420

RESUMO

Mangiterpenes A-C and 2',3'-seco-manginoid C, four undescribed sesquiterpene/monoterpene-shikimate-conjugated meroterpenoids with spiro ring systems, were isolated from Guignardia mangiferae. The structures and absolute configurations of these compounds were established by comprehensive spectroscopic analyses and electronic circular dichroism (ECD) calculations. Mangiterpenes A-C represent the first examples of sesquiterpene-shikimate-conjugated spirocyclic meroterpenoids, and 2',3'-seco-manginoid C features an unexpected 2',3'-seco-manginoids skeleton. Mangiterpene C strongly inhibited the production of NO inducted by LPS, with an IC50 value of 5.97 µM. It showed an anti-inflammatory effect by means of blocking in the NF-κB signaling pathway and decreasing the expression of inflammatory mediators.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Monoterpenos/farmacologia , Ácido Chiquímico/farmacologia , Compostos de Espiro/farmacologia , Terpenos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Relação Dose-Resposta a Droga , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Camundongos , Estrutura Molecular , Monoterpenos/química , Monoterpenos/isolamento & purificação , NF-kappa B/antagonistas & inibidores , NF-kappa B/metabolismo , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Células RAW 264.7 , Ácido Chiquímico/química , Ácido Chiquímico/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos , Compostos de Espiro/química , Compostos de Espiro/isolamento & purificação , Relação Estrutura-Atividade , Terpenos/química , Terpenos/isolamento & purificação
5.
Artigo em Inglês | MEDLINE | ID: mdl-31046561

RESUMO

Acetaminophen, a popular NSAID (Non-steroidal anti-inflammatory drug), was studied for efficacy of removal from aqueous solutions. While Octolig® (a polyethylenediimine covalently attached to silica gel) is able to remove many simple anions and some acidic pharmaceuticals having a pKa value less than 4.5, it lacked efficacy with acetaminophen. Accordingly different transition- metal derivatives of Octolig® were tested by column chromatography using as substrates Octolig® derivatives of copper(II), cobalt(II), iron(III), manganese(II), nickel(II), and zinc(II).


Assuntos
Anti-Inflamatórios não Esteroides/isolamento & purificação , Sílica Gel/química , Poluentes Químicos da Água/isolamento & purificação , Purificação da Água/métodos , Água/química , Acetaminofen/isolamento & purificação , Acetaminofen/farmacocinética , Ânions , Anti-Inflamatórios não Esteroides/farmacocinética , Cromatografia/métodos , Cobalto/química , Cobre/química , Compostos Férricos/química , Humanos , Manganês/química , Níquel/química , Polietilenos/química , Sílica Gel/metabolismo , Soluções/química , Poluentes Químicos da Água/farmacocinética , Zinco/química
6.
Planta Med ; 85(8): 670-677, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31018218

RESUMO

Quercus ilex L. (Fagaceae) is one of the most commonly used plants in folk medicine in the Mediterranean region to treat gastrointestinal disorders. The aim of the present study was to evaluate the effects of a polyphenol extract from mature leaves of Q. ilex on acute 2,4,6-trinitrobenzene sulfonic acid-induced colitis in rats. A polyphenol extract from mature leaves of Q. ilex (250 and 500 mg/kg/day) was administered by gavage 48, 24, and 1 h prior to the induction of colitis with 2,4,6-trinitrobenzene sulfonic acid as well as 24 h later. The inflammation response was assessed by histology, myeloperoxidase activity, and Th1 proinflammatory cytokine production. The protein expression of cyclooxygenase-2 and inducible nitric oxide synthase, and signaling pathways were studied by Western blotting in the colon tissues. The polyphenol extract from mature leaves of Q. ilex decreased neutrophil infiltration, interleukin-1ß and TNF-α production, and proinflammatory proteins cyclooxygenase-2 and inducible nitric oxide synthase overexpression. Also, the polyphenol extract from mature leaves of Q. ilex was capable of blocking the activation of mitogen-activated protein kinases and nuclear transcription factor-kappa B. Furthermore, the reduction of inflammation by polyphenol extract from mature leaves of Q. ilex treatment was accompanied by a recovery of Nrf2 and heme oxygenase-1 protein expression levels. In conclusion, this study demonstrates that a polyphenol extract from mature leaves of Q. ilex improves 2,4,6-trinitrobenzene sulfonic acid-induced colitis, probably through mitogen-activated protein kinase/nuclear transcription factor-kappa B inhibition and Nrf2/heme oxygenase-1 activation signaling pathways, thus reducing the production of Th1 proinflammatory cytokines and cyclooxygenase-2 and inducible nitric oxide synthase overexpression.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Colite/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Quercus/química , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Colite/induzido quimicamente , Mediadores da Inflamação/metabolismo , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Masculino , Fator 2 Relacionado a NF-E2/metabolismo , Folhas de Planta/química , Proteínas Serina-Treonina Quinases/antagonistas & inibidores , Ratos , Ácido Trinitrobenzenossulfônico
7.
Phytochemistry ; 163: 23-32, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30986687

RESUMO

The 95% ethanol extract and its EtOAc and n-BuOH fractions obtained from the leaves and twigs of Schefflera rubriflora C. J. Tseng & G. Hoo showed significant inhibitory activities (33.6%, 35.7% and 40.6%, respectively) against croton oil-induced ear inflammation in mice. Bioactivity-guided isolation and separation gave eight previously undescribed terpenes or terpene glycosides. Structural elucidation was based on UV, IR, and NMR spectroscopy, MS, experimental and calculated ECD data, and Mosher's method. To identify anti-inflammatory components from the extract, all the compounds were evaluated for tumor necrosis factor-α (TNF-α) and interleukine-6 (IL-6) inhibitory activities. Four undescribed compounds inhibited mRNA expression of TNF-α and IL-6 with IC50 values of 15.3-52.4 µM.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Araliaceae/química , Interleucina-6/antagonistas & inibidores , Extratos Vegetais/farmacologia , Terpenos/farmacologia , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Células Cultivadas , Óleo de Cróton , Relação Dose-Resposta a Droga , Orelha , Edema/induzido quimicamente , Edema/tratamento farmacológico , Interleucina-6/genética , Interleucina-6/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos , Conformação Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Células RAW 264.7 , Relação Estrutura-Atividade , Terpenos/química , Terpenos/isolamento & purificação , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo
8.
Molecules ; 24(4)2019 Feb 25.
Artigo em Inglês | MEDLINE | ID: mdl-30823585

RESUMO

The importance of chirality in drug development is unquestionable, with chiral liquid chromatography (LC) being the most adequate technique for its analysis. Among the various types of chiral stationary phases (CSPs) for LC, brush-type CSPs provide the base for interaction analysis of CSPs and enantiomers, which provide valuable results that can be applied to interaction studies of other CSP types. In order to analyze the influence of aromatic interactions in chiral recognition, we designed a set of ten new brush-type CSPs based on (S)-N-(1-aryl-propyl)-3,5-dinitrobenzamides which differ in the aromatic unit directly linked to the chiral center. Thirty diverse racemates, including several nonsteroidal anti-inflammatory drugs and 3-hydroxybenzodiazepine drugs, were used to evaluate the prepared CSPs. Chromatographic analysis showed that the three new CSPs separate enantiomers of a wide range of compounds and their chromatographic behavior is comparable to the most versatile brush-type CSP-Whelk-O1. The critical role of the nonbonding interactions in positioning of the analyte (naproxen) in the cleft of CSP-6, as well as the analysis of interactions that make enantioseparation possible, were elucidated using computational methods. Furthermore, the influence of acetic acid as a mobile phase additive, on this enantiorecognition process was corroborated by calculations.


Assuntos
Anti-Inflamatórios não Esteroides/isolamento & purificação , Benzamidas/química , Benzodiazepinas/isolamento & purificação , Química Farmacêutica/métodos , Ácido Acético/química , Cromatografia Líquida , Simulação de Acoplamento Molecular , Estrutura Molecular , Estereoisomerismo , Relação Estrutura-Atividade
9.
Photochem Photobiol Sci ; 18(5): 1138-1146, 2019 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-30768081

RESUMO

Ginsenoside extracts are often used as raw materials for various pharmaceutical, cosmetic and food supplement products. Development of a direct, rapid, cheap, and comprehensive measurement tool for the quality assessment of ginsenoside extracts, and indeed all herbal extracts, is urgently needed. In addition, a bioactivity-based assessment should be linked with quality control. In this report, we try to develop a novel quality control tool using ginsenoside extracts as an example. High-performance liquid chromatography (HPLC) was used to detect nine principal ginsenosides in 11 batches of ginsenoside extracts. Delayed luminescence (DL) was used to analyze the same ginsenoside extract samples. DL measurements showed the same results in terms of differentiating 11 ginsenoside extract samples compared with chemical analysis, and DL properties could be closely linked to index ginsenosides in the quality control of ginsenoside extracts. Next, a zebrafish tail-fin amputation model was used to study differences in anti-inflammatory effect between the ginsenoside extract batches. The results indicate that both chemical analysis and DL measurements could partially reflect biological activity. Thus, DL may serve as a rapid, direct, sensitive, and systemic tool for studying the overall properties of ginsenoside extracts. Our proposal for linking bioactivities as a tool for evaluation of the quality of ginsenoside extracts opens a new direction for quality control.


Assuntos
Anti-Inflamatórios não Esteroides/química , Ginsenosídeos/química , Luminescência , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/uso terapêutico , Cromatografia Líquida de Alta Pressão , Ginsenosídeos/isolamento & purificação , Ginsenosídeos/uso terapêutico , Inflamação/tratamento farmacológico , Modelos Biológicos , Controle de Qualidade , Peixe-Zebra
10.
Biomed Pharmacother ; 112: 108676, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30797157

RESUMO

Liver diseases cause serious public health problems because of their high global prevalence and poor long-term clinical outcomes. With its mild and broad therapeutic efficacy, traditional Chinese medicine (TCM) has played an important role in the prevention and treatment of liver diseases in China for hundreds of years. Tanshinone IIA (TIIA), a major component extracted from the traditional herbal medicine Salvia miltiorrhiza Bunge, has been broadly studied for its multiple biological activities, including antiangiogenic, antioxidant, anti-inflammatory and anticancer properties. In this article, we focus on the effects of TIIA on the development of liver diseases, including hepatic injury, fatty liver, hepatic fibrosis and hepatocellular carcinoma (HCC), as well as the mechanism underlying TIIA and its new formulations and carriers in order to provide a reference for its further study and clinical therapeutic use in liver diseases.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Antineoplásicos Fitogênicos/uso terapêutico , Diterpenos de Abietano/uso terapêutico , Hepatopatias/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Diterpenos de Abietano/isolamento & purificação , Humanos , Hepatopatias/metabolismo , Hepatopatias/patologia , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Extratos Vegetais/isolamento & purificação
11.
Biomed Pharmacother ; 112: 108693, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30798128

RESUMO

This study evaluated the pharmacological effect of the association of crude extract from the fruits of Pterodon pubescens (Pp) with the essential oil of Cordia verbenacea (Cv) in antinociception and anti-inflammatory experimental models. The effective doses of each extract and the combinations used in the associations of extracts were defined by acetic acid-induced writhing test. The separate extracts were also evaluated on formalin test. Interaction between extracts was assessed by isobologram method. The effects of different concentrations of associations (A50, A100 and A200) were evaluated on formalin test, tail flick and hot plate. The anti-inflammatory activity was evaluated in paw edema induced by carrageenan and PGE2, carrageenan-induced peritonitis and mechanical allodynia induced by Complete Freund's Adjuvant (CFA). The associations were markedly synergistic, as assessed using isobolographic analyses. On formalin and on acetic acid-induced writhing tests, associations demonstrated greater efficacy when compared to extracts separately. In paw edema models, significant reductions of edema were observed. On mechanical allodynia induced by CFA, associations were effective at acute phase with pronounced effect at chronic phase. The associations were not effective in hot plate, tail flick and carrageenan-induced peritonitis tests. Phytochemical analysis by HPLC-DAD and FID showed important concentrations of α-Humulene, trans-Caryophyllene, geranylgeraniol, isomers 6α-hydroxy-7ß-acetoxy-vouacapan-17ßoate methyl ester and 6α-acetoxy-7ß-hydroxy-vouacapan-17ß-oate methyl ester (compounds m/z 404) and 6α,7ß-dihydroxyvouacapan-17ß-oate methyl ester (m/z 362). These findings demonstrate that the associations promote synergistic antinociceptive effect and important anti-inflammatory activities, especially on chronic inflammation conditions, at lower doses than the separate crude extracts, without demonstrating side effects, probably acting in different pharmacological receptors. The inhibition of inflammation suggests a relationship with inflammatory mediators and PGE2 pathway and might be exploited to achieve greater anti-inflammatory efficacy, being considered as a potential phytotherapy.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Cordia , Modelos Animais de Doenças , Fabaceae , Dor/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Relação Dose-Resposta a Droga , Sinergismo Farmacológico , Feminino , Masculino , Camundongos , Dor/metabolismo , Medição da Dor/efeitos dos fármacos , Medição da Dor/métodos , Extratos Vegetais/isolamento & purificação
12.
Talanta ; 194: 514-521, 2019 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-30609566

RESUMO

In the present study, the author describe a method for magnetic solid phase extraction (MSPE) combined with ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) for the quantitation of seven non-steroidal anti-inflammatory drugs (NSAIDs) in environmental water samples. Core-shell Fe3O4@MIL-100(Fe) as the adsorbent in the MSPE was novelly synthesized and successfully applied for the first time. Several experimental parameters, including the effect of pH value of aqueous solution, the amount of the adsorbent, ionic strength, adsorption time, desorption solvent and its volume, and desorption time, were investigated. Under the optimal conditions, the linear ranges were 0.1-10 µg L-1 for meloxicam, carprofen, indometacin, and tolfenamic acid, 0.2-20 µg L-1 for diclofenac, and 0.3-30 µg L-1 for naproxen and mefenamic acid with the regression coefficients (r) from 0.9987 to 0.9995, respectively. The limits of detection were between 0.02 and 0.09 µg L-1. The method also exhibited excellent precision (RSD ≤ 9.6%), repeatability (RSD ≤ 9.3%), and recovery (75.2-105.2%). The method presented the advantages of simplicity, rapidly, less solvent consumption, and higher sensitivity. It's promising for the core-shell Fe3O4@MIL-100(Fe) to be used as the adsorbent of MSPE for detecting and removing residues in the environment.


Assuntos
Anti-Inflamatórios não Esteroides/análise , Anti-Inflamatórios não Esteroides/isolamento & purificação , Nanopartículas de Magnetita/química , Estruturas Metalorgânicas/química , Extração em Fase Sólida/métodos , Espectrometria de Massas em Tandem , Adsorção , Anti-Inflamatórios não Esteroides/química , Cromatografia Líquida de Alta Pressão , Concentração de Íons de Hidrogênio , Modelos Moleculares , Conformação Molecular , Concentração Osmolar , Solventes/química , Fatores de Tempo , Água/química
13.
Planta Med ; 85(7): 608-614, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30690691

RESUMO

The anti-inflammatory properties of the topical herbal composition VEL-091604 with gentian root, licorice root, and willow bark extract were assessed in a randomized, prospective, placebo-controlled, double-blind ultraviolet (UV)-erythema test study with 42 healthy volunteers in comparison to 1% hydrocortisone acetate. The efficacy and tolerability of VEL-091604 cream 2 times daily over 2 wk was evaluated in an open-label, prospective proof of concept study in 10 subjects with atopic dermatitis using a lesional SCORAD severity score. In the UV-erythema test VEL-091604 cream significantly reduced inflammation compared to placebo and was as effective as 1% hydrocortisone acetate. The clinical study with atopic subjects revealed a significant and rapid reduction of the lesional SCORAD severity score in the test areas after 1 and 2 wk. No adverse events were recorded. It is concluded that the herbal cream VEL-091604 with licorice root, willow bark, and gentian root extract display anti-inflammatory properties in vivo. It is a promising new treatment option for atopic dermatitis that warrants further investigation in controlled studies.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Dermatite Atópica/tratamento farmacológico , Gentiana/química , Glycyrrhiza/química , Medicina Herbária , Extratos Vegetais/uso terapêutico , Salix/química , Adolescente , Adulto , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/isolamento & purificação , Criança , Pré-Escolar , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Casca de Planta/química , Extratos Vegetais/administração & dosagem , Raízes de Plantas/química , Estudos Prospectivos , Creme para a Pele/uso terapêutico , Adulto Jovem
14.
Arch Pharm Res ; 42(4): 332-343, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30610615

RESUMO

As part of our ongoing program to develop anti-inflammatory agents, an extract derived from Saururus chinensis collected in Korea was found to inhibit nitric oxide (NO) production in RAW264.7 cells. Bioassay-guided fractionation led to the isolation two new (1 and 2) and six known dineolignans (3-8). To the best of our knowledge, manassatin B1 (3) was isolated from S. chinensis for the first time. All structures were elucidated using extensive spectroscopic analysis. Of these compounds, 2 and 8 inhibited lipopolysaccharide (LPS)-induced production of NO and showed IC50 values of 5.80 and 1.52 µM, respectively. LPS-induced expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) was also significantly suppressed by the administration of 2 and 8. In addition, these lignans induced the expression of heme oxygenase-1 (HO-1) in a concentration-dependent manner. Nuclear translocation of nuclear-E2-related factor 2 (Nrf2), a key regulator of HO-1 protein expression, was also induced in RAW264.7 cells treated with 2 and 8. These findings suggested that these lignans exerted anti-inflammatory effects in RAW264.7 cells through modulation of the Nrf2/HO-1 pathway and that they were potential HO-1 inducers for preventing or treating inflammation.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Heme Oxigenase-1/antagonistas & inibidores , Proteínas de Membrana/antagonistas & inibidores , Fator 2 Relacionado a NF-E2/antagonistas & inibidores , Saururaceae/química , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Heme Oxigenase-1/metabolismo , Ligantes , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Proteínas de Membrana/metabolismo , Camundongos , Conformação Molecular , Fator 2 Relacionado a NF-E2/metabolismo , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Células RAW 264.7 , Relação Estrutura-Atividade
15.
Phytomedicine ; 54: 89-97, 2019 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-30668386

RESUMO

BACKGROUND: 4-methoxycinnamyl p-coumarate (MCC) was isolated from rhizomes of Etlingera pavieana by bioactivity-guided isolation, however, the molecular mechanism underlying its anti-inflammatory activity remains inadequately understood. PURPOSE: In this study, we elucidated the suppressive effect of MCC on LPS-induced expression of inflammatory mediators and the molecular mechanisms responsible for anti-inflammatory activities in RAW 264.7 macrophages. METHODS: Cell viability of MCC-treated RAW 264.7 macrophage was measured by MTT assay. Anti-inflammatory activity was evaluated by measurement of NO, PGE2, and cytokine production in LPS-stimulated cells. qRT-PCR and Western blotting analysis were used to investigate mRNA and protein levels of inflammatory responsive genes. NF-κB activation and transactivation activity were determined by immunofluorescence and reporter gene assay, respectively. RESULTS: MCC considerably suppressed both the production of NO, PGE2, IL-1ß as well as TNF-α and their expression. MCC inactivated NF-κB by reducing phosphorylation of IκBα and inhibiting NF-κB p65 nuclear translocation. Also, MCC significantly inhibited NF-κB transactivation activity. However, the inhibitory effect of MCC was independent of the MAPK signaling pathway. Furthermore, MCC significantly decreased phosphorylation of Akt and c-Jun, a main component of AP-1. CONCLUSION: These findings suggest that the anti-inflammatory effect of MCC could be mediated by the inhibition of LPS-induced expression of inflammatory mediators by down-regulation of the NF-κB, Akt and AP-1 signaling pathways in murine macrophages.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Ácidos Cumáricos/farmacologia , Inflamação/tratamento farmacológico , Zingiberaceae/química , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Ácidos Cumáricos/isolamento & purificação , Citocinas/metabolismo , Dinoprostona/metabolismo , Avaliação Pré-Clínica de Medicamentos/métodos , Inflamação/metabolismo , Lipopolissacarídeos/farmacologia , Camundongos , NF-kappa B/metabolismo , Fosforilação/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Células RAW 264.7 , Rizoma/química , Transdução de Sinais/efeitos dos fármacos , Fator de Transcrição AP-1/metabolismo
16.
Org Lett ; 21(1): 246-251, 2019 01 04.
Artigo em Inglês | MEDLINE | ID: mdl-30571134

RESUMO

The chemical investigation of marine invertebrates from the deep Northeastern Atlantic revealed new lipoglycotripeptides named characellides isolated from the tetractinellid sponge Characella pachastrelloides. This new family of natural products features a central tripeptide linked to a rare sugar unit and a long alkyl chain ending with a 2,3-dimethyltetrahydropyran. The configurations of all 13 chiral centers were determined by extensive use of NMR data and circular dichroism spectra combined with calculations.


Assuntos
Anti-Inflamatórios não Esteroides/química , Lipoglicopeptídeos/química , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Linhagem Celular , Relação Dose-Resposta a Droga , Lipoglicopeptídeos/isolamento & purificação , Lipoglicopeptídeos/farmacologia , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Camundongos , Microglia/efeitos dos fármacos , Microglia/metabolismo , Conformação Molecular , Poríferos , Espécies Reativas de Oxigênio/metabolismo , Relação Estrutura-Atividade
17.
J. physiol. biochem ; 74(4): 539-547, nov. 2018. tab, graf
Artigo em Inglês | IBECS | ID: ibc-179032

RESUMO

The link between obesity-induced systemic inflammation and decreased insulin signalling is well-known. It is also known that peripherally produced inflammatory cytokines can cross the blood-brain barrier, resulting in the release of neurotoxins that can ultimately lead to the demise of central nervous system integrity. A high-mesembrine Sceletium tortuosum extract was recently shown to possess cytoprotective and mild anti-inflammatory properties in monocytes and to target specific p450 enzymes to reduce adrenal glucocorticoid synthesis. This is significant since the aetiology of both obesity and diabetes is linked to inflammation and excess glucocorticoid production. Given the interlinked nature of glucocorticoid action and inflammation, central immunomodulatory effects of two Sceletium tortuosum extracts prepared by different extraction methods were investigated. Human astrocytes were pre-treated for 30 min, before exposure to Escherichia coli lipopolysaccharide for 23.5 h (in the presence of treatment). Cytotoxicity, mitotoxicity and cytokine responses (basally and in response to inflammatory stimulus) were assessed. In addition, total polyphenol content, antioxidant capacity and selected neural enzyme inhibition capacity were assessed for both extracts. The high-mesembrine Sceletium extract exerted cytoprotective and anti-inflammatory effects. In contrast, the high delta7-mesembrenone extract, rich in polyphenols, exhibited potent antioxidant effect, although with relatively higher risk of adverse effects with overdose. We conclude that both Sceletium tortuosum extracts may be employed as either a preventative supplement or complimentary treatment in the context of obesity and diabetes; however, current data also highlights the impact that extraction methods can have on plant product mechanism of action


No disponible


Assuntos
Humanos , Anti-Inflamatórios não Esteroides/farmacologia , Astrócitos , Alcaloides Indólicos/farmacologia , Mesembryanthemum/química , Extratos Vegetais/farmacologia , Acetilcolinesterase/metabolismo , Anti-Inflamatórios não Esteroides/análise , Anti-Inflamatórios não Esteroides/isolamento & purificação , Antioxidantes , Linhagem Celular , Inibidores da Colinesterase , Alcaloides Indólicos/análise , Alcaloides Indólicos/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação
18.
Phytochemistry ; 156: 167-175, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30312932

RESUMO

Tripterygium hypoglaucum (H. Lév.) Hutch. has been used to remedy rheumatoid arthritis, however, it shows frequent toxicity to the body. In this study, liquid chromatograph-mass spectrometer (LC-MS) was guided to characterize abietanes diterpenoids with anti-inflammatory activity from the stem of T. hypoglaucum. Thirteen undescribed abietanes diterpenoids were isolated and purified, and their chemical structure was identified using various spectroscopic methods. These compounds belonged to abietanes with splitting C ring, abietanes with benzenoid rings, diterpene quinoids, diterpene quinoids with lactone rings, and abietanes with benzenoid and lactone rings, respectively. Lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 macrophages was used to evaluate anti-inflammatory activity of the compounds. The results indicated that hypoglicin B-G and hypoglicin J-M exhibited inhibitory activity of NO production with the IC50 values of 6.01, 25.21, 8.29, 3.63, 0.72, 0.89, 36.91, 0.82, 2.85, 11.92 µM, respectively. Among these compounds, compound hypoglicin L showed high anti-inflammatory activity and low toxicity (SI = 5.02 × 104). Further QPCR analysis revealed that hypoglicin D and hypoglicin L can inhibit the mRNA expression of iNOS in LPS-stimulated RAW264.7 cells at doses of 12.5 and 3.13 µM, respectively. Taken together, ten anti-inflammatory diterpenoids were found from T. hypoglaucum in this study.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Diterpenos/farmacologia , Óxido Nítrico/antagonistas & inibidores , Tripterygium/química , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Camundongos , Conformação Molecular , Óxido Nítrico/biossíntese , Células RAW 264.7 , Relação Estrutura-Atividade
19.
Phytochemistry ; 156: 159-166, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30308383

RESUMO

Brasilanones A-F and asperterreusines A-C, undescribed brasilane sesquiterpenoids and dihydrobenzofuran derivatives, were isolated from the marine-derived fungus Aspergillus terreus [CFCC 81836]. Their structures with absolute configurations were elucidated on the basis of spectroscopic data, X-ray crystallographic analyses, and electronic circular dichroism (ECD) calculations. Brasilanones A-F are unusual brasilane sesquiterpenoids with an α,ß-unsaturated ketone unit, interestingly, brasilanones B-D are stereo isomers. All of the isolates were evaluated for their inhibitory activities against NO production and cytotoxic activities against five human cancer cell lines (HL-60, SW-480, A-549, MCF-7, and SMMC-7721). Brasilanones A and E showed moderate inhibitory effect with NO inhibition rates of 47.7% (p < 0.001) and 37.3% (p < 0.001) at the concentration of 40 µM. Asperterreusines A showed cytotoxicity against HL-60 and SW-480 cell lines with IC50 values of 15.3 and 25.7 µM, respectively.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Aspergillus/química , Benzofuranos/farmacologia , Óxido Nítrico/antagonistas & inibidores , Sesquiterpenos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Benzofuranos/química , Benzofuranos/isolamento & purificação , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Camundongos , Modelos Moleculares , Conformação Molecular , Óxido Nítrico/biossíntese , Células RAW 264.7 , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Relação Estrutura-Atividade
20.
Phytochemistry ; 156: 193-200, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30316148

RESUMO

A phytochemical investigation of the stem barks of the Malaysian Croton oblongus Burm.f. (Syn. Croton laevifolius Blume) (Euphorbiaceae) yielded seven previously undescribed ent-neo-clerodane diterpenoids, laevifins A - G and the known crovatin (3). Structures were established by a combination of spectroscopic methods including HRESIMS, NMR spectroscopy and X-ray crystallography. The absolute configuration of crovatin and laevifins A-G was established by comparison of experimental ECD and theoretical TDDFT ECD calculated spectra. This is the first report on the occurrence of the sesquiterpenoid cryptomeridiol in a Croton species. In vitro cytotoxicity assays on laevifins A, B and G showed moderate activities against the MCF-7 cancer cell line (IC50 102, 115 and 106 µM, respectively) while ß-amyrin and acetyl aleuritolic acid showed good anti-inflammatory activity on the LPS-induced NF-κB translocation inhibition in RAW 264.7 cells assay with IC50 values of 23.5 and 35.4 µg/mL, respectively.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Croton/química , Diterpenos Clerodânicos/farmacologia , Casca de Planta/química , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Diterpenos Clerodânicos/química , Diterpenos Clerodânicos/isolamento & purificação , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Células MCF-7 , Camundongos , Conformação Molecular , NF-kappa B/antagonistas & inibidores , NF-kappa B/metabolismo , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Teoria Quântica , Células RAW 264.7 , Relação Estrutura-Atividade
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