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1.
BMC Complement Altern Med ; 19(1): 289, 2019 Oct 29.
Artigo em Inglês | MEDLINE | ID: mdl-31664997

RESUMO

BACKGROUND: Natural extracts with beneficial biological activities are nowadays of high interest, in various treatment or prophylaxis. Hypericum capitatum has been known for its curative effects for centuries and its extracts have become of interest due to their distinct activity among other Hypericaceae members. In this study, further light is aimed to be shed on the secondary-metabolites composition of H. capitatum extracts, using chromatographic techniques and Electron paramagnetic resonance profiles in alkaline medium. Considering that no previous works explored the anti-inflammatory activity of H. capitatum, here, an in vivo study is also designed in order to evaluate this property by assessing the impact of one of H. capitatum extracts in ameliorating turpentine oil-induced inflammation on rats and to quantify their blood antioxidants level. METHODS: Chromatographic techniques and Electron paramagnetic resonance spectroscopy were used in order to describe the chemical profile in different parts of the plant. The in vivo study on turpentine-oil induced inflammation in rats included three doses of H. capitatum extract expressed in rutin concentration. Oxidative stress was measured using total oxidative status, total antioxidant capacity, oxidative stress index, 3-nitrotyrosine, nitric oxide, malondialdehyde, superoxide dismutase, catalase and the inflammatory response was evaluated by performing a complete blood cells count and C reactive protein. RESULTS: The extract was remarkably rich in rutin; however, other polyphenolic-like minor components appeared important in explaining the observed biological properties. The tested extract prevents the increase of inflammation-induced white blood cell count, number of neutrophils, and serum nitric oxide, and did so in a dose-dependent manner, similarly to the positive control-diclofenac. In addition, the same extract appeared to be a good alternative to diclofenac to restore total oxidative status, thiobarbituric active reactive species, total proteins and C reactive proteins. Moreover, antioxidant enzymes such as catalase, superoxide dismutase and total serum thiol concentration were significantly increased by the tested extract. CONCLUSIONS: Due to its powerful reservoir rich in rutin, H. capitatum extract depicted its in vivo antioxidant and anti-inflammatory effects indicating it to be a good alternative to conventional drugs for oxidative stress protection.


Assuntos
Anti-Inflamatórios/administração & dosagem , Hypericum/química , Inflamação/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Rutina/administração & dosagem , Animais , Anti-Inflamatórios/química , Catalase/metabolismo , Feminino , Humanos , Inflamação/induzido quimicamente , Inflamação/metabolismo , Masculino , Malondialdeído/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Ratos , Ratos Wistar , Rutina/análise , Superóxido Dismutase/metabolismo , Terebintina/efeitos adversos
2.
J Therm Biol ; 84: 36-44, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31466775

RESUMO

It is still an open question as to whether or not aseptic injuries affect the generation of fever due to exogenous pyrogens including bacterial products. Therefore, in the present paper we have investigated the course of endotoxin fever in rats induced with lipopolysaccharide (LPS; given intraperitoneally in a dose of 50 µg/kg) 48 h after subcutaneous administration of turpentine oil (TRP; 0.1 mL per rat) that causes aseptic necrosis of tissues. We found that febrile response was significantly augmented in the animals pre-treated with turpentine compared to control rats (pre-treated with saline), and that observed excessive elevation of body temperature (Tb) was accompanied by enhanced release of fever mediators: interleukin-6 (IL-6) and prostaglandin E2 (PGE2) into plasma. Moreover, we found that sensitization to pyrogenic effects of lipopolysaccharide was associated with the increase in plasma level of high mobility group box 1 protein (HMGB1), one of the best-known damage-associated molecular patterns (DAMP), which was recently discovered as inflammatory mediator. Since the injection of anti-HMGB1 antibodies weakened observed hyperpyrexia in the animals pre-treated with turpentine, we conclude that HMGB1 is a plasma-derived factor released in the course of aseptic injury that enhances pyrogenic effects of LPS.


Assuntos
Febre/sangue , Proteína HMGB1/sangue , Animais , Dinoprostona/sangue , Febre/induzido quimicamente , Membro Posterior/patologia , Interleucina-6/sangue , Lipopolissacarídeos , Masculino , Necrose , Pirogênios , Ratos Wistar , Terebintina/farmacologia
3.
J Oleo Sci ; 68(7): 671-677, 2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-31178467

RESUMO

Conifer resins are used as chemical raw materials for daily necessities. There have been many reports on the aroma components of turpentine oil from rosin, but there has been no reports on fluctuations in the aroma components through spring to late autumn. We speculated that the aroma components in the essential oils of deciduous coniferous larches might fluctuate during maturation of the foliage. In this study, we focused on the aroma components of larch essential oils and we clarified by multivariate analysis how the aroma components fluctuate during leaf maturation. The results of analysis showed that there was a drastic seasonal fluctuation of the chemical components in larch essential oils, especially in senescent leaves in late autumn. Cryptone and linalool were identified as the characteristic aroma components in essential oil from senescent larch leaves.


Assuntos
Larix/química , Odorantes/análise , Óleos Voláteis/química , Folhas de Planta/química , Estações do Ano , Terebintina/química , Monoterpenos Acíclicos , Monoterpenos/isolamento & purificação , Óleos Voláteis/isolamento & purificação , Folhas de Planta/crescimento & desenvolvimento , Resinas Vegetais
4.
Environ Entomol ; 48(4): 765-783, 2019 08 05.
Artigo em Inglês | MEDLINE | ID: mdl-31145799

RESUMO

The black turpentine beetle, Dendroctonus terebrans Olivier is the largest pine-infesting bark beetle native to the southern and eastern United States. It generally reproduces in fresh stumps and bases of trees weakened or killed by other biotic or abiotic agents, although it can also infest and sometimes kills apparently healthy trees. Its numbers can build when large amounts of host material become available (typically through a disturbance), and black turpentine beetle-caused mortality at a local scale can become considerable. Here, we provide a complete review of the literature on this species, including its taxonomy, host, life history, chemical ecology, arthropod and microbial associates, and management options. We also provide original data on numbers of instars, acoustic signals, and pheromone chirality in this species. Our survey of the existing literature revealed that key biological characteristics of black turpentine beetles are known, but interactions with closely associated organisms, economic and ecological impacts, and improvements to monitoring and management practices have been only partially investigated.


Assuntos
Besouros , Pinus , Gorgulhos , Animais , Feromônios , Terebintina
5.
PLoS One ; 14(4): e0215842, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31017959

RESUMO

Plasma pharmacokinetic profiles and the anti-inflammatory efficacy of meloxicam were determined when administered subcutaneously (SC) or intramuscularly (IM) to sheep. Merino ewes were initially injected with 0.1 mL of oil of turpentine into a forelimb to induce inflammation, followed by either 1.0 mg/kg or 2.0 mg/kg of meloxicam administered either SC or IM (n = 6 per treatment group) or followed by no meloxicam administration (control) (n = 4). Ewes were examined to determine skin temperature, limb circumference, limb sensitivity and signs of lameness at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, 24 and 48 h following treatment, with blood collected at these time-points to quantify meloxicam plasma concentrations. Skin temperature of ewes dosed with meloxicam at 1.0 mg/kg SC and 2.0 mg/kg IM at 12 h and 1.0 mg/kg SC at 24 were significantly different to the controls (P < 0.05). Limb circumferences of ewes dosed with 1.0 mg/kg IM were significantly different to controls at 10 h and 12 h (P < 0.05). All meloxicam treatment groups resulted in reduced limb sensitivity compared to controls at 6 h, with the 1.0 and 2.0 mg/kg IM treatments significantly different at 12 h (P < 0.05) and 1.0 and 2.0 mg/kg SC groups, significantly different to controls at 48 h (P < 0.05). No significant difference in lameness scores were detected over 48 h. The 1.0 mg/kg IM treatment had a significantly greater plasma meloxicam concentration than the 1.0 mg/kg SC treatment over 0.5 to 4 h (P < 0.001). Both 1.0 mg/kg SC and IM treatments demonstrated elimination half-lives (mean ± SD) of 10.82 ± 2.46 and 12.63 ± 2.37 h, respectively. Meloxicam at all doses provided some anti-inflammatory and analgesic effects from 6 to 48 h; however no route could be distinguished as more efficacious than the others.


Assuntos
Meloxicam/sangue , Meloxicam/farmacocinética , Animais , Comportamento Animal/efeitos dos fármacos , Extremidades/fisiologia , Marcha/fisiologia , Injeções Intramusculares , Injeções Subcutâneas , Meloxicam/administração & dosagem , Ovinos , Temperatura Cutânea/efeitos dos fármacos , Resultado do Tratamento , Terebintina
6.
Bioorg Chem ; 86: 393-400, 2019 05.
Artigo em Inglês | MEDLINE | ID: mdl-30763886

RESUMO

In this study, the acid chlorides of pyrazolo[3,4-d]pyrimidine compounds were prepared and reacted with a number of nucleophiles. The novel compounds were experimentally tested via enzyme assay and they showed cyclooxygenase-2 inhibition activity in the middle micro molar range (4b had a COX-1 IC50 of 26 µM and a COX-2 IC50 of 34 µM, 3b had a COX-1 IC50 of 19 µM and a COX-2 IC50 of 31 µM, 3a had a COX-2 IC50 of 42 µM). These compounds were analyzed via docking and were predicted to interact with some of the COX-2 key residues. Our best hit, 4d (COX-1 IC50 of 28 µM, COX-2 IC50 of 23 µM), appears to adopt similar binding modes to the standard COX-2 inhibitor, celecoxib, proposing room for possible selectivity. Additionally, the resultant novel compounds were tested in several in vivo assays. Four compounds 3a (COX-2 IC50 of 42 µM), 3d, 4d and 4f were notable for their anti-inflammatory activity that was comparable to that of the clinically available COX-2 inhibitor celecoxib. Interestingly, they showed greater potency than the famous non-steroidal anti-inflammatory drug, Diclofenac sodium. In summary, these novel pyrazolo[3,4-d]pyrimidine analogues showed interesting anti-inflammatory activity and could act as a starting point for future drugs.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Inibidores de Ciclo-Oxigenase/farmacologia , Edema/tratamento farmacológico , Granuloma/tratamento farmacológico , Inflamação/tratamento farmacológico , Pirazóis/farmacologia , Pirimidinas/farmacologia , Animais , Anti-Inflamatórios não Esteroides/síntese química , Anti-Inflamatórios não Esteroides/química , Carragenina , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase/síntese química , Inibidores de Ciclo-Oxigenase/química , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Granuloma/induzido quimicamente , Humanos , Inflamação/induzido quimicamente , Masculino , Simulação de Acoplamento Molecular , Estrutura Molecular , Pirazóis/síntese química , Pirazóis/química , Pirimidinas/síntese química , Pirimidinas/química , Ratos , Ratos Wistar , Proteínas Recombinantes/metabolismo , Relação Estrutura-Atividade , Terebintina
7.
Aust Vet J ; 97(1-2): 23-32, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30693494

RESUMO

OBJECTIVE: To evaluate the efficacy of the non-steroidal anti-inflammatory drug, meloxicam, in alleviating pain and inflammation and on production-related variables in a model of sterile acute inflammation in sheep. METHODS: Groups of 12 mature Merino ewes received 0, 0.5, 1.0 or 1.5 mg/kg meloxicam subcutaneously 90 min before injection of 0.1 mL turpentine subcutaneously on the anterior aspect of the proximal phalanx of a forelimb. Pain- and inflammation-related variables were assessed at -18, 3, 6, 9, 12, 24, 48 and 72 h relative to meloxicam administration. Daily feed intake and body weight change 7 days later were also assessed. Pain-related variables measured were weight borne on each forelimb, lameness score, time each forelimb was raised in a 20-s interval and tolerance to a noxious mechanical stimulus. Inflammation-related variables measured were skin temperature, limb circumference, body temperature, plasma haptoglobin concentration and peripheral blood leucocyte parameters. RESULTS: Meloxicam was effective in improving all pain-related variables. A dose-dependent response was seen between 0 and 1.0 mg/kg, with no additional benefit provided by 1.5 mg/kg. At a dose rate of 1.0 mg/kg, meloxicam improved weight borne on the turpentine-treated limb by 14%, reduced the time the treated limb was held in a non-weight-bearing posture by 46%, reduced the lameness score by 58% and improved tolerance to pressure by 52%. No significant effects of meloxicam on inflammatory variables or appetite were observed. CONCLUSIONS: Using a validated pain model, the data suggested that 1.0 mg/kg meloxicam provided significant analgesic benefits to sheep.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Coxeadura Animal/tratamento farmacológico , Meloxicam/farmacologia , Dor/veterinária , Doenças dos Ovinos/tratamento farmacológico , Administração Intravenosa/veterinária , Análise de Variância , Animais , Relação Dose-Resposta a Droga , Feminino , Irritantes/administração & dosagem , New South Wales , Dor/tratamento farmacológico , Medição da Dor/métodos , Medição da Dor/veterinária , Distribuição Aleatória , Ovinos , Doenças dos Ovinos/sangue , Temperatura Cutânea/efeitos dos fármacos , Terebintina/administração & dosagem , Suporte de Carga
8.
Xenobiotica ; 49(5): 584-590, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-29790816

RESUMO

The pharmacokinetics of TAK-272 (SCO-272), an orally active renin inhibitor, was investigated in rats with subcutaneously injected turpentine oil, which was an inflammation animal model. Following intravenous administration of TAK-272 to the turpentine-treated rats, the systemic clearance and volume of distribution decreased with the elevated plasma α1-acid glycoprotein (AGP) levels. The elevated plasma AGP levels were negatively correlated with the plasma unbound fraction of TAK-272 in the rats. Although the AUCs of total TAK-272 in the turpentine-treated rats were higher than those in the control rats after intravenous and oral administration, those of unbound TAK-272, which seem to directly contribute to the pharmacological effect and safety, were nearly equal between the turpentine-treated and control rats in the respective dose routes. TAK-272 has been shown to primarily bind to AGP in the human plasma. These results strongly suggested that the pharmacokinetic of TAK-272 in humans would also be affected by the variation in the plasma AGP levels and should be discussed with not only the total concentrations but also the unbound concentrations in the clinical trial for patients with elevated plasma AGP levels.


Assuntos
Benzimidazóis/farmacologia , Benzimidazóis/farmacocinética , Morfolinas/farmacologia , Morfolinas/farmacocinética , Orosomucoide/metabolismo , Piperidinas/farmacologia , Piperidinas/farmacocinética , Renina/antagonistas & inibidores , Administração Oral , Animais , Benzimidazóis/efeitos adversos , Masculino , Morfolinas/efeitos adversos , Piperidinas/efeitos adversos , Ratos , Ratos Sprague-Dawley , Terebintina/farmacocinética , Terebintina/farmacologia
9.
Pharmazie ; 73(11): 676-680, 2018 11 01.
Artigo em Inglês | MEDLINE | ID: mdl-30396389

RESUMO

Cleopatra VII (69-30 BC), the last Ptolemaic ruler of Egypt, is probably best known for her love affairs with Julius Caesar (100-44 BC) and Marcus Antonius (83-30 BC). Rightly or wrongly she became the epitome of shrewd seduction, leading brave Roman commanders on a path to debauchery and destruction. Among the seductive strategies attributed to her is the ingestion of small amounts of turpentine [the resin of the terebinth tree (Pistacia terebinthus)] or of derived oil (Oleum terebinthinae) with the purpose of conferring to her urine a more pleasant scent reminding of violets. Turpentine components are metabolized among other compounds to ionones and irones, which - renally excreted - are responsible for the flowery scent. Having obviously worked with great generals, the strategy is said to have been embraced for everyday use by many affluent Roman women. Complicating the issue somewhat is the fact that juniper berries (Fructus juniperi) and derived oil (Oleum juniperi) containing many of the same terpenoids as turpentine have a similar effect on urine. The purpose of this contribution is to briefly review the pharmacology of turpentine and juniper derived compounds assumed to be responsible for altering the scent of urine and to examine the origin and veracity of the mentioned habit. While the effect of ingested turpentine on the scent of urine is well documented our attempts at identifying Greek or Latin authors mentioning its intentional use for this explicit purpose (by Cleopatra or anybody else) failed.


Assuntos
Juniperus/química , Norisoprenoides/história , Terebintina/história , Urina/química , Egito , Pessoas Famosas , Feminino , Frutas , História Antiga , Humanos , Norisoprenoides/urina , Odorantes , Terebintina/metabolismo
11.
Molecules ; 23(2)2018 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-29419733

RESUMO

Turpentine is a volatile component of resin, which is an abundant forest resource in Southern China. As one of the most important components, the integrated application of ß-pinene has been studied. The broad-spectrum evaluation of ß-pinene and its analogues has, therefore, been necessary. In an attempt to expand the scope of agro-activity trials, the preparation and the evaluation of the herbicidal activity of a series of ß-pinene analogues against three agricultural herbs were carried out. In accordance with the overall herbicidal activity, it is noteworthy that compounds 6k, 6l, and 6m demonstrated extreme activity with IC50 values of 0.065, 0.065, and 0.052 mol active ingredients/hectare against E. crus-galli. The preliminary structure-activity relationship (SAR) was analyzed and the compounds with the appropriate volatility and substituent type that had beneficial herbicidal activity were analyzed. Simultaneously, the quantitative structure-activity relationship (QSAR) model was built and the most important structural features were indicated, which was, to a certain extent, in line with the SAR study. The study aimed to study the application of the forest resource turpentine in agriculture as a potential and alternative approach for comprehensive utilization.


Assuntos
Produção Agrícola , Terebintina/análise , Terebintina/química , Monoterpenos Bicíclicos , Compostos Bicíclicos com Pontes/síntese química , Compostos Bicíclicos com Pontes/química , Herbicidas/química , Herbicidas/farmacologia , Modelos Moleculares , Estrutura Molecular , Monoterpenos/síntese química , Monoterpenos/química , Relação Quantitativa Estrutura-Atividade , Eletricidade Estática , Terebintina/farmacologia
12.
J Ayub Med Coll Abbottabad ; 29(3): 384-387, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29076666

RESUMO

BACKGROUND: Diabetes Mellitus is a pandemic of the modern era owing to our rapidly deteriorating lifestyle. Painful diabetic neuropathy is one of the costliest and disabling complications of diabetes mellitus. No single treatment exists to prevent or reverse neuropathic changes or to provide total pain relief. Topical Capsaicin and Turpentine Oil are found to be effective in treatment of painful diabetic neuropathy. METHODS: Patients of either gender with ages between 18 and 70 years having painful diabetic neuropathy already taking one oral drug for painful neuropathy and treatment for diabetes mellitus and an HbA1C less than 8.5% were included while Pregnant or lactating mothers, patients with chronic liver disease and patients with renal insufficiency (creatinine >3.0 mg/dl) and peripheral arterial disease were excluded from study. Patients were randomly divided into two groups (A & B) using computer generated random number table. Group A was given topical application of capsaicin while Group B was given topical application of commercially available turpentine oil over painful site on feet. RESULTS: 300 patients were equally divided in two groups. The patients in group A had a Visual Analog Pain Score of 7.91±5.10 at baseline and 5.10±1.343 after 3 months of treatment (p-value 0.0001). The patients in group B had a Visual Analog Pain Score of 7.83±1.012 at baseline and 5.20±1.187 after 3 months of treatment (p-value 0.0001). Chi Square test was applied to compare efficacy of both groups. It was noted that 71 (53%) had efficacy in group A and 63 (47%) had efficacy in the group B but the difference was not statistically significant. (p-value=0.399). CONCLUSIONS: It has been concluded that turpentine oil is effective in managing diabetic neuropathic pain similar to capsaicin cream.


Assuntos
Capsaicina/uso terapêutico , Neuropatias Diabéticas/tratamento farmacológico , Neuralgia/tratamento farmacológico , Terebintina/uso terapêutico , Administração Tópica , Analgésicos/uso terapêutico , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Fitoterapia , Fármacos do Sistema Sensorial
13.
J Physiol Biochem ; 73(4): 551-560, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28741242

RESUMO

A still growing body of evidence suggests the importance of epoxyeicosatrienoic acids (EETs) in the regulation of inflammatory response; therefore, drugs that stabilize their levels by targeting the soluble epoxide hydrolase (sEH), an enzyme responsible for their metabolism, are currently under investigation. The effect of sEH inhibitors on molecular components of fever mechanism, i.e., on synthesis of pro-inflammatory cytokines or prostaglandins, has been repeatedly proven; however, the hypothesis that sEH inhibitors affect febrile response has never been tested. The aim of this study was to examine if sEH inhibition affects core body temperature (Tb) as well as Tb changes during febrile response to infectious (lipopolysaccharide; LPS) or non-infectious (turpentine; TRP) stimuli. Male Wistar rats were implanted intra-abdominally with miniature biotelemeters to monitor Tb. A potent sEH inhibitor 12-(3-adamantan-1-yl-ureido)-dodecanoic acid (AUDA) was suspended in olive oil and administrated into animals in the intraperitoneal (i.p.) dose of 15 mg/kg, which, as we showed, has no significant influence on normal Tb. We have found that AUDA injected 3 h after LPS (50 µg/kg i.p.) significantly weakened febrile rise of Tb. Moreover, injection of sEH inhibitor 7 h after turpentine (administrated subcutaneously in a dose of 100 µL/rat) markedly reduced the peak period of aseptic fever. Obtained results provide first experimental evidence that sEH inhibitors possess anti-pyretic properties. Therefore, medicines targeting sEH enzymatic activity should be considered as a complement to the arsenal of topical medications used to treat fever especially in clinical situations when non-steroidal anti-inflammatory drugs are ineffective.


Assuntos
Inibidores Enzimáticos/farmacologia , Epóxido Hidrolases/antagonistas & inibidores , Febre/induzido quimicamente , Lipopolissacarídeos/administração & dosagem , Terebintina/farmacologia , Animais , Masculino , Ratos , Ratos Wistar
14.
BMC Complement Altern Med ; 17(1): 371, 2017 Jul 18.
Artigo em Inglês | MEDLINE | ID: mdl-28720131

RESUMO

BACKGROUND: The roots and stem bark of Berberis orthobotrys (Berberidaceae) have long been used traditionally to treat joint pain. Though, it has not been pharmacologically assessed for rheumatoid arthritis. The current study explores anti-arthritic activity and phytochemical analysis of aqueous-methanolic extract (30:70) and fractions (ethyl acetate, n-butanol, and aqueous) of Berberis orthobotrys roots. METHODS: Anti-arthritic potential was evaluated in vitro using protein denaturation (bovine serum albumin and egg albumin) and membrane stabilization methods at 12.5-800 µg/ml concentration and in vivo via turpentine oil, formaldehyde and Complete Freund Adjuvant (CFA) models at 50, 100 and 150 mg/kg doses. Also, in vitro antioxidant ability was appraised by reducing power assay. Moreover, total flavonoid content, Fourier transform infrared spectroscopy and High performance liquid chromatography of n-butanol fraction were performed. RESULTS: The results revealed concentration dependent inhibition of albumin denaturation and notable RBC membrane stabilization, with maximum results obtained at 800 µg/ml. Similarly, plant exhibited dose dependent anti-arthritic effect in turpentine oil and formaldehyde models, with maximum activity observed at 150 mg/kg. The results of CFA model depicted better protection against arthritic lesions and body weight alterations. Also, B.orthobotrys remarkably ameliorated altered hematological parameters, rheumatoid factor and positively modified radiographic and histopathological changes. Additionally, plant exhibited remarkable anti-oxidant activity. Moreover, phytochemical analysis revealed polyphenols and flavonoids. CONCLUSION: Taken together, these results support traditional use of B.orthobotrys as potent anti-arthritic agent that may be proposed for rheumatoid arthritis treatment.


Assuntos
Antirreumáticos/uso terapêutico , Artrite Experimental/tratamento farmacológico , Artrite Reumatoide , Berberis/química , Fitoterapia , Extratos Vegetais/uso terapêutico , Polifenóis/uso terapêutico , Albuminas/metabolismo , Animais , Antioxidantes/análise , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antirreumáticos/farmacologia , Artrite Reumatoide/sangue , Artrite Reumatoide/tratamento farmacológico , Bovinos , Membrana Celular/efeitos dos fármacos , Eritrócitos , Feminino , Flavonoides/análise , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Formaldeído , Adjuvante de Freund , Masculino , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Estruturas Vegetais , Polifenóis/análise , Polifenóis/farmacologia , Desnaturação Proteica , Ratos Sprague-Dawley , Fator Reumatoide/sangue , Albumina Sérica/metabolismo , Terebintina
15.
Exp Appl Acarol ; 72(3): 291-302, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28589297

RESUMO

Compounds with tick (Ixodes ricinus) repellent properties were isolated from sulfate turpentine consisting of Norway spruce (80%) and Scots pine (20%) from southern Sweden. The turpentine was divided into two fractions by distillation under reduced pressure resulting in one monoterpene hydrocarbon fraction and a residual containing higher boiling terpenoids. The monoterpene fraction was further oxidized with SeO2 to obtain oxygenated monoterpenes with potential tick repellent properties. The oxidized fraction and the high boiling distillation residual were each separated by medium pressure liquid chromatography. The fractions were tested for tick repellency and the compounds in those with highest tick repellency were identified by GC-MS. The fractions with highest repellency contained, mainly (-)-borneol, and mixtures of (+)- and (-)-1-terpineol and terpinen-4-ol. The enantiomers of borneol showed similar tick repellent properties.


Assuntos
Repelentes de Insetos/farmacologia , Ixodes/efeitos dos fármacos , Extratos Vegetais/farmacologia , Terebintina/química , Animais , Repelentes de Insetos/isolamento & purificação , Noruega , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Óleos Vegetais/química , Óleos Vegetais/isolamento & purificação , Óleos Vegetais/farmacologia , Sulfatos , Terpenos
16.
Nat Prod Res ; 31(13): 1536-1543, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28114804

RESUMO

A novel aziridine compound N-acetyl-1,2-azacyclo-p-menthane d was synthesised using turpentine as raw material and characterised by FT-IR, 1H NMR, 13C NMR, ESI+-MS and HRMS. The pre-emergence herbicidal activities of d and its synthetic intermediates cis- and trans-N,N'-diacetyl-p-menthane-1,8-diamine (b2 and b1) were determined. The result showed that d exhibited much higher herbicidal activities against annual ryegrass, Digitaria sanguinalis and Ixeris denticulate than b2 and b1. The IC50 of d against the root and shoot growth of these three plants were lower than 1 mmol L-1. In contrast, the IC50 of b1 and b2 against the root and shoot growth of these plants were more than 10 mmol L-1.


Assuntos
Aziridinas/síntese química , Aziridinas/farmacologia , Herbicidas/síntese química , Terebintina/química , Herbicidas/química , Herbicidas/farmacologia , Mentol/análogos & derivados , Mentol/química , Plantas/efeitos dos fármacos , Espectroscopia de Infravermelho com Transformada de Fourier , Relação Estrutura-Atividade
17.
Int Endod J ; 50(11): 1084-1088, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27917509

RESUMO

AIM: To evaluate the effect of several solvents on the weight of apically extruded debris and irrigant during retreatment using a novel agar gel model. METHODS: Orange oil, turpentine oil and chloroform were used as solvents. Eighty single straight-rooted extracted human mandibular premolar teeth with a single root canal were divided into four groups (n = 20). All specimens were root canal-filled and weighed prior to their insertion into a prepared 1.5% agar gel model. The mean initial weights were measured by subtracting the weight of the specimen from the weight of the test apparatus and recorded. Following the removal of the coronal 4 mm of root filling, the test solvent was applied onto the root filling. No solvent was used in the control group. A Reciproc R25 instrument was used to remove the root filling in all groups. Apically extruded debris and test solvent were collected during retreatment procedures. The mean weights of apically extruded debris and irrigant were calculated by subtracting the mean initial weights from the weights of test apparatus without the Teflon tape and the specimen following the retreatment procedures. Data were statistically analysed using one-way analysis of variance. RESULTS: Use of solvents resulted in significantly less extruded debris and irrigant compared to the control group (P < 0.05). Chloroform extruded significantly more debris than orange oil and turpentine oil (P < 0.05). CONCLUSION: Use of solvents during root filling removal was associated with less apically extruded debris and irrigant when compared to no solvent.


Assuntos
Irrigantes do Canal Radicular/uso terapêutico , Tratamento do Canal Radicular/métodos , Solventes/farmacologia , Clorofórmio/farmacologia , Humanos , Óleos Vegetais/farmacologia , Tratamento do Canal Radicular/instrumentação , Terebintina/farmacologia
19.
Antioxid Redox Signal ; 27(5): 251-268, 2017 08 10.
Artigo em Inglês | MEDLINE | ID: mdl-27923278

RESUMO

AIMS: Anemia of inflammation (AI), the second prevalent anemia, is associated with worse prognosis and increased mortality in numerous chronic diseases. We recently reported that the gasotransmitter hydrogen sulfide (H2S) suppressed the inflammatory activation of signal transducer and activator of transcription 3 (STAT3) and hepcidin, the critical mediators of AI. Adenosine 5'-monophosphate-activated protein kinase (AMPK) is a novel inflammatory regulator and might be activated by H2S. In this study, we determined whether AMPK played a role in H2S-mediated anti-inflammatory response in AI and evaluated the therapeutic potential of AMPK against AI by pharmacological and clinical approaches. RESULTS: We showed that AMPK mediated the inhibition of STAT3, hepcidin, and AI by H2S during inflammation. Moreover, pharmacological and genetic activation of AMPK ameliorated hepcidin production, corrected iron dysregulation, and relieved hypoferremia and anemia in both acute and chronic inflammation models in mice. Mechanistic studies indicated that AMPK suppressed STAT3/hepcidin activation by promoting proteasome-mediated Janus kinase 2 (JAK2) degradation, which was dependent on the intact function of suppressor of cytokine signaling 1 (SOCS1) and increased interactions between SOCS1 and JAK2. Most importantly, the AMPK activator metformin was associated with decreased serum hepcidin content and anemia morbidity in Chinese type 2 diabetes mellitus patients. INNOVATION: This is the first study to demonstrate the inhibition of inflammatory hepcidin and AI by AMPK-induced JAK2 degradation. Our work uncovered AMPK as a novel therapeutic target, and metformin as a potential therapy against AI. CONCLUSION: The present work demonstrated that AMPK mediated the therapeutic effects of H2S and relieved AI by promoting SOCS1-mediated JAK2 degradation. Antioxid. Redox Signal. 27, 251-268.


Assuntos
Anemia/tratamento farmacológico , Hepcidinas/metabolismo , Sulfeto de Hidrogênio/uso terapêutico , Inflamação/tratamento farmacológico , Anemia/sangue , Anemia/metabolismo , Animais , Linhagem Celular , Células Cultivadas , Imunofluorescência , Humanos , Immunoblotting , Imunoprecipitação , Inflamação/sangue , Inflamação/metabolismo , Janus Quinase 2/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Reação em Cadeia da Polimerase em Tempo Real , Fator de Transcrição STAT3/metabolismo , Transdução de Sinais/efeitos dos fármacos , Proteína 1 Supressora da Sinalização de Citocina/metabolismo , Terebintina/toxicidade , Ubiquitinação/efeitos dos fármacos
20.
Dermatitis ; 27(4): 170-5, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27427818

RESUMO

Nearly 80 essential oils (including 2 jasmine absolutes) have caused contact allergy. Fifty-five of these have been tested in consecutive patients suspected of contact dermatitis, and nine (laurel, turpentine, orange, tea tree, citronella, ylang-ylang, sandalwood, clove, and costus root) showed greater than 2% positive patch test reactions. Relevance data are generally missing or inadequate. Most reactions are caused by application of pure oils or high-concentration products. The clinical picture depends on the responsible product. Occupational contact dermatitis may occur in professionals performing massages. The (possible) allergens in essential oils are discussed. Several test allergens are available, but patients should preferably be tested with their own products. Co-reactivity with other essential oils and the fragrance mix is frequent, which may partly be explained by common ingredients. Patch test concentrations for essential oils are suggested.


Assuntos
Dermatite Alérgica de Contato/etiologia , Óleos Voláteis/efeitos adversos , Cananga/efeitos adversos , Óleo de Cravo/efeitos adversos , Dermatite Alérgica de Contato/epidemiologia , Humanos , Óleos Vegetais/efeitos adversos , Sesquiterpenos/efeitos adversos , Óleo de Melaleuca/efeitos adversos , Terebintina/efeitos adversos
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