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1.
Folia Med (Plovdiv) ; 65(4): 638-643, 2023 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-37655384

RESUMO

INTRODUCTION: Sideritisscardica, Lamiaceae, is a plant with anti-inflammatory, antirheumatic, digestive, and antimicrobial properties that is widely used in folk medicine throughout the Balkan Peninsula. The name derives from the Greek word 'sideros', meaning iron, and it is believed that the plant was also used by soldiers to heal wounds caused by cutting weapons.


Assuntos
Antirreumáticos , Lamiaceae , Sideritis , Ratos , Animais , Ratos Wistar , Ferro
2.
Medicina (Kaunas) ; 55(4)2019 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-30959829

RESUMO

Background and objectives: The clinical use of non-steroidal anti-inflammatory drugs is limited due to high incidence of adverse drug reactions. The pyrrole heterocycle is included in the chemical structure of a number of drugs with various activities and shows relatively good tolerability and safety. The objectives of our study were to evaluate the analgesic and anti-inflammatory activity, as well as possible organ toxicity, of 2-[3-acetyl-5-(4-chloro-phenyl)-2-methyl-pyrrol-1-yl]-3-(1H-indol-3-yl)-propionic acid (compound 3g), a novel N-pyrrolylcarboxylic acid structurally similar to celecoxib. Materials and methods: All experiments were performed on 6-week-old male Wistar rats divided into parallel groups (n = 8). Antinociception was assessed using animal pain models with thermal and chemical stimuli (paw withdrawal, tail-flick, and formalin tests). Criteria for the analgesic effect were increased latency in the paw withdrawal and tail-flick tests and decreased paw licking time in the formalin test compared to animals treated with saline (control). Anti-inflammatory activity was measured using a carrageenan-induced paw edema model; the criterion for anti-inflammatory effect was decreased edema compared to control. Blood samples were obtained after animals were sacrificed to assess possible organ toxicity. Statistical analysis was performed with IBM SPSS 20.0. Results: 2-[3-Acetyl-5-(4-chloro-phenyl)-2-methyl-pyrrol-1-yl]-3-(1H-indol-3-yl)-propionic acid had analgesic action against chemical stimulus after single and multiple administration and against thermal stimulus after single administration. Compound 3g significantly suppressed carrageenan-induced paw edema after both single and continuous administration. After continuous administration, hematological tests showed that compound 3g decreased leukocyte and platelet levels and elevated serum creatinine levels. Conclusions: Antinociception with the tested compound is most likely mediated by spinal, peripheral, and anti-inflammatory mechanisms. Possible tolerance of the analgesic action at the spinal level develops after continuous administration. Anti-inflammatory activity is significant and probably the leading cause of antinociception. After multiple administration, compound 3g showed signs of potential nephrotoxicity and antiplatelet activity, as well as suppression of leukocyte levels.


Assuntos
Analgésicos/química , Analgésicos/farmacologia , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Celecoxib/análogos & derivados , Celecoxib/farmacologia , Avaliação Pré-Clínica de Medicamentos , Indóis/química , Indóis/farmacologia , Analgésicos/administração & dosagem , Analgésicos/efeitos adversos , Análise de Variância , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/efeitos adversos , Comportamento Animal/efeitos dos fármacos , Plaquetas/efeitos dos fármacos , Carragenina/administração & dosagem , Carragenina/farmacologia , Celecoxib/administração & dosagem , Celecoxib/efeitos adversos , Edema/induzido quimicamente , Edema/tratamento farmacológico , Eritrócitos/efeitos dos fármacos , Hemoglobinas/análise , Leucócitos/efeitos dos fármacos , Masculino , Modelos Animais , Medição da Dor , Pirróis/química , Ratos , Ratos Wistar
3.
Folia Med (Plovdiv) ; 60(4): 571-579, 2018 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-31188766

RESUMO

BACKGROUND: Betula pendula is widespread in Europe and Asia. It has been used in traditional medicine since ancient times. Birch leaf extracts are known to exhibit a number of pharmacological activities. Antioxidant activity has also been reported. AIM: The aim of this work was to investigate the antioxidant activity of a dry leaf extract from Betula pendula Roth. MATERIALS AND METHODS: The total flavonoid content was determined. Some of the most commonly used methods were applied to evaluate the antioxidant capacity of the extract in vitro and in vivo. The ability of the extract to scavenge DPPH free radicals was evaluated by the method described by Brand-Williams with suitable modifications. ABTS decolorization assay was also applied. The in vivo assay was performed after acute and chronic administration of the extract into white albino rats, in a dose of 100 and 500 mg/kg bw. The antioxidant potential of the plasma was determined using FRAP reagent. RESULTS: A total flavonoid content of 42.5 mg/g was found, expressed as quercetin. The antioxidant activity against ABTS was concentration and time dependent. For example the concentration of 200 µg/ml led to 70.95% - 99.46% scavenging activity. DPPH scavenging activity was found to be about 98% at a concentration of 80 µg/ml. The extract possesses antioxidant potential, comparable with that of Trolox, in acute application. In chronic application, poorer results are observed, probably due to biotransformation and elimination processes. CONCLUSION: Dried birch leaf extract has a relatively high antioxidant potential and could be used as a natural source of antioxidants.


Assuntos
Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Betula/química , Animais , Flavonoides/análise , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Radicais Livres/sangue , Masculino , Medicina Tradicional , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Ratos , Ratos Wistar
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