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1.
Pak J Pharm Sci ; 34(2(Supplementary)): 671-677, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34275801

RESUMO

Rumex dentatus has been used traditionally for ailment of cardiovascular diseases. The aim of the present study was to assess cardiovascular effects in isolated perfused rabbit heart. Aqueous and n-butanolic fractions were assessed for their effect on perfusion pressure (PP), force of contraction (FC) and heart rate (HR) of rabbit heart using Langendorff's method. The possible mechanisms of action of extracts/fraction were assessed with and without application of different agonist/antagonist. Phytochemical, toxicity and anti-oxidant activities were also determined. Both extracts at 1mg/mL dose produced a highly significant decrease in FC and HR but PP remained unchanged. Moreover, aqueous fraction of Rumex dentatus at 0.001mg/mL dose produced a highly significant decrease in FC and HR but no significant change in PP was observed. Atropine 10-5 M did not inhibit the cardiac depressant response of both fractions. Furthermore, both fractions blocked the positive ionotropic and chronotropic effects of adrenaline and calcium chloride. Phytochemical studies have shown the presence of some phytochemicals. Acute and sub-chronic toxicity studies demonstrated that test extracts are safe and produced no significant changes in haematological and biochemical parameters. Crude extract showed significant antioxidant activity like ascorbic acid. This study revealed that this plant have good cardiac depressant effect.


Assuntos
Antioxidantes/farmacologia , Fármacos Cardiovasculares/farmacologia , Coração/efeitos dos fármacos , Preparação de Coração Isolado , Extratos Vegetais/farmacologia , Rumex/química , Animais , Atropina/farmacologia , Cloreto de Cálcio/farmacologia , Fármacos Cardiovasculares/efeitos adversos , Epinefrina/farmacologia , Feminino , Frequência Cardíaca/efeitos dos fármacos , Preparação de Coração Isolado/métodos , Masculino , Camundongos , Contração Miocárdica/efeitos dos fármacos , Extratos Vegetais/efeitos adversos , Coelhos , Ratos , Ratos Sprague-Dawley , Rumex/efeitos adversos
2.
Pak J Pharm Sci ; 34(2(Supplementary)): 687-691, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34275803

RESUMO

Antihypertensive studies on aqueous-methanolic extract prepared from seeds of Cydonia oblonga M. were carried out. The test extract in 200, 400 and 600 mg/kg doses was investigated in normotensive, high cholesterol and glucose fed hypertensive rats through non-invasive blood pressure measuring technique. Acute and sub-chronic toxicity studies were conducted in mice and rats, respectively. The test extract significantly decreased dose dependently the systolic, diastolic and mean arterial pressures. The test extract in 600mg/kg dose produced maximum effect and prevented rise in blood pressure of high cholesterol diet and glucose fed rats as compare to control in 21 days studies. The extract was found safe up to 4g/kg dose in mice. In sub-chronic toxicity study, no significant alteration in blood chemistry of extract treated rats was observed except reduction in the low density cholesterol levels. It is concluded that Cydonia oblonga seeds extract possess antihypertensive effect which supports its use in folklore.


Assuntos
Anti-Hipertensivos/uso terapêutico , Hipertensão/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Rosaceae/química , Animais , Anti-Hipertensivos/efeitos adversos , Pressão Sanguínea/efeitos dos fármacos , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Feminino , Masculino , Camundongos , Extratos Vegetais/efeitos adversos , Ratos , Ratos Sprague-Dawley , Rosaceae/efeitos adversos , Sementes/efeitos adversos , Sementes/química
3.
Pak J Pharm Sci ; 34(2(Supplementary)): 731-735, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34275808

RESUMO

The modern trend of research is highly focused on finding new bioactive molecules from medicinal plants. As a functional bicyclic monoterpene, Bornyl acetate (BA) has displayed antioxidant and anti-inflammatory properties in different types of cells and tissues. The purpose of this research was to evaluate the probable hypotensive effect of BA, an underlying mechanism(s) backboned by in-silico studies. Mean arterial pressure and heart rate were recorded via invasive blood pressure measuring technique in normotensive Sprague-Dawley rats following the administration of BA (1-80mg/kg). Docking studies were carried out with various targets involved in the pathophysiology of hypertension.RO5 and ADMET properties were also evaluated. In the current study dose-dependent reduction in systolic, diastolic and mean arterial pressure was observed. Pretreatment with atropine and captopril significantly (p<0.001) reduced the hypotensive effect produced by BA. On the other hand docking studies showed pronounced interactions with M2 mAch receptor in an agonistic way and ACE protein in an antagonistic way. BA justified all cut-off limits of RO5 and had an acceptable predicted computational toxicity profile. Results postulate that dose-dependent hypotensive effect of BA is mediated through the muscarinic pathway and ACE inhibitory activity corresponding well with findings of in-silico studies.


Assuntos
Anti-Hipertensivos/farmacologia , Canfanos/farmacologia , Monoterpenos/farmacologia , Animais , Anti-Hipertensivos/química , Pressão Sanguínea/efeitos dos fármacos , Canfanos/química , Simulação por Computador , Frequência Cardíaca/efeitos dos fármacos , Simulação de Acoplamento Molecular , Estrutura Molecular , Monoterpenos/química , Ratos , Ratos Sprague-Dawley
4.
Pak J Pharm Sci ; 34(2(Supplementary)): 781-785, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34275815

RESUMO

Present study was conducted to validate the folkloric claims of morus nigra l. (moraceae) using invasive blood pressure measuring and ex vivo vasorelaxant experimental techniques. Intravenous administration of mn. Aq in 0.01-30 mg/kg doses caused significant decrease in mean arterial pressure and heart rate in fructose-induced hypertensive rats. It also showed relaxation in high k+ [80 mm] and pe (1µm) mediated aortic contraction with ec50 1.25 and 3.72mg/ml values, respectively. Vaso-relaxant effect of mn.aq was partially blocked in presence of l-name with ec50, 5.32mg/ml value, but showed concentration dependent significant inhibition of ligand gated and voltage gated ca+2 channels and intracellular ca+2 release, similar to verapamil. Findings of current study designate that aqueous fraction of m. Nigra possesses antihypertensive activity with concentration-dependent vaso-relaxant effect predominantly mediated through endothelial-independent calcium channel blocking pathways accompanied by partial involvement of endothelium-dependent nos mediated relaxation.


Assuntos
Anti-Hipertensivos/farmacologia , Canais de Cálcio/efeitos dos fármacos , Endotélio Vascular/efeitos dos fármacos , Hipertensão/tratamento farmacológico , Morus/química , Extratos Vegetais/farmacologia , Administração Intravenosa , Animais , Pressão Sanguínea/efeitos dos fármacos , Modelos Animais de Doenças , Frutas/química , Frequência Cardíaca/efeitos dos fármacos , Masculino , Ratos
5.
Inflammopharmacology ; 29(5): 1413-1425, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34302591

RESUMO

Venlafaxine is a serotonin-norepinephrine reuptake inhibitor used to treat depression. Previous studies demonstrated its anti-nociceptive and anti-inflammatory activities through the suppression of pro-inflammatory cytokines. Present research aimed to explore its anti-arthritic potential. Different in-vitro assays including egg albumin, bovine serum albumin denaturation and human red blood cell (RBC) membrane stabilization assays along with in-vivo models of formaldehyde and complete Freund's adjuvant-induced arthritis were used to study its anti-arthritic effect. Venlafaxine inhibited egg albumin and bovine serum albumin denaturation and preserve the integrity of red blood cells membrane in concentration-dependent manner. In formaldehyde-induced arthritis venlafaxine significantly (p < 0.001) reduced the paw edema on treatment for 10 days. Chronic administration of venlafaxine for 28 days in Freund's adjuvant-induced arthritis model decreased the paw volume (p < 0.001), arthritic index (p < 0.01), flexion pain score (p < 0.05), mobility score (p < 0.05), and improved the stance score (p < 0.05). Venlafaxine also significantly declined the rheumatoid factor (p < 0.01) and C-reactive protein (p < 0.05) levels and increased the RBC count (p < 0.01) and Hb value (p < 0.001). Upon PCR analysis venlafaxine remarkably turndown the mRNA expression of TNF-α, IL-6, IL-1ß, and COX-2. Taken together it is inferred from current findings that venlafaxine possesses the significant anti-arthritic activity and could be a potential therapeutic option for the treatment of rheumatoid arthritis.


Assuntos
Antirreumáticos/farmacologia , Artrite Experimental/tratamento farmacológico , Artrite Reumatoide/tratamento farmacológico , Cloridrato de Venlafaxina/farmacologia , Animais , Antirreumáticos/administração & dosagem , Artrite Experimental/patologia , Artrite Reumatoide/patologia , Ciclo-Oxigenase 2/genética , Relação Dose-Resposta a Droga , Regulação para Baixo/efeitos dos fármacos , Eritrócitos/citologia , Eritrócitos/efeitos dos fármacos , Feminino , Adjuvante de Freund , Humanos , Interleucina-1beta/genética , Interleucina-6/genética , Masculino , Ratos , Ratos Sprague-Dawley , Fator de Necrose Tumoral alfa/genética , Cloridrato de Venlafaxina/administração & dosagem
6.
Artigo em Inglês | MEDLINE | ID: mdl-34065430

RESUMO

Skin cancer is one of the most dangerous forms of cancer. Skin cancer is caused by un-repaired deoxyribonucleic acid (DNA) in skin cells, which generate genetic defects or mutations on the skin. Skin cancer tends to gradually spread over other body parts, so it is more curable in initial stages, which is why it is best detected at early stages. The increasing rate of skin cancer cases, high mortality rate, and expensive medical treatment require that its symptoms be diagnosed early. Considering the seriousness of these issues, researchers have developed various early detection techniques for skin cancer. Lesion parameters such as symmetry, color, size, shape, etc. are used to detect skin cancer and to distinguish benign skin cancer from melanoma. This paper presents a detailed systematic review of deep learning techniques for the early detection of skin cancer. Research papers published in well-reputed journals, relevant to the topic of skin cancer diagnosis, were analyzed. Research findings are presented in tools, graphs, tables, techniques, and frameworks for better understanding.


Assuntos
Melanoma , Neoplasias Cutâneas , Aprendizado Profundo , Humanos , Melanoma/diagnóstico , Melanoma/epidemiologia , Pele , Neoplasias Cutâneas/diagnóstico , Neoplasias Cutâneas/epidemiologia
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