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1.
Int J Biol Macromol ; 142: 564-573, 2020 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-31747565

RESUMO

Peptic ulcer is one of the worldwide diseases where 10% of adults are affected by peptic ulcers at least once in their lifetime. The goal of this study was to evaluate the effect of levan in treating peptic ulcer. The bacterial honey isolates called Bacillus sp. levan was utilized. Levan was chemically characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), 1H and 13C NMR analysis. Levan was used to treat gastric ulcers induced in rats by oral administration of 5 mL/kg ethanol. Microscopic examination of stomach sections indicated that treatment with 200 mg/kg levan effectively healed the ulcers. Levan had no antimicrobial activity against a common cause of ulcers such as Helicobacter pylori bacteria. Rather, we proposed that the high adhesion (manifested as a protective coating) and prebiotic activity of levan may account for the observed beneficial effects. The immunohistochemical examination showed that levan led to a noticeable Bacillus sp. levan reduction in NF-κB in the upper gastric mucosa. The results concluded that the role of levan was more protective rather than preventive and suggested that levan could play a fundamental role in solving the peptic ulcer problems.


Assuntos
Bacillus/química , Frutanos/isolamento & purificação , Frutanos/farmacologia , Mel/microbiologia , Úlcera Péptica/tratamento farmacológico , Animais , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Anti-Infecciosos/uso terapêutico , Adesão Celular/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Frutanos/uso terapêutico , Masculino , Úlcera Péptica/metabolismo , Ratos , Ratos Sprague-Dawley
2.
Tissue Cell ; 49(3): 410-426, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28410798

RESUMO

Doxorubicin (DOX) is a chemotherapeutic agent used for treatment of different cancers and its clinical usage is hindered by the oxidative injury-related cardiotoxicity. This work aims to declare if the harmful effects of DOX on heart can be alleviated with the use of Coenzyme Q10 (CoQ10) or L-carnitine. The study was performed on seventy two female Wistar albino rats divided into six groups, 12 animals each: Control group; DOX group (10mg/kg); CoQ10 group (200mg/kg); L-carnitine group (100mg/kg); DOX+CoQ10 group; DOX+L-carnitine group. CoQ10 and L-carnitine treatment orally started 5days before a single dose of 10mg/kg DOX that injected intraperitoneally (IP) then the treatment continued for 10days. At the end of the study, serum biochemical parameters of cardiac damage, oxidative stress indices, and histopathological changes were investigated. CoQ10 or L-carnitine showed a noticeable effects in improving cardiac functions evidenced reducing serum enzymes as serum interleukin-1 beta (IL-1 ß), tumor necrosis factor alpha (TNF-α), leptin, lactate dehydrogenase (LDH), Cardiotrophin-1, Troponin-I and Troponin-T. Also, alleviate oxidative stress, decrease of cardiac Malondialdehyde (MDA), Nitric oxide (NO) and restoring cardiac reduced glutathione levels to normal levels. Both corrected the cardiac alterations histologically and ultrastructurally. With a visible improvements in α-SMA, vimentin and eNOS immunohistochemical markers. CoQ10 or L-carnitine supplementation improves the functional and structural integrity of the myocardium.


Assuntos
Carnitina/farmacologia , Doxorrubicina/efeitos adversos , Cardiopatias , Miocárdio/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Ubiquinona/análogos & derivados , Animais , Cardiotoxicidade/metabolismo , Cardiotoxicidade/patologia , Cardiotoxicidade/prevenção & controle , Doxorrubicina/farmacologia , Feminino , Cardiopatias/induzido quimicamente , Cardiopatias/metabolismo , Cardiopatias/patologia , Cardiopatias/prevenção & controle , Miocárdio/patologia , Ratos , Ratos Wistar , Ubiquinona/farmacologia
3.
Arch Pharm (Weinheim) ; 350(2)2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28177550

RESUMO

Series of N-(4-substitutedphenyl)-4-(1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkanamides (5a-j) and 4-chloro-N'-((1-methyl (or 1,2-dimethyl)-4-oxo-1,2-dihydroquinazolin-3(4H)-yl)-alkaloyl)benzohydrazides (6a-f) were designed based on the previously reported essential structural features for anticonvulsant activity. Several amino acids were incorporated within the synthesized quinazolin-4(3H)-ones to improve their bioavailability and the anticonvulsant activity. Synthesis of the target compounds was accomplished in four steps starting from the reaction between N-methyl isatoic anhydride and the appropriate amino acid. Then, the carboxylic acid group was utilized to synthesize the required final structures. The new quinazolinone derivatives were evaluated for their anticonvulsant activity according to the Anticonvulsant Drug Development (ADD) Program protocol. All the 16 new quinazolinones exhibited good anticonvulsant activity; especially 5f, 5b, and 5c showed superior anticonvulsant activities in comparison to the reference drug, with ED50 values of 28.90, 47.38, and 56.40 mg/kg, respectively.


Assuntos
Anticonvulsivantes/síntese química , Anticonvulsivantes/farmacologia , Quinazolinonas/síntese química , Quinazolinonas/farmacologia , Convulsões/prevenção & controle , Animais , Relação Dose-Resposta a Droga , Eletrochoque , Camundongos , Pentilenotetrazol , Teste de Desempenho do Rota-Rod , Relação Estrutura-Atividade
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