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2.
Clin Exp Pharmacol Physiol ; 49(1): 145-174, 2022 01.
Artigo em Inglês | MEDLINE | ID: mdl-34536310

RESUMO

Nowadays, quinoline scaffold is among the most vital construction compounds for the development of new drugs. The purpose of this research is to evaluate the anti-cancer activity of sodium salt of ethyl (E)-2-cyano-3-(7-hydroxy-4-methyl-2-oxoquinoline-1(2H)-yl)-3-(4-hydroxyphenyl) acrylate against Ehrlich ascites carcinoma (EAC) cells residing in female mice's peritoneal cavity. The docking study exhibited a favourable interaction between the compound and the receptors 1MOY and 3KJF of osteopontin and caspase 3, respectively. The compound's sodium salt showed potential antioxidant and anti-cancer effects against Ehrlich ascites carcinoma (EAC) cells in vivo. Herein, the results elucidated that treatment with the compound's sodium salt exerted significant chemopreventive and chemotherapeutic effects, which reduced both EAC cell volume and count. Our results revealed that treatment with the sodium salt of the compound demonstrated a remarkable in vivo apoptotic effect through elevation of the expression of caspase 3 and reduction of osteopontin levels. Histopathological examination confirmed that the compound's sodium salt improved liver and kidney tissues without any apparent adverse effects.


Assuntos
Antineoplásicos/uso terapêutico , Carcinoma de Ehrlich/tratamento farmacológico , Quinolonas/uso terapêutico , Animais , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Relação Dose-Resposta a Droga , Feminino , Dose Letal Mediana , Camundongos , Simulação de Acoplamento Molecular , Estrutura Molecular , Quinolonas/farmacologia
3.
Molecules ; 26(20)2021 10 10.
Artigo em Inglês | MEDLINE | ID: mdl-34684700

RESUMO

Background: The present study investigated the antifungal activity and mode of action of four Olea europaea leaf extracts, Thymus vulgaris essential oil (EO), and Boswellia carteri EO against Fusarium oxysporum. Methods:Fusarium oxysporum Lactucae was detected with the internal transcribed spacer (ITS) region. The chemical compositions of chloroform and dichloromethane extracts of O. europaea leaves and T. vulgaris EO were analyzed using GC-MS analysis. In addition, a molecular docking analysis was used to identify the expected ligands of these extracts against eleven F. oxysporum proteins. Results: The nucleotide sequence of the F. oxysporum Lactucae isolate was deposited in GenBank with Accession No. MT249304.1. The T. vulgaris EO, chloroform, dichloromethane and ethanol efficiently inhibited the growth at concentrations of 75.5 and 37.75 mg/mL, whereas ethyl acetate, and B. carteri EO did not exhibit antifungal activity. The GC-MS analysis revealed that the major and most vital compounds of the T. vulgaris EO, chloroform, and dichloromethane were thymol, carvacrol, tetratriacontane, and palmitic acid. Moreover, molecular modeling revealed the activity of these compounds against F. oxysporum. Conclusions: Chloroform, dichloromethane and ethanol, olive leaf extract, and T. vulgaris EO showed a strong effect against F. oxysporum. Consequently, this represents an appropriate natural source of biological compounds for use in healthcare. In addition, homology modeling and docking analysis are the best analyses for clarifying the mechanisms of antifungal activity.


Assuntos
Antifúngicos/farmacologia , Boswellia/química , Fusarium/efeitos dos fármacos , Óleos Voláteis/farmacologia , Olea/química , Extratos Vegetais/farmacologia , Thymus (Planta)/química , Fusarium/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana/métodos
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