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Eur J Med Chem ; 172: 26-35, 2019 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-30939351


Nowadays, due to spreading antibiotic resistance among clinically relevant pathogens, the requirement of novel therapeutic approaches is felt more than ever. One of the alternative strategies is anti-virulence therapy without affecting bacterial growth or viability. In Pseudomonas aeruginosa, an opportunistic human pathogen that exhibits intrinsic multi-drug resistance, both virulence factors' production and biofilm formation depends on its quorum sensing (QS) network. Therefore, targeting the key proteins involved in QS system is an attractive method to overcome P. aeruginosa pathogenicity and resistance. The transcriptional regulator PqsR, also called MvfR, is one of these major proteins which employs 3,4-dihydroxy-2-heptylquinoline (PQS) and 4-hydroxy-2-heptylquinoline (HHQ) as signaling molecules. Reviewing the advances in development of small molecules inhibit this protein, assist to open a new window to smart molecule design that may revolutionize treatment of P. aeruginosa infections.

Antibacterianos/farmacologia , Proteínas de Bactérias/antagonistas & inibidores , Pseudomonas aeruginosa/efeitos dos fármacos , Quinazolinonas/farmacologia , Quinolonas/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Proteínas de Bactérias/metabolismo , Estrutura Molecular , Quinazolinonas/síntese química , Quinazolinonas/química , Quinolonas/síntese química , Quinolonas/química , Percepção de Quorum/efeitos dos fármacos , Transativadores
Medicina (Kaunas) ; 54(4)2018 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-30344286


Introduction: Sleeplessness is the most common sleep disorder. In this study, the hypnotic effect of macerated (HAME) and soxhlet (HASE) extract of Lagenaria vulgaris (fruit and seed) and Cucurbita pepo (fruit) were studied in mice. Methods: Extracts and fractions were administered intra-peritoneally (i.p.) in mice 30 min before the sodium pentobarbital (30 mg/kg, i.p.). Moreover, the influence of flumazenil or naloxone on the hypnotic effects of the extract and its toxic effects were evaluated. Results: The HAME and HASE of C. pepo prolonged the pentobarbital-induced sleep duration at dose of 200 mg/kg. The HAME of L. vulgaris (fruit) at dose of 200 mg/kg increased the sleeping time. The HAME and HASE of L. vulgaris (seed) increased sleep duration at doses of 50 and 100 mg/kg. Besides, flumazenil (2 mg/kg) reversed the effects of both diazepam (P < 0.001 vs. diazepam group), 200 mg/kg of HAME of C. pepo and 50 mg/kg of HAME and HASE of L. vulgaris (seed). All fractions especially ethyl-acetate fraction (EAF) of L. vulgaris (seed) increased the sleep duration. Naloxone reversed the hypnotic effect of HAME and HASE of L. vulgaris (seed). The extracts showed no neurotoxic effects on PC12 and L929 cell lines. Conclusion: The results showed that L. vulgaris (seed and fruit) and C. pepo potentiated pentobarbital hypnosis without toxic influence. The hypnotic effects of L. vulgaris seed was greater than its fruit and C. pepo. The GABA and opioid receptors may play role in the sleep-induction of L. vulgaris seed.

Cucurbita , Extratos Vegetais/farmacologia , Medicamentos Indutores do Sono/farmacologia , Transtornos do Sono-Vigília/tratamento farmacológico , Sono/efeitos dos fármacos , Animais , Modelos Animais de Doenças , Frutas , Masculino , Camundongos , Pentobarbital , Extratos Vegetais/administração & dosagem , Medicamentos Indutores do Sono/administração & dosagem
Iran J Pathol ; 11(3): 222-230, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27799971


BACKGROUND: Hepatitis C virus (HCV) infection is one of the most prevalent infectious diseases responsible for high morbidity and mortality worldwide. Therefore, designing new and effective therapeutics is of great importance. The aim of the current study was to construct a DNA vaccine containing structural proteins of HCV and evaluation of its expression in a eukaryotic system. METHODS: Structural proteins of HCV (core, E1, and E2) were isolated and amplified from JFH strain of HCV genotype 2a using PCR method. The PCR product was cloned into pCDNA3.1 (+) vector and finally were confirmed by restriction enzyme analysis and sequencing methods. The eukaryotic expression of the vector was confirmed by RT-PCR. RESULTS: A recombinant vector containing 2241bp fragment of HCV structural genes was constructed. The desired plasmid was sequenced and corresponded to 100% identity with the submitted sequences in GenBank. RT-PCR results indicated that the recombinant plasmid could be expressed efficiently in the eukaryotic expression system. CONCLUSION: Successful cloning of structural viral genes in pCDNA3.1 (+) vector and their expression in the eukaryotic expression system facilitates the development of new DNA vaccines against HCV. A DNA vaccine encoding core-E1-E2 antigens was designed. The desired expression vector can be used for further attempts in the development of vaccines.