43 research outputs found

    Antimicrobial screening of new 5-(chromene-3-yl)methylene-2,4-thiazolidinediones

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    The molecular mechanisms linking metabolic syndrome to endometrial and breast cancers

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    The metabolic syndrome represents a plethora of cardio-metabolic risk factors including obesity, arterial hypertension, atherogenic dyslipidemia, hyperglycemia, accompanied by pro-inflammatory and pro-thrombotic state. The metabolic syndrome is one of the key risk factors for certain types of cancer. Among these malignancies, breast cancer and endometrial neoplasms require special attention. Incriminated major causes for the development of breast and endometrial cancer in metabolic syndrome patients are: the pro-inflammatory status and related cytokines, adipokine imbalances, hyperestrogenism, growth factors, disturbances in cancer microenvironment, insulin resistance and hyperinsulinemia. The metabolic syndrome consists of molecular dysregulations that create a pro-oncogenic status. Our review aims at providing a better understanding of the mechanisms underlying the link between the metabolic syndrome and endometrial and breast cancer

    Actualități în cercetarea de noi molecule de antibiotice

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    Pharmaceutical chemistry department, Faculty of Pharmacy, Iuliu Hațieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania, Therapeutical chemistry, Faculty of Pharmacy, Iuliu Hațieganu University of Medicine and Pharmacy, Cluj-Napoca, RomaniaRezumat. Rezistența bacteriilor la antibioticele autorizate în terapia sau profilaxia infecțiilor este în creștere. Printre măsurile de contracarare a acestui fenomen îngrijorător, în afara utilizării mai raționale a antibioticelor și a optimizării schemelor de tratament, este necesară o intensificare a cercetărilor și investiții mai mari pentru descoperirea de noi molecule de antibiotice, noi inhibitori de betalactamaze, inhibitori ai pompelor de eflux, ai procesului QS, ai formării de biofilm dar și spre identificarea de noi ținte de acțiune. Metodele utilizate pentru descoperirea de noi antibiotice sunt cele clasice (extracție, biosinteză dirijată, semisinteză, sinteză, urmate de screening antibacterian), chimia organică de sinteză asociată cu studii computerizate de andocare cu ținte specifice, studii QSAR sau identificarea de molecule prototip prin chimie combinatorială.Abstract. Bacterial resistance to approved antibiotics (used in therapy and/or as prophylaxis) is increasing. Among the measures to counterwork this alarming phenomenon, beside the more rational use of antibiotics and the optimization of treatment regimens, an intensifying research and greater investments for the discovery of new antibiotic molecules, novel beta-lactamase inhibitors, efflux pump inhibitors, quorum sensing (QS) process and biofilm formation inhibitors, as well as new target identification, are needed. The methods used for the discovery of new antibiotics are the classical ones (extraction, directed biosynthesis, semi-synthesis, synthesis, followed by antibacterial screening), but also the more modern ones, like synthetic organic chemistry associated with molecular docking studies, QSAR studies or identification of prototype molecules through combinatorial chemistry

    CANDIDIASIS IN PREGNANCY- PERSONAL STUDY

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    The impact of an intensive educational program regarding candidiasis in pregnancyon health professionals knowledge at Clinical Hospital of Obstetrics and Gynecology ”Elena Doamna” in Iași, Romania. The study was designed in three phases: Assessment phase, Implementation phase and Evaluation phase. The study was conducted from early January to the end of December 2019. The result of the study shows that its most frequent location is in the mouth and the vagina. The symptoms are reduced and the diagnosis is based on the clinical examination, the confirmation being performed by microscopic examination. Prophylactic treatment of candidiasis involves maintaining a rigorous hygiene, avoiding excessive and unprotected use of antibiotics and increasing the body's immunity through a balanced diet and through the intake of mineral salts and vitamins

    Traços de personalidade e resiliência na população geral adulta

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    Tese de mestrado, Psicologia (Secção de Psicologia Clínica e da Saúde, Núcleo de Psicologia Clínica Dinâmica), Universidade de Lisboa, Faculdade de Psicologia, 2016O estudo da Resiliência tem vindo a assumir uma importância crescente na sociedade atual. Num mundo cada vez mais voltado para o sucesso, quais serão as características da Personalidade que poderão preparar os indivíduos para lidar e superar o fracasso de uma forma positiva? Foi objetivo deste estudo a análise entre os dados sociodemográficos e a Resiliência e Traços de Personalidade, assim como, investigar os efeitos preditores da Personalidade relativamente à Resiliência. Numa amostra de 338 indivíduos da população geral portuguesa, com idades entre os 18 e os 83 anos, foram administrados os instrumentos de avaliação: Questionário Sociodemográfico (QS), Inventário dos Cinco Fatores de Personalidade (NEO-FFI) e a Escala de Resiliência de Connor-Davidson (CD-RISC). Observam-se diferenças significativas que sugerem que com o avançar da idade, o Neuroticismo tende a diminuir e a Amabilidade e a Conscienciosidade a aumentar. As mulheres mostram-se mais amáveis e conscienciosas do que os homens. Ao nível da escolaridade, os indivíduos com Licenciatura ou maior escolaridade, mostram-se, na generalidade, mais abertos à experiência do que os que possuem graus de escolaridade mais baixos. Os sujeitos solteiros mostram-se mais neuróticos e menos conscienciosos do que os sujeitos casados. Elevados níveis de Conscienciosidade e Abertura à Experiência predizem a Resiliência. Baixo Neuroticismo e uma elevada Conscienciosidade ou Extroversão são de igual modo preditores de Resiliência. A dissertação apresenta um contributo para a investigação crescente sobre as características sociodemográficas e dos Traços de Personalidade que influenciam a Resiliência. Abre a possibilidade de uma exploração mais profunda em relação aos acontecimentos de vida (e.g. conclusão de um grau de ensino, relação) e a sua influência ao nível da Resiliência.The study of resilience has become increasingly important in today's society. In a world turned more and more towards success, what are the characteristics of personality that may prepare individuals to cope and overcome failure in a positive way? The sociodemographic exploratory analysis of Resilience and Personality Traits, as well as the predictive effects of personality and their relation to Resilience were the aim of this study. A sample of 338 adults of the Portuguese population, aged between 18 and 83 years, were asked to answer a Sociodemographic Questionnaire (SQ), the Inventory of Five Personality Factors (NEO-FFI) and the Resilience Scale Connor-Davidson (CD-RISC). Significant differences were observed that suggest that with advancing age, Neuroticism tends to decline and Agreeableness and Conscientiousness tend to increase. Women appear to be, on average, kinder and more conscientious than men. In terms of education, individuals with Bachelor or Higher Degree are shown to be more open towards new experiences rather than those with lower levels of education. Singles individuals appear to be more neurotic and less conscientious than married people. Individuals with greater Conscientiousness and greater Openness seem to predict Resilience. This can also be concluded regarding individuals with lower levels of Neuroticism either with greater levels of Conscientiousness or Extroversion. This study presents a contribution to the growing research of sociodemographic characteristics and Personality Traits that influence Resilience. It opens the possibility of a deeper exploration in relation to life events (for example: completion of a teaching degree, relation) and their influence on the level of Resilience

    5-Arylidene(chromenyl-methylene)-thiazolidinediones: Potential New Agents against Mutant Oncoproteins K-Ras, N-Ras and B-Raf in Colorectal Cancer and Melanoma

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    Background and objectives: Cancer represents the miscommunication between and within the body cells. The mutations of the oncogenes encoding the MAPK pathways play an important role in the development of tumoral diseases. The mutations of KRAS and BRAF oncogenes are involved in colorectal cancer and melanoma, while the NRAS mutations are associated with melanoma. Thiazolidine-2,4-dione is a versatile scaffold in medicinal chemistry and a useful tool in the development of new antitumoral compounds. The aim of our study was to predict the pharmacokinetic/pharmacodynamic properties, the drug-likeness and lead-likeness of two series of synthetic 5-arylidene(chromenyl-methylene)-thiazolidinediones, the molecular docking on the oncoproteins K-Ras, N-Ras and B-Raf, and to investigate the cytotoxicity of the compounds, in order to select the best structural profile for potential anticancer agents. Materials and Methods: In our paper we studied the cytotoxicity of two series of thiazolidine-2,4-dione derivatives, their ADME-Tox properties and the molecular docking on a mutant protein of K-Ras, two isoforms of N-Ras and an isoform of B-Raf with 16 mutations. Results: The heterocyclic compounds strongly interact with K-Ras and N-Ras right after their posttranslational processing and/or compete with GDP for the nucleotide-binding site of the two GTPases. They are less active against the GDP-bound states of the two targets. All derivatives have a similar binding pattern in the active site of B-Raf. Conclusions: The data obtained encourage the further investigation of the 5-arylidene(chromenyl-methylene)-thiazolidinediones as potential new agents against the oncoproteins K-Ras, N-Ras and B-Raf

    New Hydrazones Bearing Thiazole Scaffold: Synthesis, Characterization, Antimicrobial, and Antioxidant Investigation

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    New series of hydrazones 5–18 were synthesized, in good yields, by reacting 4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole-5-carbohydrazide with differently substituted benzaldehyde. The resulting compounds were characterized via elemental analysis, physico-chemical and spectral data. An antimicrobial screening was done, using Gram (+), Gram (−) bacteria and one fungal strain. Tested molecules displayed moderate-to-good growth inhibition activity. 2,2-Diphenyl-1-picrylhydrazide assay was used to test the antioxidant properties of the compounds. Monohydroxy (14–16), para-fluorine (13) and 2,4-dichlorine (17) derivatives exhibited better free-radical scavenging ability than the other investigated molecules

    Synthesis and antimicrobial activity of some new N-(aryl-oxo-alkyl)-5-arylidene-thiazolidine-2,4-diones

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    A series of new 5-(2,6-dichlorobenzylidene)thiazolidine-2,4-dione and 5-(4-methoxy-benzylidene)thiazolidine-2,4-dione derivatives (3a-h and 5a-h) were synthesized starting from 5-arylidene-thiazolidine-2,4-dione and α-halo-ketones. The structural elucidation of the newly synthesized compounds was based on elemental analysis and spectroscopic data (MS, 1H-NMR, 13C-NMR). The synthesized compounds were screened for their antimicrobial activities against several pathogenic strains of Gram-positive and Gram-negative bacteria and one fungal strain (Candida albicans), assessed in vitro as growth inhibition diameters. Some of them displayed better inhibitory activities than that of the reference drug against the Gram-positive S. aureus, B. cereus, L. monocytogenes bacterial strains, and showed good antifungal activity against C. albicans, while the antibacterial activity against Gram-negative E. coli and S. typhimurium bacterial strains was moderate
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