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Biochem Med (Zagreb) ; 30(1): 010704, 2020 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-31839724


Introduction: Diabetes mellitus (DM) is one of the most prevalent diseases worldwide. The objective of this study was to find out under what preanalytical conditions routine and diagnostic glucose tests are performed across Spanish laboratories; and also what criteria are used for DM diagnosis. Materials and methods: An online survey was performed by the Commission on Quality Assurance in the Extra-Analytical Phase of the Spanish Society of Laboratory Medicine (SEQC-ML). Access to the questionnaire was available on the home page of the SEQC-ML website during the period April-July 2018. Data analysis was conducted with the IBM SPSS© Statistics (version 20.0) program. Results: A total of 96 valid surveys were obtained. Most laboratories were in public ownership, serving hospital and primary care patients, with high and medium workloads, and a predominance of mixed routine-urgent glucose testing. Serum tubes were the most used for routine glucose analysis (92%) and DM diagnosis (54%); followed by lithium-heparin plasma tubes (62%), intended primarily for urgent glucose testing; point-of-care testing devices were used by 37%; and plasma tubes with a glycolysis inhibitor, mainly sodium fluoride, by 19%. Laboratories used the cut-off values and criteria recognized worldwide for DM diagnosis in adults and glucose-impaired tolerance, but diverged in terms of fasting plasma glucose and gestational DM criteria. Conclusion: Preanalytical processing of routine and DM diagnostic glucose testing in Spain does not allow a significant, non-quantified influence of glycolysis on the results to be ruled out. Possible adverse consequences include a delay in diagnosis and possible under-treatment.

Glicemia/análise , Coleta de Amostras Sanguíneas/métodos , Coleta de Amostras Sanguíneas/instrumentação , Diabetes Mellitus/diagnóstico , Humanos , Laboratórios Hospitalares/normas , Fase Pré-Analítica , Espanha , Inquéritos e Questionários
J Med Chem ; 56(4): 1596-613, 2013 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-23327489


Five compounds displaying an unprecedented binding mode of chloroquine to ferrocene through the bridging of the cyclopentadienyl rings were studied alongside their monosubstituted ferrocene analogues and organic fragments. The antiplasmodial activity was evaluated against strains of the malaria parasite (Plasmodium falciparum). While the chloroquine-bridged ferrocenyl derivatives were less active than their five monosubstituted ferrocenyl analogues, they retained activity in the drug-resistant strains. The biological and physical properties were correlated to antiplasmodial activity. Intramolecular hydrogen bonding was associated with increased antiplasmodial action, but it is not the determining factor. Instead, balance between lipophilicity and hydrophilicity had a greater influence. It was found that calculated partition coefficient (log P) values of 4.5-5.0 and topological polar surfaces area (tPSA) values of ∼26.0 Å(2) give the best balance. The particular conformation, compact size, and lipophilicity/hydrophilicity balance observed in the bridged compounds provide them with the structural characteristics needed to escape the mechanisms responsible for resistance.

Aminoquinolinas/química , Antimaláricos/química , Cloroquina/análogos & derivados , Cloroquina/química , Compostos Ferrosos/química , Aminoquinolinas/síntese química , Aminoquinolinas/farmacologia , Antimaláricos/síntese química , Antimaláricos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Cloroquina/síntese química , Cloroquina/farmacologia , Cristalografia por Raios X , Resistência a Medicamentos , Ensaios de Seleção de Medicamentos Antitumorais , Compostos Ferrosos/síntese química , Compostos Ferrosos/farmacologia , Hemina/química , Humanos , Ligações de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Metalocenos , Modelos Moleculares , Estrutura Molecular , Testes de Sensibilidade Parasitária , Plasmodium falciparum , Relação Estrutura-Atividade
Dalton Trans ; 41(21): 6431-42, 2012 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-22378031


This work presents a new family of organometallic antimalarial compounds consisting of ferrocene bearing a chloroquine-derived moiety as well as a 1,2;3,5-diisopropylidene glucofuranose moiety at a cyclopentadienyl scaffold in a 1,2-substitution pattern. The synthetic route proceeds via a stereoselective functionalization of ferrocene carboxaldehyde to the 1,2-disubstituted conjugates. After complete characterization of these new, trifunctional conjugates, they were examined for their cytotoxicity in two cancerous cell lines (MDA-MB-435S and Caco2) and one non-cancerous cell line (MCF-10A), showing that increased cytotoxicity can be observed for the chloroquine ferrocenyl conjugates compared to their carbohydrate-substituted precursors. The antiplasmodial activity of the conjugates in a chloroquine-sensitive strain of Plasmodium falciparum (D10) and a chloroquine-resistant strain (Dd2) was determined. Monosubstituted conjugates 13, 14 and 15 exhibit decreasing activity with increasing alkyl chain length between the ferrocene and quinoline moiety, bifunctional conjugates 16, 17, 18 show constant activity, performing better than chloroquine in the Dd2 strain.

Antimaláricos/química , Antimaláricos/farmacologia , Cloroquina/química , Cloroquina/farmacologia , Compostos Ferrosos/química , Monossacarídeos/química , Antimaláricos/síntese química , Antimaláricos/toxicidade , Linhagem Celular Tumoral , Cloroquina/síntese química , Cloroquina/toxicidade , Humanos , Metalocenos , Plasmodium falciparum/efeitos dos fármacos , Relação Estrutura-Atividade