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[PMID]:29241085
[Au] Autor:Alshishani A; Salhimi SM; Saad B
[Ad] Endereço:School of Chemical Sciences, Universiti Sains Malaysia, 11800 Penang, Malaysia. Electronic address: anasshishani@gmail.com.
[Ti] Título:Salting-out assisted liquid-liquid extraction coupled with hydrophilic interaction chromatography for the determination of biguanides in biological and environmental samples.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1073:51-59, 2018 Jan 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A new salting-out assisted liquid-liquid extraction (SALLE) sample preparation method for the determination of the polar anti-diabetic biguanide drugs (metformin, buformin and phenformin) in blood plasma, urine and lake water samples were developed. The SALLE was performed by mixing samples (plasma (0.2mL), urine or lake water (1.0mL)) with acetonitrile (0.4mL for plasma, 0.5mL for urine or lake water), sodium hydroxide powder was then added for the phase separation. The effects of type of salting-out reagent, type of extraction solvent, volumes of acetonitrile and sample, amount of sodium hydroxide, vortexing and centrifugation times on the extraction efficiency were investigated. The upper layer, containing the biguanides, was directly injected into a HPLC unit using ZIC-HILIC column (150mm×2.1mm×3.5µm) and was detected at 236nm. The method was validated and calibration curves were linear with r >0.99 over the range of 20-2000µgL for plasma and 5-2000µgL for urine and lake water samples. The limits of detection were in the range (3.8-5.6)µgL , (0.8-1.5)µgL and (0.3-0.8)µgL for plasma, urine and lake water, respectively. The accuracies in the three matrices were within 87.3-103%, 87.4-109%, 82.2-109% of the nominal concentration for metformin, buformin and phenformin, respectively. The relative standard deviation for inter- and intra -day precision were in the range of 1.0-17% for all analytes in the three matrices.
[Mh] Termos MeSH primário: Biguanidas/análise
Biguanidas/isolamento & purificação
Cromatografia Líquida de Alta Pressão/métodos
Extração Líquido-Líquido/métodos
Poluentes Químicos da Água/análise
Poluentes Químicos da Água/isolamento & purificação
[Mh] Termos MeSH secundário: Acetonitrilos
Biguanidas/química
Biguanidas/urina
Seres Humanos
Interações Hidrofóbicas e Hidrofílicas
Lagos/química
Limite de Detecção
Modelos Lineares
Reprodutibilidade dos Testes
Cloreto de Sódio
Poluentes Químicos da Água/química
Poluentes Químicos da Água/urina
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acetonitriles); 0 (Biguanides); 0 (Water Pollutants, Chemical); 451W47IQ8X (Sodium Chloride); Z072SB282N (acetonitrile)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171215
[St] Status:MEDLINE


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[PMID]:29305328
[Au] Autor:Chowdhury A; Arnold LL; Wang Z; Pennington KL; Dodmane P; Farragut-Cardoso AP; Klaunig JE; Cros D; Creppy EE; Cohen SM
[Ad] Endereço:Department of Pathology and Microbiology, University of Nebraska Medical Center, Omaha, NE 68198-3135, United States.
[Ti] Título:Effect of polyhexamethylene biguanide on rat liver.
[So] Source:Toxicol Lett;285:94-103, 2018 Mar 15.
[Is] ISSN:1879-3169
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Polyhexamethylene biguanide (PHMB), an amphiphilic polymeric biocide, increased liver tumor incidence in male and female rats at 1000 and 1500 mg/L in drinking water, but not at 500 mg/L in previous studies. In another study, PHMB administered in diet at 4000 mg/kg was negative for hepatocellular tumors. The present studies evaluated bioavailability and distribution of PHMB administered in drinking water and diet and possible modes of action (MOA). PHMB in drinking water was unpalatable during the first 3 days, resulting in markedly decreased food consumption and decreased body weight. Ki-67 labeling index was increased in hepatocytes and endothelial cells dose responsively with PHMB administered in drinking water but not diet. Vitamin E had no effect on this. There was no cytotoxicity by histopathology or serum enzymes, and no increase in cytokines TNFα, IL-1α or NF-κB. Focal iron deposition in sinusoidal lining cells was detected. Microarray analyses were non-contributory. No effect on CAR or PPARα activation was detected. C-PHMB administered at 500, 1000, or 1500 mg/L in the drinking water or 4000 mg/kg in the diet was nearly completely absorbed and excreted in urine, with some fecal excretion. The hypothesized MOA for liver tumors induced by PHMB in drinking water is: 1) severe dehydration and starvation because of unpalatability, followed by ingestion with rapid absorption and urinary excretion; 2) increased hepatocyte proliferation; and 3) induction of hepatocellular foci and tumors. The PHMB-induced rat hepatocellular tumors are unlikely to pose a human cancer risk. However, the actual MOA has not been determined.
[Mh] Termos MeSH primário: Biguanidas/toxicidade
Desinfetantes/toxicidade
Fígado/efeitos dos fármacos
[Mh] Termos MeSH secundário: Administração Oral
Animais
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Feminino
Hepatócitos/efeitos dos fármacos
Hepatócitos/patologia
Fígado/metabolismo
Fígado/patologia
Testes de Função Hepática
Masculino
Estresse Oxidativo/efeitos dos fármacos
Ratos Wistar
Testes de Toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biguanides); 0 (Disinfectants); 322U039GMF (polihexanide)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180219
[Lr] Data última revisão:
180219
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180107
[St] Status:MEDLINE


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[PMID]:29025650
[Au] Autor:Lefebvre E; Lembre P; Picard J; El-Guermah L; Seyer D; Larreta Garde V
[Ad] Endereço:ERRMECe Laboratory, University of Cergy-Pontoise, France; Biology Department/ERRMECe, University of Cergy-Pontoise, France.
[Ti] Título:Ephemeral biogels to control anti-biofilm agent delivery: From conception to the construction of an active dressing.
[So] Source:Mater Sci Eng C Mater Biol Appl;82:210-216, 2018 Jan 01.
[Is] ISSN:1873-0191
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Chronic wound colonization by bacterial biofilms is common and can cause various complications. An anti-biofilm strategy was developed around the co-entrapment of a commercially available antiseptic, PHMB (polyhexamethylene biguanide 4mgmL ), with EDTA (Ethylen diamine tetra acetic acid, 20mM) in a gelatin gel. The two active compounds act synergistically against bacterial biofilms, but their efficiency is strongly reduced (16-fold) when entrapped inside the 5% gelatin gel, and they weaken the mechanical properties (50-fold) of the gel. Increasing the gelatin concentration to 7% allows for good mechanical properties but large diffusional constraints. An active ephemeral gel, a chemical gel with controlled hydrolysis, was conceived and developed. When the ephemeral gel was solubilized after 48h, PHMB delivery increased, leading to good anti-biofilm activity. The various gels were examined over 24 and 48h of contact with P. aeruginosa and S. aureus biofilms, two types of bacterial biofilms frequently encountered in chronic wounds. The ephemeral gel eradicated the dense biofilms (>6.10 CFU·cm ) produced by either single or mixed strains; a similar efficiency was measured for biofilms from strains of both laboratory and clinical origin. The formulation was then adapted to develop a dressing prototype that is active against biofilms and fulfils the requirements of an efficient wound care system.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Biguanidas/química
Biofilmes/efeitos dos fármacos
Ácido Edético/química
Géis/química
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Bandagens
Biguanidas/farmacologia
Ácido Edético/farmacologia
Gelatina/química
Pseudomonas aeruginosa/fisiologia
Reologia
Staphylococcus aureus/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Biguanides); 0 (Gels); 322U039GMF (polihexanide); 9000-70-8 (Gelatin); 9G34HU7RV0 (Edetic Acid)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180205
[Lr] Data última revisão:
180205
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171014
[St] Status:MEDLINE


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[PMID]:28456998
[Au] Autor:Shafiei-Irannejad V; Samadi N; Salehi R; Yousefi B; Zarghami N
[Ad] Endereço:Stem Cell Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
[Ti] Título:New insights into antidiabetic drugs: Possible applications in cancer treatment.
[So] Source:Chem Biol Drug Des;90(6):1056-1066, 2017 Dec.
[Is] ISSN:1747-0285
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Globally at 2014, it was estimated that there was 347 million people with diabetes in which 90 percent of them were diagnosed with type 2 diabetes mellitus (T2DM). Although the association between diabetes mellitus and cancer risk was found about 100 years ago, the issue is not still clear. Many studies especially cohort and case-control studies have suggested a higher risk of cancer in patients with diabetes mainly in those with type 2 diabetes. Insulin concentration is high in these patients, and due to its mitogenic effects, it may be a possible hypotheses for higher risk of cancer in diabetic patients. Therefore, antidiabetic drugs, which are involved in insulin secretion and sensitivity, may have beneficial effects in cancer treatment. Several groups of drugs with different mechanisms of action, mostly prescribed orally, are used for the treatment of type 2 diabetes mellitus including, insulin sensitizers (thiazolidinediones), insulin secretagogues (sulfonylureas), and biguanides. In this review, the possible effects of antidiabetic drugs (biguanides, thiazolidinediones, and sulfonylureas) and some of their mechanisms for overcoming cancer will be discussed.
[Mh] Termos MeSH primário: Hipoglicemiantes/uso terapêutico
Neoplasias/tratamento farmacológico
[Mh] Termos MeSH secundário: Biguanidas/farmacologia
Biguanidas/uso terapêutico
Proliferação Celular/efeitos dos fármacos
Diabetes Mellitus Tipo 2/tratamento farmacológico
Seres Humanos
Hipoglicemiantes/farmacologia
Metformina/uso terapêutico
Neoplasias/patologia
Proteínas Serina-Treonina Quinases/metabolismo
Compostos de Sulfonilureia/uso terapêutico
Tiazolidinedionas/farmacologia
Tiazolidinedionas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Biguanides); 0 (Hypoglycemic Agents); 0 (Sulfonylurea Compounds); 0 (Thiazolidinediones); 9100L32L2N (Metformin); EC 2.7.1.- (STK11 protein, human); EC 2.7.11.1 (Protein-Serine-Threonine Kinases)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180102
[Lr] Data última revisão:
180102
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170501
[St] Status:MEDLINE
[do] DOI:10.1111/cbdd.13013


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[PMID]:29068991
[Au] Autor:Chu WM; Ho HE; Huang KH; Tsan YT; Liou YS; Wang YH; Lee MC; Li YC
[Ad] Endereço:aInstitute of Medicine, Chung Shan Medical University, Taichung bDepartment of Family Medicine, Taichung Veterans General Hospital, Chiayi Branch, Chiayi cSchool of Medicine, National Yang-Ming University, Taipei dDepartment of Family Medicine, Taichung Armed Force General Hospital, Taichung eSchool of Medicine, National Defense Medical Center, Taipei fDepartment of Health Service Administration, College of Public Health, China Medical University gDivision of Occupational Medicine, Department of Emergency Medicine, Taichung Veterans General Hospital hSchool of Medicine, Chung Shan Medical University, Taichung iSchool of Public Health, National Defense Medical Center, Taipei jDepartment of Family Medicine, Taichung Veterans General Hospital kDepartment of Family Medicine, Taichung Hospital, Ministry of Health and Welfare, Taichung lInstitute of Population Sciences, National Health Research Institutes, Miaoli County mCollege of Management, Chao-Yung University of Technology nDepartment of Public Health, China Medical University, Taichung oDepartment of Family Medicine, Yuan Rung Hospital, Yuanlin, Changhwa, Taiwan.
[Ti] Título:The prescribing trend of oral antidiabetic agents for type 2 diabetes in Taiwan: An 8-year population-based study.
[So] Source:Medicine (Baltimore);96(43):e8257, 2017 Oct.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The purpose of this study was to evaluate the prescription trend and pattern of oral antidiabetic (OAD) medications, which are extensively used worldwide for treating type 2 diabetes, in 2 age groups.In this population-based study, data obtained from the National Health Insurance Research Database, Taiwan, were analyzed to investigate the prescription trend of all types of OAD medications during 2005 to 2012. We used descriptive statistics to demonstrate the trend of prescription patterns stratified by age (aged 65 years and above or younger than 65).Sulfonylurea (SU) was once the most commonly used drug, but the proportion of its prescription had declined gradually (76.83% in 2005 to 63.70% in 2012). Consequently, biguanide (BG) became the most commonly used drug since 2010 (64.31% in 2005 to 74.41% in 2012). In addition, the prescriptions of thiazolidinedione decreased significantly (9.20% in 2005 to 2.86% in 2012), whereas the usage of DPP-4 inhibitor increased with time (3.73% in 2009 to 19.64% in 2012). The treatment choice of SU and α-glucosidase inhibitor (AGI) was higher in elderly patients compared with the younger population (SU: 62.70% in 2012, AGI: 12.78% in 2012). Two-drug combination therapies were the prevalent treatment choices for patients with type 2 diabetes (44.77% in 2012), particularly in the elderly group; however, ≥3 drug combination therapies increased gradually during the study period, particularly in the younger group.This descriptive study presents the change in the prescription of OAD medication for different age groups during 2005 to 2012.
[Mh] Termos MeSH primário: Diabetes Mellitus Tipo 2/tratamento farmacológico
Hipoglicemiantes/uso terapêutico
Padrões de Prática Médica/estatística & dados numéricos
[Mh] Termos MeSH secundário: Administração Oral
Fatores Etários
Idoso
Biguanidas/uso terapêutico
Inibidores da Dipeptidil Peptidase IV/uso terapêutico
Quimioterapia Combinada
Inibidores de Glicosídeo Hidrolases/uso terapêutico
Seres Humanos
Meia-Idade
Compostos de Sulfonilureia/uso terapêutico
Taiwan
Tiazolidinedionas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY
[Nm] Nome de substância:
0 (Biguanides); 0 (Dipeptidyl-Peptidase IV Inhibitors); 0 (Glycoside Hydrolase Inhibitors); 0 (Hypoglycemic Agents); 0 (Sulfonylurea Compounds); 0 (Thiazolidinediones); AA68LXK93C (2,4-thiazolidinedione)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171123
[Lr] Data última revisão:
171123
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:171026
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000008257


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[PMID]:28919040
[Au] Autor:Guo Z; Sevrioukova IF; Denisov IG; Zhang X; Chiu TL; Thomas DG; Hanse EA; Cuellar RAD; Grinkova YV; Langenfeld VW; Swedien DS; Stamschror JD; Alvarez J; Luna F; Galván A; Bae YK; Wulfkuhle JD; Gallagher RI; Petricoin EF; Norris B; Flory CM; Schumacher RJ; O'Sullivan MG; Cao Q; Chu H; Lipscomb JD; Atkins WM; Gupta K; Kelekar A; Blair IA; Capdevila JH; Falck JR; Sligar SG; Poulos TL; Georg GI; Ambrose E; Potter DA
[Ad] Endereço:Department of Medicine Hematology, Oncology and Transplantation Division and Masonic Cancer Center, University of Minnesota, Minneapolis, MN, USA.
[Ti] Título:Heme Binding Biguanides Target Cytochrome P450-Dependent Cancer Cell Mitochondria.
[So] Source:Cell Chem Biol;24(10):1259-1275.e6, 2017 Oct 19.
[Is] ISSN:2451-9456
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The mechanisms by which cancer cell-intrinsic CYP monooxygenases promote tumor progression are largely unknown. CYP3A4 was unexpectedly associated with breast cancer mitochondria and synthesized arachidonic acid (AA)-derived epoxyeicosatrienoic acids (EETs), which promoted the electron transport chain/respiration and inhibited AMPKα. CYP3A4 knockdown activated AMPKα, promoted autophagy, and prevented mammary tumor formation. The diabetes drug metformin inhibited CYP3A4-mediated EET biosynthesis and depleted cancer cell-intrinsic EETs. Metformin bound to the active-site heme of CYP3A4 in a co-crystal structure, establishing CYP3A4 as a biguanide target. Structure-based design led to discovery of N1-hexyl-N5-benzyl-biguanide (HBB), which bound to the CYP3A4 heme with higher affinity than metformin. HBB potently and specifically inhibited CYP3A4 AA epoxygenase activity. HBB also inhibited growth of established ER mammary tumors and suppressed intratumoral mTOR. CYP3A4 AA epoxygenase inhibition by biguanides thus demonstrates convergence between eicosanoid activity in mitochondria and biguanide action in cancer, opening a new avenue for cancer drug discovery.
[Mh] Termos MeSH primário: Biguanidas/metabolismo
Biguanidas/farmacologia
Citocromo P-450 CYP3A/metabolismo
Heme/metabolismo
Mitocôndrias/efeitos dos fármacos
[Mh] Termos MeSH secundário: Proteínas Quinases Ativadas por AMP/metabolismo
Animais
Biguanidas/química
Neoplasias da Mama/patologia
Domínio Catalítico
Respiração Celular/efeitos dos fármacos
Citocromo P-450 CYP3A/química
Citocromo P-450 CYP3A/deficiência
Citocromo P-450 CYP3A/genética
Receptor alfa de Estrogênio/genética
Feminino
Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos
Inativação Gênica
Seres Humanos
Células MCF-7
Potencial da Membrana Mitocondrial/efeitos dos fármacos
Camundongos
Mitocôndrias/metabolismo
Mitocôndrias/patologia
Modelos Moleculares
Transporte Proteico/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biguanides); 0 (Estrogen Receptor alpha); 42VZT0U6YR (Heme); EC 1.14.14.1 (Cytochrome P-450 CYP3A); EC 2.7.11.31 (AMP-Activated Protein Kinases)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170919
[St] Status:MEDLINE


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[PMID]:28872986
[Au] Autor:Kapoor S; Manuja N; Chaudhary S; Kaur H; Tr C; Sinha AA
[Ti] Título:Effect of Qmix and Other Irrigants on Dentin Adhesives in Pulp Chambers of Primary Teeth: SEM Study.
[So] Source:J Clin Pediatr Dent;41(5):363-367, 2017.
[Is] ISSN:1053-4628
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To compare the effect of different endodontic irrigants on microleakage of adhesives used within pulp chamber of primary molars. STUDY DESIGN: 72 Primary molars were divided into 6 groups, according to 3 irrigants and 2 adhesives used. After de-roofing the pulp chamber, pulp was extirpated. In 36 samples, pulp chambers were bonded with Xeno V after irrigation with either QMix (Group1); 17%EDTA+5%NaOCl (Group2) or normal saline (Group3) and in other half samples, pulp chambers were bonded with SinglebondUniversal after irrigation with either QMix (Group 4); 17%EDTA+5% NaOCl (Group5) or normal saline (Group 6). All the samples were restored with Filtek Z350. Ten teeth from each group were assessed for dye penetration. Two samples in each group were viewed under scanning electron microscope. Data was statistically analyzed using Mann-Whitney and Kruskal Wallis tests at a significance level of P < 0.05. RESULTS: Mean microleakage scores were: Group 1-1.5±0.70, Group 2-1.6±.51, Group 3-2.4±0.96, Group 4-1.2±0.42, Group 5-1.2±0.42, Group 6-1.1±0.32. CONCLUSIONS: Irrigation with QMix significantly reduced the microleakage of XenoV but had no significant effect on microleakage of SinglebondUniversal. Irrigation with EDTA/NaOCl or QMix had no detrimental effect on the sealing ability of either of the adhesive tested.
[Mh] Termos MeSH primário: Infiltração Dentária/diagnóstico por imagem
Cavidade Pulpar/ultraestrutura
Microscopia Eletrônica de Varredura
Dente Molar/ultraestrutura
Irrigantes do Canal Radicular
[Mh] Termos MeSH secundário: Biguanidas
Cimentos Dentários
Seres Humanos
Polímeros
Dente Decíduo/ultraestrutura
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biguanides); 0 (Dental Cements); 0 (Polymers); 0 (QMix root canal irrigant); 0 (Root Canal Irrigants)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:D
[Da] Data de entrada para processamento:170906
[St] Status:MEDLINE
[do] DOI:10.17796/1053-4628-41.5.363


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[PMID]:28848174
[Au] Autor:Schunter JA; Stöcker B; Brehler R
[Ad] Endereço:Department of Dermatology, University Hospital Münster, Münster, Germany.
[Ti] Título:A Case of Severe Anaphylaxis to Polyhexanide: Cross-Reactivity between Biguanide Antiseptics.
[So] Source:Int Arch Allergy Immunol;173(4):233-236, 2017.
[Is] ISSN:1423-0097
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:We present the case of a 77-year-old female patient who suffered from severe anaphylaxis during wound care. Allergologic evaluation yielded specific IgE antibodies to chlorhexidine, but anaphylaxis to chlorhexidine was not congruent with the patient history and dermal provocation tests. However, skin prick tests provided evidence for a sensitization to polyhexanide that was further supported by the detection of specific IgE antibodies to polyhexanide, the results of basophil activation tests and IgE inhibition analysis. We presume cross-reactive IgE antibodies binding to both biguanide antiseptics and identified polyhexanide as the likely cause of the anaphylactic reaction. We recognize polyhexanide as an emerging allergen that has to be considered as a cause of anaphylaxis.
[Mh] Termos MeSH primário: Alérgenos/efeitos adversos
Anafilaxia/induzido quimicamente
Anti-Infecciosos Locais/imunologia
Biguanidas/efeitos adversos
Desinfetantes/efeitos adversos
Hipersensibilidade a Drogas/etiologia
[Mh] Termos MeSH secundário: Idoso
Alérgenos/imunologia
Anafilaxia/diagnóstico
Anafilaxia/imunologia
Biguanidas/imunologia
Reações Cruzadas
Desinfetantes/imunologia
Hipersensibilidade a Drogas/diagnóstico
Hipersensibilidade a Drogas/imunologia
Feminino
Seres Humanos
Imunoglobulina E/imunologia
Testes Cutâneos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Allergens); 0 (Anti-Infective Agents, Local); 0 (Biguanides); 0 (Disinfectants); 322U039GMF (polihexanide); 37341-29-0 (Immunoglobulin E)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171003
[Lr] Data última revisão:
171003
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170830
[St] Status:MEDLINE
[do] DOI:10.1159/000478700


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[PMID]:28814284
[Au] Autor:Ali S; Wilson APR
[Ad] Endereço:Clinical Microbiology and Virology, University College London Hospitals NHS Foundation Trust, London, UK. shanom.ali@uclh.nhs.uk.
[Ti] Título:Effect of poly-hexamethylene biguanide hydrochloride (PHMB) treated non-sterile medical gloves upon the transmission of Streptococcus pyogenes, carbapenem-resistant E. coli, MRSA and Klebsiella pneumoniae from contact surfaces.
[So] Source:BMC Infect Dis;17(1):574, 2017 Aug 17.
[Is] ISSN:1471-2334
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Reduction of accidental contamination of the near-patient environment has potential to reduce acquisition of healthcare-associated infection(s). Although medical gloves should be removed when soiled or touching the environment, compliance is variable. The use of antimicrobial-impregnated medical gloves could reduce the horizontal-transfer of bacterial contamination between surfaces. AIM: Determine the activity of antimicrobial-impregnated gloves against common hospital pathogens: Streptococcus pyogenes, carbapenem-resistant E.coli (CREC), MRSA and ESBL-producing Klebsiella pneumoniae. METHODS: Fingerpads (~1cm ) of PHMB-treated and untreated gloves were inoculated with 10 µL (~10 colony-forming-units [cfu]) of test-bacteria prepared in heavy-soiling (0.5%BSA), blood or distilled-water (no-soiling) and sampled after 0.25, 1, 10 or 15 min contact-time. Donor surfaces (~1cm computer-keys) contaminated with wet/dry inoculum were touched with the fingerpad of treated/untreated gloves and subsequently pressed onto recipient (uncontaminated) computer-keys. RESULTS: Approximately 4.50log cfu of all bacteria persisted after 15 min on untreated gloves regardless of soil-type. In the absence of soiling, PHMB-treated gloves reduced surface-contamination by ~4.5log cfu (>99.99%) within 10 min of contact-time but only ~2.5log (>99.9%) and ~1.0log reduction respectively when heavy-soiling or blood was present. Gloves became highly-contaminated (~4.52log -4.91log cfu) when handling recently-contaminated computer-keys. Untreated gloves contaminated "recipient" surfaces (~4.5log cfu) while PHMB-treated gloves transferred fewer bacteria (2.4-3.6log cfu). When surface contamination was dry, PHMB gloves transferred fewer bacteria (0.3-0.6log cfu) to "recipient" surfaces than untreated gloves (1.0-1.9log ; P < 0.05). CONCLUSIONS: Antimicrobial-impregnated gloves may be useful in preventing dissemination of organisms in the near-patient environment during routine care. However they are not a substitute for appropriate hand-hygiene procedures.
[Mh] Termos MeSH primário: Biguanidas/farmacologia
Infecção Hospitalar/prevenção & controle
Transmissão de Doença Infecciosa/prevenção & controle
Desinfetantes/farmacologia
Luvas Protetoras/microbiologia
[Mh] Termos MeSH secundário: Carbapenêmicos/farmacologia
Farmacorresistência Bacteriana
Escherichia coli/efeitos dos fármacos
Escherichia coli/patogenicidade
Seres Humanos
Controle de Infecções/métodos
Klebsiella pneumoniae/patogenicidade
Staphylococcus aureus Resistente à Meticilina/patogenicidade
Streptococcus pyogenes/patogenicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biguanides); 0 (Carbapenems); 0 (Disinfectants); 322U039GMF (polihexanide)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171101
[Lr] Data última revisão:
171101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170818
[St] Status:MEDLINE
[do] DOI:10.1186/s12879-017-2661-9


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[PMID]:28766937
[Au] Autor:Gabel SA; Duff MR; Pedersen LC; DeRose EF; Krahn JM; Howell EE; London RE
[Ad] Endereço:Genome Integrity and Structural Biology Laboratory, National Institute of Environmental Health Sciences, National Institutes of Health , 111 T. W. Alexander Drive, Research Triangle Park, North Carolina 27709, United States.
[Ti] Título:A Structural Basis for Biguanide Activity.
[So] Source:Biochemistry;56(36):4786-4798, 2017 Sep 12.
[Is] ISSN:1520-4995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Metformin is the most commonly prescribed treatment for type II diabetes and related disorders; however, molecular insights into its mode(s) of action have been limited by an absence of structural data. Structural considerations along with a growing body of literature demonstrating its effects on one-carbon metabolism suggest the possibility of folate mimicry and anti-folate activity. Motivated by the growing recognition that anti-diabetic biguanides may act directly upon the gut microbiome, we have determined structures of the complexes formed between the anti-diabetic biguanides (phenformin, buformin, and metformin) and Escherichia coli dihydrofolate reductase (ecDHFR) based on nuclear magnetic resonance, crystallographic, and molecular modeling studies. Interligand Overhauser effects indicate that metformin can form ternary complexes with p-aminobenzoyl-l-glutamate (pABG) as well as other ligands that occupy the region of the folate-binding site that interacts with pABG; however, DHFR inhibition is not cooperative. The biguanides competitively inhibit the activity of ecDHFR, with the phenformin inhibition constant being 100-fold lower than that of metformin. This inhibition may be significant at concentrations present in the gut of treated individuals, and inhibition of DHFR in intestinal mucosal cells may also occur if accumulation levels are sufficient. Perturbation of folate homeostasis can alter the pyridine nucleotide redox ratios that are important regulators of cellular metabolism.
[Mh] Termos MeSH primário: Biguanidas/química
Biguanidas/farmacologia
Hipoglicemiantes/química
Hipoglicemiantes/farmacologia
Tetra-Hidrofolato Desidrogenase/metabolismo
[Mh] Termos MeSH secundário: Sítios de Ligação
Cristalização
Escherichia coli/enzimologia
Escherichia coli/genética
Escherichia coli/metabolismo
Antagonistas do Ácido Fólico/química
Antagonistas do Ácido Fólico/farmacologia
Modelos Moleculares
Estrutura Molecular
Conformação Proteica
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biguanides); 0 (Folic Acid Antagonists); 0 (Hypoglycemic Agents); EC 1.5.1.3 (Tetrahydrofolate Dehydrogenase)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170803
[St] Status:MEDLINE
[do] DOI:10.1021/acs.biochem.7b00619



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