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[PMID]:29446579
[Au] Autor:Savchenkov MF; Efimova NV; Manueva RS; Nikolaeva LA; Shin NS
[Ti] Título:[Thyroid gland pathology in children population exposed to the combination of iodine deficiency and fluoride pollution of environment].
[So] Source:Gig Sanit;95(12):1201-5, 2016.
[Is] ISSN:0016-9900
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The article presents results of study of the impact of iodine deficiency and technogenic fluoride on the state of the thyroid gland in children. On the example of two districts of the city of Bratsk there were executed dynamic investigations (2002 and 2012), including the estimation of the pollution of ambient air and soil by fluorine compounds, levels of iodine intake by the body, the clinical examination of children aged from 5 to 7 years d and interviewing of their parents. In the course of the medical examination there were executed: physical examination by the pediatrician, endocrinologist, ultrasound examination of the thyroid gland, the determination both of serum hormone content by radioimmunoassay and urinary excretion offluorine and iodine. Concentrations of hydrogen fluoride and a solidfluorides in ambient air led to the accumulation offluoride ion in the soil. The iodine entering with drinking water and food, was established to provide only 37.5-50% of the daily requirement of iodine. Increased fluoride ion content in urine and milk teeth in children is associated with the concentrations of the fluorine-containing pollutants in the ambient air and soil. The fluoride pollution against the background of the natural iodine deficiency was established to increase the frequency of functional and morphological disorders of the thyroid gland in children.
[Mh] Termos MeSH primário: Poluição Ambiental
Iodo
Doenças da Glândula Tireoide
[Mh] Termos MeSH secundário: Criança
Monitoramento Ambiental/métodos
Poluição Ambiental/efeitos adversos
Poluição Ambiental/análise
Poluição Ambiental/prevenção & controle
Poluição Ambiental/estatística & dados numéricos
Feminino
Compostos de Flúor/efeitos adversos
Compostos de Flúor/análise
Disparidades nos Níveis de Saúde
Seres Humanos
Iodo/análise
Iodo/deficiência
Masculino
Saúde Pública/métodos
Saúde Pública/estatística & dados numéricos
Sibéria/epidemiologia
Doenças da Glândula Tireoide/diagnóstico
Doenças da Glândula Tireoide/epidemiologia
Doenças da Glândula Tireoide/etiologia
Doenças da Glândula Tireoide/prevenção & controle
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Fluorine Compounds); 9679TC07X4 (Iodine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180216
[St] Status:MEDLINE


  2 / 16582 MEDLINE  
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[PMID]:28460444
[Au] Autor:Kim H; Jang EJ; Kyum Kim S; Jin Hyung W; Kyu Choi D; Lim SJ; Seok Lim J
[Ad] Endereço:Department of Radiology, Yonsei University College of Medicine, Seoul, Republic of Korea.
[Ti] Título:Simultaneous sentinel lymph node computed tomography and locoregional chemotherapy for lymph node metastasis in rabbit using an iodine-docetaxel emulsion.
[So] Source:Oncotarget;8(16):27177-27188, 2017 Apr 18.
[Is] ISSN:1949-2553
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: A sentinel lymph node (SLN) tracer can gain multi-functionality by combining it with additional components. We developed a SLN tracer consisting of iodine and docetaxel and applied it as a theragnostic nanoparticle to simultaneously perform SLN computed tomography (CT) lymphography and locoregional chemotherapy of the draining lymphatic system. RESULTS: Docetaxel could be loaded in iodine emulsions at a drug-to-surfactant weight ratio as high as that in the drug formulation Taxotere®. The particle size and drug concentration were stable during storage for up to 3 months in optimized nanoemulsions. Popliteal LN enhancement on CT was observed in all healthy rabbits (n=3) and VX2 tumor-implanted rabbits (n=6) 12 hours after injection. The rate of SLN metastasis was significantly lower in the treatment group (29.4%, 5/17) than in the non-treatment group (70.6%, 12/17) (P=0.038). MATERIAL AND METHODS: We prepared a nanoemulsion carrying both iodine and docetaxel in a single structure by optimizing the composition of surfactants surrounding the inner iodized oil core. CT was performed 12 hours after subcutaneous injection of the emulsion in healthy rabbits (n=3) and VX2 tumor-implanted rabbits (n=6) for SLN imaging. Next, we tested the effect of treatment by histopathologically assessing the popliteal LN metastasis rate in VX2 tumor-implanted rabbits 7 days after subcutaneous injection of the emulsion (treatment group, n=17) and comparing it with that of non-treatment group rabbits (n=17). CONCLUSIONS: We developed an iodine-docetaxel emulsion and demonstrated that it can be applied to simultaneously achieve CT SLN imaging and local chemotherapy against nodal metastasis.
[Mh] Termos MeSH primário: Emulsões
Iodo
Neoplasias/diagnóstico por imagem
Neoplasias/patologia
Linfonodo Sentinela/diagnóstico por imagem
Linfonodo Sentinela/patologia
Taxoides/administração & dosagem
Tomografia Computadorizada por Raios X
[Mh] Termos MeSH secundário: Animais
Modelos Animais de Doenças
Estabilidade de Medicamentos
Emulsões/química
Iodo/química
Metástase Linfática
Masculino
Estadiamento de Neoplasias
Neoplasias/tratamento farmacológico
Tamanho da Partícula
Coelhos
Tomografia Computadorizada por Raios X/métodos
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Emulsions); 0 (Taxoids); 15H5577CQD (docetaxel); 9679TC07X4 (Iodine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.18632/oncotarget.15679


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[PMID]:29424208
[Au] Autor:Tapeshkina NV; Perevalov AY
[Ti] Título:[Assessment of the efficiency of prevention of iodine deficiency among the children's population of the city of Mezhdurechensk of the Kemerovo region].
[So] Source:Gig Sanit;95(5):471-6, 2016.
[Is] ISSN:0016-9900
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:In the article there are presented results of a study of indices of ioduria in preschool kids and school children of the city of Mezhdurechensk (south of the Kemerovo region). 411 children aged of 3-17 years participated in the study. The median of ioduria on preschooler kids was 97,0 pg/l, and the proportion of urine samples with iodine levels less than 50 pg/l - 1,0%. The median of ioduria in school children is 98,0 pg/l, the percentage of urine samples with iodine levels less than 50 pg/l accounts for 1,3%. On average, on the population of children there was established that the percentage of urine samples with iodine levels from 50-100 pg/l (mild deficiency) was detected in 53,5% of children. Comparative analysis of indices of the level of ioduria according to data obtained in 2008 and 2014 in a group of school children showed that the measures taken to prevent diseases caused by iodine deficiency (the use of iodized salt in the diet of children and adolescents from organized groups on a regular basis) have given positive results.
[Mh] Termos MeSH primário: Iodo
Doenças da Glândula Tireoide
[Mh] Termos MeSH secundário: Adolescente
Criança
Pré-Escolar
Feminino
Indicadores Básicos de Saúde
Seres Humanos
Iodo/deficiência
Iodo/farmacologia
Iodo/urina
Masculino
Necessidades Nutricionais
População
Serviços de Saúde Escolar/organização & administração
Serviços de Saúde Escolar/estatística & dados numéricos
Sibéria/epidemiologia
Cloreto de Sódio na Dieta/farmacologia
Doenças da Glândula Tireoide/epidemiologia
Doenças da Glândula Tireoide/etiologia
Doenças da Glândula Tireoide/prevenção & controle
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Sodium Chloride, Dietary); 0 (iodized salt); 9679TC07X4 (Iodine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180210
[St] Status:MEDLINE


  4 / 16582 MEDLINE  
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[PMID]:29412546
[Au] Autor:Kolomiets ND; Mokhort TV; Fedorenko EV; Mokhort EG; Petrenko SV
[Ti] Título:[The problem of iodine deficiency and its solution in the republic of Belarus].
[So] Source:Gig Sanit;95(5):417-21, 2016.
[Is] ISSN:0016-9900
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The problem of iodine deficiency is relevant to the Republic of Belarus. It's confirmed by virtually commonly found geophysical iodine deficiency in soils and waters. Data on iodine deficiency initiated the development of a state strategy for the elimination of iodine deficiency in the population. This strategy determined the mandatory use of iodized salt only in the country in the food industry and catering as the main event for the elimination of iodine deficiency. The aim of this work was a comprehensive evaluation of the results of the implementation of the strategy for elimination of iodine deficiency among the population of the Republic of Belarus. Medical monitoring of the assessment of the efficacy showed the decrease in the incidence of simple non-toxic goiter in adolescents from 1215,23 per 100,000 population in 1998 to 341,25 in 2013 (3.6 times), and indices ofprimary morbidity rate in children fell by 2.9 times. Over the period from 1998 primary morbidity rate of simple nontoxic goiter decreased significantly in adults from 379.9 to 31,71 people per 100,000 of the population in 2013 respectively (almost 12 times). Data of the assessment of ioduria in Belarus indicate that 89.2% of children enrolled in the study have iodine excretion of more than 100 pg/L. Thus, in the Republic of Belarus there was achieved the level of an adequate intake of iodine with foodstuffs. This model ofprevention of iodine deficiency, as well as the traditional approach based on the adoption of the law, is a versatile and cost-effective mode.
[Mh] Termos MeSH primário: Deficiências Nutricionais
Iodo/farmacologia
Cloreto de Sódio na Dieta/farmacologia
[Mh] Termos MeSH secundário: Adolescente
Adulto
Criança
Deficiências Nutricionais/epidemiologia
Deficiências Nutricionais/etiologia
Deficiências Nutricionais/prevenção & controle
Feminino
Seres Humanos
Iodo/análise
Iodo/deficiência
Masculino
Prevalência
Serviços Preventivos de Saúde/métodos
Serviços Preventivos de Saúde/organização & administração
República da Bielorrússia/epidemiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Sodium Chloride, Dietary); 0 (iodized salt); 9679TC07X4 (Iodine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180208
[St] Status:MEDLINE


  5 / 16582 MEDLINE  
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[PMID]:29381025
[Au] Autor:Bogatyrev AN; Dydykin AS; Asianova MA; Fedulova LV; Ustinova AV
[Ti] Título:[Assessment of the using effectiveness of iodine containing additives in development of meat products for child nutrition].
[So] Source:Vopr Pitan;85(4):68-75, 2016.
[Is] ISSN:0042-8833
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The effectiveness of iodine containing additives on the basis of whey protein and milk protein casein compared to iodized salt in the composition of meat minced semi-finished products for child nutrition was examined in the experiment on laboratory animals. Four variants of the semi-finished products were investigated: 1 - control; 2 - enriched with iodine containing milk protein casein; 3 - enriched with iodine containing whey proteins; 4 - enriched with iodized salt. The semi-finished products were enriched at the level of 15% of the daily norm of iodine requirement for children at the age of 7-12 years. Iodine content in 100 g of product was 20 µkg. Rats (initial body weight 140±20 g, n=80) were divided into five groups (control, intact and three experimental groups). Groups 1 and 5 included the animals fed with a standard vivarium diet throughout the experiment. The rats from groups 2-4 were fed with the iodine enriched diet: group 2 received diet containing semi-finished products No. 2; group 3 sample No. 3 and group 4 - sample No. 4. The first stage of the experiment was aimed at accumulation of iodine in tissues and organs of animals consumed the tested iodine containing additives in the composition of semi-finished products. The second stage of the experiment consisted in simulation of the mercazolilum-induced (50 mg/kg b.w.) hypothyroidism (iodine deficiency) and detection of preventive effects of iodine containing meat semi-finished products in a model of experimental hypothyroidism in rats. The data obtained upon the end of the experiment suggest that the highest effect for correction of iodine deficiency was achieved when using the culinary products enriched with iodine containing whey proteins (sample No. 3): the level of thyroxine (T4) was restored by 98.7% in the animals from group 3 compared to the indices of the intact group, Т3 by 100%, TSH - by 89.3%. This effect was confirmed by the hematological and biochemical blood indexes, as well as the dynamics of their weight change: the level of white blood cells was significantly lower by 28%, granulocytes by 44%, monocytes by 42% compared to control rats; the weight gain of the animals of the 3 group was 20.3%, closer to that of intact animals - 26.4%, while in the control group it was 2.6 %.
[Mh] Termos MeSH primário: Culinária
Aditivos Alimentares/farmacologia
Hipotireoidismo/sangue
Hipotireoidismo/dietoterapia
Iodo/farmacologia
Produtos da Carne
[Mh] Termos MeSH secundário: Animais
Hipotireoidismo/induzido quimicamente
Masculino
Metimazol/efeitos adversos
Metimazol/farmacologia
Ratos
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Food Additives); 554Z48XN5E (Methimazole); 9679TC07X4 (Iodine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180131
[St] Status:MEDLINE


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[PMID]:29172409
[Au] Autor:Tigabu E; Bekele KB; Dachew BA
[Ad] Endereço:Ethiopian Paediatric Association, Amhara Region, Bahir Dar, Ethiopia.
[Ti] Título:Prevalence of goiter and associated factors among schoolchildren in northeast Ethiopia.
[So] Source:Epidemiol Health;39:e2017055, 2017.
[Is] ISSN:2092-7193
[Cp] País de publicação:Korea (South)
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: Goiter is a major public health problem, especially in developing countries such as Ethiopia. Hence, this study aimed to assess the prevalence and associated factors of goiter among children in Waghimra Zone, northeast Ethiopia. METHODS: A cross-sectional study was conducted from April 8 to 25, 2015 in northeast Ethiopia. A multistage sampling method was used to select 454 schoolchildren. Data were collected using a pre-tested structured interviewer-administered questionnaire. Children were examined for the presence or absence of goiter based on the criteria of the United Nations Children's Fund, International Council for the Control of Iodine Deficiency, and the World Health Organization. Salt samples from children's homes were tested for iodine levels using a rapid iodized salt test kit. Data were entered into EpiInfo version 7 and exported to SPSS version 20 for analysis. Bivariate and multivariate logistic regression models were fitted, and adjusted odds ratio (aOR) with 95% confidence interval (CI) were computed to determine the level of significance. RESULTS: The prevalence of goiter was 62.1% (95% CI, 57.5 to 66.5%). Being female (aOR, 3.09; 95% CI, 1.57 to 6.08), having a family history of goiter (aOR, 5.18; 95% CI, 2.43 to 11.03), and using non-iodized salt (aOR, 2.20; 95% CI, 1.12 to 4.38) were factors associated with goiter among schoolchildren. CONCLUSIONS: The prevalence of goiter was high. Being female and having a family history of goiter increased the risk of goiter in children, but using iodized salt was protective. Therefore, we recommend ensuring universal access to iodized salt and increasing the awareness of the community of the importance of iodized salt utilization.
[Mh] Termos MeSH primário: Bócio/epidemiologia
[Mh] Termos MeSH secundário: Criança
Estudos Transversais
Etiópia/epidemiologia
Feminino
Seres Humanos
Iodo/administração & dosagem
Masculino
Anamnese
Prevalência
Fatores de Risco
Distribuição por Sexo
Cloreto de Sódio na Dieta/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Sodium Chloride, Dietary); 0 (iodized salt); 9679TC07X4 (Iodine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180213
[Lr] Data última revisão:
180213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE
[do] DOI:10.4178/epih.e2017055


  7 / 16582 MEDLINE  
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[PMID]:29277821
[Au] Autor:Mirka H; Baxa J; Hora M; Hes O; Topolcan O; Ferda J
[Ad] Endereço:Department of Imaging Methods, Medical School and Teaching Hospital Pilsen, Charles University in Prague, Pilsen, Czech Republic mirka@fnplzen.cz.
[Ti] Título:Iodine Content Analysis Using Dual-Energy Computed Tomography as a Biomarker of Transitional Cell Carcinoma, an Experience with Separation of the Clotted Blood and Tumorous Tissue.
[So] Source:Anticancer Res;38(1):541-545, 2018 01.
[Is] ISSN:1791-7530
[Cp] País de publicação:Greece
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIM: The aim of this study was to evaluate the possibility to discriminate the blood clot from tumorous tissue in the assessment of transitional cell carcinoma (TCC), when CT data are used only from single-phase dual-energy CT (DECT). MATERIALS AND METHODS: A total of 18 patients were included into the retrospective analysis of the prospectively collected data (the average age was 67.3 years, range=62-79 years, 12 males, 6 females). DECT was performed in all patients after intravenous administration of the iodinated contrast material. DECT analysis using three-material decomposition algorithm was used to discriminate blood and enhancing tumorous tissue. In all patients, TCC was detected and subsequently kidney surgery or endoscopy was performed within the next two weeks. The findings were compared with DECT results. RESULTS: In our cohort of patients we found 9 TCC of the renal pelvis or ureter and 7 TCC of the urinary bladder. The accuracy of the TCC detection was 94% (17/18). The presence of coagulated blood within the urinary collecting system together with a tumor was detected in 7 CT examinations. The blood coagulum without a confirmed malignant tumor was found in one case with false positive DECT finding. In other 6 cases bleeding was confirmed during surgery or endoscopy (accuracy 87%). CONCLUSION: The dual-energy data analysis enables discrimination of a blood clot from tumorous tissue. It helps in detection of UCC in cases when the excretion potential of the kidneys is decreased due to fulfillment of the collecting system with blood clots.
[Mh] Termos MeSH primário: Carcinoma de Células de Transição/diagnóstico por imagem
Carcinoma de Células de Transição/diagnóstico
Iodo/análise
Trombose/diagnóstico
Tomografia Computadorizada por Raios X/métodos
[Mh] Termos MeSH secundário: Idoso
Algoritmos
Biomarcadores Tumorais/análise
Carcinoma de Células de Transição/patologia
Meios de Contraste
Feminino
Seres Humanos
Rim/patologia
Rim/cirurgia
Masculino
Meia-Idade
Estudos Retrospectivos
Bexiga Urinária/patologia
Bexiga Urinária/cirurgia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers, Tumor); 0 (Contrast Media); 9679TC07X4 (Iodine)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180104
[Lr] Data última revisão:
180104
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171227
[St] Status:MEDLINE


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[PMID]:28448423
[Au] Autor:Nair JR; DeBlois F; Ong T; Devic S; Tomic N; Bekerat H; Rosenbloom L; Sultanem K; Forghani R
[Ad] Endereço:From the *Department of Radiology, †Division of Radiation Oncology and Medical Physics, ‡Segal Cancer Centre, §Lady Davis Institute for Medical Research, and ∥Department of Oncology, Division of Radiation Oncology, Jewish General Hospital, McGill University, Montreal, Quebec, Canada H3T 1E2.
[Ti] Título:Dual-Energy CT: Balance Between Iodine Attenuation and Artifact Reduction for the Evaluation of Head and Neck Cancer.
[So] Source:J Comput Assist Tomogr;41(6):931-936, 2017 Nov/Dec.
[Is] ISSN:1532-3145
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: Dual-energy computed tomography high energy virtual monochromatic images (VMIs) can reduce artifact but suppress iodine attenuation in enhancing tumor. We investigated this trade-off to identify VMI(s) that strike the best balance between iodine detection and artifact reduction. METHODS: The study was performed using an Alderson radiation therapy phantom. Different iodine solutions (based on estimated tumor iodine content in situ using dual-energy computed tomography material decomposition) and different dental fillings were investigated. Spectral attenuation curves and quality index (QI: 1/SD) were evaluated. RESULTS: The relationship between iodine attenuation and QI depends on artifact severity and iodine concentration. For low to average concentration solutions degraded by mild to moderate artifact, the iodine attenuation and QI curves crossed at 95 keV. CONCLUSIONS: High energy VMIs less than 100 keV can achieve modest artifact reduction while preserving sufficient iodine attenuation and could represent a useful additional reconstruction for evaluation of head and neck cancer.
[Mh] Termos MeSH primário: Artefatos
Neoplasias de Cabeça e Pescoço/diagnóstico por imagem
Imagem Radiográfica a Partir de Emissão de Duplo Fóton
Tomografia Computadorizada por Raios X/métodos
[Mh] Termos MeSH secundário: Seres Humanos
Iodo
Estudos Retrospectivos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
9679TC07X4 (Iodine)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171211
[Lr] Data última revisão:
171211
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170428
[St] Status:MEDLINE
[do] DOI:10.1097/RCT.0000000000000617


  9 / 16582 MEDLINE  
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[PMID]:28873603
[Au] Autor:Stevenson MC; Drake C; Givens DI
[Ad] Endereço:Institute for Food, Nutrition and Health, University of Reading, Earley Gate, Reading RG6 6AR, UK. Electronic address: millyclarestevenson@hotmail.com.
[Ti] Título:Further studies on the iodine concentration of conventional, organic and UHT semi-skimmed milk at retail in the UK.
[So] Source:Food Chem;239:551-555, 2018 Jan 15.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Milk is the largest source of iodine in UK diets and earlier studies showed organic summer and winter milk to be significantly lower in iodine than conventional milk. One study also showed UHT milk to have lower iodine concentration. The study on winter and UHT milk was small and accordingly a new study is reported here involving conventional, organic and UHT semi-skimmed milk from four supermarkets over a six-month period in summer and winter in two regions of the UK. The results showed organic milk to be 44% lower in iodine than conventional milk (427 vs. 241µg/L, P<0.001) and UHT milk was 27% lower in iodine than conventional milk (427 vs. 314µg/L, P<0.001) although the differences tended to be less in the summer. The results indicate that replacement of conventional milk by organic or UHT milk will increase the risk of sub-optimal iodine status especially for pregnant/lactating women.
[Mh] Termos MeSH primário: Leite
[Mh] Termos MeSH secundário: Animais
Feminino
Seres Humanos
Iodo
Lactação
Gravidez
Estações do Ano
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
9679TC07X4 (Iodine)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171128
[Lr] Data última revisão:
171128
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170907
[St] Status:MEDLINE


  10 / 16582 MEDLINE  
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[PMID]:28462836
[Au] Autor:Muralidharan VP; Alagumuthu M; Iyer SK
[Ad] Endereço:Department of Chemistry, School of Advanced Sciences, VIT University, Vellore 632014, India.
[Ti] Título:Iodine catalyzed three component synthesis of 1-((2-hydroxy naphthalen-1-yl)(phenyl)(methyl))pyrrolidin-2-one derivatives: Rationale as potent PI3K inhibitors and anticancer agents.
[So] Source:Bioorg Med Chem Lett;27(11):2510-2514, 2017 06 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of 1-((2-hydroxynaphthalen-1-yl)(phenyl)(methyl))pyrrolidin-2-one derivatives by an efficient iodine catalyzed domino reaction involving various aromatic aldehydes, 2-pyrrolidinone and ß-naphthol was achieved and the structures were elucidated by FTIR H NMR, C NMR, and HRMS. Subsequently they were evaluated for cytotoxicity against breast cancer (MCF-7), colon cancer (HCT116) cell lines. In the cytotoxicity, the relative inhibition activity was remarkably found to be high in MCF-7 cell lines as 79% (4c), 83% (4f) and the IC values were 1.03µM (4c), 0.98µM (4f). Compounds 4a, 4e, 4k-m, and 4q were found to be inactive and rest showed a moderate activity. In order to get more insight into the binding mode and inhibitor binding affinity, compounds (4a-q) were docked into the active site phosphoinositide 3-kinase (PI3K) (PDB ID: 4JPS) which is a crucial regulator of apoptosis or programmed cell death. Results suggested that the hydrophobic interactions in the binding pockets of PI3K exploited affinity of the most favourable binding ligands (4c and 4f: inhibitory constant (ki)=66.22nM and 107.39nM). The SAR studies demonstrated that the most potent compounds are 4c and 4f and can be developed into precise PI3K inhibitors with the capability to treat various cancers.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Iodo/química
Fosfatidilinositol 3-Quinases/antagonistas & inibidores
Pirrolidinonas/química
[Mh] Termos MeSH secundário: Antineoplásicos/química
Antineoplásicos/toxicidade
Apoptose/efeitos dos fármacos
Sítios de Ligação
Catálise
Desenho de Drogas
Células HCT116
Seres Humanos
Células MCF-7
Simulação de Acoplamento Molecular
Fosfatidilinositol 3-Quinases/metabolismo
Pirrolidinonas/síntese química
Pirrolidinonas/toxicidade
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Pyrrolidinones); 9679TC07X4 (Iodine); EC 2.7.1.- (Phosphatidylinositol 3-Kinases); KKL5D39EOL (2-pyrrolidone)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE



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