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1.
Indian J Cancer ; 2022 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-36861697

RESUMO

Background: : Breast cancer is the most common cancer diagnosed in women worldwide. Social media channels are a significant source of health information including breast cancer. YouTube has a broad range of educational materials on various health issues in many languages. However, the accuracy of these videos is contentious. This study aimed to examine the accuracy of the most viewed Hindi videos on YouTube related to breast cancer. Methods: : On YouTube, the "Breast Cancer-Hindi" term was searched for the 50 most viewed Hindi videos. To evaluate the videos' quality and reliability, global quality scores (GQS) and DISCERN (quality criteria for the assessment of written health information), and for credibility and usefulness Journal of the American Medical Association (JAMA) tool were used. Popularity was measured using a video power index (VPI). Comparisons of scores were made between professionals' and consumers' videos. Two health researchers independently rated the videos and their correlation was calculated for agreement. Results: : Of all the 50 videos viewed, 23 (46%) each were uploaded by consumers and professionals. GQS median 3 (1-5), DISCERN median 13 (5-23), JAMA median 2 (0.50-4), and VPI median 90.7 (50-96.93) were reported. All scores of professionals were higher than consumers at a significant level (P < 0.05). A significant correlation was found between both observers (P < 0.01). Conclusion: : YouTube has some good quality and reliable videos on breast cancer in the Hindi language. These videos are mostly of professionals in comparison with consumers with wide viewership. However, they are limited in numbers; therefore, health professionals should upload more videos with accurate information to spread awareness about breast cancer.

2.
Indian J Community Med ; 46(3): 411-415, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34759477

RESUMO

BACKGROUND: Breast cancer is the major concern worldwide and in India too. Lack of awareness is one of the causes of increasing mortality rate in India. Social media is playing an important role in health communication including breast cancer information. In India, number of women are using social media. OBJECTIVE: To explore the impact of social media usage and engagement in enhancing knowledge and practices to prevent breast cancer among women of India. METHODOLOGY: A cross-sectional study was conducted in Delhi-National Capital Region of India with a sample of 649 women (response rate 83.51%). The questionnaire consisted of three sections. In first section, sociodemographic details (four items) were collected, second section contained five items on social media use and engagement and third part included items on knowledge about risk factors (seven items), symptoms (eight items), and screening (six items) of breast cancer and practice (seven items). Descriptive statistics, Chi-square, Cramer-V test, and structural equation modeling-Analysis of a moment structure were used to identify the relationship between social media engagement and knowledge and practices of women. RESULTS: Around 80% (431/542) of women have medium level of social media engagement and 20% are highly engaged. The slope coefficient of the relationship between social media engagement and knowledge is 0.805 and between knowledge and practice is 0.309, Chi-square value is 52.053 and 29.624, Cramer-V statistics is 0.310 and 0.165, respectively, which indicates significant relationship. CONCLUSION: The study result justified significant impact of social media engagement on knowledge and practices of women to prevent breast cancer.

3.
Stem Cell Rev Rep ; 17(3): 777-784, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33140233

RESUMO

Maintenance of metaphase-II (M-II) arrest in ovum is required to present itself as a right gamete for successful fertilization in mammals. Surprisingly, instability of meiotic cell cycle results in spontaneous exit from M-II arrest, chromosomal scattering and incomplete extrusion of second polar body (PB-II) without forming pronuclei so called abortive spontaneous ovum activation (SOA). It remains unclear what causes meiotic instability in freshly ovulated ovum that results in abortive SOA. We propose the involvement of various signal molecules such as reactive oxygen species (ROS), cyclic 3',5' adenosine monophosphate (cAMP) and calcium (Ca2+) in the induction of meiotic instability and thereby abortive SOA. These signal molecules through their downstream pathways modulate phosphorylation status and activity of cyclin dependent kinase (cdk1) as well as cyclin B1 level. Changes in phosphorylation status of cdk1 and its activity, dissociation and degradation of cyclin B1 destabilize maturation promoting factor (MPF). The premature MPF destabilization and defects in other cell cycle regulators possibly cause meiotic instability in ovum soon after ovulation. The meiotic instability results in a pathological condition of abortive SOA and deteriorates ovum quality. These ova are unfit for fertilization and limit reproductive outcome in several mammalian species including human. Therefore, global attention is required to identify the underlying causes in greater details in order to address the problem of meiotic instability in ova of several mammalian species icluding human. Moreover, these activated ova may be used to create parthenogenetic embryonic stem cell lines in vitro for the use in regenerative medicine.Graphical abstract.


Assuntos
Fator Promotor de Maturação , Oócitos , Animais , Cálcio/metabolismo , Feminino , Humanos , Mamíferos/metabolismo , Fator Promotor de Maturação/metabolismo , Fosforilação
4.
Eur J Pharmacol ; 883: 173293, 2020 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-32663542

RESUMO

Cyclic nucleotide phosphodiesterases (PDEs) are group of enzymes responsible for the hydrolysis of cyclic adenosine 3', 5' monophosphate (cAMP) and cyclic guanosine 3', 5' monophosphate (cGMP) levels in wide variety of cell types. These PDEs are detected in encircling granulosa cells or in oocyte with in follicular microenvironment and responsible for the decrease of cAMP and cGMP levels in mammalian oocytes. A transient decrease of cAMP level initiates downstream pathways to cause spontaneous meiotic resumption from diplotene arrest and induces oocyte maturation. The nonspecific PDE inhibitors (caffeine, pentoxifylline, theophylline, IBMX etc.) as well as specific PDE inhibitors (cilostamide, milrinone, org 9935, cilostazol etc.) have been used to elevate cAMP level and inhibit meiotic resumption from diplotene arrest and oocyte maturation, ovulation, fertilization and pregnancy rates both in vivo as well as under in vitro culture conditions. The PDEs inhibitors are used as powerful experimental tools to demonstrate cyclic nucleotide mediated changes in ovarian functions and thereby fertility. Indeed, non-hormonal nature and reversible effects of nonspecific as well as specific PDE inhibitors hold promise for the development of novel therapeutic drugs for female fertility regulation.


Assuntos
Fármacos para a Fertilidade Feminina/uso terapêutico , Fertilidade/efeitos dos fármacos , Infertilidade Feminina/tratamento farmacológico , Oócitos/efeitos dos fármacos , Ovário/efeitos dos fármacos , Inibidores de Fosfodiesterase/uso terapêutico , Animais , Feminino , Humanos , Infertilidade Feminina/enzimologia , Infertilidade Feminina/fisiopatologia , Oócitos/enzimologia , Ovário/enzimologia , Ovário/fisiopatologia , Ovulação/efeitos dos fármacos , Gravidez
5.
Arq. gastroenterol ; 56(4): 454-454, Oct.-Dec. 2019.
Artigo em Inglês | LILACS | ID: biblio-1055166
6.
J Cell Physiol ; 234(6): 8019-8027, 2019 06.
Artigo em Inglês | MEDLINE | ID: mdl-30341907

RESUMO

The maximum number of germ cells is present during the fetal life in mammals. Follicular atresia results in rapid depletion of germ cells from the cohort of the ovary. At the time of puberty, only a few hundred (<1%) germ cells are either culminated into oocytes or further get eliminated during the reproductive life. Although apoptosis plays a major role, necrosis as well as necroptosis, might also be involved in germ cell elimination from the mammalian ovary. Both necrosis and necroptosis show similar morphological features and are characterized by an increase in cell volume, cell membrane permeabilization, and rupture that lead to cellular demise. Necroptosis is initiated by tumor necrosis factor and operated through receptor interacting protein kinase as well as mixed lineage kinase domain-like protein. The acetylcholinesterase, cytokines, starvation, and oxidative stress play important roles in necroptosis-mediated granulosa cell death. The granulosa cell necroptosis directly or indirectly induces susceptibility toward necroptotic or apoptotic cell death in oocytes. Indeed, prevention of necrosis and necroptosis pathways using their specific inhibitors could enhance growth/differentiation factor-9 expression, improve survivability as well as the meiotic competency of oocytes, and prevent decline of reproductive potential in several mammalian species and early onset of menopause in women. This study updates the information and focuses on the possible involvement of necrosis and necroptosis in germ cell depletion from the mammalian ovary.


Assuntos
Necroptose/genética , Necrose/genética , Oócitos/crescimento & desenvolvimento , Ovário/crescimento & desenvolvimento , Animais , Apoptose/genética , Feminino , Células Germinativas/crescimento & desenvolvimento , Células Germinativas/metabolismo , Células da Granulosa/metabolismo , Humanos , Mamíferos , Oócitos/metabolismo , Ovário/metabolismo , Estresse Oxidativo/genética
7.
Growth Factors ; 36(1-2): 41-47, 2018 04.
Artigo em Inglês | MEDLINE | ID: mdl-29842809

RESUMO

In mammals, preovulatory oocytes are encircled by several layers of granulosa cells (GCs) in follicular microenvironment. These follicular oocytes are arrested at diplotene arrest due to high level of cyclic nucleotides from encircling GCs. Pituitary gonadotropin acts at the level of encircling GCs and increases adenosine 3',5'-cyclic monophosphate (cAMP) and guanosine 3',5'-cyclic monophosphate (cGMP) and activates mitogen-activated protein kinase 3/1 (MAPK3/1) signaling pathway. The MAPK3/1 disrupts the gap junctions between encircling GCs and oocyte. The disruption of gap junctions interrupts the transfer of cyclic nucleotides to the oocyte that results a drop in intraoocyte cAMP level. A transient decrease in oocyte cAMP level triggers maturation promoting factor (MPF) destabilization. The destabilized MPF finally triggers meiotic resumption from diplotene arrest in follicular oocyte. Thus, MAPK3/1 from GCs origin plays important role in gonadotropin-mediated meiotic resumption from diplotene arrest in follicular oocyte of mammals.


Assuntos
Células da Granulosa/enzimologia , Meiose/fisiologia , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Oócitos/fisiologia , Animais , Feminino , Gonadotropinas Hipofisárias/fisiologia , Nucleotídeos Cíclicos/metabolismo
8.
J Cell Physiol ; 233(8): 5530-5536, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29331044

RESUMO

In mammals, journey from metaphase-I (M-I) to metaphase-II (M-II) is important since oocyte extrude first polar body (PB-I) and gets converted into haploid gamete. The molecular and cellular changes associated with meiotic cell cycle progression from M-I to M-II stage and extrusion of PB-I remain ill understood. Several factors drive oocyte meiosis from M-I to M-II stage. The mitogen-activated protein kinase3/1 (MAPK3/1), signal molecules and Rho family GTPases act through various pathways to drive cell cycle progression from M-I to M-II stage. The down regulation of MOS/MEK/MAPK3/1 pathway results in the activation of anaphase-promoting complex/cyclosome (APC/C). The active APC/C destabilizes maturation promoting factor (MPF) and induces meiotic resumption. Several signal molecules such as, c-Jun N-terminal kinase (JNK2), SENP3, mitotic kinesin-like protein 2 (MKlp2), regulator of G-protein signaling (RGS2), Epsin2, polo-like kinase 1 (Plk1) are directly or indirectly involved in chromosomal segregation. Rho family GTPase is another enzyme that along with cell division cycle (Cdc42) to form actomyosin contractile ring required for chromosomal segregation. In the presence of origin recognition complex (ORC4), eccentrically localized haploid set of chromosomes trigger cortex differentiation and determine the division site for polar body formation. The actomyosin contractile activity at the site of division plane helps to form cytokinetic furrow that results in the formation and extrusion of PB-I. Indeed, oocyte journey from M-I to M-II stage is coordinated by several factors and pathways that enable oocyte to extrude PB-I. Quality of oocyte directly impact fertilization rate, early embryonic development, and reproductive outcome in mammals.


Assuntos
Mamíferos/fisiologia , Metáfase/fisiologia , Oócitos/fisiologia , Ciclossomo-Complexo Promotor de Anáfase/metabolismo , Animais , Ciclo Celular/fisiologia , Proteínas de Ciclo Celular/metabolismo , Segregação de Cromossomos/fisiologia , Cromossomos/fisiologia , GTP Fosfo-Hidrolases/metabolismo , Mamíferos/metabolismo , Fator Promotor de Maturação/metabolismo , Oócitos/metabolismo , Proteínas Serina-Treonina Quinases/metabolismo , Proteínas Proto-Oncogênicas/metabolismo , Transdução de Sinais/fisiologia , Quinase 1 Polo-Like
9.
Arch Pharm (Weinheim) ; 349(3): 193-201, 2016 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-26773437

RESUMO

A series of benzimidazole-based quinazoline derivatives with different substitutions of primary and secondary amines at the C2 position (1-12) were evaluated for their Aurora kinase inhibitory activities. All compounds except for 3 and 6 showed good activity against Aurora kinase inhibitors, with IC50 values in the range of 0.035-0.532 µM. The ligand efficiency (LE) of the compounds with Aurora A kinase was also determined. The structure-activity relationship and the quantitative structure-activity relationship revealed that the Aurora inhibitory activities of these derivatives primarily depend on the different substitutions of the amine present at the C2 position of the quinazoline core. Molecular docking studies in the active binding site also provided theoretical support for the experimental biological data acquired. The current study identifies a novel class of Aurora kinase inhibitors, which can further be used for the treatment of cancer.


Assuntos
Aurora Quinases/antagonistas & inibidores , Benzimidazóis/química , Quinazolinas/química , Aurora Quinase A/antagonistas & inibidores , Aurora Quinase A/química , Aurora Quinases/química , Benzimidazóis/síntese química , Simulação de Acoplamento Molecular , Relação Quantitativa Estrutura-Atividade , Quinazolinas/síntese química
10.
J Food Sci Technol ; 52(12): 7783-94, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26604351

RESUMO

In present study, influence of grinding (hammer and pin mills) and moisture content (range: 6.4-13.6 % dry basis) on the quality traits of coriander powder were investigated. These include grinding parameters, colour parameters, specific heat, thermal conductivity, thermal diffusivity, glass transition temperature, essential oil, total phenolic content, total flavonoid content and DPPH scavenging (%) of coriander powder. For coriander seed, the geometric properties such as major, medium, minor dimensions, geometric mean diameter, arithmetic mean diameter, sphericity, surface area and volume of coriander seeds increased significantly with increasing moisture (6.4-13.6 % db). For coriander powder, the grinding parameters such as average particle size, volume surface mean diameter and volume mean diameter increased significantly with increasing moisture (6.4-13.6 % db). With the grinding method, the colour attributes of coriander powder such as L-value, a-value, b-value, hue angle and browning index varied significantly. It was observed that the specific heat followed second order polynomial relationship with temperature and moisture whereas thermal conductivity varied linearly with temperature and moisture content. The variation of glass transition temperature with moisture can be best represented in quadratic manner. Total flavonoid content (mg QE/g crude seed extract) and DPPH scavenging % activity of coriander powder is significantly affected by grinding methods. A lower value of specific heat was observed for hammer ground coriander powder as compared to pin mill ground coriander powder. The thermal conductivity of hammer mill ground coriander powder was higher as compared to pin mill ground coriander. It was observed that hammer mill yields more fine coriander powder in comparison to pin mill. The browning index was more in hammer mill ground coriander powder.

11.
Indian J Med Res ; 142(2): 165-74, 2015 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-26354213

RESUMO

BACKGROUND & OBJECTIVES: Acute myocardial infarction (AMI) is characterized by irreparable and irreversible loss of cardiac myocytes. Despite major advances in the management of AMI, a large number of patients are left with reduced left ventricular ejection fraction (LVEF), which is a major determinant of short and long term morbidity and mortality. A review of 33 randomized control trials has shown varying improvement in left ventricular (LV) function in patients receiving stem cells compared to standard medical therapy. Most trials had small sample size and were underpowered. This phase III prospective, open labelled, randomized multicenteric trial was undertaken to evaluate the efficacy in improving the LVEF over a period of six months, after injecting a predefined dose of 5-10 × 10 [8] autologous mononuclear cells (MNC) by intra-coronary route, in patients, one to three weeks post ST elevation AMI, in addition to the standard medical therapy. METHODS: In this phase III prospective, multicentric trial 250 patients with AMI were included and randomized into stem cell therapy (SCT) and non SCT groups. All patients were followed up for six months. Patients with AMI having left ventricular ejection fraction (LVEF) of 20-50 per cent were included and were randomized to receive intracoronary stem cell infusion after successfully completing percutaneous coronary intervention (PCI). RESULTS: On intention-to-treat analysis the infusion of MNCs had no positive impact on LVEF improvement of ≥ 5 per cent. The improvement in LVEF after six months was 5.17 ± 8.90 per cent in non SCT group and 4.82 ± 10.32 per cent in SCT group. The adverse effects were comparable in both the groups. On post hoc analysis it was noted that the cell dose had a positive impact when infused in the dose of ≥ 5 X 10 [8] (n=71). This benefit was noted upto three weeks post AMI. There were 38 trial deviates in the SCT group which was a limitation of the study. INTERPRETATION & CONCLUSIONS: Infusion of stem cells was found to have no benefit in ST elevation AMI. However, the procedure was safe. A possible benefit was seen when the predefined cell dose was administered which was noted upto three weeks post AMI, but this was not significant and needs confirmation by larger trials.


Assuntos
Infarto do Miocárdio/terapia , Transplante de Células-Tronco , Células-Tronco/citologia , Disfunção Ventricular Esquerda/terapia , Idoso , Medula Óssea , Ecocardiografia , Feminino , Humanos , Índia , Masculino , Pessoa de Meia-Idade , Infarto do Miocárdio/patologia , Resultado do Tratamento , Disfunção Ventricular Esquerda/patologia
12.
Eur J Med Chem ; 93: 414-22, 2015 Mar 26.
Artigo em Inglês | MEDLINE | ID: mdl-25728022

RESUMO

In an effort to identify novel compounds for the treatment of cancer, a diverse array of potential bioactive hybrid, purine-benzimidazole was synthesized in good yields through nucleophilic substitution at C6 position of purine ring with versatile cyclic amines at C2 position. The structures of newly prepared compounds were confirmed by IR, (1)H, (13)C NMR, mass spectroscopy and, in case of 19, by single crystal X-ray diffraction analysis. The newly synthesized compounds were evaluated against 60 human tumour cell lines at one dose concentration level. Compound 6 exhibited significant growth inhibition and was evaluated as 60 cell panel at five dose concentration levels. Compound 6 proved to be 1.25 fold more active than the positive control 5-FU, with GI50 value of 18.12 µM (MG-MID). Interaction of the compounds with Aurora-A enzyme involved in the process of propagation of cancer, has also been investigated. Compound 6 showed selectivity towards Aurora-A kinase inhibition with IC50 value of 0.0l µM. Molecular docking studies in the active binding site provided theoretical support for the experimental biological data acquired.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Benzimidazóis/química , Benzimidazóis/farmacologia , Purinas/química , Antineoplásicos/síntese química , Antineoplásicos/metabolismo , Aurora Quinase A/antagonistas & inibidores , Aurora Quinase A/química , Aurora Quinase A/metabolismo , Benzimidazóis/síntese química , Benzimidazóis/metabolismo , Domínio Catalítico , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Técnicas de Química Sintética , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Simulação de Acoplamento Molecular , Relação Quantitativa Estrutura-Atividade
13.
Stroke ; 45(12): 3618-24, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25378424

RESUMO

BACKGROUND AND PURPOSE: Pilot studies have suggested benefit from intravenous administration of bone marrow mononuclear stem cells (BMSCs) in stroke. We explored the efficacy and safety of autologous BMSCs in subacute ischemic stroke. METHODS: This was a phase II, multicenter, parallel group, randomized trial with blinded outcome assessment that included 120 patients. Patients with subacute ischemic stroke were randomly assigned to the arm that received intravenous infusion of autologous BMSCs or to control arm. Coprimary clinical efficacy outcomes were Barthel Index score and modified Rankin scale at day 180. Secondary outcomes were change in infarct volume, National Institute of Health Stroke Scale (NIHSS) at day 90 and 180. Main safety outcomes were adverse events, any new area of (18)fluorodeoxyglucose positron emission tomography uptake in any body part over 365 days. RESULTS: Fifty-eight patients received a mean of 280.75 million BMSCs at median of 18.5 days after stroke onset. There was no significant difference between BMSCs arm and control arm in the Barthel Index score (63.1 versus 63.6; P=0.92), modified Rankin scale shift analysis (P=0.53) or score >3 (47.5% versus 49.2%; P=0.85), NIHSS score (6.3 versus 7.0; P=0.53), change in infarct volume (-11.1 versus -7.36; P=0.63) at day 180. Adverse events were also similar in the 2 arms, and no patient showed any new area of (18)fluorodeoxyglucose uptake. CONCLUSIONS: With the methods used, results of this hitherto first randomized controlled trial indicate that intravenous infusion of BMSCs is safe, but there is no beneficial effect of treatment on stroke outcome. CLINICAL TRIAL REGISTRATION: URLs: http://ctri.nic.in/Clinicaltrials and http://www.clinicaltrials.gov. Unique identifiers: CTRI-ROVCTRI/2008/091/0004 and NCT0150177.


Assuntos
Transplante de Medula Óssea/métodos , Transplante de Células-Tronco Hematopoéticas/métodos , Acidente Vascular Cerebral/cirurgia , Idoso , Feminino , Humanos , Imageamento por Ressonância Magnética , Masculino , Pessoa de Meia-Idade , Recuperação de Função Fisiológica , Acidente Vascular Cerebral/patologia
15.
Trop Doct ; 44(1): 46-7, 2014 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-24231686

RESUMO

Staphylococcal infections may present in variable ways. Staphylococcal sepsis can cause significant morbidity and mortality. We report on the case of a 42-year-old man without any co-morbidities who presented with fever and purpura fulminans and later developed metastatic endophthalmitis. He was treated with intravenous and intravitreal vancomycin. The case is reported because of the rare co-occurrence of purpura fulminans and endophthalmitis.


Assuntos
Endoftalmite/etiologia , Púrpura Fulminante/etiologia , Sepse/complicações , Infecções Estafilocócicas/complicações , Staphylococcus aureus/isolamento & purificação , Adulto , Antibacterianos/uso terapêutico , Endoftalmite/tratamento farmacológico , Endoftalmite/microbiologia , Humanos , Masculino , Púrpura Fulminante/microbiologia , Sepse/tratamento farmacológico , Sepse/microbiologia , Infecções Estafilocócicas/tratamento farmacológico , Dedos do Pé , Resultado do Tratamento , Vancomicina/uso terapêutico
16.
Oxf Med Case Reports ; 2014(3): 55, 2014 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25988027
17.
Bioorg Med Chem Lett ; 24(2): 624-9, 2014 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-24360999

RESUMO

By combining the structural features of quinazoline and benzimidazole, new hybrid regioisomeric molecules with substituted primary amines have been synthesized. Evaluation of these molecules over 60 cancer cell line panel has identified three molecules as most potent anticancer agents. Compound 10 showed ten and eleven folds more activity than respective quinazoline and benzimidazole class of compounds with GI50 value of 1.64 µM. Compound 11 (GI50 value of 0.81 µM) showed almost twenty and twenty-two fold more activity than quinazoline and benzimidazole analogue, respectively while compound 12 (GI50 value of 4.52 µM) has four fold more activity than quinazoline and benzimidazole analogue. In vitro evaluation of compound 11 exhibited remarkable anticancer activity towards colon cancer cell lines and prostate cancer cell lines at five dose concentrations with GI50 values of 0.34 and 0.31 µM, respectively.


Assuntos
Antineoplásicos/síntese química , Benzimidazóis/síntese química , Quinazolinas/síntese química , Antineoplásicos/farmacologia , Benzimidazóis/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Humanos , Quinazolinas/farmacologia , Relação Estrutura-Atividade
19.
Bioorg Med Chem Lett ; 23(11): 3288-94, 2013 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-23611732

RESUMO

A series of novel regioisomeric hybrids of quinazoline/benzimidazole viz. (3-allyl-2-methyl-3H-benzimidazol-5-yl)-(2-substituted-quinazolin-4-yl)-amine and (1-allyl-2-methyl-1H-benzimidazol-5-yl)-(2-substituted-quinazolin-4-yl)-amine of biological interest were synthesized. All the synthesized compounds were well characterized by (1)H and (13)C NMR as well as mass spectroscopy. The newly synthesized compounds were screened for in vitro antitumor activities against 60 tumor cell lines panel assay. A significant inhibition for cancer cells were observed with compound 9 and also more active against known drug 5-fluorouracil (5-FU) in some tumor cell lines. Compound 9 displayed appreciable anticancer activity against leukemia, colon, melanoma, renal and breast cancer cell lines.


Assuntos
Antineoplásicos/síntese química , Benzimidazóis/química , Quinazolinas/química , Antineoplásicos/química , Antineoplásicos/toxicidade , Sítios de Ligação , Domínio Catalítico , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Conformação Molecular , Simulação de Acoplamento Molecular , Receptores Nucleares Órfãos/química , Receptores Nucleares Órfãos/metabolismo , Relação Estrutura-Atividade
20.
BMJ Case Rep ; 20132013 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-23505286

RESUMO

Liver abscess is a common pathology in the Indian subcontinent and usually results from amoebic or bacterial infection. Pyogenic abscesses usually occur in those with underlying predisposing factors like intra-abdominal infections, biliary infections or comorbidities like malignancy, immunosuppression, diabetes mellitus and previous biliary surgery or interventional endoscopy. Citrobacter is an unusual cause of pyogenic liver abscess and may occur in the setting of underlying comorbidities. We report a 56-year-old man with diabetes (operated for periampullary carcinoma 20 years ago), who presented with a history of fever for 1 week and on evaluation was found to have Citrobacter koseri-related hepatic abscess. The patient was managed with parenteral antibiotics, repeated aspiration of liver abscess and pigtail drainage.


Assuntos
Citrobacter koseri , Infecções por Enterobacteriaceae/complicações , Abscesso Hepático Piogênico/microbiologia , Humanos , Masculino , Pessoa de Meia-Idade
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