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1.
J Pharm Bioallied Sci ; 15(Suppl 1): S86-S92, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37654386

RESUMO

Malignant and potentially malignant epithelial lesions are often associated with various abnormalities such as epithelial dysplasia, abnormal DNA content, loss of heterozygosity, and chromosomal number aberrations. Screening and early detection of such abnormalities facilitates proper care and also helps to prevent further progression of potentially malignant lesions to malignancy. In such way, the presence of DNA aneuploidy in oral potentially malignant disorders (OPMDs) may serve as an indicator for the malignant transforming potential. Various assessment methods have been proposed to find the DNA ploidy status of cells. This current systematic review is mainly designed to assess the importance of ploidy status in OPMD while measuring the feasibility of using this biomarker for evaluating the hazard of malignant transformation. As an upshot of this systematic review, we can conclude that use of DNA ploidy status can serve as an independent bio-marker for predicting the malignant transformation of lesions. Furthermore, as a future scope the use of DNA ploidy analysis in normal mucosa of smokers will help to assess the malignancy risk and this technique might also help to predict the genetic predisposition of patients with malignancy.

2.
Bioorg Chem ; 102: 104046, 2020 09.
Artigo em Inglês | MEDLINE | ID: mdl-32688115

RESUMO

A novel one-pot multicomponent reaction was performed to synthesize different imidazole and benzotriazole (BTA) isatin-based medicinally important compounds using (p-TSA·H2O) as an economical and operative acid catalyst. The yield of the products was found to be up to a maximum of 92% when using this catalyst. Antioxidant, anti-breast cancer and anti-inflammatory activities of these 13 isatin-based derivatives (named as 5a-m) were assessed. The inhibitory effects of these compounds were tested in vitro against cyclooxygenase-2 (COX-2, an enzyme responsible for inflammation) and phosphoinositide-3 kinase (PI3K, a key enzyme in breast cancer). "Among the 13 isatin-based Imidazole derivatives, five compounds (5a, 5d, 5f, 5 k and 5l) were found to exhibit anti-inflammatory as well as anti-cancer activity, which was validated using HRBC stabilization assay (to show anti-inflammatory activity) and cytotoxicity in MCF-7 (breast cancer cell line) to provide proof for anti-cancer property of the compounds". The molecular interactions between the two enzymes were probed using molecular docking. Structure-Activity Relationship (SAR) and ADMET prediction results were also useful to screen the most effective imidazole derivatives and to establish them as putative COX-2 inhibitors/anti-inflammatory drugs. These selected compounds which showed appreciable activity against COX-2 and PI3K are promising drug candidates for the treatment of breast cancer and inflammation which is often associated with breast cancer pathophysiology.


Assuntos
Anti-Inflamatórios/uso terapêutico , Antineoplásicos/uso terapêutico , Imidazóis/uso terapêutico , Inflamação/tratamento farmacológico , Isatina/síntese química , Isatina/uso terapêutico , Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Desenho de Fármacos , Humanos , Imidazóis/farmacologia , Isatina/farmacologia , Simulação de Acoplamento Molecular , Estrutura Molecular , Relação Estrutura-Atividade
3.
Phys Chem Chem Phys ; 19(20): 13316-13323, 2017 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-28492651

RESUMO

The influence of carbon concentration on the electronic and magnetic properties of C-implanted ZnO thin films has been studied using synchrotron radiation based X-ray absorption spectroscopic techniques and vibrating sample magnetometer measurements. 20 keV carbon ions were implanted in ZnO films with different fluences (2 × 1016, 4 × 1016 and 6 × 1016 ions per cm2). The pristine ZnO film shows diamagnetic behaviour while the C-implanted films exhibit room temperature ferromagnetism. Our first-principles calculations based on density functional theory show an appreciable magnetic moment only when the implanted C atom sits either in the O-site (2 µB) or in the interstitial position (1.88 µB), whereas the C atom in the Zn substitutional position does not possess any magnetic moment. X-ray absorption near edge structure analysis at the O K-edge reveals that the charge transfer from O-2p to the C-defect site causes the ferromagnetism in the C-implanted ZnO film at low fluence. However at high fluence, the implanted C replaces the lattice and produces more Zn vacancies, as evidenced by extended X-ray absorption fine structure studies at the Zn K-edge, which favors the ferromagnetism. The persistence of the implanted carbon and ferromagnetism of the C-implanted ZnO film has also been studied by isothermal annealing at 500 °C and discussed in detail.

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