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1.
3 Biotech ; 12(11): 282, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36276470

RESUMO

This article shows the adequacy of the custom-built optical imaging system in the advancement investigation of obese mice. Obesity is defined as increased adipose/fatty mass resulting from a chronic imbalance between energy intake and expenditure. The in vivo investigation was performed for the tissue characterization of obese mice utilizing swept-source optical coherence tomography (SSOCT) for in situ examination and histology of delicate tissues in mice skin. It provides a noninvasive, painless visualization of the subsurface in life systems. Our SSOCT system's data is comparable to the regular invasive histology. Cross-assessment is done in various skin layers in obese mice like epidermis, papillary dermis, dermis, and fat tissue, which are likewise separated from the nonobese mice group. Histopathology results were further assessed with the obtained SSOCT results. This high precision of characterizing tissues using SSOCT helps us perform in vivo imaging and can also be used for the variable purpose of clinical practice.

2.
ChemMedChem ; 16(3): 484-498, 2021 02 04.
Artigo em Inglês | MEDLINE | ID: mdl-33030290

RESUMO

Insulin resistance is a major pathophysiological feature in the development of type 2 diabetes (T2DM). Ferulic acid is known for attenuating the insulin resistance and reducing the blood glucose in T2DM rats. In this work, we designed and synthesized a library of new ferulic acid amides (FAA), which could be considered as ring opening derivatives of the antidiabetic PPARγ agonists Thiazolidinediones (TZDs). However, since these compounds displayed weak PPAR transactivation capacity, we employed a proteomics approach to unravel their molecular target(s) and identified the peroxiredoxin 1 (PRDX1) as a direct binding target of FAAs. Interestingly, PRDX1, a protein with antioxidant and chaperone activity, has been implied in the development of T2DM by inducing hepatic insulin resistance. SPR, mass spectrometry-based studies, docking experiments and in vitro inhibition assay confirmed that compounds VIe and VIf bound PRDX1 and induced a dose-dependent inhibition. Furthermore, VIe and VIf significantly improved hyperglycemia and hyperlipidemia in streptozotocin-nicotinamide (STZ-NA)-induced diabetic rats as confirmed by histopathological examinations. These results provide guidance for developing the current FAAs as new potential antidiabetic agents.


Assuntos
Amidas/farmacologia , Ácidos Cumáricos/farmacologia , Inibidores Enzimáticos/farmacologia , Hipoglicemiantes/farmacologia , Hipolipemiantes/farmacologia , Peroxirredoxinas/antagonistas & inibidores , Amidas/síntese química , Amidas/química , Animais , Compostos de Bifenilo/antagonistas & inibidores , Sobrevivência Celular/efeitos dos fármacos , Ácidos Cumáricos/síntese química , Ácidos Cumáricos/química , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Hipoglicemia/induzido quimicamente , Hipoglicemia/tratamento farmacológico , Hipoglicemia/metabolismo , Hipoglicemiantes/síntese química , Hipoglicemiantes/química , Hipolipemiantes/síntese química , Hipolipemiantes/química , Masculino , Modelos Moleculares , Estrutura Molecular , Peroxirredoxinas/metabolismo , Picratos/antagonistas & inibidores , Ratos , Ratos Sprague-Dawley , Ratos Wistar , Estreptozocina , Relação Estrutura-Atividade , Células Tumorais Cultivadas
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