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1.
Curr Cancer Drug Targets ; 23(8): 634-642, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36718971

RESUMO

Lycopene, a potential bioactive agent, is a non-pro-vitamin A carotenoid recognized as a potent antioxidant. It is extracted from plants like tomatoes, watermelons, red carrots and papayas and has remarkable health benefits. A significant amount of research has been assisted to date to establish the anticancer activity of lycopene. Our review enhances information about the promising anticancer potential of this compound. The biological activity of lycopene has been described in several studies in regard to pancreatic, breast, prostate, liver, gastric, ovarian, kidney, skin, intestine, brain and spinal cord cancers. Lycopene resists cancer by inhibition of apoptosis, induction of cell proliferation, cell invasion, cell cycle development, metastasis and angiogenesis. The mechanisms of anticancer action of lycopene are attributed to the management of certain signal transduction pathways, such as modulation of insulin-like growth factors system, PI3K/Akt pathway, modification of important gene expression, inhibit the activity of sex steroid hormones, and the conversation of mitochondrial behavior. Hence, this review focuses on current knowledge of sources, extraction techniques, and chemistry of lycopene, as well as the prospective mechanisms of action related with its anticancer activity. Also, it summarizes the background information about lycopene and the most current research with consideration to its aspect in treating several types of cancer together with future directions.


Assuntos
Anticarcinógenos , Neoplasias , Masculino , Humanos , Licopeno/uso terapêutico , Anticarcinógenos/farmacologia , Anticarcinógenos/uso terapêutico , Fosfatidilinositol 3-Quinases , Carotenoides/farmacologia , Carotenoides/uso terapêutico , Carotenoides/metabolismo , Neoplasias/tratamento farmacológico
2.
Mol Divers ; 26(2): 1213-1225, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-34553298

RESUMO

Diabetes mellitus is a main global health apprehension. Macrovascular illnesses, neuropathy, retinopathy, and nephropathy are considered some of its severe hitches. Gliptins are a group of hypoglycemic agents that inhibit dipeptidyl peptidase-IV (DPP-IV) enzyme and support blood glucose-lowering effect of incretins. In the current research, synthesis, characterization, docking, and biological evaluation of fourteen Schiff's bases 5a-f and 9a-h were carried out. Compound 9f revealed the best in vitro anti-DPP-IV activity of 35.7% inhibition at a concentration of 100 µM. Compounds 9c and 9f with the highest in vitro DPP-IV inhibition were subjected to the in vivo glucose-lowering test using vildagliptin as a positive inhibitor. Vildagliptin, 9c, and 9f showed significant reduction in the blood glucose levels of the treated mice after 30 min of glucose administration. Moreover, induced fit docking showed that these derivatives accommodated the enzyme binding site with comparable docking scores. Schiff's bases can serve as promising lead for the development of new DPP-IV inhibitors.


Assuntos
Diabetes Mellitus Tipo 2 , Inibidores da Dipeptidil Peptidase IV , Animais , Glicemia , Diabetes Mellitus Tipo 2/metabolismo , Dipeptidil Peptidase 4/química , Inibidores da Dipeptidil Peptidase IV/química , Inibidores da Dipeptidil Peptidase IV/farmacologia , Hipoglicemiantes/química , Camundongos , Vildagliptina
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