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1.
BMC Chem ; 16(1): 42, 2022 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-35672858

RESUMO

BACKGROUND: Mangiferin is a C-glycoside xanthone molecule having a wide range of therapeutic properties. Hence, the present study aims to understand the efficacy of mangiferin against colorectal cancer (CRC) and to elucidate the mechanisms of action of mangiferin on colorectal cancer. METHOD: The molecular mechanism of mangiferin against colorectal cancer was studied using Autodock Vina software. Pharmacophore analysis of mangiferin concerning five COX-2 inhibitor drugs was carried out using the PharmaGist server to analyze the possibility of using mangiferin as a COX-2 inhibitor. In vitro analysis of Mangiferin against various cancer cell lines was performed. RESULTS: The molecular mechanism of action of mangiferin against CRC was assessed by docking with multiple target proteins involved in the progression of CRC. Docking studies showed good binding scores (kcal/mol) ranging from - 10.3 to - 6.7. Mangiferin showed a good affinity towards enzymes like COX-2 and LA4H involved in Arachidonic acid (AA) metabolism with a binding score(kcal/mol) of - 10.1 and - 10.3 respectively. The pharmacophore feature assessment of mangiferin was done for COX-2 inhibitor drugs, which further confirmed that mangiferin poses the same pharmacophore feature as that of COX-2 inhibitor drugs. Furthermore, the binding affinity of mangiferin was compared with five COX-2 inhibitor drugs to prove its efficacy as an inhibitor. Mangiferin also had a cytotoxic effect against colorectal cancer (HT 29), cervical cancer (HeLa), and breast cancer (MCF 7) cell lines. The study could establish that Mangiferin might be a promising candidate for the treatment of colorectal cancer. CONCLUSION: In short, these studies exploited the possibility of mangiferin as a lead molecule to develop anticancer/anti-inflammatory drugs for the treatment of CRC.

2.
Int J Biol Macromol ; 151: 36-46, 2020 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-32070742

RESUMO

Oxidative stress is considered to be the leading cause of many chronic and degenerative diseases leading to death and disability. Antioxidant therapy could be efficient in preventing oxidative stress-induced damages in cells. In the present study the efficacy of mangiferin-chitosan nanoparticles (MCNs) as a therapeutic agent against the oxidative stress, since mangiferin (MGF), a polyphenol protects and attenuates oxidative stress against various diseases. However, the bioactivity of MGF does not result in vivo biological effect owing to its low bioavailability and poor solubility. Mangiferin nanoparticles (NPs) were developed to improve the solubility and bioavailability of mangiferin. Nanoparticles had significant free radical scavenging activity in the cell-free system and had a synergistic action with phase II antioxidant enzymes such as catalases and peroxidases. A nephropathic system was developed to investigate the attenuative role of mangiferin-chitosan nanoparticles against induced oxidative stress, on normal kidney epithelial (NKE) cells. Pre-treatment with the nanoparticles exclusively prevented the induction of cytotoxicity induced by NaF and maintained the level of intracellular antioxidant enzyme in the cells. Nanoparticles had significant lipid peroxidation and protein oxidation inhibition activities. These nanoparticles can be used in food and pharmaceutical industries as a therapeutic agent to prevent the oxidative stress-induced health disorders.


Assuntos
Antioxidantes/química , Antioxidantes/farmacologia , Quitosana/química , Nanopartículas/química , Estresse Oxidativo/efeitos dos fármacos , Xantonas/química , Sobrevivência Celular , Células Cultivadas , Espaço Intracelular/metabolismo , Rim/citologia , Rim/efeitos dos fármacos , Rim/metabolismo , Modelos Biológicos , Oxirredução , Espécies Reativas de Oxigênio/metabolismo , Análise Espectral
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