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J Agric Food Chem ; 68(43): 11975-11986, 2020 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-33054205

RESUMO

Garcinia mangostana L. (mangosteen) is a famous tropical fruit that contains a large number of xanthones. Regular consumption of mangosteen may confer health benefits and prevent some diseases, such as malaria. Quinone reductase 2 (QR-2) is a cytosolic enzyme found in human red blood cells, and it is becoming a target for chemoprevention because it is involved in the mechanisms of several diseases, including malaria. To understand whether the xanthones present in mangosteen might inhibit the activity of QR-2, blood samples were collected from rat following the oral administration of mangosteen extract and then incubated with QR-2 followed by UF-HPLC-QTOF/MS analysis to rapidly screen for and identify the QR-2-inhibiting xanthones. A total of 16 xanthones were identified, and six of these (α-mangostin, γ-mangostin, 8-deoxyartanin, 1,3,7-trihydroxy-2,8-di(3-methylbut-2-enyl)xanthone, garcinone E, and 9-hydroxycalabaxanthone) were subjected to QR-2 inhibition assay. γ-Mangostin exhibited the strongest inhibition, achieving an IC50 value of 3.82 ± 0.51 µM. Its interaction with QR-2 was found to involve hydrogen bond and arene-arene interaction as revealed by molecular docking. The present study could provide new insight into the potential application of mangosteen as functional food ingredients for inhibiting the activity of QR-2. However, the extent of daily intake of mangosteen required and the exact contribution of mangosteen to the prevention and treatment of malaria remain subjects of further study.


Assuntos
Inibidores Enzimáticos/farmacocinética , Garcinia mangostana/química , Extratos Vegetais/farmacocinética , Quinona Redutases/antagonistas & inibidores , Administração Oral , Animais , Cromatografia Líquida , Inibidores Enzimáticos/administração & dosagem , Inibidores Enzimáticos/química , Frutas/química , Humanos , Simulação de Acoplamento Molecular , Estrutura Molecular , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Quinona Redutases/química , Quinona Redutases/metabolismo , Ratos , Ratos Sprague-Dawley , Espectrometria de Massas em Tandem , Xantonas/administração & dosagem , Xantonas/química , Xantonas/farmacocinética
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