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J Enzyme Inhib Med Chem. 2019 Dec;34(1):1623-1632. doi: 10.1080/14756366.2019.1660653.

Competitive α-glucosidase inhibitors, dihydrobenzoxanthones, from the barks of Artocarpus elasticus.

Author information

1
Research Center for Medicinal Plants, Al-Farabi Kazakh National University , Almaty , Kazakhstan.
2
Division of Applied Life Science (BK21 plus), IALS, Gyeongsang National University , Jinju , Republic of Korea.
3
Division of Applied Life Science (BK21 plus), PMBBRC, RINS, Gyeongsang National University , Jinju , Republic of Korea.

Abstract

This study aimed to search the α-glucosidase inhibitors from the barks part of Artocarpus elasticus. The responsible compounds for α-glucosidase inhibition were found out as dihydrobenzoxanthones (1-4) and alkylated flavones (5-6). All compounds showed a significant enzyme inhibition toward α-glucosidase with IC50s of 7.6-25.4 μM. Dihydrobenzoxanthones (1-4) exhibited a competitive inhibition to α-glucosidase. This competitive behaviour was fully characterised by double reciprocal plots, Yang's method, and time-dependent experiments. The compound 1 manifested as the competitive and reversible simple slow-binding, with kinetic parameters k3 = 0.0437 µM-1 min-1, k4 = 0.0166 min-1, and Kiapp = 0.3795 µM. Alkylated flavones (5-6) were mixed type I (KI < KIS) inhibitors. The binding affinities (KSV) represented by all inhibitors were correlated to their concentrations and inhibitory potencies (IC50). Moreover, compounds 1 and 5 were identified as new ones named as artoindonesianin W and artoflavone B, respectively. Molecular modelling study proposed the putative binding conformation of competitive inhibitors (1-4) to α-glucosidase at the atomic level.

KEYWORDS:

; artoflavone B and α-glucosidase inhibition; artoindonesianin W; dihydrobenzoxanthones

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