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Cinnamoyl Sucrose Esters as Alpha Glucosidase Inhibitors for the Treatment of Diabetes.


ABSTRACT: Cinnamoyl sucrose esters (CSEs) were evaluated as AGIs and their enzyme inhibition activity and potency were compared with gold standard acarbose. The inhibition activity of the CSEs against ?-glucosidase and ?-amylase depended on their structure including the number of the cinnamoyl moieties, their position, and the presence or absence of the acetyl moieties. The inhibitory values of the CSEs 2-9 generally increases in the order of mono-cinnamoyl moieties < di-cinnamoyl ? tri-cinnamoyl < tetra-cinnamoyl. This trend was supported from both in vitro and in silico results. Both tetra-cinnamoyl CSEs 5 and 9 showed the highest ?-glucosidase inhibitory activities of 77 ± 5%, 74 ± 9%, respectively, against acarbose at 27 ± 4%, and highest ?-amylase inhibitory activities of 98 ± 2%, 99 ± 1%, respectively, against acarbose at 93 ± 2%. CSEs 3, 4, 6, 7, 8 showed desired higher inhibition of ?-glucosidase than ?-amylase suggesting potential for further development as AGIs with reduced side effects. Molecular docking studies on CSEs 5 and 9 attributed the high inhibition of these compounds to multiple ?-? interactions and favorable projection of the cinnamoyl moieties (especially O-3 cinnamoyl) in the enzyme pockets. This work proposes CSEs as new AGIs with potentially reduced side effects.

SUBMITTER: Devaraj S 

PROVIDER: S-EPMC7830900 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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Cinnamoyl Sucrose Esters as Alpha Glucosidase Inhibitors for the Treatment of Diabetes.

Devaraj Surabhi S   Yip Yew Mun YM   Panda Parthasarathi P   Ong Li Lin LL   Wong Pooi Wen Kathy PWK   Zhang Dawei D   Judeh Zaher Z  

Molecules (Basel, Switzerland) 20210118 2


Cinnamoyl sucrose esters (CSEs) were evaluated as AGIs and their enzyme inhibition activity and potency were compared with gold standard acarbose. The inhibition activity of the CSEs against α-glucosidase and α-amylase depended on their structure including the number of the cinnamoyl moieties, their position, and the presence or absence of the acetyl moieties. The inhibitory values of the CSEs <b>2</b>-<b>9</b> generally increases in the order of mono-cinnamoyl moieties < di-cinnamoyl ≤ tri-cinn  ...[more]

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