Pentacylic triterpenes from Lavandula coronopifolia: structure related inhibitory activity on α-glucosidase

dc.contributor.authorElsbaey, M
dc.contributor.authorMwakalukwa, R
dc.contributor.authorShimizu, K
dc.contributor.authorMiyamoto, T
dc.date.accessioned2022-10-11T07:38:03Z
dc.date.available2022-10-11T07:38:03Z
dc.date.issued2019
dc.description.abstractTen pentacyclic triterpenes (1-10) were isolated from Lavandula coronopifolia. We evaluated their a-glucosidase inhibitory activity, and found that the aglycones, 1, 2, 3, 4, 7 and 10 showed superior IC50 values to the positive control. In order to explain the structural requirements for a-glucosidase inhibitory activity, eleven derivatives were prepared, including one new compound, 2-formyl-( A)1–19a-hydroxy-1-norursane-2, 12-dien-28-oic acid 10c. The results demonstrated that a free hydroxyl at ring-A and a free carboxylic group at position 28 are key structural features for the a-glucosidase inhibitory activity, also that an ursane skeleton is optimum for the activity. Additionally, enzyme kinetic analysis of pomolic acid 2, the most potent compound, revealed that it inhibited a-glucosidase in a mixed-type manner. The molecular docking simulation validated this type of inhibition and highlighted the role of the C-3 hydroxyl and C-28 carboxylic groups in interaction with the enzyme in silico.en_US
dc.identifier.urihttp://dspace.muhas.ac.tz:8080/xmlui/handle/123456789/2994
dc.language.isoenen_US
dc.publisherTaylor and Francisen_US
dc.subjectPentacylic triterpenesen_US
dc.subjectLavandula coronopifolia:en_US
dc.subjectinhibitoryen_US
dc.titlePentacylic triterpenes from Lavandula coronopifolia: structure related inhibitory activity on α-glucosidaseen_US
dc.typeArticleen_US

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