Pentacylic triterpenes from Lavandula coronopifolia: structure related inhibitory activity on α-glucosidase
| dc.contributor.author | Elsbaey, M | |
| dc.contributor.author | Mwakalukwa, R | |
| dc.contributor.author | Shimizu, K | |
| dc.contributor.author | Miyamoto, T | |
| dc.date.accessioned | 2022-10-11T07:38:03Z | |
| dc.date.available | 2022-10-11T07:38:03Z | |
| dc.date.issued | 2019 | |
| dc.description.abstract | Ten 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.uri | http://dspace.muhas.ac.tz:8080/xmlui/handle/123456789/2994 | |
| dc.language.iso | en | en_US |
| dc.publisher | Taylor and Francis | en_US |
| dc.subject | Pentacylic triterpenes | en_US |
| dc.subject | Lavandula coronopifolia: | en_US |
| dc.subject | inhibitory | en_US |
| dc.title | Pentacylic triterpenes from Lavandula coronopifolia: structure related inhibitory activity on α-glucosidase | en_US |
| dc.type | Article | en_US |
