Study on structure–activity relationships (SARs) of epoxylignan compounds with α- glucosidase inhibitory activity

Abstract

Epoxylignans are polyphenolic compounds, which possess various biological activities such as antiproliferative activity on cancer cells, antioxidant, antihyperglycemic,… In this research, we study on α- glucosidase inhibitory activity of 11 epoxylignans isolated from the stem of Artocarpus heterophyllus, the stem of Willughbeia cochinchinensis, the stem bark of Crateva religiosa, and the propolis of Trigona minor. The results showed that, compounds 1–4 and 7–10 were more potent inhibitory activity than that of positive control acarbose (IC50, 214.5 µM). Based on the results, their structure-activity relationships showed that the presence of the hydroxyl group at C-4, and C-4ʹ positions play an important role in increasing the activity. Furthermore, diepoxylignans having a ketone group at C-9′ exhibited stronger activity. In contrast, the opening of an epoxy ring at C-7 the C-9′ positions reduced the activity.