Engelheptanoxides behave as liver X receptor α agonists

In this study, the activity of engelheptanoxide A and C against LXR α was evaluated by the transient transfection reporter and mammalian one-hybrid assays. The results showed that engelheptanoxide A and C respectively transactivated CYP7A1, ABCA1, and Gal4 promoters in the dose-dependent manner. Furthermore, the docking study demonstrated that engelheptanoxide A an d C can contact with the LXRα ligand binding pocket in the similar manner as 22(R)-hydroxycholesterol, an endogenous LXRα agonist, to agonize LXRα. These results indicated thatEngelhardia roxburghiana might be able to exert pharmacological effects through LXR α pathway.

http://link.springer.com/10.1007/s00044-023-03016-y

Source: Medicinal Chemistry Research - January 13, 2023 Category: Chemistry Source Type: research