Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus . Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC 50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms
In Vitro
When tamoxifen is used as the substrate metabolized by UGT1A4 in HLMs, Gitogenin exhibits potent inhibition of tamoxifen, with an IC 50 value of 6.13 µM. Similarly, for midazolam as the substrate of UGT1A4, the IC 50 value is 5.7 µM. In addition, when olanzapine is used as a substrate of UGT1A4, the IC 50 value is determined as 6.0 µM. Finally, we also evaluats Gitogenin for asenapine glucuronidation mediated by UGT1A4, and similar inhibition effect is observed, with an IC 50 value of 22.0 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Stimulation of growth hormone release is investigated on rat pituitary cells in vitro. Gitogenin (20 μg/mL) shows rat growth-hormone (rGH) release stimulating activities (26.1 ng/mL). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
