Gitogenin

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 IC₅₀ 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^[1][2]. IC50 & Target: IC50: 0.69 µM (UDP-glucuronosyltransferase 1A4)^[1]; IC50: 37.2 μM (α-glucosidase)^[2] In Vitro: When tamoxifen is used as the substrate metabolized by UGT1A4 in HLMs, Gitogenin exhibits potent inhibition of tamoxifen, with an IC₅₀ value of 6.13 µM. Similarly, for midazolam as the substrate of UGT1A4, the IC₅₀ value is 5.7 µM. In addition, when olanzapine is used as a substrate of UGT1A4, the IC₅₀ 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 IC₅₀ value of 22.0 µM^[1]. 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)^[3].