Gitogenin 是从 Tribulus longipetalus 整株中分离出来的一种天然类固醇，是 UDP-葡萄糖醛酸转移酶 1A4 (UGT1A4) 和 α-葡萄糖苷酶的选择性抑制剂，其 IC50 值分别为 0.69 µM (使用三氟拉嗪为底物) 和 37.2 μM，并且不抑制人类主要细胞色素 P450 亚型的活性。
货号:ajcx14236
CAS:511-96-6
分子式:C27H44O4
分子量：432.64
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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].

[1]. Xu M, et al. Drug interaction study of natural steroids from herbs specifically toward human UDP-glucuronosyltransferase (UGT) 1A4 and their quantitative structure activity relationship (QSAR) analysis for prediction. Pharmacol Res. 2016 Aug;110:139-150. [2]. Naveed MA, et al. Longipetalosides A-C, new steroidal saponins from Tribulus longipetalus. Steroids. 2014 May;83:45-51. [3]. Shim SH, et al. Rat growth-hormone release stimulators from fenugreek seeds. Chem Biodivers. 2008 Sep;5(9):1753-61.