Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br. Gymnestrogenin is a LXR antagonist with IC50s of 2.5 and 1.4 μM for LXRα and LXRβ transactivation, respectively. Gymnestrogenin reduces the transcriptional activity of LXR even on its own promoter, thus reducing the mRNA expression.
Gymnestrogenin, reducing the expression of SREBP1c and ABCA1 in vitro, is able to decrease lipid accumulation in HepG2 cells[2].
[1]. Stöcklin W, et al. [Gymnestrogenin, a new pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br]. Helv Chim Acta. 1968;51(6):1235-42.
[2]. Renga B, et al. Molecular decodification of gymnemic acids from Gymnema sylvestre. Discovery of a new class of liver X receptor antagonists. Steroids. 2015 Apr;96:121-31.