Gigantol isomer-1

Gigantol isomer-1 is a bibenzyl compound derived from Dendrobium nobile. Gigantol isomer-1 shows promising therapeutic potential against cancer cells. Gigantol isomer-1 is a novel inhibitor of the Wnt/β-catenin pathway. IC50 & Target:Wnt^[1] In Vitro: Gigantol isomer-1 decreases the level of phosphorylated LRP6 and cytosolic β-catenin in HEK293 cells. In breast cancer MDA-MB-231 and MDA-MB-468 cells, treatment with Gigantol isomer-1 reduces the level of phosphorylated LRP6^[1]. Gigantol isomer-1 significantly inhibits the proliferation and induces apoptosis of the HepG2 cells. Gigantol isomer-1 at concentrations of 1, 40 and 150 μM markedly decreases the cell viability by 11.7, 30.0 and 56.4% at 24 h and 21.1, 66.8 and 85.5% at 48 h, respectively. The IC₅₀ value is 9.30 μM^[2]. In Vivo: LDD and Gigantol isomer-1 (25–100 mg/kg, p.o.) significantly increase the hot-plate latency in comparison to vehicle-treated mice and decreased carrageenaninduced inflammation in rats^[2].