Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors^[1]. IC50 & Target: IC50: EGFR^[1] In Vitro: Cyasterone exerts cytotoxicity on multiple cell lines: HeLa (IC₅₀=77.24 μg/ml); HepG-2 (IC₅₀=52.03 μg/ml); MCF-7 (IC₅₀=82.07 μg/ml) and MCF-7 (IC₅₀=82.07 μg/ml). And It has none cytotoxicity (IC₅₀>400 μg/ml) on 3 types of carcinoma (HT-29, Caco-2, T47D) and 1 type of normal (NIH 3T3) cell lines^[1].
Cyasterone (0-60 μg/ml; 48 hours) causes a significantly decreasing of the cell proliferation. It inhibits cell growth as a dose-dependent manner, exhibits IC₅₀ values of 38.50 μg/ml and 32.96 μg/ml, respectively^[1].
Cyasterone (0-60 μg/ml; 24 hours) decreases p-EGFR, p-MEK, and p-mTOR as a dose-dependent manner in A549 cells, it affects the MAPK signaling pathway activities^[1].
In Vivo: Cyasterone (intraperitoneal injection; 5 mg/kg, 10 mg/kg and 15 mg/kg; 21 days) has anti-proliferation effect in vivo and inhibits MGC823 cells xenografted tumor growth in vivo with few changes in body weights^[2].