Icariin protects against radiation-induced mortality and damage in vitro and in vivo.

Purpose: The present study aimed to investigate the potential protective effects of icariin both in vivo and in vitro, an active flavonoid glucoside derived from medicinal herb Epimedium, and its possible mechanisms against radiation-induced injury. Methods: Male C57BL/6 mice were exposed to lethal dose (7 Gy) or sub-lethal dose (4 Gy) of whole body radiation by X-ray at a dose rate of ∼0.55 Gy/min, and icariin was given three times at 24 h and 30 min before and 24 h after the irradiation. After irradiation, hematological, biochemical, and histological evaluations were performed. We further determined the effect of icariin on radiation-induced cytotoxicity and changes in apoptosis-related protein expression. Results: Icariin enhanced the 30-day survival rates (20 and 40 mg/kg) in a dose-dependent manner, and protected the radiosensitive organs such as intestine and testis from the radiation damages. Moreover, hematopoietic damage by radiation was significantly decreased in icariin-treated mice as demonstrated by the increases in number of peripheral blood cells, bone marrow cells (1.7-fold), and spleen colony forming units (1.7-fold). In addition, icariin decreased the radiation-induced oxidative stress by modulating endogenous antioxidant levels. Subsequent in vitro studies showed that icariin effectively increased cell viability (1.4-fold) and suppressed the expression of apoptosis-related proteins after irradiation. Conclusion: These results suggest that icariin has significant protective effects against radiation-induced damages partly through its anti-oxidative and anti-apoptotic properties.