The 20-hydroryecdysone (20E) has been used in traditional medicine for a long time and acquired attention in the last decade as a food supplement and stimulant in phys-ical activities. This polyhydroxylated cholesterol is found in the highest concentration in plants and it is one of the secondary plant products that has a real hormonal influ-ence in arthropods. Various beneficial effects have been reported in vivo and in vitro for 20E and its related compounds in mammals. Trials for safety of clinical application showed a remarkable high tolerance in human. This review aims to assess the latest development in the involvement of various pathways in tissues and organs and look if it is plausible to find a single primary target of this compound. The similarities with agens mimicking calorie restriction and anti-aging effects are also elucidated and discussed.