Protodioscin (5 and 10 mg/kg) significantly improves glucose intolerance and reduced the levels of serum UA, BUN, Cr, TC and TG. Protodioscin significantly reduces renal concentrations of IL-1β, IL-6 and TNF-α by inhibiting the activation of nuclear factor-κB, c-Jun N-terminal kinase, p38 mitogen-activated protein kinase and extracellular signal-regulated kinase. Protodioscin ameliorates the death rate, inhibits the increase in neurological deficit scores and infarct volume, and reduces the apoptotic nerve cells induced by MCAO in rats. Protodioscin attenuates the change of relevant apoptins, suppresses the release of pro-inflammatory cytokines in serum and reverses the protein expression of NF-κB (in nucleus and cytoplasm) and IκBα (in cytoplasm) induced by MCAO in rats. Protodioscin (0.5 mg/kg, i.p.) increases the coagulation time by appr 50?% as compared to that of high-fat diet control rats. Protodioscin possesses a promising effect in lowering the blood levels of both lipoproteins, especially LDL, thus resulting in a high ratio of HDL/LDL.