Ruscogenin is a major steroid sapogenin found in the traditional Chinese medicinal herb Ophiopogon japonicus. It was first isolated from Ruscus aculeatus. Ruscogenin has multiple bioactivities and possesses a variety of pharmacological activities: anti-inflammatory properties, platelet aggregation inhibition, pulmonary hypertension lowering properties, acute lung injury alleviation and other effects. It was shown, that ruscogenin inhibited activation of neutrophil through cPLA2, PAK, Akt, MAPKs, cAMP, and PKA signaling pathways. In addition, Ruscogenin decreased expression of genes involved in hepatic lipogenesis through downregulation of NF-κB-mediated inflammatory responses. It was shown that ruscogenin significantly attenuate LPS-induced acute lung injury (ALI) via inhibiting expressions of TF and iNOS and NF-κB p65 activation, indicating it was a potential therapeutic agent for ALI or sepsis.