Asperuloside, an iridoid glycoside found in Herba Paederiae, is a component from traditional Chinese herbal medicine. Asperuloside is extracted from many traditional Chinese medicinal plants, including Herba Paederiae, Asperula odorata, Goldhair Hedyotis Herb and Hedyotis diffusa. It has been proved that there are many kinds of pharmacological effects such as anti-tumor and anti-obesity activities. Asperuloside can significantly downregulate tumor necrosis factor alpha (TNF-α), interleukin (IL)-1β, and IL-6 levels in vitro and in vivo, and treatment with asperuloside significantly reduced the lung wet-to-dry weight, histological alterations and myeloperoxidase activity in a murine model of LPS-induced acute lung injury (ALI). Asperuloside exerts its anti-inflammatory effect in correlation with inhibition of a pro-inflammatory mediator through suppressing nuclear factor kappa-B (NF-κB) nuclear translocation and MAPK phosphorylation. Asperuloside can be a potential treatment for ALI and can be used as a clinical anti-infective drug.