Neferine, a bisbenzylisoquinoline alkaloid derived from the seed embryo of Nelumbo nucifera, a traditional Chinese medicine, has been studied for its therapeutic potential in various disease models. Research indicates that neferine exhibits significant pharmacological activities, including anti-tumor, anti-inflammatory, anti-fibrosis, anti-oxidative stress, anti-platelet aggregation, and anti-arrhythmic effects. Inflammation is an adaptive response to diverse signals, and this paper reviews the anti-inflammatory properties and underlying mechanisms of neferine observed in both in vivo and in vitro studies, offering new insights into the treatment of inflammation-related diseases.