Aloperine　is　an　alkaloid　found　in　the　seeds　and　leaves　of　the　medicinal　plant　Sophora　alopecuroides　L.　It　has　been　used　as　herbal　medicine　in　China　for　centuries　due　to　its　potent　anti-inflammatory,　antioxidant,　antibacterial,　and　antiviral　properties.　Recently,　aloperine　has　been　widely　investigated　for　its　therapeutic　activities.　Aloperine　is　proven　to　be　an　effective　therapeutic　agent　against　many　human　pathological　conditions,　including　cancer,　viral　diseases,　and　cardiovascular　and　inflammatory　disorders.　Aloperine　is　reported　to　exert　therapeutic　effects　through　triggering　various　biological　processes,　including　cell　cycle　arrest,　apoptosis,　autophagy,　suppressing　cell　migration,　and　invasion.　It　has　also　been　found　to　be　associated　with　the　modulation　of　various　signaling　pathways　in　different　diseases.　In　this　review,　we　summarize　the　most　recent　knowledge　on　the　modulatory　effects　of　aloperine　on　various　critical　biological　processes　and　signaling　mechanisms,　including　the　PI3K,　Akt,　NF-kappa　B,　Ras,　and　Nrf2　pathways.　These　data　demonstrate　that　aloperine　is　a　promising　therapeutic　candidate.　Being　a　potent　modulator　of　signaling　mechanisms,　aloperine　can　be　employed　in　clinical　settings　to　treat　various　human　disorders　in　the　future.