BACKGROUND:Inflammation is a critical process in both physiological defense and the pathogenesis of numerous diseases. While current anti-inflammatory drugs such as NSAIDs and corticosteroids are effective, their long-term use is associated with significant adverse effects, highlighting the need for safer alternatives. Phillyrin, a primary bioactive lignan extracted from the traditional Chinese medicine Forsythiae Fructus (Lianqiao), has emerged as a promising natural anti-inflammatory agent.
METHODS:Data regarding the pharmacology, pharmacokinetics, and toxicology of phillyrin were collected through PubMed, Web of Science, and China National Knowledge Infrastructure (CNKI) databases. In this review, we conducted relevant searches using the key words "phillyrin", "forsythin (synonym of phillyrin)", "Forsythiae Fructus", "Forsythia, Forsythia suspensa", "lianhua qingwen", "shuanghuanglian", "pharmacokinetics", "bioavailability", "application", "molecular mechanism", "adverse reactions", "preclinical and clinical trial", and "animal study", and included studies reported up to and including October 2025.
RESULTS:Available toxicological data from animal studies and early-phase clinical trials indicate that phillyrin has a favorable safety profile, with only mild and transient adverse effects reported. Preclinical studies reveal that phillyrin exerts potent anti-inflammatory effects across a broad spectrum of acute and chronic conditions, including viral pneumonia, acute lung injury, arthritis, colitis, and central nervous system injuries. Phillyrin exerts multi-target effects, primarily by suppressing key pro-inflammatory signaling pathways such as NF-κB and MAPK, and by inhibiting the NLRP3 inflammasome. Furthermore, phillyrin shows protective effects on vital end-organs like the heart, liver, and kidneys in chronic metabolic and cardiovascular diseases.
CONCLUSIONS:Phillyrin represents a promising multi-target anti-inflammatory candidate. However, challenges such as phillyrin's low bioavailability, limited mechanistic insights, and the lack of validation in large-scale clinical trials must be addressed to fully realize its therapeutic potential.