Source, biological activity, molecular mechanism, pharmacokinetics, and preparation of luteoloside

Luteoloside, a flavonoid compound, is widely distributed in various plant families. Preclinical studies have demonstrated that luteoloside exhibits a broad spectrum of pharmacological activities in vitro and in vivo, including anti-inflammatory, antibacterial, antiviral, anticancer, antioxidant, and cardioprotective effects. However, its therapeutic potential is significantly constrained by poor aqueous solubility, extensive presystemic metabolism, and consequently low oral bioavailability. Pharmacokinetic studies reveal route-dependent behaviour and rapid clearance. To overcome these hurdles, advanced delivery systems such as microemulsions, polymeric nanocarriers, and hydrogels have been developed. Toxicological assessments indicate a wide therapeutic window with low acute toxicity. In conclusion, this review consolidates the substantial preclinical evidence supporting luteoloside’s multi-target mechanisms. Nevertheless, it also critically highlights the existing gaps, particularly the absence of clinical data and the challenges in pharmacokinetics, which must be addressed through rigorous future research to evaluate its true clinical potential.