Abstract
Arzanol, a prenylated phloroglucinol-α-pyrone heterodimer, displays a broad range of pharmacological properties. This review compiles findings from 2007 to 2025 on its chemistry, conformational behavior, bioactivities, molecular targets, and pharmacokinetics. Arzanol shows potent anti-inflammatory activity through NF-κB inhibition and dual suppression of mPGES-1 and 5-LOX, antioxidant and cytoprotective effects via radical scavenging and metal chelation, and selective antibacterial activity. Arzanol also modulates autophagy, mitochondrial function, and metabolic pathways, with high-affinity binding to brain glycogen phosphorylase and SIRT1. Pharmacokinetic data indicate gastrointestinal stability, intestinal absorption, and limited blood-brain barrier penetration. In vivo, arzanol exhibits neuroprotective, neurobehavioral, and metabolic effects, while showing selective cytotoxicity toward cancer cells with minimal impact on normal cells. This review evaluates the diverse biological activities of arzanol, analyzing the relationship between its unique conformational flexibility and multitarget pharmacological effects.