Recent Insights Into the Protective Mechanisms of Paeoniflorin in Neurological, Cardiovascular, and Renal Diseases

The monoterpene glycoside paeoniflorin is the principal active constituent of the traditional Chinese herbal medicines, Radix Paeoniae Alba (RPA) and Radix Paeoniae Rubra (RPR), which have been used for millennia to treat cardiovascular diseases (e.g., hypertension, bleeding, and atherosclerosis) and neurological ailments (e.g., headaches, vertigo, dementia, and pain). Recent evidence has revealed that paeoniflorin exerts inhibitory effects on inflammation, fibrosis, and apoptosis by targeting several intracellular signaling cascades. In this review, we address the current knowledge about the pharmacokinetic properties of paeoniflorin and its molecular mechanisms of action. We also present results from recent pre-clinical studies supporting the utility of paeoniflorin for the treatment of pain, cerebral ischemic injury, and neurodegenerative diseases, such as Alzheimer’s and Parkinson’s diseases. Moreover, new evidence suggests a general protective role of paeoniflorin in heart attack, diabetic kidney, and atherosclerosis. Mechanistically, paeoniflorin exerts multiple anti-inflammatory actions by targeting Toll-like receptor (TLR)-mediated signaling in both parenchymal and immune cells (in particular, macrophages and dendritic cells). A better understanding of the molecular actions of paeoniflorin may lead to the expansion of its therapeutic uses.