Paeoniflorin is a natural compound found in the roots of the white peony (Paeonia lactiflora). It is a monoterpene glycoside and an active component of the plant’s extracts. For over a millennium, the roots of Paeonia lactiflora have been used in traditional Chinese medicine (TCM), where they are known as “Shaoyao”. Historically, white peony was used to balance the body’s Qi and blood, and it has since gained international scientific interest for its pharmacological effects.
Biological Actions
Paeoniflorin exhibits biological activities, including anti-inflammatory properties that reduce inflammatory markers. It has demonstrated direct anti-inflammatory effects in various animal models by inhibiting the production of prostaglandin E2, leukotriene B4, and nitric oxide. This compound also shows analgesic (pain-relieving) effects, confirmed in animal models. Its pain-relieving actions may be partly mediated by adenosine A1 receptors.
The compound also displays immunomodulatory effects, balancing immune responses. For instance, paeoniflorin has been observed to downregulate pro-inflammatory cytokines like interleukin-2 (IL-2) while upregulating anti-inflammatory cytokines such as interleukin-4 (IL-4) and transforming growth factor-beta1 (TGF-β1). Paeoniflorin also possesses neuroprotective properties, protecting against neuroinflammation and depression-like behaviors in mice. Furthermore, it exhibits antioxidant activity, protecting cells against oxidative stress.
Cellular Mechanisms
Paeoniflorin exerts its biological actions by modulating various signaling pathways within cells. It can inhibit the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway, a key regulator of inflammatory cytokine production and cell survival. By attenuating NF-κB activation, paeoniflorin can reduce the expression of pro-inflammatory cytokines such as interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α).
The compound also influences mitogen-activated protein kinase (MAPK) pathways, specifically inhibiting the activation of extracellular signal-regulated kinase (ERK1/2) and p38 MAPK. These pathways are deeply involved in inflammatory responses, leading to the production of inflammatory mediators. Paeoniflorin’s ability to suppress these pathways contributes to its anti-inflammatory and neuroprotective effects. Additionally, it can regulate gene expression by affecting protein phosphorylation, influencing the production of inflammatory molecules and cell survival.
Practical Considerations
Paeoniflorin’s safety profile is still under investigation, with comprehensive human studies ongoing. One significant consideration for paeoniflorin is its low oral bioavailability, meaning only a small percentage (around 3% to 4%) of an orally administered dose is absorbed. This low absorption is partly due to it being a substrate of P-glycoprotein 1 (Pgp) and undergoing transformation by intestinal bacteria.
Potential interactions with other medications or supplements exist, particularly with those that inhibit Pgp, as co-administration could alter paeoniflorin’s absorption. Consulting a healthcare professional before use is highly recommended, especially given potential interactions and varying individual responses. Specific dosages for human use are still under investigation, with no generally established recommendations.
When considering supplements containing paeoniflorin, the quality and sourcing of the product are paramount. Extracts from Paeonia lactiflora can vary significantly in their paeoniflorin content and overall composition, which can affect their efficacy. Therefore, choosing reputable manufacturers that provide transparent information about their sourcing and standardization practices is advisable. Further research, including clinical trials, is needed to fully understand paeoniflorin’s therapeutic potential and to establish standardized dosages for various applications.