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Therapeutic potential of plant-derived flavonoids against inflammation
Therapeutic potential of plant-derived flavonoids against inflammation
- Pathological pain can occur following inflammation and/or peripheral nerve injury. It isn't merely a symptom; rather, it results from the abnormal functioning of the nervous system. In fact, pain represents a substantial social, health, and economic burden globally.
- Flavonoids are plant - derived compounds that are commonly present in numerous fruits and vegetables and are part of our daily diet. Flavonoids are classified into different groups. Although they have unique structures, they all share a fundamental structure composed of three rings, referred to as the flavan nucleus. Structural variations exist in the substitution pattern of one of these rings. The position of the hydroxyl group (–OH) in one of the rings determines the mechanisms of action of flavonoids and exhibits a complex, multifunctional activity.
- Flavonoids have been extensively utilized due to their antioxidant, analgesic, and anti - inflammatory properties, as well as their favorable pre - clinical and clinical safety profiles. In this review, we will explore the pre - clinical and clinical evidence regarding the analgesic and anti - inflammatory characteristics of flavonoids. Additionally, we will emphasize how the development of flavonoid - containing formulations, combined with an understanding of their structure - activity relationship, can be utilized to identify novel flavonoid - based treatments for pathological pain and inflammation.
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- Inhibition of Inflammatory Mediator Release: Flavonoids can inhibit the expression and activity of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS), thereby reducing the production of prostaglandin E2 (PGE2) and nitric oxide (NO), which are important inflammatory mediators.
- Regulation of Cytokine Production: Flavonoids can regulate the production of cytokines such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6). For example, some flavonoids can inhibit the activation of nuclear factor-κB (NF-κB), a key transcription factor in the regulation of cytokine production, thereby reducing the secretion of pro-inflammatory cytokines.
- Antioxidant Effects: Flavonoids have antioxidant properties and can scavenge reactive oxygen species (ROS), reducing oxidative stress damage and inhibiting the activation of inflammatory signaling pathways mediated by ROS.
- Modulation of Signal Pathways: Flavonoids can also act on other signal transduction pathways, such as the mitogen-activated protein kinase (MAPK) pathway, and play an anti-inflammatory role by inhibiting the phosphorylation and activation of kinases in the MAPK pathway.
Pre-Clinical Data
- In Vitro Studies: In cell culture experiments, flavonoids have been shown to have anti-inflammatory and analgesic effects. For example, luteolin can inhibit the production of NO and PGE2 in lipopolysaccharide (LPS)-induced RAW264.7 macrophages, and baicalein can inhibit the activation of NF-κB and the expression of COX-2 and iNOS in TNF-α-induced human umbilical vein endothelial cells.
- In Vivo Animal Models: In animal models of inflammation and pain, flavonoids have also demonstrated good therapeutic effects. For instance, in a rat model of rheumatoid arthritis, treatment with flavonoids such as quercetin and rutin can significantly reduce joint swelling and pain, improve joint function, and inhibit the production of inflammatory cytokines and cartilage degradation in the joint. In a mouse model of neuropathic pain, treatment with flavonoids such as apigenin and naringenin can relieve pain hypersensitivity and reduce the expression of inflammatory mediators in the spinal cord.
Clinical Data
- Pain Relief: Some clinical studies have shown that flavonoids have a certain analgesic effect. For example, in a randomized, double-blind, placebo-controlled trial, patients with chronic low back pain who took a flavonoid-rich extract of Harpagophytum procumbens for 4 weeks had a significant reduction in pain intensity compared with the placebo group.
- Anti-Inflammatory Effects: In patients with inflammatory diseases such as rheumatoid arthritis and osteoarthritis, flavonoid supplements have been shown to have some anti-inflammatory effects. For example, in a study of patients with osteoarthritis, treatment with a flavonoid-rich extract of Boswellia serrata for 12 weeks significantly reduced joint pain and swelling and improved joint function.
- Safety and Tolerability: In general, flavonoids have good safety and tolerability. However, in some cases, flavonoid supplements may cause mild gastrointestinal discomfort, allergic reactions, or interactions with other drugs.
Pharmaceutical Development
- Formulation Optimization: In order to improve the bioavailability and therapeutic efficacy of flavonoids, researchers are constantly exploring the optimization of flavonoid formulations. For example, the development of nanoparticle formulations, liposome formulations, and microemulsion formulations of flavonoids can improve their solubility, stability, and absorption in the body.
- Structure-Activity Relationship Studies: By studying the structure-activity relationship of flavonoids, it is possible to design and synthesize more effective flavonoid derivatives. For example, modifications at specific positions of the flavonoid structure can enhance its anti-inflammatory and analgesic activities.
- Combination Therapy: The combination of flavonoids with other drugs may have synergistic effects and improve the therapeutic efficacy. For example, the combination of flavonoids with non-steroidal anti-inflammatory drugs or immunosuppressive drugs may be more effective in the treatment of inflammatory and autoimmune diseases.
