The pharmacological mechanism of Citrus Bioflavonoids is characterized by multi-targets and multi-pathways, the following is a systematic combing of its core mechanism from molecular to cellular level:<\/p>\n\n\n\n
1. Antioxidant mechanism<\/p>\n\n\n\n
Free radical scavenging<\/p>\n\n\n\n
Phenolic hydroxyl effect: the A-ring 5.7-dihydroxyl structure of flavonoids (e.g., hesperidin, naringin) endows it with strong reducing properties, which can directly neutralize free radicals such as DPPH and ABTS+.<\/p>\n\n\n\n
Enzyme system regulation: activate superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) to enhance the cell’s own antioxidant capacity.<\/p>\n\n\n\n
Metal chelation: inhibit Fe\u00b2\u207a\/Cu\u00b2\u207a-induced Fenton reaction and reduce hydroxyl radical (-OH) generation.<\/p>\n\n\n\n
Oxidative stress modulation<\/p>\n\n\n\n
Inhibits the generation of lipid peroxidation products (e.g. MDA) and protects cell membrane integrity.<\/p>\n\n\n\n
Up-regulates nuclear factor E2-related factor 2 (Nrf2) expression and promotes the synthesis of antioxidant proteins (e.g. heme oxygenase-1).<\/p>\n\n\n\n
2. Anti-inflammatory mechanism<\/p>\n\n\n\n
Inflammatory signaling blockade<\/p>\n\n\n\n
NF-\u03baB pathway: inhibit I\u03baB kinase (IKK) phosphorylation, reduce p65 nuclear translocation, and down-regulate transcription of pro-inflammatory factors such as TNF-\u03b1 and IL-6.<\/p>\n\n\n\n
MAPK pathway: block ERK1\/2. p38 phosphorylation, inhibit inflammatory cascade response.<\/p>\n\n\n\n
Inflammatory mediator regulation<\/p>\n\n\n\n
Inhibit the expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS), and reduce the production of prostaglandin E2 (PGE2), NO and other inflammatory substances.<\/p>\n\n\n\n
Promote the release of anti-inflammatory factor IL-10 to restore the pro-inflammatory\/anti-inflammatory balance.<\/p>\n\n\n\n
4. Regulation of gastrointestinal function<\/p>\n\n\n\n
Hormone regulation<\/p>\n\n\n\n
Pro-secretin: increase secretion of gastrin (GAS) and gastric motrin (MTL), accelerate gastric emptying.<\/p>\n\n\n\n
Inhibitory inhibitory hormone: inhibit the release of vasoactive intestinal peptide (VIP), relieve excessive intestinal spasm.<\/p>\n\n\n\n
Smooth muscle regulation<\/p>\n\n\n\n
Blocks L-type calcium channels, reduces Ca\u00b2\u207a concentration in intestinal smooth muscle cells, relieves acetylcholine-induced spasm.<\/p>\n\n\n\n
Activate M3 receptor, enhance the smooth muscle tone of gastric fundus, improve the symptoms of gastroparesis.<\/p>\n\n\n\n
5. Antibacterial and antiviral mechanism<\/p>\n\n\n\n
Bacterial inhibition<\/p>\n\n\n\n
Cell wall disruption: insertion of flavonoids into bacterial cell membrane, leading to increased permeability and leakage of contents.<\/p>\n\n\n\n
Metabolic interference: Inhibit bacterial DNA rotary enzyme (Topoisomerase), blocking DNA replication.<\/p>\n\n\n\n
Virus inhibition<\/p>\n\n\n\n
HA blockade: Binds to influenza virus hemagglutinin (HA) and prevents viral adsorption to host cells.<\/p>\n\n\n\n
Protease inhibition: Inhibits HIV protease activity and interferes with maturation of viral particles.<\/p>\n\n\n\n
Other mechanisms of action<\/p>\n\n\n\n
Hypoglycemia: regulates voltage-gated potassium channels (Kv), affects calcium inward flow in pancreatic \u03b2-cells, and promotes insulin secretion.<\/p>\n\n\n\n
Immunomodulation: Enhance macrophage phagocytic activity, promote lymphocyte proliferation, enhance NK cell toxicity.<\/p>\n","protected":false},"excerpt":{"rendered":"
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