Troxerutin for Anti-oxidation, Microcirculation Improvement, Anti-aging and Skin Protection

1. Description

Troxerutin, Chemical name: 7,3,4-tri(O-(2-hydroxyhexyl))rutin; it is a mixture of hydroxyethylrutin obtained by hydroxyethylation of rutin. It appears as a yellow, yellow-green, or light brownish-yellow powder, is odorless, slightly salty, and hygroscopic; its main hydrolysis product is hyperoside. Troxerutin is a semi-synthetic flavonoid compound produced by the hydroxylation of rutin. It inhibits red blood cell and platelet aggregation while increasing blood oxygen levels, improving microcirculation, and promoting the formation of new blood vessels. It is an effective drug for treating occlusive cerebrovascular diseases, protecting endothelial cells, and treating acute ischemic brain injury; it also has anti-radiation, anti-inflammatory, anti-allergic, and anti-ulcer effects. It is the main component of Weinaolutong and is commonly formulated into tablets .

2. Application

(1) Studies on Chronic Venous Insufficiency: Used to treat chronic venous insufficiency, clinical studies have shown that it reduces leg edema and improves subjective symptoms, and has a positive effect on capillary perfusion and venous stasis. Research indicates that trichlouridine reduces red blood cell aggregation, improves capillary perfusion, and has a positive effect on the nutritional complications of chronic venous insufficiency.

(2) Neuroprotection and Cognitive Studies: In D-galactose-induced models of oxidative stress and cognitive impairment, it is used to investigate the mechanisms underlying the alleviation of cognitive decline. Studies indicate that trichloroacetic acid reduces levels of protein carbonyls, reactive oxygen species, and advanced glycation end products (AGEs), enhances PI3K/Akt activation, and improves learning and memory abilities.

(3) Ocular Disease Research: In early-stage models of streptozotocin-induced diabetic retinopathy, it is being studied for its role in inhibiting retinal neovascularization and vascular endothelial growth factor (VEGF) expression.

(4) Cardiovascular Disease Research: In studies involving patients with acute myocardial infarction, it is used to investigate its role in reducing plasma levels of α-aminocaproic acid, homocysteine, triglycerides, cholesterol, and low-density lipoprotein apolipoprotein B.

(5) Oxidative Stress and DNA Protection Research: Used to investigate the mechanisms by which it protects membrane structures from oxidative DNA damage, effectively inhibiting oxidative damage caused by neutrophils and γ-radiation.

(6) Anti-inflammatory and Immunomodulatory Research: Used to investigate the anti-inflammatory mechanisms involving the inhibition of lipid peroxidation and the regulation of NF-κB p65, iNOS, and COX-2 expression.

3. Main Efficacy

(1) Antioxidant effects: Inhibits the production of reactive oxygen species, reduces levels of protein carbonyls and advanced glycation end products, and protects cells from oxidative stress damage. Trichlouridine effectively inhibits the generation of superoxide anions and hydroxyl radicals, protecting red blood cell membranes from lipid peroxidation damage.

(2) Anti-inflammatory effects: Inhibits endoplasmic reticulum stress-mediated activation of the NOD-like receptor 3 inflammasome, regulates the NF-κB signaling pathway, reduces the production of pro-inflammatory cytokines such as tumor necrosis factor-α, interleukin-1β, and interleukin-6, and alleviates inflammatory responses.

(3) Vascular protective effects: It reduces erythrocyte aggregation, lowers blood viscosity, improves capillary perfusion, and protects vascular endothelial function, exerting a positive effect on nutritional complications associated with chronic venous insufficiency.

(4) Antithrombotic effects: It inhibits platelet aggregation, lowers fibrinogen levels, enhances fibrinolytic activity, and prevents thrombus formation.

(5) Neuroprotective effects: By enhancing PI3K/Akt activation, it attenuates D-galactose-induced oxidative stress and cognitive impairment, and improves learning and memory abilities.

(6) Cardiovascular protection: Reduces plasma levels of homocysteine, triglycerides, cholesterol, and LDL in patients with acute myocardial infarction, thereby improving the lipid profile.

(7) DNA protection: Protects membrane structures from oxidative DNA damage and effectively inhibits γ-radiation-induced DNA strand breaks.

(8) Ocular protection: In the early stages of diabetic retinopathy, it inhibits the upregulation of vascular endothelial growth factor (VEGF) in the retina, reducing neovascularization and microaneurysms.

(9) Enzyme inhibitory activity: It inhibits aldose reductase activity (IC₅₀ = 3.0 μM), potentially playing a role in preventing diabetic complications.