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Mechanism of Action

Tiliroside (kaempferol 3-O-(2″-O-(E)-p-coumaroyl)-β-glucopyranoside) activates peroxisome proliferator-activated receptor alpha (PPARα), promoting fatty acid oxidation and reducing serum lipids. It inhibits aldose reductase, protecting against advanced glycation end product formation in hyperglycaemic conditions. Anti-inflammatory activity is mediated through inhibition of NF-κB transcription factor activation and downstream pro-inflammatory cytokine gene expression. It also modulates adenosine receptor signalling, contributing to the observed relaxation and mild sedation associated with linden flower.
Activates peroxisome proliferator-activated receptor gamma (PPARγ), a nuclear transcription factor regulating adipogenesis, insulin sensitivity, and inflammatory gene expression — providing a mechanistic basis for anti-inflammatory and metabolic effects. Inhibits NF-κB signaling and reduces pro-inflammatory cytokine transcription (TNF-α, IL-6). Activates Nrf2/HO-1 antioxidant pathway. Inhibits fatty acid synthase (FAS) and stimulates fatty acid β-oxidation via AMPK activation, contributing to anti-obesity and lipid-lowering effects in animal models.

Research Notes

Tiliroside has been identified as the primary bioactive flavonoid in linden flower by multiple European research groups using HPLC-MS profiling. Animal studies demonstrate anti-obesity, lipid-lowering, and anti-inflammatory effects in diet-induced obesity models. In vitro studies confirm PPARα activation and NF-κB inhibition at physiologically relevant concentrations. Limited human pharmacokinetic data exist, but absorption and metabolite profiles have been characterised in plasma after oral consumption of linden flower tea by healthy volunteers.

Tiliroside's PPARγ agonist activity has been characterized in adipocyte cell culture models and in high-fat diet obese mouse models, demonstrating significant improvements in insulin sensitivity, lipid profile, and body weight. Anti-inflammatory activity has been confirmed in multiple in vitro and rodent models at pharmacologically relevant doses. Direct clinical human trials specifically for tiliroside from linden are lacking; evidence is primarily preclinical with mechanistic plausibility for the traditional uses.

Found In 2 Herbs

3D Molecular Structure

Acylated flavonoid glycoside (kaempferol derivative)
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Tiliroside

Acylated flavonoid glycoside (kaempferol derivative)Polyphenolic antioxidants protecting cells from oxidative damage

Representative pattern: C₁₅H₁₀O₃

Atoms
Carbon
Oxygen

Live Research

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