Tiliroside

Tiliroside is a kaempferol-based flavonoid glycoside found in plants such as rosehip, strawberry, and linden flower, where it exerts antioxidant and anti-inflammatory effects primarily by scavenging reactive oxygen species and inhibiting pro-inflammatory enzyme cascades. Most evidence for its health effects comes from in vitro and animal models, with no completed human clinical trials to date.

Origin & History

Tiliroside is a natural glycosidic flavonoid (kaempferol 3-O-β-D-(6''-E-p-coumaroyl)-glucopyranoside) found in various plants including Tilia (linden), Rosa rugosa (rose hips), strawberries, raspberries, and Potentilla chinensis. It is extracted using ethanol or ethyl acetate partitioning followed by silica gel chromatography, yielding compounds with >98-99% purity.

Historical & Cultural Context

Tiliroside occurs in plants with traditional medicinal uses, including Agrimonia pilosa in Traditional Chinese Medicine and Tilia americana (basswood) in folklore. While found in common dietary sources like rose hips, strawberries, and raspberries, specific traditional applications for tiliroside itself are not documented.

Health Benefits

• Antioxidant activity - reported in preclinical studies only, no human evidence
• Anti-inflammatory effects - based solely on preclinical research, no clinical trials
• Antidiabetic potential - preliminary evidence from non-human studies only
• Antimicrobial properties - limited to laboratory studies without human data
• Hepatoprotective effects - suggested by preclinical research but lacking human validation

How It Works

Tiliroside inhibits nuclear factor kappa-B (NF-κB) signaling and suppresses cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression, reducing downstream production of pro-inflammatory cytokines such as TNF-α and IL-6. It activates AMP-activated protein kinase (AMPK), which enhances glucose uptake in skeletal muscle cells and improves insulin sensitivity in animal models of type 2 diabetes. Its antioxidant activity is attributed to the catechol-like hydroxyl groups on its kaempferol backbone, which directly neutralize superoxide and hydroxyl radicals and upregulate endogenous antioxidant enzymes including superoxide dismutase and catalase.

Scientific Research

No human clinical trials, randomized controlled trials, or meta-analyses for tiliroside were identified in the available sources. All evidence is limited to preclinical laboratory and animal studies reporting various bioactivities without any human data or specific study designs with PMIDs.

Clinical Summary

To date, no published randomized controlled trials have examined tiliroside in human subjects, meaning all efficacy data derive from cell culture studies and rodent experiments. In murine models of type 2 diabetes, oral tiliroside administration at doses of 10–30 mg/kg/day reduced fasting blood glucose by approximately 20–35% and improved insulin tolerance test outcomes compared to controls. Anti-inflammatory findings are similarly limited to lipopolysaccharide-stimulated macrophage assays and carrageenan-induced paw edema rodent models, which demonstrated significant but non-translatable reductions in inflammatory markers. The overall evidence base is preliminary and insufficient to support clinical recommendations or therapeutic dosing guidelines for humans.

Nutritional Profile

Tiliroside is a glycosidic flavonoid (kaempferol 3-O-glucoside esterified with p-coumaric acid), classified as an acylated flavonol glycoside with molecular formula C30H26O13 and molecular weight of 594.52 g/mol. It is not a food ingredient per se but a bioactive phytochemical found in trace concentrations across multiple plant sources: rose hips (Rosa canina) at approximately 0.1–1.2 mg/g dry weight, strawberry (Fragaria species) leaves at 0.5–2.0 mg/g dry weight, linden flowers (Tilia species) at 0.3–0.8 mg/g dry weight, and raspberry leaves at measurable but low concentrations. As a pure compound, it contains no macronutrients (zero protein, fat, or carbohydrate caloric value in dietary context), no vitamins, and no minerals. Its bioactive value lies entirely in its polyphenolic structure: the kaempferol aglycone backbone provides the core flavonoid activity, the glucose moiety influences water solubility (moderate aqueous solubility ~0.1 mg/mL), and the p-coumaroyl ester group contributes to lipophilic interactions and membrane permeability. Bioavailability is limited and variable: oral bioavailability is considered low due to intestinal hydrolysis and first-pass metabolism; gut microbiota partially hydrolyze the glycoside to release kaempferol and glucose, with kaempferol then undergoing further microbial metabolism to phenolic acids. Studies in rodents suggest peak plasma concentrations are reached within 1–2 hours post-ingestion. No standardized human pharmacokinetic data are available. It is typically studied in isolated or standardized extract form at experimental doses of 10–100 mg/kg in preclinical models, with no established dietary reference intake or therapeutic dose in humans.

Preparation & Dosage

No clinically studied dosage ranges have been established for tiliroside as human trials are absent. No forms (extract, powder, standardized) or standardization details have been reported in clinical contexts. Consult a healthcare provider before starting any new supplement.

Synergy & Pairings

Kaempferol, quercetin, apigenin, rose hip extract, vitamin C

Safety & Interactions

No formal human safety trials have been conducted for isolated tiliroside, so a comprehensive adverse effect profile has not been established. Because tiliroside activates AMPK pathways that influence glucose metabolism, concurrent use with insulin or oral hypoglycemic agents such as metformin theoretically carries a risk of additive hypoglycemia, warranting caution. Its structural similarity to kaempferol suggests a potential for weak inhibition of cytochrome P450 enzymes (particularly CYP3A4 and CYP2C9), which could affect the metabolism of co-administered drugs, though this has not been confirmed in human pharmacokinetic studies. Pregnant and breastfeeding individuals should avoid isolated tiliroside supplements due to the complete absence of safety data in these populations.