Luteoloside (Luteolin 7-O-glucoside)

Luteoloside, also called luteolin 7-O-glucoside, is a flavone glycoside found in plants such as peanut hulls, celery, and perilla leaves, where luteolin is bound to glucose at the 7-position for improved water solubility. Its primary mechanisms include inhibition of NF-κB signaling and activation of SIRT1, driving anti-inflammatory and antifibrotic effects documented in preclinical models.

Origin & History

Luteoloside (luteolin 7-O-glucoside) is a flavonoid glycoside, specifically a monoglucoside derivative of luteolin. While naturally occurring in various plants, specific source organisms were not detailed in available research. It is commercially available as a high-purity compound (≥98% HPLC) from suppliers like Shanghai Yuan Ye Biotechnology Co., Ltd.

Historical & Cultural Context

No information on historical or traditional medicinal uses of luteoloside was found in available research. Current data focuses exclusively on modern pharmacological research conducted since recent decades.

Health Benefits

• Anti-inflammatory effects: Reduced inflammatory pain and cytokine levels (IL-1β) in mouse models at 20-80 mg/kg doses (preclinical evidence only)
• Pulmonary fibrosis protection: Demonstrated reduced lung fibrosis and oxidative stress via SIRT1 activation in bleomycin-induced mouse models (PMID: 41162593, animal study)
• Anti-cancer properties: Inhibited cervical cancer cell proliferation and induced apoptosis through MAPK/mTOR pathways (in vitro evidence only)
• Neuroprotective potential: Suppressed neuroinflammation markers and microglial activation in preclinical pain models (animal evidence)
• Cellular senescence prevention: Reduced age-related cell markers in pulmonary tissues through SIRT1 pathway (preclinical models only)

How It Works

Luteoloside suppresses the NF-κB signaling pathway, reducing transcription of pro-inflammatory cytokines including IL-1β, TNF-α, and IL-6. It activates the NAD-dependent deacetylase SIRT1, which in turn downregulates TGF-β1-driven fibroblast activation and collagen deposition, explaining its antifibrotic activity in lung tissue. Additionally, it scavenges reactive oxygen species and upregulates endogenous antioxidant enzymes such as superoxide dismutase and catalase, reducing oxidative stress markers.

Scientific Research

No human clinical trials, RCTs, or meta-analyses were identified for luteoloside. All available evidence comes from preclinical studies including mouse inflammatory pain models (20-80 mg/kg IP doses), bleomycin-induced pulmonary fibrosis models (PMID: 41162593), and in vitro cancer cell studies. Human dental pulp cell studies also showed protective effects against methylglyoxal damage (PMID: 38505968).

Clinical Summary

Available evidence for luteoloside is currently limited to in vitro cell studies and rodent in vivo models; no published human clinical trials exist for this specific glycoside form. In bleomycin-induced pulmonary fibrosis mouse models, luteoloside reduced lung hydroxyproline content and oxidative stress markers via SIRT1 activation. Anti-inflammatory studies in mouse models used doses of 20–80 mg/kg, demonstrating significant reductions in IL-1β and inflammatory pain behaviors compared to controls. The translation of these preclinical findings to human efficacy and safe dosing ranges has not yet been established.

Nutritional Profile

Luteoloside (Luteolin 7-O-glucoside) is a flavone glycoside, not a macronutrient source. It is a pure bioactive compound with molecular formula C21H20O11 and molecular weight of 448.38 g/mol. It consists of the flavone aglycone luteolin attached to a glucose moiety at the 7-position via a glycosidic bond. As a compound rather than a food, it contains no meaningful protein, fat, or fiber content. Key bioactive characteristics: flavone backbone with hydroxyl groups at positions 3', 4', 5, and 7, conferring antioxidant capacity. Naturally occurring in chrysanthemum flowers (Chrysanthemum morifolium) at concentrations ranging approximately 0.5–8 mg/g dry weight depending on cultivar and extraction method; also found in peanut hulls, celery, and various herbs. Bioavailability is limited by the glycosidic bond — intestinal and microbial beta-glucosidases cleave glucose to release free luteolin in the gut, with absorption primarily in the small intestine and colon. Oral bioavailability of luteolin-type flavones is generally estimated at 3–10% in humans based on pharmacokinetic studies. Peak plasma concentrations in rodent studies at 20–80 mg/kg doses show detectable serum levels within 1–2 hours post-administration. Undergoes hepatic phase II metabolism (glucuronidation, sulfation, methylation). No established Dietary Reference Intake (DRI) or Recommended Daily Allowance (RDA) exists; it is not classified as an essential nutrient. Micronutrient content is not applicable as this is an isolated phytochemical compound.

Preparation & Dosage

No human dosage data available. Preclinical mouse studies used intraperitoneal doses of 20-80 mg/kg, with peak effects at 2 hours and sustained benefits after 13-14 daily doses. All studies used pure luteoloside powder (>98% purity) rather than plant extracts. Consult a healthcare provider before starting any new supplement.

Synergy & Pairings

Celecoxib (low-dose), SIRT1 activators, PPARγ agonists, Nrf2 activators, Anti-inflammatory compounds

Safety & Interactions

No formal human safety or toxicology studies have been conducted specifically on luteoloside, making definitive side-effect and interaction profiles unavailable. As a flavone glycoside structurally related to luteolin, it may share luteolin's potential to inhibit cytochrome P450 enzymes (particularly CYP1A2 and CYP2C8), which could theoretically alter metabolism of co-administered drugs such as warfarin or statins. Pregnant and breastfeeding individuals should avoid supplemental use due to a complete absence of safety data in these populations. Individuals on anticoagulant or anti-platelet medications should exercise caution given the anti-inflammatory and potential platelet-modulating properties of flavonoids in this class.