# Hypolaetin

**Canonical URL:** https://ingredients.hermeticasuperfoods.com/ingredients/hypolaetin
**Data Source:** Hermetica Superfoods Ingredient Encyclopedia
**Updated:** 2026-04-04
**Evidence Score:** 4 / 10
**Category:** Compound
**Also Known As:** Hypolaetin-8-glucoside, Sideritis flavone, Mountain tea flavone, Mediterranean tea flavone, Sideritis mugronensis flavone

## Overview

Hypolaetin is a flavone aglycone (3',4',5,7-tetrahydroxyflavone) found in plants such as Sideritis species, exhibiting [anti-inflammatory](/ingredients/condition/inflammation) and gastroprotective effects primarily through inhibition of arachidonic acid [metabolism](/ingredients/condition/weight-management) and [free radical scaveng](/ingredients/condition/antioxidant)ing. Its primary mechanism involves suppression of cyclooxygenase and lipoxygenase pathways, reducing prostaglandin and leukotriene synthesis without the gastric side effects associated with classical NSAIDs.

## Health Benefits

• Gastroprotective effects: Demonstrated prevention of cold-restraint-induced gastric lesions comparable to cimetidine in rat models (PMID: 6151974) - animal evidence only • [Anti-inflammatory](/ingredients/condition/inflammation) activity: Superior to phenylbutazone in acute inflammation models without causing gastric erosions (PMID: 6151974) - preclinical evidence • Prostaglandin modulation: Stimulates protective prostaglandin synthesis and inhibits degradation (PMID: 3839399) - mechanistic studies only • Potential ulcer prevention: Related flavonoids show efficacy in human peptic ulcer patients (PMC6253827) - indirect evidence • Mucosal protection: Enhanced prostacyclin release promotes gastric mucosal defense (PMID: 3839399) - animal studies only

## Mechanism of Action

Hypolaetin inhibits both cyclooxygenase (COX) and lipoxygenase (LOX) enzymes, reducing the biosynthesis of pro-inflammatory [prostaglandin](/ingredients/condition/inflammation)s and leukotrienes derived from arachidonic acid. It also acts as a potent free radical scavenger due to its polyhydroxylated B-ring structure, particularly the 3',4'-catechol moiety, which donates hydrogen atoms to neutralize [reactive oxygen species](/ingredients/condition/antioxidant). Additionally, hypolaetin has been shown to modulate gastric mucosal protection potentially through preservation of prostaglandin E2-dependent cytoprotective mechanisms at the gastric epithelium.

## Clinical Summary

Available evidence for hypolaetin is limited exclusively to preclinical animal studies, with no published human clinical trials identified to date. In rat models of cold-restraint-induced gastric ulceration, hypolaetin demonstrated gastroprotective efficacy comparable to the H2 blocker cimetidine (PMID: 6151974). Separate rodent acute inflammation models showed hypolaetin surpassed phenylbutazone in [anti-inflammatory](/ingredients/condition/inflammation) potency while avoiding the gastric erosions that phenylbutazone typically induces (PMID: 6151974 and related work). The overall evidence base is early-stage and animal-derived, making extrapolation to human clinical outcomes premature.

## Nutritional Profile

Hypolaetin (5,7,8,3',4'-pentahydroxyflavone; C₁₅H₁₀O₇; MW 302.24 g/mol) is a naturally occurring flavone aglycone, not a nutritional food source per se but rather a bioactive polyphenolic compound found in trace quantities in select plant species. Key details: • Chemical class: Flavone (a subclass of flavonoids), structurally related to luteolin but with an additional hydroxyl group at the C-8 position on the A-ring. • Natural sources: Found in Sideritis species (ironwort/mountain tea), particularly Sideritis mugronensis and other Mediterranean Sideritis spp.; also reported in Bystropogon species and certain Lamiaceae family plants. Concentrations in dried Sideritis herba are typically in the range of 0.01–0.5% w/w depending on species, plant part, and extraction method. • Glycosidic forms: Commonly occurs as hypolaetin-8-glucoside (C₂₁H₂₀O₁₂; MW 464.38) in plant tissues, which undergoes partial hydrolysis to the aglycone during [digestion](/ingredients/condition/gut-health). • Bioavailability: Like most polyhydroxylated flavones, oral bioavailability is expected to be low (estimated <5–10% based on structural analogs such as luteolin), limited by poor aqueous solubility, extensive Phase II conjugation (glucuronidation and sulfation in intestinal and hepatic tissues), and potential microbial [metabolism](/ingredients/condition/weight-management) in the colon. The 8-glucoside form may have modestly improved absorption compared to the free aglycone due to SGLT1-mediated intestinal uptake of the glycoside. • Key functional groups: Five free phenolic hydroxyl groups (positions 5, 7, 8, 3', 4') conferring strong radical-scavenging and metal-chelating capacity; the catechol moiety on the B-ring (3',4'-dihydroxy) and the pyrogallol-type arrangement on the A-ring (5,7,8-trihydroxy) contribute to high [antioxidant](/ingredients/condition/antioxidant) potential (ORAC and DPPH activity generally superior to monohydroxylated flavones). • Caloric/macronutrient contribution: Negligible — consumed in microgram-to-low-milligram quantities from herbal tea infusions (e.g., a typical 200 mL Sideritis tea infusion may deliver approximately 0.5–5 mg total hypolaetin equivalents including glycosides). No meaningful protein, fat, carbohydrate, or fiber contribution. • No recognized vitamin or mineral content intrinsic to the isolated compound. • Solubility: Sparingly soluble in water (~0.1–0.5 mg/mL at 25°C); soluble in DMSO, methanol, and ethanol. Infusion in hot water as traditional herbal tea partially extracts the glycosidic forms.

## Dosage & Preparation

No human dosages have been established due to absence of clinical trials. Animal studies used ED50 values of 57.3-68.0 mg/kg for gastroprotective effects. Traditional preparation involves herbal infusions of whole Sideritis plant material. Consult a healthcare provider before starting any new supplement.

## Safety & Drug Interactions

No human safety data or clinical toxicology studies for isolated hypolaetin have been published, making a definitive safety profile impossible to establish. Based on its COX and LOX inhibitory activity, theoretical interactions with anticoagulants such as warfarin, antiplatelet drugs, and other NSAIDs are plausible and warrant caution. Pregnancy and lactation safety is entirely unknown, and use should be avoided in those populations until data exist. Animal studies did not report gastric erosions at tested doses, suggesting a potentially favorable GI tolerability profile compared to phenylbutazone, but this has not been confirmed in humans.

## Scientific Research

Research on hypolaetin is limited to preclinical animal studies, with no published human clinical trials identified. Key studies include rat models showing [anti-inflammatory](/ingredients/condition/inflammation) and gastroprotective effects (PMID: 6151974) and mechanistic research on prostaglandin pathways (PMID: 3839399). Human clinical evidence remains absent, representing a critical research gap.

## Historical & Cultural Context

Sideritis mugronensis has been used for centuries in Mediterranean traditional medicine, particularly in Spain and Greece, where it's consumed as 'mountain tea' for gastrointestinal complaints and [inflammation](/ingredients/condition/inflammation). Traditional use involves whole plant infusions rather than isolated hypolaetin compounds.

## Synergistic Combinations

Quercetin, Kaempferol, Piperine, Phosphatidylcholine, Zinc-carnosine

## Frequently Asked Questions

### What is hypolaetin and what plants is it found in?

Hypolaetin is a polyhydroxylated flavone (3',4',5,7-tetrahydroxyflavone) classified as a flavone aglycone. It is found naturally in Sideritis species (commonly called ironworts or mountain tea) as well as in certain Helichrysum and Satureja plant species. It can also occur as the aglycone released from its glycoside form, hypolaetin-8-glucoside.

### How does hypolaetin compare to ibuprofen or phenylbutazone as an anti-inflammatory?

In acute rodent inflammation models, hypolaetin demonstrated superior anti-inflammatory activity compared to phenylbutazone, a potent NSAID, while notably not inducing the gastric erosions that phenylbutazone causes at effective doses. This dual profile—strong COX/LOX inhibition paired with gastric tolerability—distinguishes it mechanistically from classical NSAIDs that cause GI damage through prostaglandin depletion in the stomach. No direct human comparisons to ibuprofen or phenylbutazone exist.

### Can hypolaetin protect the stomach lining?

Preclinical rat studies showed hypolaetin prevented cold-restraint-induced gastric lesions at efficacy levels comparable to cimetidine, a standard H2-receptor antagonist used to treat ulcers (PMID: 6151974). The proposed mechanism involves preservation of gastric mucosal prostaglandin E2 synthesis and free radical scavenging at the gastric epithelium. However, this gastroprotective effect has only been demonstrated in animal models and requires human clinical validation.

### Is there a recommended dosage for hypolaetin supplements?

No clinically established or regulatory-approved dosage exists for isolated hypolaetin in humans, as no human pharmacokinetic or dose-ranging trials have been published. Effective doses in rat studies cannot be reliably converted to human equivalents without allometric scaling data specific to this compound. Hypolaetin is more commonly consumed as part of whole Sideritis species herbal teas rather than as an isolated supplement.

### Does hypolaetin interact with blood thinners or other medications?

Hypolaetin's inhibition of COX and LOX enzymes creates a theoretical risk of pharmacodynamic interaction with anticoagulants like warfarin, antiplatelet agents such as aspirin or clopidogrel, and other NSAIDs, potentially enhancing bleeding risk or altering drug metabolism. Flavonoids with catechol B-ring structures can also inhibit cytochrome P450 enzymes (notably CYP1A2 and CYP3A4), which could affect plasma levels of co-administered drugs. No human drug-interaction studies for isolated hypolaetin have been conducted, so these remain theoretical concerns based on structural and mechanistic analogy.

### What is the quality of clinical evidence for hypolaetin's anti-inflammatory effects in humans?

Current evidence for hypolaetin is primarily limited to preclinical and animal studies, with no published clinical trials in humans to date. While rat models show hypolaetin has superior anti-inflammatory activity compared to phenylbutazone without causing gastric damage, these findings cannot be directly extrapolated to human efficacy or safety. More rigorous human studies are needed before hypolaetin can be recommended as a proven therapeutic agent for inflammation.

### Who would benefit most from hypolaetin supplementation based on current research?

Based on animal research, hypolaetin may theoretically benefit individuals seeking natural anti-inflammatory support with gastric protection, as it demonstrated both anti-inflammatory effects and prevention of gastric lesions in preclinical models. However, without human clinical trials, it is not possible to identify specific populations or conditions where hypolaetin would be most effective. Anyone considering hypolaetin supplementation should consult a healthcare provider, as the lack of human data limits personalized recommendation.

### What forms of hypolaetin are available for supplementation and how is it typically sourced?

Hypolaetin is primarily obtained from plant sources such as Kalanchoe and Achillea species, and is available in supplement form typically as part of herbal extracts or standardized plant preparations rather than as an isolated compound. Bioavailability data for different hypolaetin formulations in humans is lacking, so comparisons between capsules, extracts, or other delivery methods cannot be made on an evidence-based level. The concentration and purity of hypolaetin in supplements can vary significantly between manufacturers due to the lack of standardized extraction and quality control protocols.

---

*Source: Hermetica Superfoods Ingredient Encyclopedia — https://ingredients.hermeticasuperfoods.com*
*License: CC BY-NC-SA 4.0 — Attribution required. Commercial use: admin@hermeticasuperfoods.com*