# Cineole (1,8-Cineole / Eucalyptol)

**Canonical URL:** https://ingredients.hermeticasuperfoods.com/ingredients/cineole-18-cineole-eucalyptol
**Data Source:** Hermetica Superfoods Ingredient Encyclopedia
**Updated:** 2026-04-02
**Evidence Score:** 1 / 10
**Category:** Compound
**Also Known As:** C₁₀H₁₈O, 1,8-Epoxy-p-menthane, Eucalyptol, Cajeputol, Eucalyptol (1,8-Cineole), 1,8-Cineole

## Overview

1,8-Cineole is a lipophilic monoterpene that simultaneously modulates multiple inflammatory signaling pathways—including COX-2, NF-κB, MAPK, IL-6, and TNF-α—through polypharmacological binding with affinities ranging from −5.2 to −6.8 kcal/mol. In a cerulein-induced acute pancreatitis animal model, oral doses of 100–400 mg/kg significantly reduced serum amylase, lipase, and [pro-inflammatory cytokine](/ingredients/condition/inflammation)s (TNF-α, IL-1β, IL-6) while elevating anti-inflammatory IL-10 at all tested doses (p < 0.05).

## Health Benefits

- **[Anti-Inflammatory](/ingredients/condition/inflammation) Action**: 1,8-Cineole suppresses key inflammatory mediators including COX-2, NF-κB, and TNF-α through polypharmacological binding, making it relevant across multiple inflammatory conditions rather than a single disease target.
- **Expectorant and Mucolytic Effects**: By modulating airway secretion and ciliary beat frequency, cineole facilitates mucus clearance from the respiratory tract, supporting its traditional and contemporary use in bronchitis and upper respiratory conditions.
- **[Antioxidant Activity](/ingredients/condition/antioxidant)**: Cineole reduces oxidative stress markers in inflamed tissues, contributing to its cytoprotective effects observed in acute pancreatitis models where it lowered lipid peroxidation alongside cytokine suppression.
- **CNS Penetration and [Neuroprotective](/ingredients/condition/cognitive) Potential**: Its strong blood-brain barrier permeability, confirmed by pharmacokinetic modeling, suggests potential neuroprotective roles, though human clinical evidence for this indication remains limited.
- **[Antimicrobial](/ingredients/condition/immune-support) Properties**: Essential oils standardized to high cineole content demonstrate broad-spectrum antimicrobial activity against respiratory pathogens, supporting its use as an adjunct in infectious respiratory conditions.
- **Pancreatic Cytoprotection**: At oral doses of 200–400 mg/kg in rodent models, cineole reduced cerulein-induced pancreatic edema and normalized serum amylase and lipase levels, suggesting a protective role in acute pancreatitis.
- **Analgesic Activity**: Via inhibition of MAPK signaling and reduction of pro-inflammatory prostaglandins, cineole contributes to pain attenuation in models of inflammatory pain, though robust human trials are lacking.

## Mechanism of Action

1,8-Cineole operates through polypharmacological inhibition, simultaneously binding to and modulating multiple inflammatory targets rather than acting on a single receptor; molecular docking studies demonstrate binding energies of −5.2 to −6.8 kcal/mol against COX-2, IL-6, MAPK, NF-κB, and TNF-α. At the transcriptional level, cineole suppresses NF-κB nuclear translocation, thereby reducing downstream expression of [pro-inflammatory cytokine](/ingredients/condition/inflammation)s including TNF-α, IL-1β, and IL-6, while concurrently upregulating the anti-inflammatory cytokine IL-10. Its lipophilic character (log P favorable for membrane penetration) allows it to integrate into cell membranes and modulate lipid raft-dependent signaling cascades involved in immune cell activation. Additionally, cineole's 92.7% plasma protein binding and strong BBB permeability suggest it may engage central neuroimmune pathways, extending its anti-inflammatory reach beyond peripheral tissues.

## Clinical Summary

Clinical evidence for 1,8-cineole is currently strongest in preclinical and computational domains, with mechanistic support from molecular docking studies showing consistent binding to five key [inflammatory](/ingredients/condition/inflammation) mediators. The most controlled experimental data derive from rodent acute pancreatitis models demonstrating statistically significant normalization of pancreatic enzymes and inflammatory cytokines across a dose range of 100–400 mg/kg. Human trials with defined endpoints, blinding, and adequate power are largely absent from the peer-reviewed record as of the current evidence review, meaning effect sizes and number-needed-to-treat figures cannot be reliably extrapolated to clinical practice. Confidence in cineole's efficacy for respiratory indications is somewhat higher due to its established pharmacopoeial status in eucalyptus oil formulations and long history of clinical use, but rigorously controlled human RCT data remain needed to confirm optimal dosing and comparative effectiveness.

## Nutritional Profile

1,8-Cineole is a pure monoterpene oxide (C₁₀H₁₈O; molecular weight 154.25 g/mol) and does not contribute meaningful macronutrients, vitamins, or minerals in typical supplemental doses. It is a colorless, lipophilic liquid with a melting point of −1.3 °C and boiling point of 177 °C, properties that confer its volatility in essential oil matrices. As a bioactive phytochemical rather than a nutrient, its health relevance derives entirely from pharmacological activity rather than nutritional contribution. Key bioavailability factors include high lipophilicity enabling membrane penetration, 92.7% plasma protein binding yielding prolonged systemic exposure, a volume of distribution of 0.44 L/kg indicating moderate tissue partitioning, and full compliance with Lipinski's rule of five supporting oral absorption.

## Dosage & Preparation

- **Eucalyptus Essential Oil (inhalation)**: Standardized to ≥70% 1,8-cineole per European Pharmacopoeia; used via steam inhalation or diffuser for upper respiratory support; no universally established inhalation dose in mg.
- **Oral Capsules/Enteric-Coated Softgels**: Pharmaceutical preparations such as Soledum (cineole 200 mg capsules) have been used clinically in Europe for bronchitis and sinusitis at doses of 200–400 mg two to three times daily in adults.
- **Topical/Chest Rub Formulations**: Eucalyptus oil preparations applied externally to the chest for decongestant effects; concentration typically 1–5% cineole in carrier oil.
- **Animal Study Reference Doses**: 100–400 mg/kg oral dosing produced significant [anti-inflammatory](/ingredients/condition/inflammation) effects in rodent models; these doses do not directly translate to human equivalents without allometric scaling.
- **Standardization Note**: Commercial eucalyptus oil should be verified to contain ≥70% cineole for therapeutic consistency; rosemary and myrtle oils contain lower concentrations (15–31%) and are not equivalent on a per-volume basis.
- **Timing**: Oral enteric-coated forms are typically taken with meals to minimize gastric irritation; the short plasma half-life (~1.14 hours) suggests divided dosing may be necessary for sustained effect.

## Safety & Drug Interactions

At supplemental doses used in oral pharmaceutical preparations (200–400 mg/day in adults), 1,8-cineole is generally well tolerated, though formal human safety data are limited; the acute oral LD₅₀ in mice is 680 mg/kg, and no adverse effects were observed at single doses up to 400 mg/kg, while dose-dependent toxicity appeared at 800–1000 mg/kg (83.3% mortality at 1000 mg/kg in rodents). Sub-chronic rodent studies at up to 20 mg/kg over 14 days showed no significant changes in body weight, behavior, renal function, or hematological parameters, and in silico toxicity prediction identified no mutagenic, carcinogenic, hepatotoxic, or cardiotoxic signals. Direct topical application or ingestion of undiluted eucalyptus essential oil poses a risk of mucous membrane irritation, and oral ingestion of large amounts of the neat oil has caused toxicity in children, necessitating that products be kept away from pediatric populations. Specific drug interaction data are sparse in the current literature; given its CYP450 [metabolism](/ingredients/condition/weight-management) as a terpene, potential interactions with CYP-metabolized drugs (e.g., anticoagulants, sedatives) cannot be excluded, and use during pregnancy or lactation should be avoided until human safety data are established.

## Scientific Research

The current body of evidence for 1,8-cineole is predominantly preclinical, consisting of in vitro receptor-binding and molecular docking studies alongside animal models; robust, large-scale randomized controlled trials in humans are sparse. The most quantitatively detailed animal study (Lima et al., 2013) employed a cerulein-induced acute pancreatitis model and demonstrated dose-dependent reductions in serum amylase and lipase at 100, 200, and 400 mg/kg oral doses, with pancreatic edema reduction at the two higher doses (p < 0.05). Pharmacokinetic parameters including a half-life of 1.14 hours, plasma protein binding of 92.7%, and compliance with Lipinski, Pfizer, and GSK drug-likeness rules have been computationally established, supporting theoretical oral bioavailability. Human clinical trial data with defined sample sizes, effect sizes, and controlled designs remain limited in the published literature reviewed, and the evidence base does not yet support definitive therapeutic dosing guidelines for humans.

## Historical & Cultural Context

1,8-Cineole was first chemically described by the French chemist Cloez in 1870, though the medicinal use of eucalyptus-derived preparations predates its chemical isolation by indigenous Australian Aboriginal communities who used eucalyptus leaves for wound treatment and respiratory ailments. In European phytomedicine, eucalyptus oil rich in cineole became a standard pharmacopoeial ingredient during the 19th century, incorporated into remedies for bronchitis, colds, and febrile infections in British, German, and French pharmacopoeias. Traditional Mediterranean herbalism also leveraged rosemary and myrtle, both significant cineole sources, as culinary and medicinal plants for digestive, [antimicrobial](/ingredients/condition/immune-support), and invigorating purposes. The compound's enduring presence in modern pharmacopoeia and over-the-counter respiratory products across Europe and Asia reflects a centuries-long convergence of traditional and evidence-based use.

## Synergistic Combinations

1,8-Cineole may exhibit additive or synergistic [anti-inflammatory](/ingredients/condition/inflammation) effects when combined with other terpene-based anti-inflammatory compounds such as alpha-pinene and limonene, as found in full-spectrum eucalyptus preparations, where combined modulation of NF-κB and COX-2 pathways may exceed isolated-compound activity. In the context of respiratory health, formulations pairing cineole with thymol or menthol leverage complementary mucolytic and [antimicrobial](/ingredients/condition/immune-support) mechanisms, a rationale underlying many traditional compound chest preparations. Preliminary evidence also suggests that cineole's upregulation of anti-inflammatory IL-10 may complement the action of omega-3 fatty acids (EPA/DHA), which similarly shift cytokine balance toward resolution, though direct combination studies in humans are not yet available.

## Frequently Asked Questions

### What is 1,8-cineole and what are its main health benefits?

1,8-Cineole, also called eucalyptol, is a monoterpene oxide found in eucalyptus, rosemary, and myrtle essential oils that acts as a natural anti-inflammatory and expectorant. Its primary benefits include suppression of COX-2, NF-κB, TNF-α, and IL-6 inflammatory pathways, mucus clearance from the respiratory tract, and antimicrobial activity against respiratory pathogens, with preclinical data also supporting pancreatic cytoprotection at oral doses of 100–400 mg/kg.

### What is the recommended dose of cineole for respiratory conditions?

European pharmaceutical preparations such as Soledum deliver 200 mg of 1,8-cineole per enteric-coated capsule, typically dosed two to three times daily in adults for bronchitis or sinusitis. There is no universally validated human RCT-established optimal dose; animal studies used 100–400 mg/kg orally, which does not directly translate to human dosing, and individuals should follow product labeling or consult a healthcare provider.

### Is cineole safe to take orally?

Oral enteric-coated cineole at pharmaceutical doses (200–400 mg per day in adults) is generally considered well tolerated based on available data, with an oral LD₅₀ of 680 mg/kg in mice and no adverse effects at single doses up to 400 mg/kg. However, ingestion of undiluted eucalyptus essential oil is hazardous and potentially fatal in children; undiluted oil should never be ingested, and formal long-term human safety studies are still limited.

### How does cineole work as an anti-inflammatory?

Cineole exerts anti-inflammatory effects through polypharmacological binding to multiple inflammatory targets simultaneously, including COX-2, NF-κB, MAPK, IL-6, and TNF-α, with molecular docking binding energies of −5.2 to −6.8 kcal/mol. It suppresses NF-κB nuclear translocation to reduce cytokine gene expression while upregulating anti-inflammatory IL-10, and its lipophilicity allows it to integrate into cell membranes to modulate signaling cascades driving immune activation.

### Which plants contain the highest amounts of cineole?

Eucalyptus globulus essential oil contains the highest concentrations, with medicinal-grade oil required to contain at least 70% 1,8-cineole per the European Pharmacopoeia. Other significant sources include myrtle essential oil (~31%), rosemary (Rosmarinus officinalis, 15–30%), and Lavandula pedunculata (12–34%), though these lower-concentration sources are not equivalent to eucalyptus oil for therapeutic cineole delivery.

### Does cineole interact with asthma medications or bronchodilators?

Cineole may potentiate the effects of bronchodilators like salbutamol by enhancing airway relaxation through complementary mechanisms, though clinical interactions are not well-documented. Because cineole can affect airway smooth muscle and mucus production, concurrent use with prescription respiratory medications should be discussed with a healthcare provider to avoid unintended synergistic effects. No major contraindications have been reported, but dosing adjustments may be warranted in patients on active asthma management.

### Is cineole safe for children, and what age groups can use it?

Cineole is generally recognized as safe for children in food-based sources like eucalyptus tea or lozenges, but concentrated supplements should be used cautiously in children under 6 years due to limited safety data and risk of aspiration. Children aged 6–12 may tolerate diluted forms or herbal products containing cineole at reduced doses, though parental supervision is essential. For children over 12, dosing can approach adult recommendations, but consultation with a pediatrician is advised before supplementation.

### What is the difference between inhaled, oral, and topical forms of cineole for respiratory effects?

Inhaled cineole (via steam or nebulization) delivers the compound directly to airways, maximizing mucolytic and expectorant effects with minimal systemic absorption, making it fastest-acting for acute congestion. Oral cineole supplements reach the respiratory tract systemically but undergo hepatic metabolism, resulting in delayed onset (2–4 hours) but prolonged anti-inflammatory effects in the lungs and broader tissues. Topical application (chest rubs, oils) provides local airway stimulation and mild mucolytic action but with the least bioavailability compared to inhalation or oral ingestion.

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