Cineol

Mucolytic, expectorant. Important, phytotherapeutically relevant component of essential oils. Cineole is mainly obtained by steam distillation from the leaves and branches of eucalyptus. Oils containing cineole are used as an inhalant, as an antimicrobial therapeutic agent (1% oil) or as a balm for colds.

The mucolytic monoterpene 1,8-cineole (eucalyptol), the main constituent of eucalyptus species, is known for its anti-inflammatory, antioxidant, bronchodilator, antiviral and antimicrobial effects.

The main protective antiviral, anti-inflammatory and mucolytic mechanisms of 1,8-cineole are induction of interferon regulatory factor 3 (IRF3), control of nuclear factor kappa light chain enhancer of activated B cells (NF-κB) and reduction of mucin genes (MUC2, MUC19/Juergens LJ et al. 2020).

In normal human monocytes, direct inhibition of reactive oxygen species (ROS)-mediated mucus hypersecretion and steroid resistance-inducing superoxides (O2--) and proinflammatory hydrogen peroxides (H2O2) with partial control of superoxide dismutase (SOD), which converts O2-- to H2O2, has been demonstrated.

By inhibiting NF-κB, 1,8-cineole strongly and significantly inhibited lipopolysaccharide (LPS)-stimulated cytokines relevant to exacerbation (tumor necrosis factor alpha (TNFα), interleukin (IL)-1β and systemic inflammation (IL-6, IL-8) at relevant plasma concentrations (1.5 µg/ml) in normal human monocytes.

In lymphocytes from healthy human donors, 1,8-cineole inhibited TNFα, IL-1β, IL-4 and IL-5. At relevant plasma levels, 1,8-cineole additively inhibited the efficacy of the inhaled lead drugs budesonide (BUD) and budesonide + formoterol in vitro. Preliminary data also showed increased efficacy of long-acting muscarinic receptor antagonist (LAMA)-mediated cytokine inhibition in vitro (Juergens LJ et al. 2020).

In randomized controlled trials, additional therapy with 1,8-cineole (3 × 200 mg/day) over 6 months resulted in an improvement in uncontrolled asthma through a significant improvement in lung function, nocturnal asthma and quality of life scores as well as a reduction in exacerbations in COPD (- 38.5 %)

External: ^Soledum®, ^{Transpulmin®}.

Systemic: Soledum capsules; Soledum capsules forte 100 mg cineole / capsule or 200 mg for forte. For asthma requiring steroids: significant reduction in the need for cortisone; dosage 3 x 200 mg/day.

1. Juergens LJ et al. (2020) New Perspectives for Mucolytic, Anti-inflammatory and Adjunctive Therapy with 1,8-Cineole in COPD and Asthma: Review on the New Therapeutic Approach. Adv Ther 37:1737-1753.
2. Edited by Facharztmagazine. Cineole has anti-inflammatory and antiviral effects. MMW Fortschr Med. 164:64.
3. Schumacher B (2022) Cineole is much more than a mucolytic. MMW Fortschr Med 164:62.
4. Shahi SK et al. (2000) Broad spectrum herbal therapy against superficial superficial fungal infections. Skin Pharmacol Appl Skin Physiol 13: 60-64