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Rosmarinic Acid as a Novel Agent in the Treatment of Allergies and Asthma

Abstract

Rosmarinic acid, a caffeic acid ester and a component of several members of the Lamiaceae family including Rosmarinus officinalis, Perilla spp., and Salvia officinialis, has antioxidant and anti-inflammatory effects and is used for the treatment of asthma and reactive airway diseases, allergic disorders such as allergic rhinitis, otitis media, chemical sensitivity and multiple allergen reactivity. Rosmarinic acid can be used alone or in combination with other agents such as antioxidants, essential fatty acid supplements and other plant derived products. Rosmarinic acid can be administered orally and no adverse drug interactions have been reported. Nausea or mild stomach upset has been reported in sensitive patients in association with its oral intake and it is therefore recommended that Rosmarinic acid be ingested with food. Rosmarinic acid has shown free radical scavenging ability and suppression of allergic immunoglobulin and inflammatory responses of polymorphonuclear leukocytes, which may underlie its effectiveness in the treatment of allergic disorders, as demonstrated in clinical trials. Rosmarinic acid is a valuable agent for the treatment of allergic conditions, which is of importance considering the recent increase in the incidence of allergies, asthma and lung diseases associated with airborne pollutants.

AARM REFERENCE REVIEWS:

These are AARM reference reviews in which clinicians can obtain a quick overview of understanding with respect to how herbs, nutrients, and hormones can be used effectively in clinical practice. The dosages recommended are based on therapeutic results. Side effects that have not been seen in clinical experience or found in clinical studies but only been theorized have been identified and depicted as Unsubstantiated Theoretical Concerns.

Since many nutrients and herbs on the market have not gone through double-blind studies but have been used extensively in clinical settings for hundreds, and for some thousands of years, these reference reviews have attempted to give a unified opinion on how to use these herbs effectively. The opinions expressed are from different professors and experts in the field of nutritional and botanical medicine. Some information is based on personal opinions and can not be quantified as fact. However, if clinicians only restricted themselves to what is fully proven by double-blind studies, the art of healing and restoring health with nutrients and herbs would be lost.

CLINICAL IMPLICATIONS:

PRIMARY INDICATIONS:

Asthma and reactive airway diseases, allergic disorders such as allergic rhinitis, serious otitis media, chemical sensitivity, and multiple allergen reactivity.

ADJUNCTIVE OR STAND ALONE TREATMENT:

May be either adjunctive or stand alone.

BIOACTIVE CONSTITUENTS

150 mg rosmarinic acid per capsule.

CAPSULE DOSE:

A minimum of 150 mg twice per day and a maximum of 4 or 5 times this amount.

TIME TO CLINICAL EFFICACY:

A minimum of 4 weeks.

LAB TESTS TO ASSESS EFFICACY:

Eosinophil count when elevated, nasal swabs for eosinophils.

SYNERGISTIC COMBINATION:

Combines well with antioxidant vitamins, essential fatty acid supplements, and other herbs specific to the individual patient.

SIDE EFFECTS:

Those with gastric ulcers or sensitive digestive systems may experience nausea, irritation, or mild stomach upset at the higher doses; consume with food to reduce this potential reaction.

PROVEN DRUG INTERACTION:

None documented.

DISCUSSION

Rosmarinus officinalis L. (common name, rosemary) is a woody herb, native to Mediterranean regions. It has been used in traditional medicine for many centuries, for respiratory disorders, depression, renal colic, and hair loss. Culpepper’s Herbal recommends rosemary especially for conditions affecting the mind, for maladies of the eye, stomach and joints due to effects of cold, and for coughs. Rosemary was traditionally thought to dispel negative thoughts, and is used in aromatherapy for anxiety.

Rosmarinic acid is an ester of caffeic acid present in several members of the Lamiaceae family including Rosmarinus officinalis, Perilla spp., andSalvia officinialis among others (Fig. 1). These plants have been traditionally used to treat upper respiratory and allergic symptoms. Rosmarinic acid is one of the more abundant caffeic esters occurring in plants, and becomes active in humans when it is auto-oxidized.

jrm.2014.3.0109_fig1

Figure 1:Rosmarinic acid (left); caffeic acid (right).

Rosmarinic acid is well absorbed from the gastrointestinal tract. It is readily assimilated in humans by all major organ systems, with higher concentrations found in the lungs. This may explain why it shows higher efficacy in the treatment of asthma and respiratory allergies than in other types of allergic responses. It has also shown promise as an effective treatment for pulmonary eosinophilia.

ROSMARINIC ACID DISPLAYS NUMEROUS ANTI-INFLAMMATORY EFFECTS:

Numerous antioxidant and anti-inflammatory effects have been reported for Rosmarinic acid, which may contribute to its anti-allergy activity. Rosmarinic acid has demonstrated free radical scavenging ability against superoxide anions and hydroxyl radicals. Additionally, animal studies have shown that Rosmarinic acid suppresses the allergic immunoglobulin response and inflammatory responses of polymorphonuclear leukocytes. All of these actions are putative mechanisms for Rosmarinic acid’s anti-inflammatory effect.

Plants That Contain Rosmarinic Acid Tend to Have Anti-Allergy EffectsIndividual herbs known to be high in Rosmarinic acid also have anti-inflammatory properties. Rosmarinus is a powerful antioxidant, and Perilla frutescens extracts and several Salvia species that contain Rosmarinic acid have antioxidant and anti-inflammatory effects including inhibition of lipoxygenase.Although the combined total of the chemical constituents in each plant contributes to its medicinal effects, Rosmarinic acid is increasingly being identified as a major anti-inflammatory and immune modulating substance (Fig. 2).

jrm.2014.3.0109_fig2

Figure 2:Anti-inflammatory effects of Rosmarinic acid. Left: Eosinophils infiltrating respiratory submucosa, capillaries and smooth muscle. Right: Eosinophils infiltration is reduced under the influence of Rosmarinic acid.

Copyright 2014 ₩ AARM

Perilla frutescens is both a popular culinary garnish and part of the Asian herbal medicine tradition, with much of the research emanating from Japan and Korea. Perilla has been used traditionally for allergies and as an antidote against allergic reactions triggered by the consumption of seafood and shellfish.Perilla frutescens has also been used for the treatment of bronchial asthma. The anti-inflammatory activity of Perilla was demonstrated in an animal model in which a Perilla decoction was effective in blocking the passive cutaneous anaphylaxis (PCA)-reaction, reducing the inflammatory reaction in the injured animal’s skin compared to untreated control animals.

Rosmarinic Acid for Respiratory Allergies and AsthmaAirborne pollutants have been implicated in the increasing incidence of allergies, asthma, and lung diseases in the general population and especially in children. Previous work in animals has demonstrated that intratracheal instillation of diesel exhaust particles will generate reactive oxygen species (ROS). In one study, pre-exposure oral supplementation with Rosmarinic acid prevented inflammation caused by diesel exhaust. The authors provided evidence of reduced pro-inflammatory proteins, decreased neutrophil infiltration, and less lung parenchymal and interstitial edema in animals treated with Rosmarinic acid.

Dust mites are another pervasive and potent instigator of allergy and asthma symptoms. One mouse model of allergic asthma uses tracheal tissue that has been sensitized to dust mites. This model reproducibly causes eosinophilic inflammation and measurable changes in interleukin and eotaxin levels. Eotaxin, found in a variety of mucosal tissues, is a chemokine that regulates and activates eosinophils. Mice pretreated with Perilla extract containing a high concentration of Rosmarinic acid exhibited only a blunted inflammatory response. Likewise, eosinophils, interleukins, and eotaxin levels were proportionally lower in mice treated with Rosmarinic acid.

HUMAN CLINICAL TRIALS ON ROSMARINIC ACID:

Takano and colleagues conducted a 21-day, randomized, double-blind, clinical trial in which various doses of a Rosmarinic acid-enriched Perilla extract were compared with placebo in the treatment of allergic conjunctivitis. Study subjects received the enriched extract at 200 mg per day or 50 mg per day, or placebo. Symptoms were recorded in a daily log along with periodic nasal lavage. There was a dose-dependent decrease in subject-reported symptoms including itchy nose, itchy eyes, and watery eyes. The treatment groups also had significantly lower neutrophil and eosinophil levels by nasal lavage. In another study, the same group administered Rosmarinic acid to subjects with seasonal allergic rhinitis and examined cytokine concentrations from nasal cells obtained by lavage. Again, the treatment groups had decreased neutrophil and eosinophil counts compared to the placebo group.

SUMMARY:

The antioxidant and anti-inflammatory effects of Rosmarinic acid (and plants high in this compound) make it a valuable tool in the treatment of allergic conditions, especially respiratory allergies. In vitro and in vivo studies along with clinical trials support the use of Rosmarinic acid in the prevention and treatment of asthma and allergy. Furthermore, herbs that contain Rosmarinic acid have a long history of safe use in alternative and traditional therapies.

DISCLOSURE OF INTERESTS

Dr. Stansbury has nothing to disclose.

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DOI: http://dx.doi.org/10.14200/jrm.2014.3.0109