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Natural compounds in the fight against allergy

Aiming to provide a solution for human allergic disorders, European scientists explored the development of a series of small, drug-like molecules based on a natural product. By disrupting essential protein interactions these molecules exhibit promising anti-allergy treatment potential.
Natural compounds in the fight against allergy
Epidemiological studies indicate that more than 25  % of the population in industrialised countries suffers from some kind of allergy. The economic impact of this phenomenon due to health care costs and work absenteeism mounts to nearly EUR 3  000  million.

Allergic disorders are caused by inflammatory mediators such as leukotrienes that are released by mast cells and basophils following conjugation of immunoglobulin E (IgE) proteins on the Fc epsilon RI receptors on these cells. As a result, small molecules that disrupt this interaction could be efficacious in treating allergic disorders.

Based on this, the EU-funded 'Total synthesis of (+)-aspercyclide A and analogues' (TSASPERA) project examined the potential of using aspercyclide A as an antagonist against the human IgE-Fc epsilon RI protein–protein interaction. This molecule is found in the Tanzanian soil bacterium Aspergillus spp. And constitutes a promising strategy for the treatment of asthma and allergies.

Scientists synthesised various analogues of aspercyclide A in order to understand how the molecule's structure determines its activity. The (+)-enantiomer that shares the same configuration with natural aspercyclide A shows significant antagonist activity against the human IgE-Fc epsilon RI interaction. In contrast, the (-)-enantiomer proved less active, indicating a specific mode of action.

To rule out that the activity of aspercyclide A is caused by the reaction of the aldehyde moiety with protein lysine side chains leading to irreversible toxicity, scientists are evaluating the biological impact of two analogues that do not contain an aldehyde group. This would dictate whether (+)-aspercyclide A could serve as a lead for further development towards a therapeutic agent for asthma and allergy. Current treatments for allergy and asthma are often associated with debilitating side-effects and may be generally unsatisfactory. Further observations based on TSASPERA results could result in effective that would improve the quality of life for millions of sufferers worldwide.

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