Azelaic Acid Esters as Pluripotent Immunomodulatory Molecules: Nutritional Supplements or Drugs

Azelaic acid and its esters, the azelates, occur naturally in organisms ranging from plants to humans. We have shown that diethyl azelate (DEA) exhibits a broad range of immunomodulatory activities vitro vivo, mitigates insulin resistance. To further investigate therapeutic utility DEA, we evaluated mutagenicity Salmonella typhimurium strains, examined metabolism DEA rat, dog, monkey human primary hepatocytes saliva, determined pharmacokinetics after an oral dose rats, queried physicochemical properties for drug-like characteristics. was not mutagenic bacterial strains ± rat liver metabolic activation system S-9. It chemically unstable hepatocyte culture medium with half-life <1 h depleted by <5 min, suggesting rapid hepatic metabolism. also quickly degraded saliva vitro. After administration di- monoester were undetectable plasma while levels azelaic increased over time, reached maximum at <2 h, declined rapidly thereafter. The observed pharmacological suggest it has value both as drug or nutritional supplement.