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Article

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

New Frontier Labs LLC, San Antonio, TX 78209, USA
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Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Anna Iwaniak and Luisa Tesoriere
Nutraceuticals 2021, 1(1), 42-53; https://doi.org/10.3390/nutraceuticals1010006
Received: 22 October 2021 / Revised: 4 December 2021 / Accepted: 13 December 2021 / Published: 17 December 2021
(This article belongs to the Special Issue Current State of the Art—Nutraceutical Components of Foods)
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 in vitro and in vivo, and mitigates insulin resistance. To further investigate the therapeutic utility of DEA, we evaluated its mutagenicity in Salmonella typhimurium strains, examined metabolism of DEA in rat, dog, monkey and human primary hepatocytes and in human saliva, determined pharmacokinetics of DEA after an oral dose in rats, and queried its physicochemical properties for drug-like characteristics. DEA was not mutagenic in bacterial strains ± rat liver metabolic activation system S-9. It was chemically unstable in hepatocyte culture medium with a half-life of <1 h and was depleted by the hepatocytes in <5 min, suggesting rapid hepatic metabolism. DEA was also quickly degraded by human saliva in vitro. After an oral administration of DEA to rats, the di- and monoester were undetectable in plasma while the levels of azelaic acid increased over time, reached maximum at <2 h, and declined rapidly thereafter. The observed pharmacological properties of DEA suggest that it has value both as a drug or a nutritional supplement. View Full-Text
Keywords: azelaic acid ester; diethyl azelate; immunomodulation; nutritional supplement; drug metabolism azelaic acid ester; diethyl azelate; immunomodulation; nutritional supplement; drug metabolism
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MDPI and ACS Style

Izbicka, E.; Streeper, R.T. Azelaic Acid Esters as Pluripotent Immunomodulatory Molecules: Nutritional Supplements or Drugs. Nutraceuticals 2021, 1, 42-53. https://doi.org/10.3390/nutraceuticals1010006

AMA Style

Izbicka E, Streeper RT. Azelaic Acid Esters as Pluripotent Immunomodulatory Molecules: Nutritional Supplements or Drugs. Nutraceuticals. 2021; 1(1):42-53. https://doi.org/10.3390/nutraceuticals1010006

Chicago/Turabian Style

Izbicka, Elzbieta, and Robert T. Streeper. 2021. "Azelaic Acid Esters as Pluripotent Immunomodulatory Molecules: Nutritional Supplements or Drugs" Nutraceuticals 1, no. 1: 42-53. https://doi.org/10.3390/nutraceuticals1010006

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