A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator Article Swipe
YOU?
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· 2021
· Open Access
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· DOI: https://doi.org/10.3390/cells10020450
Palmitoylethanolamide (PEA) is an endogenous anti-inflammatory lipid mediator and a widely used nutraceutical. In this study, we designed, realized, and tested a drug-carrier conjugate between PEA (the active drug) and glucuronic acid (the carrier). The conjugate, named GLUPEA, was characterized for its capability of increasing PEA levels and exerting anti-inflammatory activity both in vitro and in vivo. GLUPEA treatment, compared to the same concentration of PEA, resulted in higher cellular amounts of PEA and the endocannabinoid 2-arachidonoyl glycerol (2-AG), and increased 2-AG-induced transient receptor potential vanilloid type 1 (TRPV1) channel desensitization to capsaicin. GLUPEA inhibited pro-inflammatory monocyte chemoattractant protein 2 (MCP-2) release from stimulated keratinocytes, and it was almost as efficacious as ultra-micronized PEA at reducing colitis in dinitrobenzene sulfonic acid (DNBS)-injected mice when using the same dose. GLUPEA is a novel pro-drug able to efficiently mimic the anti-inflammatory and endocannabinoid enhancing actions of PEA.
Related Topics
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.3390/cells10020450
- https://www.mdpi.com/2073-4409/10/2/450/pdf?version=1614242368
- OA Status
- gold
- Cited By
- 6
- References
- 61
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W3132922739
Raw OpenAlex JSON
- OpenAlex ID
-
https://openalex.org/W3132922739Canonical identifier for this work in OpenAlex
- DOI
-
https://doi.org/10.3390/cells10020450Digital Object Identifier
- Title
-
A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential BioregulatorWork title
- Type
-
articleOpenAlex work type
- Language
-
enPrimary language
- Publication year
-
2021Year of publication
- Publication date
-
2021-02-20Full publication date if available
- Authors
-
Emiliano Manzo, Aniello Schiano Moriello, Francesco Tinto, Roberta Verde, Marco Allarà, Luciano De Petrocellis, Ester Pagano, Angelo A. Izzo, Vincenzo Di Marzo, Stefania PetrosinoList of authors in order
- Landing page
-
https://doi.org/10.3390/cells10020450Publisher landing page
- PDF URL
-
https://www.mdpi.com/2073-4409/10/2/450/pdf?version=1614242368Direct link to full text PDF
- Open access
-
YesWhether a free full text is available
- OA status
-
goldOpen access status per OpenAlex
- OA URL
-
https://www.mdpi.com/2073-4409/10/2/450/pdf?version=1614242368Direct OA link when available
- Concepts
-
Palmitoylethanolamide, Chemistry, Pharmacology, Glucuronic acid, TRPV1, Conjugate, Endocannabinoid system, Biochemistry, Drug delivery, Capsaicin, In vivo, Cannabinoid, Cannabinoid receptor, Receptor, Transient receptor potential channel, Biology, Polysaccharide, Agonist, Organic chemistry, Mathematics, Biotechnology, Mathematical analysisTop concepts (fields/topics) attached by OpenAlex
- Cited by
-
6Total citation count in OpenAlex
- Citations by year (recent)
-
2025: 2, 2024: 2, 2022: 2Per-year citation counts (last 5 years)
- References (count)
-
61Number of works referenced by this work
- Related works (count)
-
10Other works algorithmically related by OpenAlex
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