A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:10 |
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| Enthalten in: |
Cells - 10(2021), 2 vom: 20. Feb. |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Manzo, Emiliano [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 26.08.2021 Date Revised 26.02.2024 published: Electronic Citation Status MEDLINE |
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| doi: |
10.3390/cells10020450 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 500 | |a Date Revised 26.02.2024 | ||
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a 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 | ||
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| 700 | 1 | |a Schiano Moriello, Aniello |e verfasserin |4 aut | |
| 700 | 1 | |a Tinto, Francesco |e verfasserin |4 aut | |
| 700 | 1 | |a Verde, Roberta |e verfasserin |4 aut | |
| 700 | 1 | |a Allarà, Marco |e verfasserin |4 aut | |
| 700 | 1 | |a De Petrocellis, Luciano |e verfasserin |4 aut | |
| 700 | 1 | |a Pagano, Ester |e verfasserin |4 aut | |
| 700 | 1 | |a Izzo, Angelo A |e verfasserin |4 aut | |
| 700 | 1 | |a Di Marzo, Vincenzo |e verfasserin |4 aut | |
| 700 | 1 | |a Petrosino, Stefania |e verfasserin |4 aut | |
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