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A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator
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| Zeitschriftentitel: | Cells |
|---|---|
| Personen und Körperschaften: | , , , , , , , , , |
| In: | Cells, 10, 2021, 2, S. 450 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
MDPI AG
|
| Schlagwörter: |
| author_facet |
Manzo, Emiliano Schiano Moriello, Aniello Tinto, Francesco Verde, Roberta Allarà, Marco De Petrocellis, Luciano Pagano, Ester Izzo, Angelo A. Di Marzo, Vincenzo Petrosino, Stefania Manzo, Emiliano Schiano Moriello, Aniello Tinto, Francesco Verde, Roberta Allarà, Marco De Petrocellis, Luciano Pagano, Ester Izzo, Angelo A. Di Marzo, Vincenzo Petrosino, Stefania |
|---|---|
| author |
Manzo, Emiliano Schiano Moriello, Aniello Tinto, Francesco Verde, Roberta Allarà, Marco De Petrocellis, Luciano Pagano, Ester Izzo, Angelo A. Di Marzo, Vincenzo Petrosino, Stefania |
| spellingShingle |
Manzo, Emiliano Schiano Moriello, Aniello Tinto, Francesco Verde, Roberta Allarà, Marco De Petrocellis, Luciano Pagano, Ester Izzo, Angelo A. Di Marzo, Vincenzo Petrosino, Stefania Cells A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator General Medicine |
| author_sort |
manzo, emiliano |
| spelling |
Manzo, Emiliano Schiano Moriello, Aniello Tinto, Francesco Verde, Roberta Allarà, Marco De Petrocellis, Luciano Pagano, Ester Izzo, Angelo A. Di Marzo, Vincenzo Petrosino, Stefania 2073-4409 MDPI AG General Medicine http://dx.doi.org/10.3390/cells10020450 <jats:p>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.</jats:p> A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator Cells |
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10.3390/cells10020450 |
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| title |
A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_unstemmed |
A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_full |
A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_fullStr |
A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_full_unstemmed |
A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_short |
A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_sort |
a glucuronic acid-palmitoylethanolamide conjugate (glupea) is an innovative drug delivery system and a potential bioregulator |
| topic |
General Medicine |
| url |
http://dx.doi.org/10.3390/cells10020450 |
| publishDate |
2021 |
| physical |
450 |
| description |
<jats:p>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.</jats:p> |
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| author | Manzo, Emiliano, Schiano Moriello, Aniello, Tinto, Francesco, Verde, Roberta, Allarà, Marco, De Petrocellis, Luciano, Pagano, Ester, Izzo, Angelo A., Di Marzo, Vincenzo, Petrosino, Stefania |
| author_facet | Manzo, Emiliano, Schiano Moriello, Aniello, Tinto, Francesco, Verde, Roberta, Allarà, Marco, De Petrocellis, Luciano, Pagano, Ester, Izzo, Angelo A., Di Marzo, Vincenzo, Petrosino, Stefania, Manzo, Emiliano, Schiano Moriello, Aniello, Tinto, Francesco, Verde, Roberta, Allarà, Marco, De Petrocellis, Luciano, Pagano, Ester, Izzo, Angelo A., Di Marzo, Vincenzo, Petrosino, Stefania |
| author_sort | manzo, emiliano |
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| description | <jats:p>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.</jats:p> |
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| imprint_str_mv | MDPI AG, 2021 |
| institution | DE-L229, DE-D275, DE-Bn3, DE-Brt1, DE-Zwi2, DE-D161, DE-Gla1, DE-Zi4, DE-15, DE-Pl11, DE-Rs1, DE-105, DE-14, DE-Ch1 |
| issn | 2073-4409 |
| issn_str_mv | 2073-4409 |
| language | English |
| last_indexed | 2024-03-01T11:24:10.516Z |
| match_str | manzo2021aglucuronicacidpalmitoylethanolamideconjugateglupeaisaninnovativedrugdeliverysystemandapotentialbioregulator |
| mega_collection | MDPI AG (CrossRef) |
| physical | 450 |
| publishDate | 2021 |
| publishDateSort | 2021 |
| publisher | MDPI AG |
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| spelling | Manzo, Emiliano Schiano Moriello, Aniello Tinto, Francesco Verde, Roberta Allarà, Marco De Petrocellis, Luciano Pagano, Ester Izzo, Angelo A. Di Marzo, Vincenzo Petrosino, Stefania 2073-4409 MDPI AG General Medicine http://dx.doi.org/10.3390/cells10020450 <jats:p>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.</jats:p> A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator Cells |
| spellingShingle | Manzo, Emiliano, Schiano Moriello, Aniello, Tinto, Francesco, Verde, Roberta, Allarà, Marco, De Petrocellis, Luciano, Pagano, Ester, Izzo, Angelo A., Di Marzo, Vincenzo, Petrosino, Stefania, Cells, A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator, General Medicine |
| title | A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_full | A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_fullStr | A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_full_unstemmed | A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_short | A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| title_sort | a glucuronic acid-palmitoylethanolamide conjugate (glupea) is an innovative drug delivery system and a potential bioregulator |
| title_unstemmed | A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator |
| topic | General Medicine |
| url | http://dx.doi.org/10.3390/cells10020450 |