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一种葡萄糖醛酸-棕榈酰乙醇酰胺缀合物（GLUPEA）是一种创新的药物传递系统和有潜力的生物调节剂。

A Glucuronic Acid-Palmitoylethanolamide Conjugate (GLUPEA) Is an Innovative Drug Delivery System and a Potential Bioregulator.

机构信息

Istituto di Chimica Biomolecolare, CNR, 80078 Pozzuoli, Napoli, Italy.

Endocannabinoid Research Group, 80078 Pozzuoli, Napoli, Italy.

出版信息

Cells. 2021 Feb 20;10(2):450. doi: 10.3390/cells10020450.

DOI:10.3390/cells10020450
PMID:33672574
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7924038/
Abstract

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.

摘要

棕榈酰乙醇酰胺（PEA）是一种内源性抗炎脂质介质，也是一种广泛应用的营养保健品。在本研究中，我们设计、实现并测试了 PEA（活性药物）和葡萄糖醛酸（载体）之间的药物载体缀合物。该缀合物命名为 GLUPEA，其具有增加 PEA 水平和发挥抗炎活性的能力，无论是在体外还是体内。与相同浓度的 PEA 相比，GLUPEA 处理导致细胞内 PEA 和内源性大麻素 2-花生四烯酸甘油（2-AG）的含量增加，并增加了 2-AG 诱导的瞬时受体电位香草酸型 1（TRPV1）通道对辣椒素的脱敏作用。GLUPEA 抑制了刺激角质形成细胞释放的促炎单核细胞趋化蛋白 2（MCP-2），并且当使用相同剂量时，它在降低二硝基苯磺酸（DNBS）注射小鼠的结肠炎方面几乎与超微化 PEA 一样有效。GLUPEA 是一种新型前药，能够有效地模拟 PEA 的抗炎和内源性大麻素增强作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/279bcf3a0553/cells-10-00450-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/6af5377e1d7c/cells-10-00450-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/0e0d68fa85fd/cells-10-00450-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/d95fae0af3dc/cells-10-00450-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/11044000c84b/cells-10-00450-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/7344e51e7c89/cells-10-00450-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/3bb82c074dba/cells-10-00450-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/a342e6b4609c/cells-10-00450-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/571e911b559d/cells-10-00450-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/279bcf3a0553/cells-10-00450-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/6af5377e1d7c/cells-10-00450-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/0e0d68fa85fd/cells-10-00450-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/d95fae0af3dc/cells-10-00450-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/11044000c84b/cells-10-00450-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/7344e51e7c89/cells-10-00450-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/3bb82c074dba/cells-10-00450-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/a342e6b4609c/cells-10-00450-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/571e911b559d/cells-10-00450-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a63e/7924038/279bcf3a0553/cells-10-00450-g007.jpg

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