The anti-anaphylactoid effects of Piperine through regulating MAS-related G protein-coupled receptor X2 activation
© 2020 John Wiley & Sons, Ltd..
Mast cells play an important role in inflammatory and allergic diseases. MAS-related G protein-coupled receptor X2 (MRGPRX2) is a novel G protein-coupled receptor in mast cells that mediates drug-induced anaphylactoid reactions. Piperine has been reported to have anti-inflammatory and anti-allergic pharmacological activities. However, whether the pharmacological effects are regulated by MRGPRX2 has not yet been reported. The purpose of this study was to assess the anti-anaphylactoid effect of Piperine and to explore its potential mechanism. The anti-anaphylactoid effect of Piperine was assessed by an in vivo mouse hindpaw extravasation model. Mast cell intracellular calcium mobilization was measured by a calcium imaging assay. An enzyme immunoassay was used to evaluate the release of pro-inflammatory factors from stimulated mast cells. Activated mast cell related signals were assessed by western blot. A cell membrane chromatography assay was used to determine the binding characteristics of Piperine and MRGPRX2. The results showed that Piperine suppressed mast cell intracellular Ca2+ mobilization, inhibited cytokines and chemokines release, and down-regulated the phosphorylation level of phospholipase Cγ1, protein kinase C, inositol 1,4,5-triphate receptor, P38, protein kinase B, and ERK. Meanwhile, Piperine can bind to MRGPRX2 as a specific antagonist. Hence, Piperine can be served as a novel therapeutic drug candidate for MRGPRX2-mediated anaphylactoid reactions.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2020 |
|---|---|
| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:34 |
|---|---|
| Enthalten in: |
Phytotherapy research : PTR - 34(2020), 6 vom: 28. Juni, Seite 1409-1420 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Qiao, Chuchu [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
Alkaloids |
|---|
| Anmerkungen: |
Date Completed 30.07.2020 Date Revised 30.07.2020 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1002/ptr.6615 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM305858882 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM305858882 | ||
| 003 | DE-627 | ||
| 005 | 20231225122105.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2020 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1002/ptr.6615 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1019.xml |
| 035 | |a (DE-627)NLM305858882 | ||
| 035 | |a (NLM)31989711 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Qiao, Chuchu |e verfasserin |4 aut | |
| 245 | 1 | 4 | |a The anti-anaphylactoid effects of Piperine through regulating MAS-related G protein-coupled receptor X2 activation |
| 264 | 1 | |c 2020 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 30.07.2020 | ||
| 500 | |a Date Revised 30.07.2020 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2020 John Wiley & Sons, Ltd. | ||
| 520 | |a Mast cells play an important role in inflammatory and allergic diseases. MAS-related G protein-coupled receptor X2 (MRGPRX2) is a novel G protein-coupled receptor in mast cells that mediates drug-induced anaphylactoid reactions. Piperine has been reported to have anti-inflammatory and anti-allergic pharmacological activities. However, whether the pharmacological effects are regulated by MRGPRX2 has not yet been reported. The purpose of this study was to assess the anti-anaphylactoid effect of Piperine and to explore its potential mechanism. The anti-anaphylactoid effect of Piperine was assessed by an in vivo mouse hindpaw extravasation model. Mast cell intracellular calcium mobilization was measured by a calcium imaging assay. An enzyme immunoassay was used to evaluate the release of pro-inflammatory factors from stimulated mast cells. Activated mast cell related signals were assessed by western blot. A cell membrane chromatography assay was used to determine the binding characteristics of Piperine and MRGPRX2. The results showed that Piperine suppressed mast cell intracellular Ca2+ mobilization, inhibited cytokines and chemokines release, and down-regulated the phosphorylation level of phospholipase Cγ1, protein kinase C, inositol 1,4,5-triphate receptor, P38, protein kinase B, and ERK. Meanwhile, Piperine can bind to MRGPRX2 as a specific antagonist. Hence, Piperine can be served as a novel therapeutic drug candidate for MRGPRX2-mediated anaphylactoid reactions | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Ca2+ influx | |
| 650 | 4 | |a MRGPRX2 | |
| 650 | 4 | |a Piperine | |
| 650 | 4 | |a antianaphylactoid effects | |
| 650 | 4 | |a mast cells | |
| 650 | 7 | |a Alkaloids |2 NLM | |
| 650 | 7 | |a Benzodioxoles |2 NLM | |
| 650 | 7 | |a Piperidines |2 NLM | |
| 650 | 7 | |a Polyunsaturated Alkamides |2 NLM | |
| 650 | 7 | |a Receptors, G-Protein-Coupled |2 NLM | |
| 650 | 7 | |a piperine |2 NLM | |
| 650 | 7 | |a U71XL721QK |2 NLM | |
| 700 | 1 | |a Hu, Shiling |e verfasserin |4 aut | |
| 700 | 1 | |a Che, Delu |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Jue |e verfasserin |4 aut | |
| 700 | 1 | |a Gao, Jiapan |e verfasserin |4 aut | |
| 700 | 1 | |a Ma, Ruiping |e verfasserin |4 aut | |
| 700 | 1 | |a Jiang, Wenjun |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Tao |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Rui |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Phytotherapy research : PTR |d 1996 |g 34(2020), 6 vom: 28. Juni, Seite 1409-1420 |w (DE-627)NLM08871747X |x 1099-1573 |7 nnns |
| 773 | 1 | 8 | |g volume:34 |g year:2020 |g number:6 |g day:28 |g month:06 |g pages:1409-1420 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1002/ptr.6615 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 34 |j 2020 |e 6 |b 28 |c 06 |h 1409-1420 | ||