ReferenceID 1296
Berbamine Reduces Chloroquine-Induced Itch in Mice through Inhibition of MrgprX1
Int J Mol Sci
Chloroquine (CQ) is an antimalaria drug that has been widely used for decades. However, CQ-induced pruritus remains one of the major obstacles in CQ treatment for uncomplicated malaria. Recent studies have revealed that
Relationship Network
Interactive first-hop connections across herbs, ingredients, formulas, targets, diseases, symptoms, syndromes, evidence, and monographs.
Click a node to open it in a new tab
Ingredient: 1Reference: 1Links: 1
Arranging relationship network...
Record Fields
Scalar fields from the final reference record.
- Reference Id
- 1296
- Evidence Id
- 17886
- Core Evidence Id
- 17886
- Source Reference Id
- 2583
- Herb2 Reference Id
- HBREF003380
- Subject Paper Key
- HBIN017888_36430803
- Pubmed Id
- 36430803
- Doi
- 10.3390/ijms232214321
- Paper Title
- Berbamine Reduces Chloroquine-Induced Itch in Mice through Inhibition of MrgprX1
- Paper Abstract
- Chloroquine (CQ) is an antimalaria drug that has been widely used for decades. However, CQ-induced pruritus remains one of the major obstacles in CQ treatment for uncomplicated malaria. Recent studies have revealed that MrgprX1 plays an essential role in CQ-induced itch. To date, a few MrgprX1 antagonists have been discovered, but they are clinically unavailable or lack selectivity. Here, a cell-based high-throughput screening was performed to identify novel antagonists of MrgprX1, and the screening of 2543 compounds revealed two novel MrgprX1 inhibitors, berbamine and closantel. Notably, berbamine potently inhibited CQ-mediated MrgprX1 activation (IC 50 = 1.6 μM) but did not alter the activity of other pruritogenic GPCRs. In addition, berbamine suppressed the CQ-mediated phosphorylation of ERK1/2. Interestingly, CQ-induced pruritus was significantly reduced by berbamine in a dose-dependent manner, but berbamine had no effect on histamine-induced, protease-activated receptors 2-activating peptide-induced, and deoxycholic acid-induced itch in mice. These results suggest that berbamine is a novel, potent, and selective antagonist of MrgprX1 and may be a potential drug candidate for the development of therapeutic agents to treat CQ-induced pruritus.
- Journal
- Int J Mol Sci
- Publish Year
- 2022
- Experiment Subject
- mouse
- Experiment Type
- Cell Experiment
- Phenotype Related
- Malaria; Cq-induced Pruritus
- Paper Title Cn
- Paper Title En
- Berbamine Reduces Chloroquine-Induced Itch in Mice through Inhibition of MrgprX1
- Bilingual Status
- semi_complete