γ-Mangostin increases serotonin2A/2C, muscarinic, histamine and bradykinin receptor mRNA expression
| Autor: | Monrudee Sukma, Boonyong Tantisira, Michihisa Tohda, Sunit Suksamran |
|---|---|
| Rok vydání: | 2011 |
| Předmět: |
Pharmacology
medicine.medical_specialty Ketanserin Reverse Transcriptase Polymerase Chain Reaction medicine.drug_class Chemistry Xanthones Receptors Cell Surface Histamine H1 receptor Muscarinic acetylcholine receptor M1 Receptor antagonist Cell Line Histamine receptor Endocrinology Internal medicine Drug Discovery medicine Muscarinic acetylcholine receptor M4 RNA Messenger Histamine H4 receptor Bradykinin receptor medicine.drug |
| Zdroj: | Journal of Ethnopharmacology. 135:450-454 |
| ISSN: | 0378-8741 |
| Popis: | Aim of the study γ-Mangostin is a xanthone found in the fruit hulls of Garcinia mangostana L., which have long been used in Southeast Asia as a traditional medicine for the treatment of abdominal pain, dysentery, wound infections, fever and convulsions. Recent studies have revealed that γ-mangostin exhibits a variety of pharmacological activities, including serotonin 2 (5-HT2) receptor antagonism, anti-inflammatory effects and analgesic effects. To explore the mechanism of γ-mangostin responsible for these pharmacological activities, especially its effects on some related receptors, we investigated the effects of γ-mangostin on 5-HT2, histamine (H1) and bradykinin (BK2) receptor gene expression in neuroblastoma (NG 108-15) cells in vitro. Additionally, to extend the study of the pharmacological properties, we examined the effect of γ-mangostin on the muscarinic (M4) receptor. Materials and methods NG 108-15 cells were cultured in vitro and treated with γ-mangostin or a 5-HT2 receptor antagonist (either imipramine or ketanserin). Then, the levels of mRNA for 5-HT2A/2C receptors were evaluated by semi-quantitative RT-PCR. The preventive effect of serotonin on the enhancement effects was also revealed. Additionally, the effects of γ-mangostin on the muscarinic, histamine and bradykinin receptors were determined. Results Chronic application of γ-mangostin at a concentration of 0.1 μM induced a significant increase in the level of 5-HT2A/2C receptor mRNA. These effects were prevented by serotonin. Moreover, γ-mangostin up-regulated the M4, H1 and BK2 receptors. Conclusion The ability of γ-mangostin to enhance the expression of 5-HT2A/2C, muscarinic, histamine and bradykinin receptor mRNA suggests that this compound has antagonistic effects. These pharmacological properties may partly account for the benefits of using mangosteen in the treatment of inflammation, pain and neuropsychiatric symptoms. |
| Databáze: | OpenAIRE |
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