Pharmacological Survey of Medicinal Plants for Activity at Ligand-Gated Ion Channels: Selective Interaction with 5-HT3 Receptors
| Autor: | Cathy L. Bell-Horner, Robert R. Luedtke, Glenn H. Dillon, Michael Volk, Manfred G. Reinecke |
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| Rok vydání: | 2004 |
| Předmět: | |
| Zdroj: | Pharmaceutical Biology. 42:73-82 |
| ISSN: | 1744-5116 1388-0209 |
| DOI: | 10.1080/13880200490505654 |
| Popis: | The ligand-gated anion-selective ion channels are part of a superfamily of ligand-gated ion channels (LGICs) that are responsible for a majority of inhibitory signaling in the central nervous system and are the targets of numerous therapeutics. Aqueous, organic and alcoholic extracts of 47 Chinese, Bolivian and Pakistani medicinal plants were evaluated for the ability to modulate the activity of GABAA receptors. Extracts were initially screened for their ability to modulate activity of α1β2γ2 GABAA receptors expressed in HEK 293 cells. Based on the initial screen, two extracts derived from members of the Asteraceae family, Xanthium spinosum and Senecio mathewsii, were chosen for more detailed analysis. Xanthium spinosum inhibited GABAA receptor function, with an IC50 of 50 ± 10 µg/ml, while Senecio mathewsii inhibited GABAA receptor activity with an IC50 of 35 ± 3.0 µg/ml. To assess the selectivity of interaction, these extracts were also tested on two other members of the LGIC superfamily a) glycine rece... |
| Databáze: | OpenAIRE |
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