Marine cyanobacteria-derived serotonin receptor 2C active fraction induces psychoactive behavioral effects in mice
| Autor: | Kevin Tidgewell, Christopher M Ignatz, N. Lax, Benedict J. Kolber, Kh Tanvir Ahmed, Carmenza Spadafora |
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| Rok vydání: | 2016 |
| Předmět: |
Male
0301 basic medicine Cyanobacteria Ethyl acetate Pharmaceutical Science Motor Activity Pharmacognosy Pharmacology High-performance liquid chromatography Article Mice 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Column chromatography Drug Discovery Receptor Serotonin 5-HT2C Animals Receptor IC50 Chromatography High Pressure Liquid Psychotropic Drugs biology General Medicine biology.organism_classification Antidepressive Agents Mice Inbred C57BL 030104 developmental biology Anti-Anxiety Agents Complementary and alternative medicine chemistry Molecular Medicine Serotonin 030217 neurology & neurosurgery |
| Zdroj: | Pharmaceutical Biology. 54:2723-2731 |
| ISSN: | 1744-5116 1388-0209 |
| Popis: | Context: Marine cyanobacteria offer a robust resource for natural products drug discovery due to the secondary metabolites they produce.Objective: To identify novel cyanobacterial compounds that exhibit CNS psychoactive effects.Materials and methods: Cyanobacteria were collected from Las Perlas Archipelago, Panama and subjected to dichloromethane/methanol extraction and fractionation by column chromatography before being screened for affinity against a panel of CNS targets. A 50:50 ethyl acetate:methanol fraction of one cyanobacterial extract (2064H) was subjected to HPLC and the major peak was isolated (2064H3). At a dose of 20 μg per animal, 2064H and 2064H3 were tested in mice using behavioral assays that included the forced swim, open field and formalin tests.Results: 2064H was shown to bind to the serotonin 2C (5-HT2C) receptor, a known target for depression and pain treatment. 2064H showed 59.6% inhibition of binding of [3H]-mesulergine with an IC50 value of 179 ng/mL and did not show inhibi... |
| Databáze: | OpenAIRE |
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