5-Hydroxytryptamine2A receptor binding activity of compounds from Litsea sessilis |
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Authors: | Chung Lip Yong Lo Mee Wah Mustafa Muhammad Rais Goh Swee Hock Imiyabir Zamrie |
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Institution: | Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia. chungly@hotmail.com |
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Abstract: | A 96-well microplate filtration based 5-HT(2A) receptor-radioligand binding assay was optimized and adopted to carry out a bioassay-guided fractionation of the methanol extract of the leaves of Litsea sessilis. This purification led to the isolation of two compounds identified as (+)-boldine (1) and (+)-dehydrovomifoliol (2). (+)-Boldine binds to 5-HT(2A) receptors at high concentrations with a K(i) value of 2.16 microm. However, (+)-dehydrovomifoliol showed minimal competitive inhibition on the binding of (3)H]ketanserin to the same receptor with a K(i) value of 2.06 mm. These results suggest that (+)-boldine influences the activity of 5-HT(2A) receptors through competitive binding as an agonist or antagonist. |
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Keywords: | boldine dehydrovomifoliol 5‐hydroxytryptamine receptor binding Lauraceae Litsea sessilis serotonin |
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