Muscarinic receptor binding activity of polyoxygenated flavones from Melicope subunifoliolata

The bark extract of Melicope subunifoliolata (Stapf) T.G. Hartley showed competitive muscarinic receptor binding activity. Six polymethoxyflavones [melibentin (1);melisimplexin(3);3,30,40,5,7pentamethoxyflavone(4);melite rnatin (5); 3,5,8-trimethoxy-30,40,6,7 bismethylenedioxyflavone (6); and isokanugi...

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Bibliographic Details
Main Authors: Chung, L.Y., Yap, K.F., Mustafa, Mohd Rais, Goh, S.H., Imiyabir, Z.
Format: Article
Language:English
Published: Elsevier 2008
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Online Access:http://eprints.um.edu.my/2453/1/Muscarinic_receptor_binding_activity_of_polyoxygenated_flavones_from_Melicope_subunifoliolata.pdf
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Summary:The bark extract of Melicope subunifoliolata (Stapf) T.G. Hartley showed competitive muscarinic receptor binding activity. Six polymethoxyflavones [melibentin (1);melisimplexin(3);3,30,40,5,7pentamethoxyflavone(4);melite rnatin (5); 3,5,8-trimethoxy-30,40,6,7 bismethylenedioxyflavone (6); and isokanugin (7)] and one furanocoumarin [5-methoxy-8-geranyloxypsoralen (2)]were isolated fromthe bark extract. Compounds 2 and 6 were isolated for the first time from M. subunifoliolata. Themethoxyflavones (compounds 1, 3, 4, 5, 6, and 7) show moderate inhibition in a muscarinic receptor binding assay, while the furanocoumarin (compound 2) is inactive. The potency of the methoxyflavones to inhibit [ 3 H]NMS-muscarinic receptor binding is influenced by the position and number of methoxy substitution. The results suggest these compounds are probably muscarinic modulators, agonists or partial agonists/antagonists.