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.
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