Journal of Enzyme Inhibition and Medicinal Chemistry · 2008 · 47 citations · 15 references
MedicineChemistryPharmacologyEnzymologyNeuropharmacologyStructure-activity RelationshipsCholinergic NeurochemistryCholinergic PharmacologyEnzyme InhibitionHeterocyclic ChemistryNatural Product Drug DiscoveryStructure-activity Relationship AnalysisAcetylcholinesterase FunctionAcetylcholinesterase InhibitorsMass Spectral Data AnalysisPlant Alkaloids
Two new diterpenoid alkaloids, heterophyllinine-A (1) and heterophyllinine-B (2), along with two known alkaloids dihydroatisine (3) and lycoctonine (4) were isolated from the roots of Aconitum heterophyllum Wall. The structure of (1) and (2), were deduced on the basis of spectral data. Compounds 1-2 inhibited acetylcholinesterase (AChE, EC 3.1.1.7) and butyrylcholinesterase (BChE, EC 3.1.1.8) enzymes in a concentration-dependent manner with percent inhibition ranging between 4.24% and 6.94 % and 79.1 % and 82.75 % for AChE and BChE, respectively indicating that compounds 1 and 2 are about thirteen times more specific to BChE than AChE.
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