ABSTRACT
In a bioassay-guided search for acetylcholinesterase inhibitors from Korean natural resources, four isoquinoline alkaloids, corynoxidine (1), protopine (2), palmatine (3), and berberine (4) have been isolated from the methanolic extract of the aerial parts of Corydalis speciosa. Structures of these compounds were elucidated on the basis of spectroscopic techniques. These compounds inhibited acetylcholinesterase activity in a dose-dependent manner, and the IC50 values of compounds 1-4 were 89.0, 16.1, 5.8, and 3.3 microM, respectively.
Subject(s)
Cholinesterase Inhibitors/isolation & purification , Corydalis/chemistry , Plant Extracts/isolation & purification , Acetylcholinesterase/metabolism , Animals , Benzophenanthridines , Berberine/chemistry , Berberine/pharmacology , Berberine Alkaloids/chemistry , Berberine Alkaloids/isolation & purification , Berberine Alkaloids/pharmacology , Cholinesterase Inhibitors/chemistry , Cholinesterase Inhibitors/pharmacology , Dose-Response Relationship, Drug , Kinetics , Magnetic Resonance Spectroscopy/methods , Male , Mice , Mice, Inbred ICR , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Plant Stems/chemistryABSTRACT
The effect was investigated of the aqueous extract of Rubus coreanus Miq. (Rosaceae) fruits (RCAE) on systemic and local anaphylaxis. RCAE (0.01-1 g/kg) dose-dependently inhibited systemic anaphylaxis induced by compound 48/80 in mice. RCAE (1 g/kg) also significantly inhibited local anaphylaxis activated by anti-DNP IgE. Pretreatment with RCAE at the same concentration before systemic anaphylaxis reduced the plasma histamine levels in a dose-dependent manner. RCAE (0.001-1 mg/mL) dose-dependently inhibited the histamine release from rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-DNP IgE. The level of cAMP in RPMC, when RCAE was added, significantly increased, compared with that of the normal control. Moreover, RCAE (0.01-1 mg/mL) had a significant inhibitory effect on anti-DNP IgE-induced tumour necrosis factor-alpha production from RPMC. These results indicate that RCAE may possess antianaphylactic action.
Subject(s)
Anaphylaxis/drug therapy , Plant Extracts/therapeutic use , Rosaceae , Anaphylaxis/chemically induced , Animals , Cyclic AMP/metabolism , Dose-Response Relationship, Drug , Fruit/chemistry , Histamine/blood , Histamine Release/drug effects , Immunoglobulin E/drug effects , Immunoglobulin E/immunology , Mast Cells/drug effects , Mice , Mice, Inbred ICR , Peritoneum/drug effects , Phytotherapy , Rats , Rats, Sprague-Dawley , p-Methoxy-N-methylphenethylamine/pharmacologyABSTRACT
In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dose-dependent manner, and the IC50 values of compounds 1-3 were 74.6, 63.7 and 89.1 microM, respectively.
