Inhibitory effect of corynoline isolated from the aerial parts of Corydalis incisa on the acetylcholinesterase.
ABSTRACT In the course of screening Korean natural products for acetylcholinesterase (AChE) inhibitory activity, it was found that a methanolic extract of the aerial parts of Corydalis incisa (Papaveraceae) showed significant inhibitory effects on AChE. Corynoline isolated from this plant inhibited AChE activity in a dose-dependent manner, and the IC50 value of corynoline was 30.6 microM. The AChE inhibitory activity of corynoline was reversible and noncompetitive.
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ABSTRACT: In the present investigation termiticidal effects of Capparis decidua and its combinatorial mixtures on biochemical and enzymatic pa-rameters of Odontotermes obesus (Isoptera: Termitidae) were observed. C. decidua has shown very high termiticidal activity to O. obesus (Ram-bur) when termites were exposed with 40% and 80% of LD 50 . It's aqueous extract and combinatorial mixtures significantly (p < 0.05) inhibited the level of glycogen, amino acid, lipid, DNA, RNA and protein in termites. Besides this, both single and combinatorial mixtures of C. decidua signif-icantly (p < 0.05) decreased the level of acid phosphatase, alkaline phos-phatase, lactic dehydrogenase, glutamate oxaloacetate transaminase and glutamate pyruvate transaminase enzymes at very low concentrations af-ter 8 h treatment. More specifically, aqueous extract and combinatorial mixtures significantly inhibited the AChE activity, which the confirms the presence of neurotoxic compounds. However, it can be concluded that C. decidua active ingredients can easily kill field termites if used in the poison baits and as fumigant in storehouses.
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ABSTRACT: Corynoline and acetycorynoline are active compounds of Corydalis bungeana Turcz. with various pharmacological effects such as sedation, anti-leptospira and liver injury protection effects. A specific, simple and sensitive UHPLC-ESI-MS/MS method was developed and validated for the pharmacokinetic study of corynoline and acetycorynoline in rat plasma. Corynoline and acetycorynoline were extracted from plasma samples by liquid-liquid extraction. The analysis was carried out on an Agilent SB-C18 column (1.8μm, 50mm×2.1mm) with the mobile phase of acetonitrile-0.1% formic acid (80:20, v/v). The detection was performed on a triple quadrupole tandem mass spectrometer by multiple reaction monitoring (MRM) mode via electrospray ionization (ESI) source in positive mode. The current UHPLC-ESI-MS/MS assay was validated for linearity, intra-day and inter-day precisions, accuracy, extraction recovery and stability. The lower limits of quantification were 0.10ng/mL for corynoline and 0.353ng/mL for acetycorynoline. Intra-day and inter-day precision were less than 12.3% and accuracy ranged from 0.18% to 14.9%. The mean extraction recoveries of analytes and internal standard (IS) from rat plasma were all more than 76.2%. This validated method was successfully applied to pharmacokinetic study in rats after oral administration of corynoline, acetycorynoline and the extract of Corydalis bungeana Turcz.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 04/2014; 960C:59-66. · 2.78 Impact Factor
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ABSTRACT: The use of Pd catalysis as a means to synthesize organic halides has recently received increased attention. Among the reported methods is the Pd-catalyzed carboiodination, which uses extremely bulky ligands to facilitate carbon-halogen reductive elimination from Pd(II) as the key catalytic step. When approaching substrates exhibiting low stereoselectivity, catalyst troubleshooting becomes difficult as there are few ligands known to promote the key reductive elimination. Herein, we present our finding that tertiary amines act as weakly coordinating ligands which significantly enhance diastereoselectivity in the Pd/QPhos-catalyzed carboiodination of chiral N-allyl carboxamides. This methodology allows efficient access to enantioenriched and densely functionalized dihydroisoquinolinones, and has been applied toward the asymmetric formal synthesis of (+)-corynoline.Angewandte Chemie International Edition in English 06/2014; · 13.45 Impact Factor