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Kuca, Kamil,Cabal, Jiri,Jung, Yung Sik,Musilek, Kamil,Soukup, Ondrej,Jun, Daniel,Pohanka, Miroslav,Musilova, Lucie,Karasová,, Jana,Novotný,, Ladislav,Hrabinova, Martina Blackwell Publishing Ltd 2009 Basic & clinical pharmacology & toxicology Vol.105 No.3
<P>Abstract: </P><P>Newly developed acetylcholinesterase reactivators K117 [1,5-bis(4-hydroxyiminomethylpyridinium)-3-oxapentane dichloride] and K127 [(1-(4-hydroxyiminomethylpyridinium)-5-(4-carbamoylpyridinium)-3-oxapentane dibromide)] were tested for their potency to reactivate tabun-inhibited human brain cholinesterases. Pralidoxime and trimedoxime were chosen as standard reference reactivators. Human tissue was used, as that was closer on the real treatment of human beings. As a result, oxime K127 was found as the best tested reactivator according to the constant <I>k</I><SUB>r</SUB>, characterizing the overall reactivation process. On the contrary, the maximal reactivation ability expressed as percentage of reactivation was the best for trimedoxime. This differences were caused as a result of using the enzyme from different species. Due to this, experiments on human tissue should be conducted after <I>in vitro</I> and <I>in vivo</I> tests on animals to eliminate such important failures of promising oximes.</P>
Marcela S ˇ afratova,Anna Hosˇt’a´lkova,Daniela Hulcova,Katerˇina Breiterova,Veronika Hrabcova,Marta Machado,Diana Fontinha,Miguel Prudeˆncio,Jirˇı´ Kunes,Jakub Chlebek,Daniel Jun,Martina Hrabinova,Lu 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.2
Fifteen Amaryllidaceae alkaloids (1–15) of variousstructural types were isolated by standard chromatographicmethods from fresh bulbs of Narcissus poeticus cv. Pink Parasol. The chemical structures were elucidated byMS, and 1D and 2D NMR spectroscopic analyses, and bycomparison with literature data. Narcipavline (5) and narcikachnine(6) are reported here for the first time. In theirstructure are combined two basic structural types ofAmaryllidaceae alkaloids (galanthamine- and galanthindole-structural types), which represent a new structuraltype of these compounds. Alkaloids isolated in sufficientamounts were evaluated for their human erythrocyticacetylcholinesterase, and human serum butyrylcholinesterase(HuBuChE) inhibition activity using Ellman’smethod. Z-Gly-Pro-p-nitroanilide was used assubstrate in the prolyl oligopeptidase (POP) assay. Untestedalkaloids were also screened for their cytotoxic activityagainst a small panel of human cancer cells, which spannedcell lines from different tissue types. In parallel, MRC-5human fibroblasts were employed to determine overalltoxicity against noncancerous cells. Some compounds wereevaluated for their antiprotozoal activity. The newly isolatedalkaloid narcipavline (5) showed interestingHuBuChE inhibition activity (IC50 = 24.4 ± 1.2 lM), andnorlycoramine (11) demonstrated promising POP inhibition(IC50 = 0.21 ± 0.01 mM).