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Nostotrebin 6, a bis(cyclopentenedione) with cholinesterase inhibitory activity isolated from Nostoc sp. str. Lukešová 27/97
Authors: Zelik Petr | Lukešová Alena | Čejka Jan | Buděšínský Miloš | Havlíček Vladimír | Čegan Alexander
Year: 2010
Type of publication: článek v odborném periodiku
Name of source: Journal of enzyme inhibition and medicinal chemistry
Publisher name: Taylor & Francis Ltd.
Place: Abingdon
Page from-to: 414-420
Titles:
Language Name Abstract Keywords
cze Nostotrebin 6 je inhibitor cholinesterázy na bázi bis(cyklopentendionu) izolovaný z bakterií Nostoc sp. str. Lukešová 27/97 Nostotrebin 6 je nová polyfenolická sloučenina s plně substituovaným 2,2'-bis(cyclopent-4-en-1,3-dione) skeletem, která byla izolována z methanolového extraktu kyanobakterie Nostoc sp. str. Lukesova 27/97. Struktura této sloučeniny byla stanovena pomocí rentgenostrukturní krystalografické analýzy a dále prokázána pomocí NMR, IR spektroskopie a hmotnostní spektrometrie. Nostotrebin 6 je S-parabolický a I-parabolický nekompetitivní inhibitor acetylcholinesterázy (IC50 = 5.5 mu M) a S-parabolický a I-parabolický smíšený inhibitor butyrylcholinesterázy (IC50 = 6.1-7.5 mu M). Inhibiční aktivita nostotrebinu 6 byla porovnána s inhibiční aktivitou tacrinu a galanthaminu. Nostotrebin 6; kyanobakterie; cholinesteráza; inhibiční aktivita; Nostoc; sp.; takrin, galanthamin
eng Nostotrebin 6, a bis(cyclopentenedione) with cholinesterase inhibitory activity isolated from Nostoc sp. str. Lukešová 27/97 Nostotrebin 6, a new polyphenolic compound with a fully substituted 2,2'-bis(cyclopent-4-en-1,3-dione) skeleton, was isolated from a methanolic extract of the cyanobacterial strain Nostoc sp. str. Lukesova 27/97. The structure of this compound was determined using X-ray crystallography and further supported by NMR, IR spectroscopy, and MS. Nostotrebin 6 is an S-parabolic I-parabolic noncompetitive inhibitor of acetylcholinesterase (IC50 = 5.5 mu M) and an S-parabolic I-parabolic mixed inhibitor of butyrylcholinesterase (IC50 = 6.1-7.5 mu M). The inhibitory potency of nostotrebin 6 was compared with that of tacrine and galanthamine. Nostotrebin 6; cyanobacteria; cholinesterase; inhibitory activity; Nostoc sp.; tacrine; galanthamine

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