About: New derivatives of silybin and 2,3-dehydrosilybin and their cytotoxic and P-glycoprotein modulatory activity

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About: New derivatives of silybin and 2,3-dehydrosilybin and their cytotoxic and P-glycoprotein modulatory activity Goto Sponge Distinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	Large series of O-alkyl derivatives of silybin and 2,3-dehydrosilybin was prepared. All prepared silybin/2,3-dehydrosilybin derivatives were tested for cytotoxicity on a panel of drugs sensitive against multidrug resistant cell lines and the ability to inhibit P-glycoprotein mediated efflux activity. We have identified effective and relatively non-cytotoxic inhibitors of P-gp derived from 2,3-dehydrosilybin. Some of them were more effective inhibitors than a standard P-gp efflux inhibitor cyclosporin A. In the frame of this study were established structural requirements for improving inhibitory activity and reducing toxicity of 2,3-dehydrosilybin as well Large series of O-alkyl derivatives of silybin and 2,3-dehydrosilybin was prepared. All prepared silybin/2,3-dehydrosilybin derivatives were tested for cytotoxicity on a panel of drugs sensitive against multidrug resistant cell lines and the ability to inhibit P-glycoprotein mediated efflux activity. We have identified effective and relatively non-cytotoxic inhibitors of P-gp derived from 2,3-dehydrosilybin. Some of them were more effective inhibitors than a standard P-gp efflux inhibitor cyclosporin A. In the frame of this study were established structural requirements for improving inhibitory activity and reducing toxicity of 2,3-dehydrosilybin as well (en) Byla připravena řada selektivně alkylovaných derivátů silybinu a 2,3-dehydrosilybinu určených pro strukturně-aktivitní studie jejich efektu na inhibici effluxní funkce P-glykoproteinu. Připravené deriváty silybinu/2,3-dehydrosilybinu byly testovány rovněž na cytotoxicitu v panelu buněk citlivých a rezistentních k léčivu. Identifikovali jsme efektivní a relativně netoxické inhibitory P-gp odvozené od 2,3-dehydrosilybinu. Řada z nich vykazovala lepší inhibiční aktivitu než standardní P-gp inhibitor cyklosporin A. V rámci této studie byly také stanoveny strukturní požadavky pro zlepšení inhibiční aktivity a snížení toxicity 2,3-dehydrosilybinu (cs)
Title	New derivatives of silybin and 2,3-dehydrosilybin and their cytotoxic and P-glycoprotein modulatory activity Nové deriváty silybinu a 2,3-dehydrosilybinu - jejich cytotoxicita a P-glykoprotein modulační aktivita (cs) New derivatives of silybin and 2,3-dehydrosilybin and their cytotoxic and P-glycoprotein modulatory activity (en)
skos:prefLabel	New derivatives of silybin and 2,3-dehydrosilybin and their cytotoxic and P-glycoprotein modulatory activity Nové deriváty silybinu a 2,3-dehydrosilybinu - jejich cytotoxicita a P-glykoprotein modulační aktivita (cs) New derivatives of silybin and 2,3-dehydrosilybin and their cytotoxic and P-glycoprotein modulatory activity (en)
skos:notation	RIV/61388971:_____/06:00043280!RIV07-GA0-61388971
http://linked.open.../vavai/riv/strany	3793;3810
http://linked.open...avai/riv/aktivita	P Z
http://linked.open...avai/riv/aktivity	P(GA303/02/1097), Z(AV0Z50200510), Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika	-
http://linked.open...vai/riv/dodaniDat	2007
http://linked.open...aciTvurceVysledku	Gažák, Radek Sedmera, Petr Křen, Vladimír
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Mikrobiologický ústav AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	488494
http://linked.open...ai/riv/idVysledku	RIV/61388971:_____/06:00043280
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	silymarin; silybin; dehydrosilybin (en)
http://linked.open.../riv/klicoveSlovo	silybin silymarin dehydrosilybin
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[F16AE4BB8A4F]
http://linked.open...i/riv/nazevZdroje	Bioorganic Medical Chemistry
http://linked.open...in/vavai/riv/obor	EE
http://linked.open...ichTvurcuVysledku	3 (xsd:int)
http://linked.open...cetTvurcuVysledku	8 (xsd:int)
http://linked.open...vavai/riv/projekt	Synthesis and Biological Characterization of New Compounds Derived from Silibinin for Potential Use as Chemoprotectants in Dermatology
http://linked.open...UplatneniVysledku	2006
http://linked.open...v/svazekPeriodika	14
http://linked.open...iv/tvurceVysledku	Gažák, Radek Křen, Vladimír Sedmera, Petr Svobodová, A. Džubák, P. Hajdúch, M. Walterová, Daniela Psotová, J.
http://linked.open...n/vavai/riv/zamer	Microorganisms in Research and Biotechnology Modulation of signalling and regulatory pathways in normal and cancer cells
issn	0968-0896
number of pages	8 (xsd:int)
is http://linked.open...avai/riv/vysledek of	New derivatives of silybin and 2,3-dehydrosilybin and their cytotoxic and P-glycoprotein modulatory activity New derivatives of silybin and 2,3-dehydrosilybin and their cytotoxic and P-glycoprotein modulatory activity

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