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

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388971%3A_____%2F06%3A00043280" target="_blank" >RIV/61388971:_____/06:00043280 - isvavai.cz</a>

Alternative codes found

RIV/61989592:15110/06:00002756

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

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

Original language 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

Czech name

Nové deriváty silybinu a 2,3-dehydrosilybinu - jejich cytotoxicita a P-glykoprotein modulační aktivita

Czech description

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

Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

EE - Microbiology, virology

OECD FORD branch

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Project

<a href="/en/project/GA303%2F02%2F1097" target="_blank" >GA303/02/1097: Synthesis and Biological Characterization of New Compounds Derived from Silibinin for Potential Use as Chemoprotectants in Dermatology</a><br>

Continuities

Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year

2006

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Bioorganic Medical Chemistry

ISSN

0968-0896

e-ISSN

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Volume of the periodical

14

Issue of the periodical within the volume

-

Country of publishing house

GB - UNITED KINGDOM

Number of pages

8

Pages from-to

3793-3810

UT code for WoS article

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EID of the result in the Scopus database

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