About: Biomedical investigation of optically pure silybin derivatives – from “soft” nutraceuticals to targeted anticancer drug.     Goto   Sponge   NotDistinct   Permalink

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Description
  • Silybin is natural flavonolignan used as nutraceutical and exhibiting antioxidative, hepato and cardioprotective activities. In the last years high antineoplastic and antiangiogenic activity of this compound was discovered that is effective mainly against prostate carcinomas. The aim of the project is the synthesis and biological testing of new derivatives of silybin and isosilybin with favourable pharmacological properties. Library of new derivatives of silybin and isosilybin will be prepared. Optically pure stereomers of silibin and isosilybin will be starting materials for synthesis of other derivatives, namely their 2,3-dehydro derivatives, esters, sulfates and other. Synthesized derivatives will then undergo test of anticancer activity at the partner institution in USA against several cancer cell lines. The main focuss will point towards effect against prostate carcinomas cell lines. Derivatives showing high activity will be in the next level subjected to in vivo tests on mice mode (en)
  • Bude připravena skupina derivátů a potenciálních metabolitů silybinu a isosilybinu. Bude stanovena protinádorová aktivita připravených derivátů. Úspěšné sloučeniny budou předmětem dalšího zkoumání s cílem získat protinádorová léčiva s nízkou toxicitou.
Title
  • Biomedical investigation of optically pure silybin derivatives – from “soft” nutraceuticals to targeted anticancer drug. (en)
  • Biomedicínský výzkum opticky čistých derivátů silybinu - od potravinového doplňku k cílené protinádorové léčbě.
skos:notation
  • ME10027
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  • Silymarin; silybin; silibinin; prostate cancer; nutraceutics (en)
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  • Byla vyvinuta preparativní metoda pro přípravu opticky čistých isosiiybinů a disulfátů silybinu. Byly provedeny in vitro testy protinádorové aktivity připravených derivátů ve spolupráci s partnerem v USA. Byla připravena serie sulfátů silybinu, a to jak chemickou syntézou, tak i pomocí enzymové syntézy pomocí rekombinantní sulfotransferasy. Byly vyvinuty analytické metody k určení čistoty látek. (cs)
  • New preparatory method for preparation of optically pure isosilybins and silybin disulfates was developed.In vitro tests for anticancer activity of the new compounds were done in collaboration with the US partner. Silybin sulfates using recombinant sulfotransferase were prepared. Analytical methods for purity verification of the compounds designed for biological tests were developed and validated. (en)
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  • Silymarin
  • prostate cancer
  • silybin
  • silibinin
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