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| Description
| - Trilobolide (Tb), a potent natural counterpart of thapsigargin, is a sesquiterpene lactone of guaianolide type isolated from horse caraway (Laser trilobum) Tb exerts remarkable pharmacol. properties based on irreversible inhibition of sarco/endoplasmic reticulum calcium ATPase (SERCA), thus being of increasing interest for cancer cure. Addnl., another pharmacol. activity of Tb, as well as of thapsigargin, was reported in several studies, Tb as being an effective inductor of nitric oxide and cytokine prodn. These extraordinary biol. properties move these mols. in further pre-clin. evaluation. Because of ubiquitous character of SERCA expression, development of specifically targeted bioactive mols. is inevitable. Since it is well known that porp. are preferentially taken up by cancer cells, we have designed and synthesized novel Tb-porphyrin conjugates. Copper-catalyzed azide-alkyne cycloaddn. was used to link Tb with porphyrin at once. Two model conjugates of Tb and porphyrin were synthesized and properly characterized. Employing naturally occurring fluorescence properties of porphyrins, we investigated the intracellular localization of the conjugates employing fluorescence microscopy in living cells. Intriguingly, the prepd. conjugates localized both in mitochondria and lysosomes of HeLa and LNCaP cells. Furthermore, the cytotoxicity of Tb-porphyrin conjugates was assessed in a no. of human cancer cell lines and rat peritoneal cells. Likewise in cancer cell lines, viability of rat peritoneal cells was not affected by the tested conjugates. Interestingly, we obsd. dose-dependent nitric oxide (iNOS) prodn. induced by the tested conjugates. The effect was related to the type of a linker used and the overall size of the mol. Another potent immunobiol. effects are under evaluation. In summary, the results presented here indicate notable immunobiol. potential of the prepd. Tb conjugates.
- Trilobolide (Tb), a potent natural counterpart of thapsigargin, is a sesquiterpene lactone of guaianolide type isolated from horse caraway (Laser trilobum) Tb exerts remarkable pharmacol. properties based on irreversible inhibition of sarco/endoplasmic reticulum calcium ATPase (SERCA), thus being of increasing interest for cancer cure. Addnl., another pharmacol. activity of Tb, as well as of thapsigargin, was reported in several studies, Tb as being an effective inductor of nitric oxide and cytokine prodn. These extraordinary biol. properties move these mols. in further pre-clin. evaluation. Because of ubiquitous character of SERCA expression, development of specifically targeted bioactive mols. is inevitable. Since it is well known that porp. are preferentially taken up by cancer cells, we have designed and synthesized novel Tb-porphyrin conjugates. Copper-catalyzed azide-alkyne cycloaddn. was used to link Tb with porphyrin at once. Two model conjugates of Tb and porphyrin were synthesized and properly characterized. Employing naturally occurring fluorescence properties of porphyrins, we investigated the intracellular localization of the conjugates employing fluorescence microscopy in living cells. Intriguingly, the prepd. conjugates localized both in mitochondria and lysosomes of HeLa and LNCaP cells. Furthermore, the cytotoxicity of Tb-porphyrin conjugates was assessed in a no. of human cancer cell lines and rat peritoneal cells. Likewise in cancer cell lines, viability of rat peritoneal cells was not affected by the tested conjugates. Interestingly, we obsd. dose-dependent nitric oxide (iNOS) prodn. induced by the tested conjugates. The effect was related to the type of a linker used and the overall size of the mol. Another potent immunobiol. effects are under evaluation. In summary, the results presented here indicate notable immunobiol. potential of the prepd. Tb conjugates. (en)
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| Title
| - Trilobolide-porphyrin conjugates: On synthesis and biological effects evaluation
- Trilobolide-porphyrin conjugates: On synthesis and biological effects evaluation (en)
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| skos:prefLabel
| - Trilobolide-porphyrin conjugates: On synthesis and biological effects evaluation
- Trilobolide-porphyrin conjugates: On synthesis and biological effects evaluation (en)
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| skos:notation
| - RIV/60461373:22330/14:43897195!RIV15-GA0-22330___
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
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| http://linked.open...iv/cisloPeriodika
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
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| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
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| http://linked.open...ai/riv/idVysledku
| - RIV/60461373:22330/14:43897195
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - Fluorescence microscopy; Nitric oxide; Porphyrin; Trilobolide (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
| - US - Spojené státy americké
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
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| http://linked.open...in/vavai/riv/obor
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| http://linked.open...ichTvurcuVysledku
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| http://linked.open...cetTvurcuVysledku
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| http://linked.open...vavai/riv/projekt
| |
| http://linked.open...UplatneniVysledku
| |
| http://linked.open...v/svazekPeriodika
| |
| http://linked.open...iv/tvurceVysledku
| - Buděšínský, Miloš
- Drašar, Pavel
- Ruml, Tomáš
- Kmoníčková, Eva
- Rimpelová, Silvie
- Tomanová, Pavla
- Jurášek, Michal
- Vejvodová, Lucie
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| issn
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| number of pages
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| http://bibframe.org/vocab/doi
| - 10.1016/j.steroids.2014.08.024
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| http://localhost/t...ganizacniJednotka
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