Trilobolide-porphyrin conjugates: On synthesis and biological effects evaluation

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11140%2F15%3A10282770" target="_blank" >RIV/00216208:11140/15:10282770 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/60461373:22330/14:43897195 RIV/61388963:_____/15:00444157

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0039128X14002219" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0039128X14002219</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.steroids.2014.08.024" target="_blank" >10.1016/j.steroids.2014.08.024</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Trilobolide-porphyrin conjugates: On synthesis and biological effects evaluation

Popis výsledku v původním jazyce

Trilobolide (Tb), a potent natural counterpart of thapsigargin, is a sesquiterpene lactone of guaianolide type isolated from horse caraway (Laser trilobum, L. Borkh). Since it is well known that porphyrins are preferentially taken up by cancer cells, wehave designed and synthesized novel Tb-porphyrin conjugates. Copper-catalyzed azide-alkyne cycloaddition was used to link Tb with porphyrin at once. Two model conjugates of Tb and porphyrin were synthesized and properly characterized. Employing naturallyoccurring fluorescence properties of porphyrins, we investigated the intracellular localization of the conjugates employing fluorescence microscopy in living cells. Intriguingly, the prepared conjugates localized both in mitochondria and lysosomes of HeLa and LNCaP cells. Furthermore, the cytotoxicity of Tb-porphyrin conjugates was assessed in a number of human cancer cell lines and rat peritoneal cells. Likewise in cancer cell lines, viability of rat peritoneal cells was not affected b

Název v anglickém jazyce

Trilobolide-porphyrin conjugates: On synthesis and biological effects evaluation

Popis výsledku anglicky

Trilobolide (Tb), a potent natural counterpart of thapsigargin, is a sesquiterpene lactone of guaianolide type isolated from horse caraway (Laser trilobum, L. Borkh). Since it is well known that porphyrins are preferentially taken up by cancer cells, wehave designed and synthesized novel Tb-porphyrin conjugates. Copper-catalyzed azide-alkyne cycloaddition was used to link Tb with porphyrin at once. Two model conjugates of Tb and porphyrin were synthesized and properly characterized. Employing naturallyoccurring fluorescence properties of porphyrins, we investigated the intracellular localization of the conjugates employing fluorescence microscopy in living cells. Intriguingly, the prepared conjugates localized both in mitochondria and lysosomes of HeLa and LNCaP cells. Furthermore, the cytotoxicity of Tb-porphyrin conjugates was assessed in a number of human cancer cell lines and rat peritoneal cells. Likewise in cancer cell lines, viability of rat peritoneal cells was not affected b

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2015

Kód důvěrnosti údajů

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

Název periodika

Steroids

ISSN

0039-128X

e-ISSN

—

Svazek periodika

97

Číslo periodika v rámci svazku

May

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

5

Strana od-do

8-12

Kód UT WoS článku

000353178800003

EID výsledku v databázi Scopus

2-s2.0-84925460002