Cytotoxic activities of Amaryllidaceae alkaloids against gastrointestinal cancer cells

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F15%3A39900072" target="_blank" >RIV/00216275:25310/15:39900072 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/60460709:41210/15:67647 RIV/00216208:11160/15:10312334

Výsledek na webu

<a href="http://dx.doi.org/10.1016/j.phytol.2015.08.004" target="_blank" >http://dx.doi.org/10.1016/j.phytol.2015.08.004</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.phytol.2015.08.004" target="_blank" >10.1016/j.phytol.2015.08.004</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Cytotoxic activities of Amaryllidaceae alkaloids against gastrointestinal cancer cells

Popis výsledku v původním jazyce

The treatment of many diseases is highly dependent on natural products and natural products can also be used as design templates for future anticancer drugs. Thirteen Amaryllidaceae alkaloids possessing alpha-crinane, beta-crinane, galantamine, lycorine and tazettine-type skeleton have been isolated in our laboratory, and their cytotoxicity against p53-mutated gastrointestinal cancer cells were evaluated. At the same time, healthy small intestine cells were used to determine overall toxicity against noncancerous cells. In this study, we demonstrated that haemanthamine, haemanthidine and lycorine showed strong cytotoxicity against p53-mutated Caco-2 and HT-29 colorectal adenocarcinoma cells as quantified in terms of IC50 values. We for the first time observed approximately 20 times higher IC(50)values against normal intestine epithelial cells FHs-74 Int after haemanthamine and lycorine treatment when compared with Caco-2 and HT-29 cancer cells. In conclusion, our data indicate that alpha-C2 bridged haemanthamine may be perspective anticancer drug candidate for further semisynthetic modification and structure-activity relationship study.

Název v anglickém jazyce

Cytotoxic activities of Amaryllidaceae alkaloids against gastrointestinal cancer cells

Popis výsledku anglicky

The treatment of many diseases is highly dependent on natural products and natural products can also be used as design templates for future anticancer drugs. Thirteen Amaryllidaceae alkaloids possessing alpha-crinane, beta-crinane, galantamine, lycorine and tazettine-type skeleton have been isolated in our laboratory, and their cytotoxicity against p53-mutated gastrointestinal cancer cells were evaluated. At the same time, healthy small intestine cells were used to determine overall toxicity against noncancerous cells. In this study, we demonstrated that haemanthamine, haemanthidine and lycorine showed strong cytotoxicity against p53-mutated Caco-2 and HT-29 colorectal adenocarcinoma cells as quantified in terms of IC50 values. We for the first time observed approximately 20 times higher IC(50)values against normal intestine epithelial cells FHs-74 Int after haemanthamine and lycorine treatment when compared with Caco-2 and HT-29 cancer cells. In conclusion, our data indicate that alpha-C2 bridged haemanthamine may be perspective anticancer drug candidate for further semisynthetic modification and structure-activity relationship study.

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

<a href="/cs/project/EE2.3.20.0235" target="_blank" >EE2.3.20.0235: Vybudování výzkumného týmu experimentální a aplikované biofarmacie</a><br>

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2015

Kód důvěrnosti údajů

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

Název periodika

Phytochemistry Letters

ISSN

1874-3900

e-ISSN

—

Svazek periodika

13

Číslo periodika v rámci svazku

September 2015

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

5

Strana od-do

394-398

Kód UT WoS článku

000362174600069

EID výsledku v databázi Scopus

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