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The novel brassinosteroid analog BR4848 inhibits angiogenesis in human endothelial cells and induces apoptosis in human cancer cells in vitro
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SYSNO ASEP 0489630 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název The novel brassinosteroid analog BR4848 inhibits angiogenesis in human endothelial cells and induces apoptosis in human cancer cells in vitro Tvůrce(i) Rárová, L. (CZ)
Sedlák, David (UMG-J) RID
Oklešťková, Jana (UEB-Q) RID, ORCID, SAI
Steigerová, J. (CZ)
Liebl, J. (DE)
Zahler, S. (DE)
Bartůněk, Petr (UMG-J) RID
Kolář, Z. (CZ)
Kohout, Ladislav (UEB-Q)
Kvasnica, Miroslav (UEB-Q) RID, ORCID
Strnad, Miroslav (UEB-Q) RID, ORCIDCelkový počet autorů 11 Zdroj.dok. Journal of Steroid Biochemistry and Molecular Biology. - : Elsevier - ISSN 0960-0760
Roč. 178, April (2018), s. 263-271Poč.str. 9 s. Jazyk dok. eng - angličtina Země vyd. GB - Velká Británie Klíč. slova Brassinosteroid analog ; Cancer cell lines ; Apoptosis ; HUVEC ; Angiogenesis Vědní obor RIV EB - Genetika a molekulární biologie Obor OECD Organic chemistry CEP LO1204 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy LO1220 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy LM2015063 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Institucionální podpora UMG-J - RVO:68378050 ; UEB-Q - RVO:61389030 UT WOS 000428483800030 DOI https://doi.org/10.1016/j.jsbmb.2018.01.005 Anotace We report the synthesis and detailed biological study of the synthetic brassinosteroid analog 2 alpha,3 alpha-dihydroxy-6-oxo-5 alpha-androstan-17 beta-yl N-(tert-butoxycarbonyl)-D,L-valinate (BR4848). The panel of cancer cell lines was used for characterization of its antiproliferative activity, yet had no adverse effects in normal human fibroblasts. In HeLa cells, BR4848-induced apoptosis was accompanied by increase of apoptotic subG(1) cells, PARP-1 and caspase-7 fragmentation, downregulation of Bcl-2 and Mcl-1, an increase in caspase activity and G(2)/M phase cell cycle arrest. Antiproliferative properties of BR4848 were exhibited by inhibition of phosphorylation of Akt, Erk1/2 and FAK. Furthermore, the developed analog exhibited in vitro antiangiogenic activity in human umbilical vein endothelial cells (HUVECs). BR4848-induced apoptosis accompanied with G2/M arrest was detected in endothelial cells. BR4848 also inhibited adhesion, tube formation and migration of endothelial cells by inhibition of FAY, Erk 1/2, CDK5, VEGFR2, TNF alpha-stimulated production of IL-6, angiopoietin-2 and Jagged1. Finally, BR4848 did not modulate the activity nor nuclear translocation of any of the steroid receptors (ER alpha, ER beta, AR, MR and PR) included in reporter cell-based assays, which excludes the genomic activity of steroid receptors as a contributing factor to the observed biological activities of BR4848. Pracoviště Ústav molekulární genetiky Kontakt Nikol Škňouřilová, nikol.sknourilova@img.cas.cz, Tel.: 241 063 217 Rok sběru 2019
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