Počet záznamů: 1

Synthesis and Antiangiogenic Activity of New Silybin Galloyl Esters

SYSNO ASEP	0369330
Druh ASEP	J - Článek v odborném periodiku
Zařazení RIV	J - Článek v odborném periodiku
Poddruh J	Článek ve WOS
Název	Synthesis and Antiangiogenic Activity of New Silybin Galloyl Esters
Tvůrce(i)	Gažák, Radek (MBU-M)_{RID, ORCID} Valentová, K. (CZ) Fuksová, Kateřina (MBU-M)_RID Marhol, Petr (MBU-M)_RID Kuzma, Marek (MBU-M)_{ORCID, RID} Medina, M. A. (ES) Oborná, I. (CZ) Ulrichová, J. (CZ) Křen, Vladimír (MBU-M)_{RID, ORCID}
Zdroj.dok.	Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623 Roč. 54, č. 20 (2011), s. 7397-7407
Poč.str.	11 s.
Jazyk dok.	eng - angličtina
Země vyd.	US - Spojené státy americké
Klíč. slova	Silybin ; gallates ; HUVEC
Vědní obor RIV	CC - Organická chemie
CEP	GAP207/10/0288 GA ČR - Grantová agentura ČR
	GAP301/11/0767 GA ČR - Grantová agentura ČR
	OC08049 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy
CEZ	AV0Z50200510 - MBU-M (2005-2011)
UT WOS	000296205900031
DOI	10.1021/jm201034h
Anotace	The synthesis of various silybin monogalloyl esters was developed, and their antiangiogenic activities were evaluated in a variety of in vitro tests with human umbilical vein endothelial cells (HUVECs). A structure-activity relationship (SAR) study found the regioselectivity of the silybin galloylation to be highly significant. Silybin (as an equimolar mixture of two diastereomers A and B) exhibited quite poor antiangiogenic activities, whereas its B isomer is more active than silybin A. Galloylation of phenolic OH groups of natural silybin (a mixture of both isomers) leads to increases in their antiangiogenic activities, which is more apparent with the 7-OH than the 20-OH. In contrast, gallates at aliphatic OH groups either had a comparable activity to the parent compound or are even worse than silybin, which was observed in the case of 3-O-galloylsilybin. The most effective 7-O-galloylsilybin has also been prepared from pure silybins A and B. B isomer was more active than A isomer
Pracoviště	Mikrobiologický ústav
Kontakt	Eliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231
Rok sběru	2012

Počet záznamů: 1