Biocatalytic synthesis and antitumor activities of novel silybin acylated derivatives with dicarboxylic acids

Theodosiou, E; Loutrari, H; Stamatis, H; Roussos, C; Kolisis, FN

dc.contributor.author	Theodosiou, E	en
dc.contributor.author	Loutrari, H	en
dc.contributor.author	Stamatis, H	en
dc.contributor.author	Roussos, C	en
dc.contributor.author	Kolisis, FN	en
dc.date.accessioned	2014-03-01T01:35:21Z
dc.date.available	2014-03-01T01:35:21Z
dc.date.issued	2011	en
dc.identifier.issn	1871-6784	en
dc.identifier.uri	https://dspace.lib.ntua.gr/xmlui/handle/123456789/21014
dc.subject	Antitumor Activity	en
dc.subject	Dicarboxylic Acid	en
dc.subject.other	Acyl donors	en
dc.subject.other	Anti-angiogenic activity	en
dc.subject.other	Anti-tumor activities	en
dc.subject.other	Anti-tumors	en
dc.subject.other	Antiproliferative effect	en
dc.subject.other	Biocatalytic synthesis	en
dc.subject.other	Biological functions	en
dc.subject.other	Candida antarctica lipase B	en
dc.subject.other	Dicarboxylic acid	en
dc.subject.other	Monoesters	en
dc.subject.other	Novozym435	en
dc.subject.other	Reaction parameters	en
dc.subject.other	Silybin	en
dc.subject.other	Vascular endothelial growth factor	en
dc.subject.other	Endothelial cells	en
dc.subject.other	Organic compounds	en
dc.subject.other	Organic solvents	en
dc.subject.other	Synthesis (chemical)	en
dc.subject.other	Acylation	en
dc.subject.other	dicarboxylic acid derivative	en
dc.subject.other	ester	en
dc.subject.other	lipase B	en
dc.subject.other	silibinin	en
dc.subject.other	vasculotropin	en
dc.subject.other	antiangiogenic activity	en
dc.subject.other	antineoplastic activity	en
dc.subject.other	article	en
dc.subject.other	cancer cell	en
dc.subject.other	Candida antarctica	en
dc.subject.other	catalysis	en
dc.subject.other	drug structure	en
dc.subject.other	drug synthesis	en
dc.subject.other	lymphoblastoma	en
dc.subject.other	priority journal	en
dc.subject.other	solvent extraction	en
dc.subject.other	Acetylation	en
dc.subject.other	Antineoplastic Agents	en
dc.subject.other	Cell Survival	en
dc.subject.other	Dicarboxylic Acids	en
dc.subject.other	Humans	en
dc.subject.other	K562 Cells	en
dc.subject.other	Lipase	en
dc.subject.other	Silymarin	en
dc.subject.other	Candida antarctica	en
dc.title	Biocatalytic synthesis and antitumor activities of novel silybin acylated derivatives with dicarboxylic acids	en
heal.type	journalArticle	en
heal.identifier.primary	10.1016/j.nbt.2011.01.006	en
heal.identifier.secondary	http://dx.doi.org/10.1016/j.nbt.2011.01.006	en
heal.language	English	en
heal.publicationDate	2011	en
heal.abstract	Novel silybin acylated derivatives with dicarboxylic acids were prepared in various organic solvents using immobilized Candida antarctica lipase B (Novozym 435®). The reaction parameters affecting the silybin conversion, such as the nature of the organic solvent and the acyl donor used were investigated. The antiproliferative effects of silybin monoesters, and their ability to modulate the secretion of vascular endothelial growth factor (VEGF) were estimated using K562 human lymphoblastoma cells and compared to the parental compound. The synthesized esters retained the biological function of silybin and in some cases were more effective, indicating that target biotransformation may generate novel compounds with improved antitumor and antiangiogenic activities. © 2011 Elsevier B.V.	en
heal.publisher	ELSEVIER SCIENCE BV	en
heal.journalName	New Biotechnology	en
dc.identifier.doi	10.1016/j.nbt.2011.01.006	en
dc.identifier.isi	ISI:000292717500007	en
dc.identifier.volume	28	en
dc.identifier.issue	4	en
dc.identifier.spage	342	en
dc.identifier.epage	348	en