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Anti-Cancer Efficacy of Silybin Derivatives - A Structure-Activity Relationship

SYSNO ASEP	0392676
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	Anti-Cancer Efficacy of Silybin Derivatives - A Structure-Activity Relationship
Author(s)	Agarwal, Ch. (US) Wadhwa, R. (US) Deep, G. (US) Biedermann, David (MBU-M)_{RID, ORCID} Gažák, Radek (MBU-M)_{RID, ORCID} Křen, Vladimír (MBU-M)_{RID, ORCID} Agarwal, R. (US)
Source Title	PLoS ONE. - : Public Library of Science - ISSN 1932-6203 Roč. 8, č. 3 (2013), e00074
Number of pages	11 s.
Language	eng - English
Country	US - United States
Keywords	Silybin ; silibinin ; anti-cancer efficacy
Subject RIV	CE - Biochemistry
R&D Projects	ME10027 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
Institutional support	MBU-M - RVO:61388971
UT WOS	000317262200079
DOI	10.1371/journal.pone.0060074
Annotation	Silybin or silibinin, a flavonolignan isolated from Milk thistle seeds, is one of the popular dietary supplements and has been extensively studied for its antioxidant, hepatoprotective and anti-cancer properties. We have envisioned that potency of silybin could be further enhanced through suitable modification/s in its chemical structure. Accordingly, here, we synthesized and characterized a series of silybin derivatives namely 2,3-dehydrosilybin (DHS), 7-O-methylsilybin (7OM), 7-Ogalloylsilybin (7OG), 7,23-disulphatesilybin (DSS), 7-O-palmitoylsilybin (7OP), and 23-O-palmitoylsilybin (23OP); and compared their anti-cancer efficacy using human bladder cancer HTB9, colon cancer HCT116 and prostate carcinoma PC3 cells. In all the 3 cell lines, DHS, 7OM and 7OG demonstrated better growth inhibitory effects and compared to silybin, while other silybin derivatives showed lesser or no efficacy. Next, we prepared the optical isomers (A and B) of silybin, DHS, 7OM and 7OG, and compared their anti-cancer efficacy. Isomers of these three silybin derivatives also showed better efficacy compared with respective silybin isomers, but in each, there was no clear cut silybin A versus B isomer activity preference
Workplace	Institute of Microbiology
Contact	Eliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231
Year of Publishing	2014

Number of the records: 1