In vitro study of 2,3-dehydrosilybin and its galloyl esters as potential inhibitors of angiogenesis

被引：2

作者：

Pivodova, V. ^{[1
,2
]}

Zahler, S. ^{[3
]}

Karas, D. ^{[1
,2
]}

Valentova, K. ^{[4
]}

Ulrichova, J. ^{[1
,2
]}

机构：

[1] Palacky Univ Olomouc, Fac Med & Dent, Dept Med Chem & Biochem, Hnevotinska 3, Olomouc 77515, Czech Republic

[2] Palacky Univ Olomouc, Fac Med & Dent, Inst Mol & Translat Med, Olomouc, Czech Republic

[3] Univ Munich, Dept Pharm, Ctr Drug Res, Pharmaceut Biol, Munich, Germany

[4] Czech Acad Sci, Inst Microbiol, Prague, Czech Republic

来源：

PHARMAZIE | 2016年 / 71卷 / 08期

关键词：

NF-KAPPA-B; VASCULAR ENDOTHELIAL-CELLS; GROWTH-FACTOR; PROSTATE-CANCER; DOWN-REGULATION; SILYBUM-MARIANUM; TUMOR-GROWTH; CYCLE ARREST; SILIBININ; AKT;

D O I：

10.1691/ph.2016.6579

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2,3-Dehydrosilybin exhibits substantial anticancer and antiangiogenic effects, which can be potentially improved by semi-synthetic modification such as esterification with gallic acid. The aim of this study was to examine the potential antiangiogenic effect of 2,3-dehydrosilybin and its galloyl esters (3-O-galloyl-2,3-dehydrosilybin; 7-O-galloyl-2,3-dehydrosilybin; 20-O-galloyl-2,3-dehydrosilybin and 23-O-galloyl-2,3-dehydrosilybin) and to determine which molecular mechanism could be responsible for their activity. The effect on cell proliferation, tube formation, signal transduction pathways (PI3K/Akt and ERK) and the cell cycle was studied in human microvascular endothelial cells (HMEC). The results showed that all compounds decreased the growth of HMEC, but the strongest effect was observed for 20-O-galloyl-2,3-dehydrosilybin at 5 mu mol/l. In addition, at 5 and 10 mu mol/l, this was the only compound that significantly inhibited HMEC tube formation. Based on an assessment of Akt and ERK1/2 expression, we suggest that 20-O-galloyl-2,3-dehydrosilybin influences the angiogenic process through the Akt pathway.

引用

页码：478 / 483

页数：6

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