Effect of selected flavones on cancer and endothelial cells

Abstract

Abstract. In our study we used quercetin (3,3´,4´,5,7-pentahydroxyflavone) as the reference standard to compare antiproliferative and antiangiogenic effects of chrysin (5,7-dihydroxyflavone) and 3-hydroxyflavone.Our data indicates that chrysin and 3-hydroxyflavone showed significantly higher cytotoxic effect than reference standard quercetin. These tested agents significantly decreased cell survival with the efficacy of 65-85% at the concentration 100 µmol/l for HUVEC, lung carcinoma and leukemic cells being the most sensitive. Cell cycle analysis indicates that quercetin and 3-hydroxyflavone might affect the cell cycle of Jurkat cells by a similar or the same mechanism of action which lead to G 2 /M arrest as well as to an increase in sub-G 0 /G 1 fraction. Treatment of Jurkat cells with chrysin resulted only increase in the fraction of cells with sub-G 0 /G 1 DNA content, which is considered to be a marker of apoptotic cell death. Apoptosis was confirmed by DNA fragmentation and by staining with annexin V.All three tested flavones inhibited endothelial cell migration after 24 h of incubation at a concentration 100 µmol/l. At a lower concentration (10 µmol/l) only quercetin significantly inhibited migration of endothelial cells. Furthermore, in our experiments decreased secretion of matrix metalloproteinases (MMP-2 and MMP-9) was observed after a 72 h treatment with quercetin. No decrease in secretion of MMP-2 and MMP-9 was seen after chrysin and 3-hydroxyflavone treatment. On the other hand, our results showed that none of three flavonoids blocked microcapillary tube formation.Further studies are necessary to investigate the mechanism of action and to find out the relationship between the structure, character and position of substituents of natural substances and their biological activities.

Effect of Antioxidant Treatment on Fibrogenesis in Rats with Carbon Tetrachloride-Induced Cirrhosis

“…However, during fibrogenesis, the expression of MMP-1 or MMP-13 is very limited, whereas that of MMP-2 increases [29]. Our study showed a reduction in the expression of MMP-2 after treatment with quercetin and these results are consistent with an in vitro study that demonstrated decreased secretion of matrix metalloproteinases (MMP-2 and MMP-9) after a 72-hour treatment with quercetin [30]. …”

Combined treatment of 3-hydroxyflavone and imatinib mesylate increases apoptotic cell death of imatinib mesylate-resistant leukemia cells

“…3-HF is the backbone of all flavonols, a type of flavonoid, which are commercially available synthetic flavonoid derivatives. Other studies also reported cytotoxic effect of 3-HF on cancer cells [32,33]. There are few examples applying 3-HF to animal models.…”

Soy and Breast Cancer: Focus on Angiogenesis

“…Tumor angiogenesis can be inhibited by blocking some of these steps. Several papers have been published referring on the modulatory effect of flavonoids on angiogenesis [71,72,73,74,75,76,77,78]. Soy isoflavonoids also exhibit anti-angiogenic activities, but the precise mechanism of inhibition remains unclear.…”