Evaluation of Selected Flavonoids as Antiangiogenic, Anticancer, and Radical Scavenging Agents: An Experimental and In Silico Analysis

Abstract

Developing antiangiogenic agents using natural products has remained a significant hope in the mainstream of anticancer research. In the present investigation series of flavonoids possessing di-, tri-, tetra-, and penta-hydroxy substitutions were evaluated as antiangiogenic agents using in vivo choriallantoic membrane model. The MTT-based cytotoxicity against selected cancer cell lines was carried out to determine the anticancer potential. The kinetics of free radical scavenging activities of these compounds was demonstrated using 2,2-diphenyl-1-picryl hydrazine (DPPH) and superoxide anion radicals (SORs). To understand the possible antiangiogenic mechanism, the selected flavonoids were docked in silico onto the proangiogenic peptides such as vascular endothelial growth factor (VEGF), hypoxia inducible factor (HIF-1α), and vascular endothelial growth factor receptor-2 (VEGFR2) from human origin. The results of the study shows that amongst the tested flavonoids, genistein (87.1%), kaempferol, (86.3%), and quercetin (84.7%) were found to be effective inhibitors of angiogenesis in CAM model. The antiangiogenic, cytotoxic, and antioxidant activities are discussed in light of structure-activity relationship using in silico approach and other drug-related properties were also calculated using BioMed CAChe V. 6.1.10. The results of the present study focus the isoflavone genistein, kaempferol, and quercetin as lead molecules for designing novel anti-tumor/antioxidant agents targeting angiogenesis.

Evaluation of Curcumin Capped Copper Nanoparticles as Possible Inhibitors of Human Breast Cancer Cells and Angiogenesis: a Comparative Study with Native Curcumin

“…Previous studies have shown that CU has accounted to inhibit the invasion and migration of breast cancer cells by various mechanisms, such as CU inhibited the invasive potential of MDA-MB-231 cells by downregulation of MMP-2, MMP-3 and MMP-9 and upregulation of tissue inhibitor metalloproteinase We performed an MTT assay to study the effects of CU and CU-NPs on the proliferation of breast cancer cell line. The principle of the assay is that a mitochondrial enzyme in living cells, succinate dehydrogenase, cleaves the tetrazolium ring and converts the MTT to an insoluble purple formazan wherein the amount of formazan produced is directly proportional to the number of viable cells (34). Breast cancer cells treated with different concentrations of CU resulted in the inhibition of cell proliferation in a dose-and time-dependent manner.…”

“…The chorioallantoic membrane (CAM) assay was performed in an identical manner as depicted by (34). The fertilized chicken eggs were purchased from local markets at Nanded City, and then the eggs were cleaned for the disinfection.…”

“…The effect of CU and CU-NPs on cell proliferation was examined by performing MTT assay described elsewhere (34). In brief, the MDA-MB-231 cells were seeded into 96-well culture plate containing L-15 cell culture medium at a density of 1×10 4 cells/well.…”

Soybean extracts enriched with free isoflavones promote nitric oxide synthesis and affect the proliferation of breast adenocarcinoma cells

“…The antiproliferative activity of isoflavones has been well documented in various human tumor cell lines (Gacche et al, 2011). As the soybean exudates prepared by elicitation with 100 mmol.L -1 SNP for 20 h produced the best response in terms of aglycone forms (Figure 2), their effects on MCF-7 and 3T3 cell lines were evaluated and compared with those of nonelicited extracts.…”

Effects of quercetin on CDK4 mRNA and protein expression in A549 cells infected by H1N1

“…Previous studies demonstrated that quercetin possesses significant antitumor, anti-inflammatory, antioxidant and other biological properties (4,5). Several previous studies demonstrated that quercetin directly interacts with different types of viruses, reducing their infective potential (6,7).…”