Procyanidin B2 cytotoxicity to MCF-7 human breast adenocarcinoma cells

Abstract

Procyanidins have attracted some attention due to their demonstrated chemopreventive action, a relatively new and promising strategy to prevent cancer. Breast cancer is one of the leading causes of death in women worldwide and its treatment needs improvements. The aim of this work was to verify the procyanidin dimmer B2 cytotoxic effect to MCF-7 human breast cancer cells. MCF-7 cells were cultured in RPMI medium, containing 20% fetal bovine serum and antibiotics in a CO2 chamber. The cells were treated with different concentrations of B2 and its cytotoxic potential was assessed by the sulforhodamine B assay, morphologically through haematoxylin-eosin staining and by DNA fragmentation analysis. The significance of differences between experimental conditions was determined using the ANOVA test, followed by the Tukey test when P<0.05. Cell proliferation decreased in a concentration and time-dependent manner upon procyanidin dimmer B2 treatment, being 19.20 μM the IC50. Procyanidin dimmer B2 treatment displayed concentration and time-dependent decline in MCF-7 cells compared to control and also induced morphological alterations compatible with cell-death induction. Cell condensation and cell diameter decreased (3.5 folds compared to control cells), after 48 h cell-exposure to 50 μM procyanidin dimmer B2, but the DNA ladder formation was not observed. In conclusion, our results demonstrated that procyanidin dimmer B2 exhibits cytotoxic activity to MCF-7 cells and it could be a potential antineoplastic agent. Further studies are necessary to clarify the procyanidin dimmer B2 mechanism of action. The evaluation of biological efficacy of individual components is an important step towards drug discovery and development.

Proanthocyanidins Protect Epithelial Cells from Zearalenone-Induced Apoptosis via Inhibition of Endoplasmic Reticulum Stress-Induced Apoptosis Pathways in Mouse Small Intestines

“…The results were consistent with our previous findings that PCs affected the growth of Sertoli TM4 cells [ 42 ]. Our results further confirmed that in an appropriate concentration range, PCs had growth-promoting effects, and when the maximum concentration range was exceeded, this could cause cytotoxicity [ 42 , 43 , 44 ].…”

“…Additionally, at this concentration, PCs did not significantly reduce the increase in the expression of these proteins induced by ZEA. Previous studies have also shown that PCs at a high dose (500 mg/mL) could increase cell death [ 43 ] and that procyanidin dimmer B2 (50 μM) was more cytotoxic than cyclophosphamide in MCF-7 human breast adenocarcinoma cells [ 44 ]. However, it was generally safe when the oral intake of PCs was up to 2500 mg for 4 weeks in humans [ 58 ], and a rat diet containing 2% of PCs produced no observed adverse effect level (NOAEL) [ 59 ].…”

Direct Effects of (−)-Epicatechin and Procyanidin B2 on the Respiration of Rat Heart Mitochondria

“…Meanwhile, procyanidins and especially procyanidin B2 have been demonstrated to exert chemopreventive action, a relatively new and promising strategy to prevent cancer [ 6 ], as well as modulation of signal transduction pathway, anti-inflammatory properties [ 7 ], and antioxidant and prooxidant activity [ 8 ].…”

Cancer Chemopreventive Potential of Procyanidin

“…Oligomers and polymers of flavan-3-ol have a higher antiproliferative effect in cells than do monomers and dimers ( 32 , 33 ). Recently, synthesized procyanidin B2 (100 μM) was shown to significantly inhibit nuclear transcription factor kappa B (NF-κB), activator protein-1 (AP1) transcriptional activity, and nuclear translocation of signal transducer and activator of transcription 3 (Stat 3) in prostate cancer cells ( 34 ), whereas natural procyanidin B2 (50 μM) showed cytotoxicity without apoptosis in MCF-7 cells ( 8 ). Mackenzie et al .…”

“…Through research compilations that compared the chemopreventive potentials and probable mechanisms of polyphenolic compounds since 1995, procyanidin has received increasing interest for its pharmacological properties and antioxidant effects ( 5 – 7 ). Recent cell culture studies have shown that treatment of human breast cancer MCF-7 ( 8 ) and MDA-MB-468 ( 9 ), human lung cancer A427 ( 10 ), human oral squamous cell cancers CAL27 and SCC25 ( 11 ), human prostate cancer DU145 ( 12 , 13 ) and LNCaP ( 14 , 15 ), human bladder cancer BIU87 ( 16 ), and human colorectal cancer HCT-8, HT29, LoVo, and Caco-2 cells ( 17 – 23 ) with procyanidin resulted in an inhibition of cell proliferation and/or an induction of cell apoptosis without an additional cytotoxic effect on normal cells ( 20 , 24 – 26 ). Procyanidin can alter gene expression in animal models, which indicates its potential as a chemopreventive agent.…”