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Cytotoxic activity of caffeic acid and gallic acid against MCF-7 human breast cancer cells: An in silico and in vitro study.

ABSTRACT: Objective:Phenolic compounds have been considered inhibitors of various cancers. Material and Methods:In this study, caffeic acid and gallic acid were appraised for their possible effects on apoptotic genes expression in a breast cancer cell line in vitro. We also evaluated ligand interaction and ligand binding with estrogen receptor alpha by molecular docking. To determine half maximal inhibitory concentration, MCF-7 cells were treated with different concentrations of caffeic acid and gallic acid by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay. Furthermore, morphological changes in cells and alterations in P53, Mcl-1 and P21 gene expression were studied by real-time RT-PCR. Also, protein network and different interactions between the desired genes were analyzed using GeneMANIA database. Results:Evaluation of cell survival by MTT assay revealed that the half-maximal inhibitory concentration values for caffeic acid and gallic acid against MCF-7 cells, were 159 and 18 µg/ml, respectively. These compounds were found to affect P53, Mcl-1 and P21 gene expression; this alteration in gene expression probably occurred along with the activation of intrinsic apoptotic signaling pathway. Conclusion:Via apoptosis induction, caffeic acid and gallic acid have induce toxic effects and morphological changes in breast cancer cells, suggesting their possible future application as antitumor agents.

SUBMITTER: Rezaei-Seresht H

PROVIDER: S-EPMC6823530 | biostudies-literature | 2019 Nov-Dec

REPOSITORIES: biostudies-literature

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Cytotoxic activity of caffeic acid and gallic acid against MCF-7 human breast cancer cells: An <i>in silico</i> and <i>in vitro</i> study.

Rezaei-Seresht Hasan H Cheshomi Hamid H Falanji Farahnaz F Movahedi-Motlagh Fatemeh F Hashemian Maryam M Mireskandari Erfan E

Avicenna journal of phytomedicine 20191101 6

<h4>Objective</h4>Phenolic compounds have been considered inhibitors of various cancers.<h4>Material and methods</h4>In this study, caffeic acid and gallic acid were appraised for their possible effects on apoptotic genes expression in a breast cancer cell line <i>in vitro</i>. We also evaluated ligand interaction and ligand binding with estrogen receptor alpha by molecular docking. To determine half maximal inhibitory concentration, MCF-7 cells were treated with different concentrations of caff ...[more]

PMID: 31763216

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Project description:BackgroundCancer is a leading cause of death worldwide, with breast cancer being the most common invasive cancer type in women. Several therapeutic strategies have been explored to reduce the mortality rates of breast cancer. Chemotherapy is the most commonly used systemic treatment, but associated with numerous side-effects. Development of anticancer agents with high efficacy and minimal negative effects is therefore an important focus of research. Natural materials provide an excellent source of bioactive compounds. For instance, Garcinia porrecta from the Clusiaceae family has multiple pharmacological activities, including antioxidant, anti-inflammatory, antibacterial, antiviral, anti-HIV, antidepressant, and anticancer properties.PurposeThe main objective of this study was to investigate the potential anticancer effects of compounds extracted from the bark of G. porrecta.Materials and methodsOur experiments were divided into three steps: (1) chromatographic isolation of compounds using various separation techniques, such as extraction, separation and purification, (2) characterization via infrared (IR), nuclear magnetic resonance (NMR) and mass spectroscopy, and (3) evaluation of anticancer activity in vitro (MTT assay) and in silico (via analysis of molecular docking against caspase-9, tumor necrosis factor alpha (TNF-α), estrogen receptor alpha (ER-α), and human epidermal growth factor receptor 2 (HER-2)).ResultsDepsidone (1) and benzophenone (2) from the ethyl acetate extract of bark of G. porrecta were identified as bioactive components. Examination of the activities of these compounds against MCF-7 cells revealed an IC50 value of 119.3 µg/mL for benzophenone, whereas IC50 for depsidone could not be estimated. Benzophenone activity was lower than that of the positive control doxorubicin (6.9 µg/mL). Depsidone showed the highest binding affinity for HER-2 (-9.2 kcal.mol-1) and benzophenone for ER-α (-8.0 kcal.mol-1).ConclusionBenzophenone displays potency as an anticancer agent through blocking ER-α.

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Cytotoxic activity of caffeic acid and gallic acid against MCF-7 human breast cancer cells: An in silico and in vitro study.

Publications

Cytotoxic activity of caffeic acid and gallic acid against MCF-7 human breast cancer cells: An <i>in silico</i> and <i>in vitro</i> study.

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