Effectiveness and Anticancer Activity of a Novel Phenolic Compound from Garcinia porrecta Against the MCF-7 Breast Cancer Cell Line in vitro and in silico

Abstract

Background Cancer 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. Purpose The main objective of this study was to investigate the potential anticancer effects of compounds extracted from the bark of G. porrecta . Materials and Methods Our 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)). Results Depsidone ( 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 IC 50 value of 119.3 µg/mL for benzophenone, whereas IC 50 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). Conclusion Benzophenone displays potency as an anticancer agent through blocking ER-α.

On Overview Of Bioactive Compounds, Biological And Pharmacological Effects Of Mistletoe (Viscum Album L)

“…Polyphenols occupy an important place in the life of plants by intervening in their metabolism. There are known about 8.000 plant-derived polyphenol compounds with antioxidant and antitumor properties [53][54][55][56][57][58]. Polyphenols are organic, watersoluble compounds that contain in their molecule one or more aromatic rings with one or more hydroxyl groups.…”

Breast cancer research: in vitro models, markers, and in silico analysis - a narrative review

“…Doxorubicin was used to check the sensitivity of MCF-7 and T47D cell lines, where doxorubicin and NK immunotherapy in combination supported the BC treatment [11]. Further, a research study evaluated effect of phenolic compound on MCF7 cell line and showed that used compound has anti-cancer potential [12]. Trilla-Fuertens and his team in 2018 used CAMA1, T47D, MCF7, MDA-MB-468, HCC1143 and MDA-MB-231 cell lines in order to check metabolic drug response using metformin and rapamycin [13].…”

Biological Screening of Polyphenol Derivatives for Anti‐Proliferative, Anti‐Apoptotic and Anti‐Migrative Activities in Human Breast Cancer Cell Lines MCF‐7

“…The MCF‐7 cancer cell line has complex morphological and molecular characteristics. One of the reasons for the widespread use of the MCF‐7 cell line in laboratories around the world is its identification as an advantageous cancer model due to its known cytological and molecular characteristics [2–4] …”

“…One of the reasons for the widespread use of the MCF-7 cell line in laboratories around the world is its identification as an advantageous cancer model due to its known cytological and molecular characteristics. [2][3][4] Breast epithelial cell homeostasis requires the balance of cell proliferation with apoptosis. Cancer cells treated with anti-cancer compounds usually loss their viability using apoptotic pathways.…”