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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Research Article

Morelloflavone as Potential Anticancer Agent Against MCF-7 Breast Cancer Cell Lines: In vitro and In silico Studies

Author(s): Darwati, Nurlelasari, Tri Mayanti, Nurul Ambardhani and Dikdik Kurnia*

Volume 19, Issue 4, 2022

Published on: 06 July, 2021

Page: [293 - 303] Pages: 11

DOI: 10.2174/1570180818666210706110538

Price: $65

Abstract

Background: Breast cancer is most commonly reported to contribute to people's death. Nowadays, cancer treatment is focused on investigating anticancer drugs from natural compounds. Various methods, including in vitro, in vivo, and in silico methods, are used to assess the potential of anticancer compounds. The efficacy of bioactive compounds from medicinal plant origin lies in their affordability and minimized side effects. The Garcinia genus contains bioactive compounds, such as xanthones, benzophenones, triterpenes, biflavonoids, and benzoquinones.

Objective: The study aimed at investigating an active compound that can inhibit cancer cell growth and proteins that contribute to cancer cell growth, such as Caspase-9, TNF-α, ER-α, and HER-2.

Methods: This study is divided into three steps. The first step is the isolation of the active compound from G. cymosa. The second step is an assessment of cytotoxic activity against MCF-7 cell by using MTT assay, and the last one is an investigation of the molecular mechanism of an active compound against Caspase-9, TNF-α, ER-α, and HER-2 by using in silico studies utilizing various programs, such as PyRx 0.8, PYMOL, and Discovery Studio.

Results: Morelloflavone from G. cymosa stem barks has exhibited anticancer activity (55.84 μg/mL) eight times lower than doxorubicin (6.99 μg/mL), but it can block the activity of Caspase-9, TNF-α, ER- α, and HER-2. The binding affinity of morelloflavone is the strongest of all ligands.

Conclusion: The natural flavonoid, morelloflavone, may be a new lead candidate for anticancer agent inhibiting action mechanism of Caspase-9, TNF-α, ER-α, and HER-2, respectively.

Keywords: Garcinia cymosa, morelloflavone, caspase-9, TNF-α, ER-α, HER-2.

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