Antiproliferative Activity of Two Unusual Dimeric Flavonoids, Brachydin E and Brachydin F, Isolated from Fridericia platyphylla (Cham.) L.G.Lohmann: In Vitro and Molecular Docking Evaluation

Despite the breakthrough in the development of anticancer therapies, plant-derived chemotherapeutics continue to be the basis of treatment for most types of cancers. Fridericia platyphylla is a shrub found in Brazilian cerrado biome which has cytotoxic, anti-inflammatory, and analgesic properties. T...

Full description

Saved in:

Bibliographic Details
Published in:	BioMed research international Vol. 2022; pp. 3319203 - 12
Main Authors:	de Lima, Carolina A., Cubero, Mayra C. Z., Franco, Yollanda E. M., Rodrigues, Carla D. P., do Nascimento, Jessyane R., Vendramini-Costa, Débora B., Sciani, Juliana M., da Rocha, Cláudia Q., Longato, Giovanna B.
Format:	Journal Article
Language:	English
Published:	United States Hindawi 11-02-2022 John Wiley & Sons, Inc Hindawi Limited
Subjects:	Adenocarcinoma Analgesics Anticancer properties Antimitotic agents Antineoplastic agents Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antiproliferatives Antitumor activity Bignoniaceae - chemistry Bioflavonoids Brazil Cancer therapies Cell death Cell Line, Tumor Cell viability Chemical properties Cytotoxicity Dimers Flavones Flavonoids Flavonoids - pharmacology Fridericia platyphylla Glioblastoma Glucocorticoids Health aspects Humans Humidity Inflammation Lamiales Medical research Medicine, Experimental Molecular docking Molecular Docking Simulation Nuclear receptors Physiological aspects Plant Extracts - chemistry Plant Roots - chemistry Prostate Prostate cancer Receptors Shrubs Tumor cell lines Tumors Wound healing Brazil United States > US
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	Despite the breakthrough in the development of anticancer therapies, plant-derived chemotherapeutics continue to be the basis of treatment for most types of cancers. Fridericia platyphylla is a shrub found in Brazilian cerrado biome which has cytotoxic, anti-inflammatory, and analgesic properties. The aim of this study was to investigate the antiproliferative potential of the crude hydroethanolic extract, subfraction (containing 59.3% of unusual dimeric flavonoids Brachydin E and 40.7% Brachydin F), as well as Brachydin E and Brachydin F isolated from F. platyphylla roots. The cytotoxic activity was evaluated in glioblastoma, lung, prostate, and colorectal human tumor cell lines. The crude hydroethanolic extract did not present cytotoxic activity, but its subfraction presented lower IC50 values for glioblastoma (U-251) and prostate adenocarcinoma (PC-3) cell lines. Brachydins E and F significantly reduced cell viability, proliferation, and clonogenic potential of PC-3, inducing them to the process of regulated cell death. In silico studies have indicated nuclear receptors as targets for Brachydins E and F, and molecular docking has pointed out their binding into glucocorticoid receptor (GR) ligand pocket. Targeting GR pathway has been described as a therapeutic strategy, especially for prostate cancer. These results suggest that Brachydin E and Brachydin F are promising compounds to be further explored for their antitumor effects.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 Academic Editor: Dorota Formanowicz
ISSN:	2314-6133 2314-6141
DOI:	10.1155/2022/3319203