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Molecules ; 25(5)2020 Feb 25.
Article in English | MEDLINE | ID: mdl-32106546

ABSTRACT

The present study is intended to carry out the chemical standardization and evaluation of the anti-proliferative activity of A. elliptica fruit extract. A. elliptica fruit powder was extracted with ethanol. The obtained extract was assessed for total phenolic content using the Folin-Ciocalteu method. Moreover, a simple, accurate, and precise reversed phase high-performance liquid chromatographic method was developed and validated to determine the embelin content of A. elliptica fruit extract. Then, the extract and embelin were investigated for their anti-proliferative effect against HCT-116 cells. Finally, the mechanisms of inhibition of the extract and embelin on the mRNA expression of pro-apoptotic genes Bad, Bax, and Caspase-8 and anti-apoptotic genes c-IAP1, Mcl-1, and XIAP were determined by real-time qRT-PCR. The phenolic content and embelin content of the extract were 5.20 ± 0.01 g of gallic acid equivalent per 100 g of dried fruit (g% GAE) and 5.57 ± 0.56 mg/g of extract, respectively. The extract and embelin showed strong anti-proliferative effects on HCT-116 cells with 50% inhibition concentration (IC50) values of 19.16 ± 1.09 µg/mL and 25.93 ± 1.75 µg/mL, respectively. The A. elliptica extract exhibited a significant increase in the mRNA level of Bad, Bax, and Caspase-8 and a significant decrease in c-IAP1, Mcl-1, and XIAP. Embelin showed a significant decrease in Mcl-1 and XIAP.


Subject(s)
Apoptosis/drug effects , Ardisia/chemistry , Cell Proliferation/drug effects , Colonic Neoplasms/drug therapy , Antioxidants/chemistry , Antioxidants/pharmacology , Caspase 8/genetics , Colonic Neoplasms/genetics , Colonic Neoplasms/pathology , Fruit/chemistry , Gene Expression Regulation, Neoplastic/drug effects , HCT116 Cells , Humans , Neoplasm Proteins/genetics , Phenols/chemistry , Phenols/pharmacology , bcl-2-Associated X Protein/genetics , bcl-Associated Death Protein/genetics
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