Antiproliferative Activity of Stokesia laevis Ethanolic Extract in Combination with Several Food-Related Bioactive Compounds; In Vitro (Caco-2) and In Silico Docking (TNKS1 and TNKS2) Studies
Autor: | Adrian Albulescu, Amalia Stefaniu, Lucia Pintilie, Georgeta Neagu, Lucia Pirvu |
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Jazyk: | angličtina |
Rok vydání: | 2021 |
Předmět: |
antiproliferative activity
Technology Stokesia laevis QH301-705.5 QC1-999 chemistry.chemical_compound health effects food bioactive compounds Caffeic acid General Materials Science Viability assay Gentisic acid Biology (General) stokes aster ethanolic extracts Caco-2 cells docking TNKS1 TNKS2 Instrumentation QD1-999 Fluid Flow and Transfer Processes biology Process Chemistry and Technology Physics General Engineering biology.organism_classification Engineering (General). Civil engineering (General) In vitro Computer Science Applications Chemistry chemistry Biochemistry Caco-2 Polyphenol Docking (molecular) TA1-2040 |
Zdroj: | Applied Sciences, Vol 11, Iss 9944, p 9944 (2021) Applied Sciences; Volume 11; Issue 21; Pages: 9944 |
ISSN: | 2076-3417 |
Popis: | This study evaluates in vitro cytotoxic and antiproliferative activity on human colon tumor cell line Caco-2 (ATCC-HTB-37) of a standardized (5 mg GAE/mL) ethanolic extract from Stokesia laevis (Slae26), of five polyphenols compounds (reference substances, ref.), namely luteolin-7-O-glucoside, luteolin-8-C-glucoside, caffeic acid, gentisic acid, and p-aminobenzoic acid (PABA), as well as of Slae26 combinations with the five reference substances, 1:1 mass rate (GAE, ref.). Cell viability studies (MTS test) have revealed IC50 values of 36 μg GAE/mL in the case of Slae26 ethanolic extract, while Slae26 combinations with the five phenolics indicated IC50 values around 5 μg GAE/mL. In silico docking studies on the molecular targets human tankyrase 1 (TNKS1) and human tankyrase 2 (TNKS2) in complex with their native ligands, Co-crystallized 3J5A and Co-crystallized FLN, indicated score values of −104.15 and −76.97, respectively; in the series of the reference compounds studied, luteolin-7-O-glucoside was revealed with the best score values on both molecular targets (−80.49 and −85.17), together signifying real antiproliferative potential against human colon cancer of Slae26, of luteolin-7-O-glucoside, and of Slae26 combinations with all food-related bioactive compounds tested. |
Databáze: | OpenAIRE |
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