Antiproliferative Activity of <i>Stokesia laevis</i> Ethanolic Extract in Combination with Several Food-Related Bioactive Compounds; In Vitro (Caco-2) and In Silico Docking (TNKS1 and TNKS2) Studies

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 <i>Stokesia laevis</i> (Slae26), of five polyphenols compounds (reference substances, ref.), namely luteolin-7...

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Autores principales: Georgeta Neagu, Amalia Stefaniu, Adrian Albulescu, Lucia Pintilie, Lucia Camelia Pirvu
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Lenguaje:EN
Publicado: MDPI AG 2021
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spelling oai:doaj.org-article:455bcc5ab3df4c2fad9ae6b7ccccf5412021-11-11T15:02:44ZAntiproliferative Activity of <i>Stokesia laevis</i> Ethanolic Extract in Combination with Several Food-Related Bioactive Compounds; In Vitro (Caco-2) and In Silico Docking (TNKS1 and TNKS2) Studies10.3390/app112199442076-3417https://doaj.org/article/455bcc5ab3df4c2fad9ae6b7ccccf5412021-10-01T00:00:00Zhttps://www.mdpi.com/2076-3417/11/21/9944https://doaj.org/toc/2076-3417This 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 <i>Stokesia laevis</i> (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 IC<sub>50</sub> values of 36 μg GAE/mL in the case of Slae26 ethanolic extract, while Slae26 combinations with the five phenolics indicated IC<sub>50</sub> 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.Georgeta NeaguAmalia StefaniuAdrian AlbulescuLucia PintilieLucia Camelia PirvuMDPI AGarticlefood bioactive compoundsstokes aster ethanolic extractshealth effectsantiproliferative activityCaco-2 cellsdockingTechnologyTEngineering (General). Civil engineering (General)TA1-2040Biology (General)QH301-705.5PhysicsQC1-999ChemistryQD1-999ENApplied Sciences, Vol 11, Iss 9944, p 9944 (2021)
institution DOAJ
collection DOAJ
language EN
topic food bioactive compounds
stokes aster ethanolic extracts
health effects
antiproliferative activity
Caco-2 cells
docking
Technology
T
Engineering (General). Civil engineering (General)
TA1-2040
Biology (General)
QH301-705.5
Physics
QC1-999
Chemistry
QD1-999
spellingShingle food bioactive compounds
stokes aster ethanolic extracts
health effects
antiproliferative activity
Caco-2 cells
docking
Technology
T
Engineering (General). Civil engineering (General)
TA1-2040
Biology (General)
QH301-705.5
Physics
QC1-999
Chemistry
QD1-999
Georgeta Neagu
Amalia Stefaniu
Adrian Albulescu
Lucia Pintilie
Lucia Camelia Pirvu
Antiproliferative Activity of <i>Stokesia laevis</i> Ethanolic Extract in Combination with Several Food-Related Bioactive Compounds; In Vitro (Caco-2) and In Silico Docking (TNKS1 and TNKS2) Studies
description 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 <i>Stokesia laevis</i> (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 IC<sub>50</sub> values of 36 μg GAE/mL in the case of Slae26 ethanolic extract, while Slae26 combinations with the five phenolics indicated IC<sub>50</sub> 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.
format article
author Georgeta Neagu
Amalia Stefaniu
Adrian Albulescu
Lucia Pintilie
Lucia Camelia Pirvu
author_facet Georgeta Neagu
Amalia Stefaniu
Adrian Albulescu
Lucia Pintilie
Lucia Camelia Pirvu
author_sort Georgeta Neagu
title Antiproliferative Activity of <i>Stokesia laevis</i> Ethanolic Extract in Combination with Several Food-Related Bioactive Compounds; In Vitro (Caco-2) and In Silico Docking (TNKS1 and TNKS2) Studies
title_short Antiproliferative Activity of <i>Stokesia laevis</i> Ethanolic Extract in Combination with Several Food-Related Bioactive Compounds; In Vitro (Caco-2) and In Silico Docking (TNKS1 and TNKS2) Studies
title_full Antiproliferative Activity of <i>Stokesia laevis</i> Ethanolic Extract in Combination with Several Food-Related Bioactive Compounds; In Vitro (Caco-2) and In Silico Docking (TNKS1 and TNKS2) Studies
title_fullStr Antiproliferative Activity of <i>Stokesia laevis</i> Ethanolic Extract in Combination with Several Food-Related Bioactive Compounds; In Vitro (Caco-2) and In Silico Docking (TNKS1 and TNKS2) Studies
title_full_unstemmed Antiproliferative Activity of <i>Stokesia laevis</i> Ethanolic Extract in Combination with Several Food-Related Bioactive Compounds; In Vitro (Caco-2) and In Silico Docking (TNKS1 and TNKS2) Studies
title_sort antiproliferative activity of <i>stokesia laevis</i> ethanolic extract in combination with several food-related bioactive compounds; in vitro (caco-2) and in silico docking (tnks1 and tnks2) studies
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/455bcc5ab3df4c2fad9ae6b7ccccf541
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AT amaliastefaniu antiproliferativeactivityofistokesialaevisiethanolicextractincombinationwithseveralfoodrelatedbioactivecompoundsinvitrocaco2andinsilicodockingtnks1andtnks2studies
AT adrianalbulescu antiproliferativeactivityofistokesialaevisiethanolicextractincombinationwithseveralfoodrelatedbioactivecompoundsinvitrocaco2andinsilicodockingtnks1andtnks2studies
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