Abstract
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.
Highlights
Green plants contain an impressive number ofcompounds, which are classified as either derivatives of primary metabolism or derivatives of the secondary metabolism [1,2,3,4,5]
Food bioactive compounds mainly belong to the secondary metabolism derivatives and they refer to compounds that have an adaptive role for green plants, as they ensure the interaction between the plant and the environment [6,7,8,9]
The goal of this paper was to study the antiproliferative activity of an ethanolic extract from Stokesia laevis (Slae26) and its combinations with several polyphenols compounds on the human colon tumor cell line Caco-2 (ATCC-HTB-37), in an attempt to increase the biological activity of Slae26 [33,34] by concentrating it in own active compounds and other food-related bioactive compounds with high bioavailability and benefits in cancer fight at humans
Summary
Green plants contain an impressive number of (phyto)compounds (estimated at several thousand distinct molecules), which are classified as either derivatives of primary metabolism or derivatives of the secondary metabolism [1,2,3,4,5]. Compounds from flavonoids subclasses (e.g., flavones, flavonols, flavanones, flavanonols, flavanols/catechins, anthocyanins, isoflavones, neoflavonoids, and chalcones) and other non-flavonoids phenolics such as phenolic acids, tannins, terpenoids, volatile oils, coumarins, lignans, and triterpene acids have been proved to have certain health benefits in humans [1,2]. In this context, food-related bioactive compounds are significant in their number, and possess very complex molecules with numerous pharmacological activities and benefits for human health. Plant compounds druggability studies proved that the first four rules of Lipinski [14] do not apply to the natural products or other molecules that are the subject of an active transport system [15,16,17]
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