In Vitro Cytotoxic and Antiproliferative Activity of Cydonia oblonga flower petals, leaf and fruit pellet ethanolic extracts. Docking simulation of the active flavonoids on anti-apoptotic protein Bcl-2

Abstract

AbstractThis study aimed to compare in vitro cell cytotoxicity and antiproliferative potency of three standardized ethanolic extracts (5mg GAE/mL sample) from quince flower petals, leaves and fruit pellet on four cell lines (L-929, and HepG2, Caco-2 and BT-20 respectively). Comparative analytical qualitative studies (HPTLC) indicated that if quince leaf extracts (Col40) mainly contain quercetin and kaempferol derivates, the flower petal extracts (Cof40) contain caffeoylquinic acid derivates, while the fruit pellet extracts (Cop40) are comprised of quercetin and caffeoylquinic acid derivates. Pharmacological studies demonstrated the lack of toxicity of test extracts; the most important antiproliferative effects were observed on the hepatic cancer cell line HepG2 (up to 75%, 53% and 70% inhibition in the case of Col40, Cof40 and Cop40 test extracts), followed by the colon cancer cell line Caco-2 (up to 69%, 77% and 40% inhibition) and breast cancer cell line BT-20 (up to 54%, 61% and 19% inhibition). The docking simulations on hyperoside, isoquercitrin, astragalin, and quercetin and kaempferol compared to the synthetic co-crystallized LI0 A1000 ligand (a strong inhibitor of anti-apoptotic protein Bcl-2) indicated astragalin as the most feasible protein inhibitor, but quercetin and kaempferol respected all the parameters involved in the Lipinski rule, making them the most promising antiproliferative candidates.