Interaction of Arylidenechromanone/Flavanone Derivatives with Biological Macromolecules Studied as Human Serum Albumin Binding, Cytotoxic Effect, Biocompatibility Towards Red Blood Cells

研究亚芳基色酮/黄酮衍生物与生物大分子的相互作用,包括其与人血清白蛋白的结合、细胞毒性作用以及对红细胞的生物相容性。

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Abstract

The aim of this study was to determine the cytotoxic effect of 3-arylidenechromanone (1) and 3arylideneflavanone (2) on HL-60 and NALM-6 cell lines (two human leukemia cell lines) and a WM-115 melanoma cell line. Both compounds exhibited high cytotoxic activity with higher cytotoxicity exerted by compound 2, for which IC(50) values below 10 µM were found for each cell line. For compound 1, the IC(50) values were higher than 10 µM for HL-60 and WM-115 cell lines, but IC(50) < 10 µM was found for the NALM-6 cell line. Both compounds, at the concentrations close to IC(50) (concentration range: 5⁻24 µM/L for compound 1 and 6⁻10 µM/L for compound 2), are not toxic towards red blood cells. The synthesized compounds were characterized using spectroscopic methods ¹H- and (13)C-NMR, IR, MS, elemental analysis, and X-ray diffraction. The lipophilicity of both synthesized compounds was determined using an RP-TLC method and the logP values found were compared with the theoretical ones taken from the Molinspiration Cheminformatics (miLogP) software package. The mode of binding of both compounds to human serum albumin was assessed using molecular docking methods.

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