Antiproliferative and ROS Regulation Activity of Photoluminescent Curcumin-Derived Nanodots.

Abstract

Recently, various types of nanomaterials have been employed to design delivery vehicles for curcumin to address the problems of poor bioavailability, low aqueous solubility, and rapid metabolism. The present study focuses on a direct one-pot synthesis of curcumin-derived nanoparticles and exploits their potential therapeutic properties in cancer cells in vitro without additional delivery vehicles. The nanoparticles, named E-Curc-dots, are synthesized using three precursor molecules, ethylenediamine (EDA), curcumin, and citric acid. The structure, composition, and physichemical properties of the nanodots are characterized and identified by employing spectroscopic and microscopic techniques. The as-synthesized E-Curc-dots exhibit bright blue photoluminescence due to the incorporation of nitrogen from the EDA precursor molecule. The characterization studies show a uniform distribution of dots with an average size of 4.6 ± 1.7 nm and, notably, that the dots retain some of the major characteristics of native curcumin with much improved water solubility and bioavailability. The E-Curc-dots show antioxidation activity at low concentrations (<0.08 mg/mL) with low levels of reactive oxygen species (ROS) generation, i.e., 82% of the ROS level in cells without treatment for A549 cells; however, at high concentrations, the nanodots exhibit a pro-oxidant effect on both the cancer cells (A549) and normal cells (EA.hy926) by inducing more ROS generation and dose-dependent cytotoxicity. The E-Curc-dots demonstrate higher cytotoxicity toward cancer cells compared to native curcumin at a lower concentration. The results indicate the efficacy of E-Curc-dots as an antiproliferative and ROS regulator with the ability of cellular bioimaging.