Abstract
Neohesperidin (NH) is a natural flavonoid glycoside compound with considerable physiological and pharmacological activities. However, its bioavailability is limited due to poor solubility, and few studies have so far attempted improve the solubility and bioavailability of NH. In this study, we structurally modified NH using an immobilized lipase to improve lipophilicity and therefore expand its applicability in lipophilic media as well as enhance its bioavailability in vivo. In addition, we aimed investigated the pro-apoptoptotic activity of this new compound (propionyl neohesperidin ester, PNHE) in MCF-7 breast cancer cells using a variety of cellular assays, including the MTT (3-(4, 5-dimethyl- 2-thiazolyl)-2, 5-diphenyl-2-h-tetrazolium bromide assay, assessment of intracellular reactive oxygen species (ROS) levels, and flow cytometry. We successfully synthesized PNHE using immobilized lipases, and the esterification of NH was confirmed by Fourier transform-infrared spectroscopy (FT-IR). Compared to NH, HNPE showed higher anti-proliferative and pro-apoptotic in MCF-7 breast cancer cells, which may be explained by its increased lipophilicity compared to neohesperidin, benefiting to the action of NH on the cancer cell wall. The IC50 of PNHE for inducing apoptosis of MCF-7 cells was 185.52 μg/mL. PNHE increased both the proportion of cells in Sub-G1 phase and the cellular ROS content, indicating a certain therapeutic effect of HNPE on breast cancer.
Highlights
Cancer is a critical global medical issue (Taher et al, 2012), and nearly 13% of deaths each year are caused by cancer (Bashandy et al, 2014)
We used the MTT assay to investigate the anti-proliferative effect of NH and PNHE on MCF-7 breast cancer cells
Our results show that both NH and PNHE can significantly inhibit the proliferation of MCF-7 cells in a dosedependent manner
Summary
Cancer is a critical global medical issue (Taher et al, 2012), and nearly 13% of deaths each year are caused by cancer (Bashandy et al, 2014). Lung cancer, breast cancer, colorectal cancer, stomach cancer, and prostate cancer are among main causes of death globally (Taher and Hegazy, 2013). There are several effective treatments for cancer, these often still carry many adverse. Synthesis of Propionyl Neohesperidin Ester effects including toxicity to normal cells and tissues. There is a need to identify safe and natural and safe substances that could be employed as anti-cancer drugs. Some natural flavonoids, including hesperidin and naringin, have been reported to have anti-proliferative activity (Dai et al, 2009; Wang et al, 2015). Natural flavonoid derivatives have shown potential anticancer properties by inducing tumor apoptosis (Chen and Yu, 2017)
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