Abstract
We synthesized twelve hybrids based on curcumin and resveratrol, and their structures were elucidated by spectroscopic analysis. The chemopreventive potential of these compounds was evaluated against SW480 human colon adenocarcinoma cells, its metastatic derivative SW620, along with the non-malignant CHO-K1 cell line. Among the tested compounds, hybrids 3e and 3i (for SW480) and 3a, 3e and 3k (for SW620) displayed the best cytotoxic activity with IC50 values ranging from 11.52 ± 2.78 to 29.33 ± 4.73 µM for both cell lines, with selectivity indices (SI) higher than 1, after 48 h of treatment. Selectivity indices were even higher than those reported for the reference drug, 5-fluorouracil (SI = 0.96), the starting compound resveratrol (SI = 0.45) and the equimolar mixture of curcumin plus resveratrol (SI = 0.77). The previous hybrids showed good antiproliferative activity.
Highlights
SW480) and 3a, 3e and 3k displayed the best cytotoxic activity with IC50 values ranging from 11.52 ± 2.78 to 29.33 ± 4.73 μM for both cell lines, with selectivity indices (SI) higher than 1, after 48 h of treatment
Various growth factor receptors and cell adhesion molecules involved in tumor growth, metastasis, apoptosis and multidrug resistance are affected by curcumin [5,6,7]
We showed for the first time that the synthesized hybrids based on curcumin and resveratrol have chemopreventive potential in an in vitro model of Colorectal cancer (CRC), involving selective growth inhibition and antiproliferative activity, with changes in size and shape after treatment, better results than parental compounds and exhibiting higher selectivity than the conventional chemotherapeutic (5-FU)
Summary
SW480) and 3a, 3e and 3k (for SW620) displayed the best cytotoxic activity with IC50 values ranging from 11.52 ± 2.78 to 29.33 ± 4.73 μM for both cell lines, with selectivity indices (SI) higher than 1, after 48 h of treatment. Curcumin is one of the bioactive components of Curcuma longa Linn Several studies with this compound have revealed important functions in cancer control [3], including antiproliferative activity against different cancer cell lines and inhibition at different stages of cancer cell progression [4]. Different studies have shown the importance of hydroxyl group for the biological activity; resveratrol analogs containing methoxy groups have increased the activity [8,9,17] Both curcumin and resveratrol alone have shown restricted clinical efficacy due to different factors, including low bioavailability and stability stands out [18,19]. Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations
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