Hesperetin is a class of natural products with a wide range of sources and remarkable biological activities. In this study, we described the synthesis of a series of novel hesperetin derivatives and evaluated the in vitro antioxidant and antitumor activity of these compounds. Eleven novel compounds were synthesized in moderate yields. The compounds synthesized in this work exhibited antioxidant activities against DPPH and ABTS free radicals in a dose-dependent manner. Among them, compound 3f had the best antioxidant activity, with IC50 of 1.2 μM and 24 μM for DPPH and ABTS, respectively. The antitumor activity of the compounds against human cancer cell lines, such as breast MCF-7, liver HepG2, and cervical Hela, was determined by a standard 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay. Three compounds had moderate IC50 values. Interestingly, compound 3f had better biological activity than hesperetin, which matches the prediction by Maestro from Schrödinger. Therefore, the new hesperidin derivative is a promising drug for the treatment of cancer due to its effective antitumor activity. The results also suggested that the antitumor activities of hesperetin derivatives may be related to their antioxidant activities.
The novel porphyrin-based 5-fluorouracil and its metal complexes were synthesized. Through the combination of porphyrin and anticancer drug 5-fluorouracil (5-FU), it provides ideas for how to maximize the antitumor activity of drugs. The new porphyrin and its metal complexes take advantage of the enrichment of porphyrins in tumor cells, which makes them have higher cytotoxicity to tumor cells than normal cells, thus reducing the toxic and side effects. Excellent photophysical properties were illustrated by UV-vis absorption and emission spectra with enhanced absorbance between 650 and 750 nm and fluorescence emission within 600-800 nm. Besides, manganese porphyrin and non-central metalloporphyrin were evaluated in vitro by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay against MCF-7, HepG2, and HeLa. In addition, compared with free 5-fluorouracil, the novel manganese porphyrin shows higher antitumor activity. Therefore, the novel manganese porphyrin-based 5-fluorouracil is a promising drug for cancer treatment due to its effective antitumor activity, and near-infrared absorption.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.