Journal
MOLECULES
Volume 18, Issue 9, Pages 11496-11511Publisher
MDPI
DOI: 10.3390/molecules180911496
Keywords
synthesis; biological evaluation; apigenin derivatives; antibacterial activity; antiproliferative activity; MTT assay
Funding
- State Forestry Administration of the People's Republic of China [200904004]
- National Natural Science Foundation of China [21175107, 21375106, 21202132]
- Ministry of Education of the People's Republic of China [NCET-08-0464]
- Northwest AF University
Ask authors/readers for more resources
Two series of apigenin [5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one] derivatives, 3a-3j and 4a-4j, were synthesized. The apigenin and alkyl amines moieties of these compounds were separated by C-2 or C-3 spacers, respectively. The chemical structures of the apigenin derivatives were confirmed using H-1-NMR, C-13-NMR, and electrospray ionization mass spectroscopy. The in vitro antibacterial and antiproliferative activities of all synthesized compounds were determined. Among the tested compounds, 4a-4j displayed significant antibacterial activity against the tested strains (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa). Additionally, 4i showed the best inhibitory activity with minimum inhibitory concentrations of 1.95, 3.91, 3.91, and 3.91 mu g/mL against S. aureus, B. subtilis, E. coli, and P. aeruginosa, respectively. The antiproliferative activity of the apigenin derivatives was evaluated by an MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] assay. We determined that 4a-4j displayed better growth inhibition activity against four human cancer cell lines, namely, human lung (A549), human cervical (HeLa), human hepatocellular liver (HepG2), and human breast (MCF-7) cancer cells, than the parent apigenin. Compound 4j was found to be the most active antiproliferative compound against the selected cancer cells. Structure-activity relationships were also discussed based on the obtained experimental data.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available