Synthesis and cytotoxic activity of metallic complexes of lawsone |
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| Authors: | Sandra Oramas-Royo Concepción Torrejón Irene Cuadrado Rita Hernández-Molina Sonsoles Hortelano Ana Estévez-Braun Beatriz de las Heras |
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| Affiliation: | 1. Instituto Universitario de Bio-Orgánica ‘Antonio González’, Departamento de Química Orgánica, Universidad de La Laguna, Avda. Astrofísico Fco. Sánchez 2, 38206 La Laguna, Tenerife, Spain;2. Instituto Canario de Investigaciones del Cáncer (ICIC), Spain;3. Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain;4. Departamento de Química Inorgánica, Facultad de Farmacia, Universidad de La Laguna, Tenerife, Spain;5. Unidad de Inflamación y Cáncer. Centro Nacional de Microbiología, Instituto de Salud Carlos III, Madrid, Spain |
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| Abstract: | In the present study, a series of metallic complexes of the 1,4-naphthoquinone lawsone (2–6) were synthesized and evaluated for potential cytotoxicity in a mouse leukemic macrophagic RAW 264.7 cell line. Cell viability was determined by the MTT assay. Significant growth inhibition was observed for the copper complex (4) with an IC50 value of 2.5 μM. This compound was selected for further evaluation of cytotoxic activity on several human cancer cells including HT-29 (human colorectal adenocarcinoma), HepG2 (human hepatocellular carcinoma) and HeLa, (human cervical adenocarcinoma cells). Significant cell viability decrease was also observed in HepG2 cells. The apoptotic potential of this complex was evaluated in these cells. Compound 4 induced apoptosis by a mechanism that involves the activation of caspases 3, 8 and 9 and modulation of apoptotic-related proteins such as Bax, Bad, and p53. These results indicate that metal complexes of lawsone derivatives, in particular compound 4, might be used for the design of new antitumoral agents. |
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| Keywords: | HepG2 Apoptosis Lawsone Metallic complexes Cytotoxicity |
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