Title:Zidovudine Glycosylation by Filamentous Fungi Leads to a Better Redox Stability and Improved Cytotoxicity in B16F10 Murine Melanoma Cells
Volume: 20
Issue: 14
Author(s): Evilanna L. Arruda*, Kamila B. Japiassu, Paula L. de Melo Souza, Kelly C.F. Araújo, Douglas V. Thomaz, Alane P. Cortez, Luane F. Garcia, Marize C. Valadares, Eric de Souza Gil and Valéria de Oliveira
Affiliation:
- Laboratorio de Bioconversao, Faculdade de Farmacia, Universidade Federal de Goias, P.O. Box 131, Goiania, GO,Brazil
Keywords:
Glycoconjugate, zidovudine, antioxidant, anticancer, biotransformation, Cunninghamella echinulata.
Abstract:
Background: The strategic development of therapeutic agents, capable of being targeted at their
active sites, has been a major goal in treatment of cancer. The delivery of drugs for tumors has as its main challenge
the development of safe and effective drugs, since the goal of chemotherapy is to eliminate the tumor
completely without affecting healthy cells. The aim of present study was to investigate the antioxidant, anticancer
activities of zidovudine and its α-O-glycosylated derivative obtained by biosynthesis of a filamentous fungi,
Cunninghamela echinulata.
Methods: An evaluation of the cytotoxic potential of zidovudine and its α-O-glycosylated was performed in
fibroblasts and melanoma cells by the tetrazolium reduction method (MTT) and the antioxidant activity of this
derivative was observed.
Results: The antioxidant activity of zidovudine demonstrated an electrochemical oxidation potential of 0.91V,
while the α-O-glycosylated derivative did not exhibit any antioxidant activity. The zidovudine exhibited low
cytotoxicity for melanoma and fibroblast cells, while the α-O-glycosylated derivative presented better cytotoxicity
on melanoma cells at a concentration of 10mg. mL-1.
Conclusion: This study demonstrates the specific cytotoxicity of the glycoconjugate and suggests that glycosylation
by biosynthesis can be a useful strategy for obtaining new anticancer compounds.
