Synthesis and biological evaluation of Piroxicam derivative as a lead chelator

• Main Authors: Hosseini Sayed Masoud, Imani Ali, Rahimzadegan Milad, Mohammadi Saeid, Golaghaei Alireza
• Format: Article
• Language: English
• Published: De Gruyter 2019-06-01
• Series: Main Group Metal Chemistry
• Subjects: piroxicam derivative; chelator; toxic metal; antioxidant
• Online Access: https://doi.org/10.1515/mgmc-2019-0008
• ISSN: 0792-1241; 2191-0219

Lead as a potent environmental and occupational pollutant, exerts its toxic effect mainly through oxidative stress induction. Currently, chelation therapy is the only medical management of metal intoxications in clinic, but its administration is associated with various side effects as well. In this study the protective effect of synthetized Piroxicam derivative was evaluated against lead toxicity in vitro. First the chelating activity of Piroxicam derivative was studied through Jobs method and 13C{1H} NMR spectroscopy. Then the cytoprotective effect of Piroxicam derivative (10, 20, 50, 100 and 200 μg/mL) was evaluated and compared with that of EDTA (30 μg/mL) in the presence of lead nitrate (30 μg/mL). The EC50 value of Piroxicam derivative was calculated as well. Finally, the chelation efficacy and antioxidant effects of Piroxicam derivative in EC50 and 2EC50 values was assessed and compared with that of EDTA. Results showed that Piroxicam derivative chelates lead ion as much as EDTA. Moreover, Piroxicam derivative prevented lead-induced cells death more effectively than EDTA which is may due to its potent innate antioxidant activity. In conclusion, the synthetized Piroxicam derivative with possessing potent chelating activity as well as potent antioxidant activity, could be considered as potential drug target in management of toxic metals poisoning.