Abstract
Abstract 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.
Highlights
Some other studies have shown that lead exposure result in glutathione level decrease and malondialdehyde (MDA) levels increase as a lipid peroxidation biomarker (Patrick, 2006)
In the 13C{1H} NMR spectra of Pb-Pir derivative we observed down field shifting in chemical shifts of carbonyl functional groups compared to free ligand (Figure 3)
This study demonstrated that synthetized Pir derivative could effectively chelate lead ion and its chelating activity was comparable to Ethylenediaminetetraacetic acid (EDTA)
Summary
Sayed Masoud Hosseini, Department of Pharmacology and GR inhibition by lead results in GSH level reduction and Toxicology, School of Medicine, AJA University of Medical Sciences, antioxidant defense system dysfunction Et al, 2005; Sugawara et al, 1991). Reactive species produced in oxidative stress can attack essential biomolecules like as lipids, proteins, nucleic acids, and even cell structures, followed by oxidative damages and many pathological processes (Van Antwerpen and Neve, 2004). Some other studies have shown that lead exposure result in glutathione level decrease and malondialdehyde (MDA) levels increase as a lipid peroxidation biomarker (Patrick, 2006)
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