Repository of Research and Investigative Information

Repository of Research and Investigative Information

Hormozgan University of Medical Sciences

Protective effects of isatin and its synthetic derivatives against iron, copper and lead toxicity

(2019) Protective effects of isatin and its synthetic derivatives against iron, copper and lead toxicity. Toxicology in Vitro.

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Official URL: https://www.sciencedirect.com/science/article/pii/...

Abstract

Introduction While some metals are required for physiological functions in the form of essential trace elements, they can cause toxicity in the excessive concentrations. Chelation therapy was used to reduce the adverse effects of acute and chronic poisoning by metals. Isatin derivatives form complexes with copper ions indicating that they may have protective activity against metal overload. Method In this study, four compounds (isatin and three isatin-derivatives Mj1, TR and Mk1) were evaluated for drug-likeliness. Then their potency inhibiting cell proliferation was determined in HEK293 cell culture assay. Finally, IC50 values for lead, copper, and iron was evaluated in the absence and also the presence of isatin and its derivatives. Results Isatin and its derivatives used in this study complied with the Lipinski criteria for drug-likeliness. The greatest difference between the IC50 values and the non-toxic dose was obtained for TR and Mj1, respectively. Pretreatment with the Mj1 increased the IC50 values for lead, iron, and copper, by 2.1, 1.7 and 1.7 times, respectively. At non-toxic dose, TR has only increased the IC50 values for lead and copper by 1.4 and 1.3 times without affecting iron cytotoxicity. Mk1 increased the IC50 values for lead, copper, and iron by 1.3, 1.8 and 1.7 times, respectively. Conclusions Mj1 is suggested as a lead compound for developing therapeutic agents for lead (Pb) toxicity and Mk1 for copper and iron.

Item Type: Article
Keywords: Isatin Derivatives Cytotoxicity HEK293 Copper Iron Lead
Subjects: WA Public Health > WA 670-847 Environmental Pollution. Sanitation
Depositing User: هدی فهیم پور
URI: http://eprints.hums.ac.ir/id/eprint/6168

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