Abstract
Iron chelation therapy is the main treatment for iron overload disease. Iron chelators were recently reported to be useful for cancer therapy; however, they cause side effects that make them difficult to use in some cancer patients. Thus, a novel oral iron chelator, super-polyphenol (SP), was developed for cancer therapy to decrease the side effects. SP is either water soluble or insoluble, and has different isoforms according to the number of side chains. Of these isoforms, water-soluble SP6 and SP10 appear to be the best candidates, as they have the strongest chelating abilities. In this study, we focused on the usefulness and safety of SP6 and SP10 as anti-cancer drugs, and examined their anti-cancer effects and toxicity. The results showed that SP6 and SP10 inhibited cancer cell proliferation by inducing apoptosis in HCT116, HSC-2, A549, and MCF-7 cancer cells. SP10 also inhibited tumor growth in an HCT116 xenograft model. SP6 and SP10 had no acute toxicities. An intravenous injection test revealed that SP6 and SP10 had better safety profiles than the iron chelator deferoxamine. In conclusion, SP is a novel oral iron chelator with anti-cancer effects and few adverse side effects. This is the first report of SP in the literature.
Highlights
Iron is an essential element for all living organisms and plays an important role in critical cellular processes such as energy production and DNA synthesis
Iron chelators were recently reported to be useful for cancer therapy; they cause side effects that make them difficult to use in some cancer patients
A dose of 0.5 mg/mL SP6 chelated more than 75% of iron, and 0.1 mg/mL SP10 chelated more than 80% of iron
Summary
Iron is an essential element for all living organisms and plays an important role in critical cellular processes such as energy production and DNA synthesis. Iron overload is a common complication in patients receiving blood transfusion as a treatment for conditions such as aplastic anemia and myelodysplastic syndrome [2]. Iron overload causes carcinogenesis in some organs [3] by causing oxidative damage of DNA by the Fenton reaction [4]. Iron chelators can cause potentially serious side effects. Deferasirox (DFX), an oral iron chelator, has superior iron chelation ability, but causes digestive, liver, and kidney disorders [9]. Deferoxamine (DFO) is an intravenous iron chelator that has toxic side effects [10]. Decreasing the side effects of iron chelators may improve cancer treatment compliance, thereby improving clinical outcomes
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