A novel, nontoxic iron chelator, super-polyphenol, effectively induces apoptosis in human cancer cell lines
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Toshiaki Ohara1,2, Yasuko Tomono3, Xing Boyi1, Sun Yingfu1, Kazuhiro Omori4 and Akihiro Matsukawa1
1Department of Pathology & Experimental Medicine, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama, Japan
2Department of Gastroenterological Surgery, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama, Japan
3Shigei Medical Research Institute, Okayama, Japan
4Department of Periodontics and Endodontics, Okayama University Hospital, Okayama, Japan
Toshiaki Ohara, email: [email protected]
Keywords: iron; chelation; chelator; apoptosis; toxicity
Received: April 11, 2017 Accepted: July 29, 2018 Published: August 28, 2018
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.
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