Benzodifurans for Biomedical Applications: BZ4, a Selective anti-proliferative and anti-amyloid Lead Compound

Abstract

Aim: Our goal is to evaluate benzodifuran-based scaffolds for biomedical applications. Methodology: We here explored the anticancer and anti-amyloid activities of a novel compound (BZ4) in comparison with other known benzodifuran analogs, previously studied in our group, and we have explored its ability to interact with different DNA model systems. Results: BZ4 shows antiproliferative activity on different cancer cells; does not affect noncancerous control cells and alters the aggregation properties of β-amyloid, as ascertained by circular dichroism, fluorescence spectroscopy and scanning electron microscopy analysis. An overall, qualitative picture on the mechanistic aspects related to the biological activities is discussed in light of the dynamic light scattering, UV, circular dichroism and fluorescence data, as well as of the metal ion-binding properties of BZ4.

Graphical abstract

Keywords: :

• anti-amyloid
• anticancer
• synthesis

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at:www.tandfonline.com/doi/full/10.2217/epi-2016-0184

Acknowledgments

We are grateful to A Roviello, Federico II University, Naples for his precious suggestions on the synthesis and characterization of BZ4. We also thank U Eisel and D Dekens, University of Groningen, for technical assistance in performing the primary neuronal cell culture assays.

Financial & competing interests disclosure

Thanks to ZonMw Memorabel for the financial support in buying the peptide and chemicals for the experiments performed in The Netherlands. This work was supported by the Italian Association for Cancer Research (AIRC) (IG2015 n. 17037 to D.M.) and Ministero dell'Istruzione, dell'Università e della Ricerca (MIUR) [grant number PON03PE_00060_4]. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Ethical conduct

The authors state that they have obtained appropriate institutional review board approval or have followed the principles outlined in the Declaration of Helsinki for all human or animal experimental investigations.