Functional evaluation of synthetic flavonoids and chalcones for potential antiviral and anticancer properties. Issue 11 (1st June 2017)

• Record Type: Journal Article
• Authors: Mateeva, Nelly; Eyunni, Suresh V.K.; Redda, Kinfe K.; Ononuju, Ucheze; Hansberry, Tony D.; Aikens, Cecilia; Nag, Anita
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 11(2017)
• Page Start: 2350
• Page End: 2356
• Publication Date: 2017-06-01
• Subjects: Chalcone -- HCV -- Cancer -- mTOR -- rsp6; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.04.034
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Flavonoids, stilbenes, and chalcones are plant secondary metabolites that often possess diverse biological activities including anti-inflammatory, anti-cancer, and anti-viral activities. The wide range of bioactivities poses a challenge to identify their targets. Here, we studied a set of synthetically generated flavonoids and chalcones to evaluate for their biological activity, and compared similarly substituted flavonoids and chalcones. Substituted chalcones, but not flavonoids, showed inhibition of viral translation without significantly affecting viral replication in cells infected with hepatitis C virus (HCV). We suggest that the chalcones used in this study inhibitm ammaliant argeto fr apamycin (mTOR) pathway by ablating phosphorylation of ribosomal protein 6 (rps6), and also the kinase necessary for phosphorylating rps6 in Huh7.5 cells (pS6K1). In addition, selected chalcones showed inhibition of growth in Ishikawa, MCF7, and MDA-MB-231 cells resulting an IC50 of 1–6 µg/mL. When similarly substituted flavonoids were used against the same set of cancer cells, we did not observe any inhibitory effect. Together, we report that chalcones show potential for anti-viral and anti-cancer activities compared to similarly substituted flavonoids.