Functional evaluation of synthetic flavonoids and chalcones for potential antiviral and anticancer properties

[Display omitted] 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...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 27; no. 11; pp. 2350 - 2356
Main Authors:	Mateeva, Nelly, Eyunni, Suresh V.K., Redda, Kinfe K., Ononuju, Ucheze, Hansberry, Tony D., Aikens, Cecilia, Nag, Anita
Format:	Journal Article
Language:	English
Published:	England Elsevier Ltd 01-06-2017
Subjects:	Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antiviral Agents - chemistry Antiviral Agents - pharmacology Cancer Cell Line, Tumor Chalcone Chalcones - chemistry Chalcones - pharmacology Flavonoids - chemistry Flavonoids - pharmacology HCV Humans mTOR rsp6 Structure-Activity Relationship mTOR rsp6 HCV Chalcone Cancer
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Summary:	[Display omitted] 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 inhibit mammalian target of rapamycin (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 1–6µg/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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2017.04.034