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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:27

Article

Mateeva, Nelly¹  Eyunni, Suresh V. K.²  Redda, Kinfe K.²  Ononuju, Ucheze¹  Hansberry, Tony D., II¹  Aikens, Cecilia¹  Nag, Anita³ 

[1] Florida A&M Univ, Dept Chem, 1530 S MLK Blvd, Tallahassee, FL 32307 USA

[2] Florida A&M Univ, Dept Pharm & Pharmaceut Sci, Tallahassee, FL 32307 USA

[3] Furman Univ, Dept Chem, 3300 Poinsett Highway, Greenville, SC 29613 USA

关键词: Chalcone;    HCV;    Cancer;    mTOR;    rsp6;   

DOI  :  10.1016/j.bmcl.2017.04.034

来源: Elsevier

【 摘 要 】

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 1-6 mu g/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. (C) 2017 Elsevier Ltd. All rights reserved.

【 授权许可】

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