Antiplasmodial flavanones and a stilbene from Carpha glomerata

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:28

Article

Cho, Namki^1,2,3,4  Valenciano, Ana Lisa^5,6  Du, Yongle^1,2  Clement, Jason⁷  Cassera, Maria B.^5,6  Goetz, Michael⁷  Kingston, David G., I^1,2 

[1] Virginia Tech, Dept Chem, M-C 0212, Blacksburg, VA 24061 USA

[2] Virginia Tech, Virginia Tech Ctr Drug Discovery, M-C 0212, Blacksburg, VA 24061 USA

[3] Chonnam Natl Univ, Coll Pharm, Gwangju 500757, South Korea

[4] Chonnam Natl Univ, Res Inst Drug Dev, Gwangju 500757, South Korea

[5] Univ Georgia, Dept Biochem & Mol Biol, Athens, GA 30602 USA

[6] Univ Georgia, Ctr Trop & Emerging Global Dis, Athens, GA 30602 USA

[7] Nat Prod Discovery Inst, 2805 Old Easton Rd, Doylestown, PA 18902 USA

关键词: Carpha glomerata;    Cyperaceae;    Bioassay-guided discovery;    Antiplasmodial activity;   

DOI  :  10.1016/j.bmcl.2018.09.003

来源: Elsevier

【 摘 要 】

Bioassay-guided fractionation of an extract of Carpha glomerata (Cyperaceae) led to the isolation of seven compounds. Compounds 1 (carphorin A), 3 (carphorin C), 4 (carphorin D), and 5 (carphabene) are new compounds, and compound 2 (8-(3-hydroxyisoamyl)-naringenin) was isolated for the first time as a natural product. All structures were elucidated based on analyses of their HR-ESIMS and 1D and 2D NMR data. Compounds 1, 2, and 6, which have prenyl or hydroxyprenyl side chains, exhibited antiplasmodial activities with IC50 values of 5.2 +/- 0.6, 3.4 +/- 0.4, and 6.7 +/- 0.8 mu M against the drug-resistant Dd2 strain of Plasmodium falciparum. In addition the prenylated stilbene 5 also showed good activity, with IC50 5.8 +/- 0.7 mu M.

【 授权许可】

Free