Chemistry and Selective Tumor Cell Growth Inhibitory Activity of Polyketides from the South China Sea Sponge Plakortis sp.
Mar Drugs
; 15(5)2017 May 03.
Article
em En
| MEDLINE
| ID: mdl-28467388
ABSTRACT
Simplextone E (1), a new metabolite of polyketide origin, was isolated with eight known analogues (2-9) from the South China Sea sponge Plakortis sp. The relative configuration of the new compound was elucidated by a detailed analysis of the spectroscopic data and quantum mechanical calculation of NMR chemical shifts, aided by the newly reported DP4+ approach. Its absolute configuration was determined by the TDDFT/ECD calculation. Simplextone E (1) is proven to be one of the isomers of simplextone D. The absolute configuration at C-8 in alkyl chain of plakortone Q (2) was also assigned based on the NMR calculation. In the preliminary in vitro bioassay, compounds 6 and 7 showed a selective growth inhibitory activity against HCT-116 human colon cancer cells with IC50 values of 8.3 ± 2.4 and 8.4 ± 2.3 µM, corresponding to that of the positive control, adriamycin (IC50 4.1 µM). The two compounds also showed selective activities towards MCF-7 human breast cancer and K562 human erythroleukemia cells while compound 3 only displayed weak activity against K562 cells.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Poríferos
/
Plakortis
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Proliferação de Células
/
Policetídeos
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Antineoplásicos
Limite:
Animals
/
Humans
País/Região como assunto:
Asia
Idioma:
En
Revista:
Mar Drugs
Assunto da revista:
BIOLOGIA
/
FARMACOLOGIA
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
China