Structure Elucidation and Anticancer Activity of 7-Oxostaurosporine Derivatives from the Brazilian Endemic Tunicate Eudistoma vannamei

Marine Drugs

Paula Christine Jimenez⁴  Diego Veras Wilke³  Elthon Gois Ferreira⁴  Renata Takeara²  Manoel Odorico de Moraes³  Edilberto Rocha da Silveira¹  Tito Monteiro da Cruz Lotufo⁴  Norberto Peporine Lopes² 

[1] Department of Organic and Inorganic Chemistry, Federal University of Ceará, Fortaleza, CE 60021-970, Brazil;Department of Chemistry and Physics, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP 14040-903, Brazil;Department of Physiology and Pharmacology, School of Medicine, Federal University of Ceará, Fortaleza, CE 60430-270, Brazil;Institute of Marine Sciences, LABOMAR, Federal University of Ceará, Fortaleza, CE 60165-081, Brazil;

关键词: cell cycle arrest;    ascidians;    staurosporine;   

DOI  :  10.3390/md10051092

来源: mdpi

【 摘 要 】

The present study reports the identification of two new staurosporine derivatives, 2-hydroxy-7-oxostaurosporine (1) and 3-hydroxy-7-oxostaurosporine (2), obtained from mid-polar fractions of an aqueous methanol extract of the tunicate Eudistoma vannamei, endemic to the northeast coast of Brazil. The mixture of 1 and 2 displayed IC₅₀ values in the nM range and was up to 14 times more cytotoxic than staurosporine across a panel of tumor cell lines, as evaluated using the MTT assay.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.