Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/21437
Título: Apoptosis induction and modulation of P-glycoprotein mediated multidrug resistance by new macrocyclic lathyrane-type diterpenoids
Autor: Duarte, Noelia
Varga, Andras
Cherepnev, Georg
Radics, Rita
Molnar, Joseph
Ferreira, Maria-Jose U.
Palavras-chave: Biochemistry & Molecular Biology
Chemistry, Medicinal
Chemistry, Organic
Data: 2007
Citação: BIOORGANIC & MEDICINAL CHEMISTRY. - Vol. 15, n. 1 (2007), p. 546-554
Resumo: The macrocyclic lathyrane diterpenes, latilagascenes D-F (1-3) and jolkinol B (4), were isolated from the methanol extract of Euphorbia lagascae, and evaluated for multidrug resistance reversing activity on mouse lymphoma cells. All compounds displayed very strong activity compared with that of the positive control, verapamil. The structure-activity relationship is discussed. The evaluation of compounds 1 and 4, and of latigascenes A-C (5-7), isolated from the same species, as apoptosis-inducers was also carried out. Compound I was the most active. Furthermore, in the model of combination chemotherapy, the interaction between the doxorubicine and latilagascene B (6) was studied in vitro, on human MDR1 gene transfected mouse lymphoma cells, showing that the type of interaction was synergistic. Latilagascenes D-F (1-3) are new compounds whose structures were established on the basis of spectroscopic methods, including 2D NMR experiments (COSY, HMQC, HMBC and NOESY). (c) 2006 Elsevier Ltd. All rights reserved.
URI: http://hdl.handle.net/10451/21437
DOI: http://dx.doi.org/10.1016/j.bmc.2006.09.028
ISSN: 0968-0896
Aparece nas colecções:FF - Produção Científica 2000-2009

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