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Título : | Structural modification of berberine alkaloids in relation to cytotoxic activity in vitro |
Autor : | Orfila, Luz Rodríguez, María del C. Colman, Trina Hasegawa, Masahisa Merentes, Elizabeth Arvelo, Francisco |
Palabras clave : | Cytotoxicity Cell growth Human tumor cells Berberine alkaloids |
Fecha de publicación : | 2000 |
Editorial : | Journal of Ethnopharmacology |
Citación : | Journal of Ethnopharmacology 71 (2000) 449–456 |
Resumen : | The cytotoxicity of two protoberberine alkaloids: berberine and lincangenine, their 8-hydroxy-7,8-dihydro-derivatives
and tetrahydroprotoberberine:thaicanine, was evaluated. The cellular responses through the [3-(4,5-dimethylthiazol-
2-yl)-2,5-diphenyl-2H-tetrazolium bromide] (MTT) method were measured in Hela (uterus carcinoma), SVKO3
(ovary carcinoma), Hep-2 (larynx carcinoma), primary culture from mouse embryon, and human fibroblast cells at
the concentration: 10–1000 ppm (mg:ml) for 24 h. Berberine showed the highest cytotoxicity among the compounds
tested, giving LC50 values for all cell lines at the concentration of 10 ppm. The results indicated that the cytotoxicity
was notably decreased by structural changes, i.e. by modulation of the planarity caused by the introduction of
hydroxyl group at C-8 and concomitant saturation of double bond between N-C8 in protoberberine molecules. In the
case of berberine, the cytotoxic effect changed from 98.8 (berberine) to 39% for 8-hydroxydihydroberberine at the
concentration of 100 ppm in Hela cells line. The same effect was observed with lincangenine and 8-OH-lincangenine
(cytotoxicities 70 and 25%, respectively, at 1000 ppm in SVKO3 cells). On the other hand, these compounds showed
a low selectivity for the different human cancer cell lines tested. |
URI : | http://hdl.handle.net/10872/14068 |
ISSN : | 0022-3573 |
Aparece en las colecciones: | Artículos Publicados
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