In vitro cytotoxicity of some natural and semi-synthetic isocoumarins from Paepalanthus bromelioides

• Autor(a) principal: Devienne, Karina F. [UNESP]
• Data de Publicação: 2002
• Outros Autores: Raddi, Maria Stella Gonçalves [UNESP], Varanda, Eliana Aparecida [UNESP], Vilegas, Wagner [UNESP]
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Institucional da UNESP
• Texto Completo: http://www.znaturforsch.com/ac/v57c/c57c.htm; http://hdl.handle.net/11449/66790
• topic: Cytotoxicity Activity; Isocoumarin; Paepalanthus bromelioides; antiinfective agent; cisplatin; coumarin derivative; angiosperm; animal; cell line; cell survival; chemistry; drug effect; fibroblast; metabolism; mouse; structure activity relation; Animals; Anti-Infective Agents; Cell Line; Cell Survival; Cisplatin; Coumarins; Fibroblasts; Liliaceae; Mice; Structure-Activity Relationship

Numerous natural compounds have a potential for therapeutic applications, but may have to be chemically modified to alter toxic side effects. We investigated structural parameters that could affect the cytotoxicity of isocoumarins similar to 9,10-dihydroxy-5,7-dimethoxy-1H-naphtho(2,3c)pyran-1-one (paepalantine 1). Paepalantine 1 has antimicrobial activity, as well as significant in vitro cytotoxic effects in the McCoy cell line. Two other natural and two semi-synthetic isocoumarins with similar structures obtained from the capitula of Paepalanthus bromelioides were tested on the same cell line by the neutral red assay. Substitution of the 9 and/or 10-OH group made these compounds less cytotoxic.