Furanoditerpenes from Pterodon pubescens benth with selective in vitro anticancer activity for prostate cell line

Autor(es)

Spindola, Humberto M. ^{[1, 2]} ; de Carvalho, Joao E. ^{[1, 2]} ; Ruiz, Ana Lucia T. G. ^[1] ; Rodrigues, Rodney A. F. ^[1] ; Denny, Carina ^{[1, 2]} ; de Oliveira Sousa, Ilza M. ^[1] ; Tamashiro, Jorge Y. ^[3] ; Foglio, Mary Ann ^{[1, 2]}

Afiliação do(s) autor(es)

^[1] Univ Estadual Campinas, CPQBA, BR-13083970 Campinas, SP - Brazil

^[2] Univ Estadual Campinas, Fac Odontol, Dept Farmacol Anestesiol & Terapeut, BR-13414903 Piracicaba, SP - Brazil

^[3] Univ Estadual Campinas, Inst Biol, BR-13083970 Campinas, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Journal of the Brazilian Chemical Society; v. 20, n. 3, p. 569-U241, 2009.
• Citações Web of Science: 27

Resumo

Activity guided fractionation of Pterodon pubescens Benth. methylene chloride-soluble fraction afforded novel 6α-acetoxi 7β-hydroxy-vouacapan 1 and four known diterpene furans 2, 3, 4, 5. The compounds were evaluated for in vitro cytotoxic activities against human normal cells and tumour cell lines UACC-62 (melanoma), MCF-7 (breast), NCI-H460 (lung, non-small cells), OVCAR-03 (ovarian), PC-3 (prostate), HT-29 (colon), 786-0 (renal), K562 (leukemia) and NCI-ADR/RES (ovarian expressing phenotype multiple drugs resistance). Results were expressed by three concentration dependent parameters GI50 (concentration that produces 50% growth inhibition), TGI (concentration that produces total growth inhibition or cytostatic effect) and LC50 (concentration that produces -50% growth, a cytotoxicity parameter). Also, in vitro cytotoxicity was evaluated against 3T3 cell line (mouse embryonic fibroblasts). Antiproliferative properties of compounds 1, 4 and 5 are herein reported for the first time. These compounds showed selectivity in a concentration-dependent way against human PC-3. Compound 1 demonstrated selectivity 26 fold more potent than the positive control, doxorubicin, for PC-3 (prostrate) cell line based on GI50 values, causing cytostatic effect (TGI value) at a concentration fifteen times less than positive control. Moreover comparison of 50% lethal concentration (LC50 value) with positive control (doxorubicin) suggested that compound 1 was less toxic. (AU)

• Processo FAPESP: 02/10226-1 - Avaliacao farmacologica de fracoes e principios ativos obtidos de pterodon pubescens.
• Beneficiário: Mary Ann Foglio
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 05/54582-4 - Microencapsulacao de extratos de plantas do cerrado brasileiro com potencial acao antiproliferativa e antimicrobiana.
• Beneficiário: Rodney Alexandre Ferreira Rodrigues
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 06/52454-1 - Atividade antinociceptiva e anticancer, isolamento e identificacao das fracoes ativas da pterodon pubescens benth.
• Beneficiário: Mary Ann Foglio
• Modalidade de apoio: Auxílio à Pesquisa - Regular