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

Journal of the Brazilian Chemical Society

Humberto M. Spindola²  João E. De Carvalho²  Ana Lúcia T. G. Ruiz²  Rodney A. F. Rodrigues²  Carina Denny²  Ilza M. De Oliveira Sousa²  Jorge Y. Tamashiro¹  Mary Ann Foglio² 

[1] ,Universidade Estadual de Campinas CPQBA Campinas SP ,Brazil

关键词: Pterodon pubescens;    leguminosae;    furanoditerpenes;    in vitro assay;    prostate cell line;    cytotoxicity;   

DOI  :  10.1590/S0103-50532009000300024

来源: SciELO

【 摘 要 】

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.

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