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

Journal of the Brazilian Chemical Society

Foglio, Mary Ann¹  Spindola, Humberto M.¹  Sousa, Ilza M. de Oliveira¹  Tamashiro, Jorge Y.¹  Ruiz, Ana Lúcia T. G.¹  Universidade Estadual de Campinas, Campinas, Brazil¹  Universidade Estadual de Campinas, Piracicaba, Brazil¹  Carvalho, João E. de¹  Rodrigues, Rodney A. F.¹  Denny, Carina¹ 

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

DOI  :  10.1590/S0103-50532009000300024

学科分类：化学（综合）

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.

【 授权许可】

Unknown