Furanoditerpenes from Pterodon pubescens Benth with Selective in vitro Anticancer Activity for Prostate Cell Line

Activity guided fractionation of Pterodon pubescens Benth. methylene chloride-soluble fraction afforded novel 6 alpha-acetoxi 7 beta-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 ce...

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Published inJournal of the Brazilian Chemical Society Vol. 20; no. 3; pp. 569 - U241
Main Authors Spindola, Humberto M., de Carvalho, Joao E., Ruiz, Ana Lucia T. G., Rodrigues, Rodney A. F., Denny, Carina, de Oliveira Sousa, Ilza M., Tamashiro, Jorge Y., Foglio, Mary Ann
Format Journal Article
LanguageEnglish
Published SAO PAULO Soc Brasileira Quimica 01.01.2009
Sociedade Brasileira de Química
Subjects
Chemistry
CHEMISTRY, MULTIDISCIPLINARY
Physical Sciences
Science & Technology
CYPROTERONE
ASSAY
furanoditerpenes
NATURAL-PRODUCTS
Pterodon pubescens
leguminosae
prostate cell line
DITERPENOIDS
PHARMACOLOGY
LEADS
in vitro assay
cytotoxicity
EXTRACT
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Summary:Activity guided fractionation of Pterodon pubescens Benth. methylene chloride-soluble fraction afforded novel 6 alpha-acetoxi 7 beta-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 GI(50) (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 GI(50) 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.
ISSN:0103-5053
1678-4790
1678-4790
DOI:10.1590/S0103-50532009000300024