| Full text | |
| Author(s): |
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]
Total Authors: 8
|
| Affiliation: | [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
Total Affiliations: 3
|
| Document type: | Journal article |
| Source: | Journal of the Brazilian Chemical Society; v. 20, n. 3, p. 569-U241, 2009. |
| Web of Science Citations: | 27 |
| Abstract | |
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) | |