CONICET | Buscador de Institutos y Recursos Humanos

Human prostate cancer (PCa) is the mostcommon form of non-cutaneous cancer, and metastatic late-stage PCa represents asignificant challenge with few successful treatment options. Statistics showsthatPCa is themost common cancer in American men(WHO, 2012). Recent investigations suggest that consumption of fruits,vegetables and medicinal plants rich in triterpenoids, could be beneficialagainst a variety of diseases, including cancer, due to their ability to targetmultiple signaling pathways, their cost-effectiveness, and most importantly,their wide acceptance [1]. Lupeol, a pentacyclic triterpenoid, has shown growthinhibitionof androgen-responsive and unresponsive human PCa cells lines,withoutexhibitingtoxicity towards normal human prostate epithelial cells [2]. Also, novelsynthetic triterpenoids which mimic natural ones, have been effective insuppressing inflammation and inducing apoptosis ina wide variety of tumor cells,throughdiverse mechanisms [3,4].Recently, we have prepared a series of derivativesfrom natural calenduladiol that were evaluatedfor its in vitro cytotoxic activity against human tumor cell lines. Thesestudies have revealed that the introduction of sulfate groups enhancescytotoxic activity of these compounds [5]. These results prompted us tosynthesize some lupeol derivatives by transformations on C-3.Thesesemisynthetic compounds were evaluatedas anti-tumor agents against two humanprostate carcinoma cell lines, LNCaP (androgen dependent) and PC-3 (androgenindependent). The pharmacological results show that some of thesecompounds exhibit higher growth inhibition activities than lupeol (IC50 7-42 μM). Both lupeol andcalenduladiol were obtained from Chuquiragaerinacea (Asteraceae), an endemic species growing wildly in our region