Antitumor Activity of the Essential Oil from the Leaves of Croton regelianus and Its Component Ascaridole

Abstract

Croton regelianus Muell. Arg., popularly known as 'velame-de-cheiro', is a native plant from the Northeast of Brazil used in folk medicine to treat diseases of different kinds, including malignant tumors. In this study, the in vitro and in vivo antitumor effects of the essential oil from the leaves of C. regelianus and ascaridole, one of the main constituents, were investigated. In vitro, the essential oil and ascaridole displayed cytotoxicity, showing IC(50) values in the range of 22.2 to 48.0 microg/ml in HL-60 and SF-295 cell lines for the essential oil, and 6.3 to 18.4 microg/ml in HL-60 and HCT-8 cells lines for ascaridole, respectively. The in vivo study, using sarcoma 180 as a tumor model, demonstrated inhibition rates of 28.1 and 31.8% for essential oil, at the 50 and 100 mg/kg, while ascaridole inhibition rates were 33.9% at 10 mg/kg and 33.3% at 20-mg/kg doses. Histopathological examination showed that the organs were only weakly affected by the treatment. In conclusion, ascaridole has an interesting antitumor activity in sarcoma 180 murine model, probably related to the described cytotoxic activity, and, moreover, its presence in the essential oil from the leaves of C. regelianus could explain, at least in part, the ethnopharmacological use of this plant in the treatment of cancer.

Phytochemicals: cancer chemoprevention and suppression of tumor onset and metastasis

“…CCRF-CEM; HL60; MDA-MB-231 Antineoplastic effects [170] Modest inhibition in sarcoma 180 tumor model [171] Bisacurone [190], inhibited DNMT2 activity, reduced HDAC1; induced p53 [191] Augmented efficacy of docetaxel and restored sensitivity to anti-androgen therapy in xenograft mice [192] Ganoderic acid T (GA-T)…”

A phytochemical of modern medicinal perspective

“…Ascaridole showed antitumor activity in sarcoma 180 murine model which signified the ethnopharmacological use of this plant for the treatment of cancer [21]. Fifty three phytochemicals isolated from plants were tested for their differential cytotoxic effects in the cell lines which were having defect in the nucleotide excision repair genes ERCC6 or XPC, and from the result it was found that ascaridol was the most effective [22].…”

Análise de terpenóides de espécies de Croton sect. Lamprocroton (Mull. Arg.) Pax (Euphorbiaceae)

“…Entre elas temos C. regelianus com atividade anticâncer (Bezerra et al, 2009) e Securinega suffruticosa (Euphorbiaceae), típica do cerrado brasileiro, com atividade antitumoral (Yuan et al, 2005;Mesquita, 2010). Este grupo não é muito comum a Croton, tendo sido detectada em C. salutaris, com 12-hidroxi-13-metilpodocarpa-9,11,13-trien-ona (Itokawa, 1991) e em C. regelianus, (5β,8α,10α)-8-hidroxi-13-metilpodocarpa-9(11),13-diene-3,12-diona (Torres et al, 2010).…”

“…Os podocarpanos apresentam até o momento, distribuição restrita, tendo sido detectado apenas no Brasil em espécies coletadas nos estados do Ceará (C. regelianus - Bezerra et al, 2009) e São Paulo (C. salutaris - Itokawa et al, 1991). Com os dados deste estudo, diterpenos com este tipo de esqueleto foram identificados para mais cinco espécies de Croton coletadas nos estados de Minas Gerais (C. ceanothifolius e C. pseudoadipatus), São Paulo (C. pallidulus var.…”