In vitro evaluation of the cytotoxic and trypanocidal activities of Ampelozizyphus amazonicus (Rhamnaceae)

Abstract

Ampelozizyphus amazonicus Ducke is a tree commonly found in the Amazon region and an extract of its stem bark is popularly used as an antimalarial and anti-inflammatory agent and as an antidote to snake venom. Ursolic acid; five lupane type triterpenes: betulin, betulinic acid, lupenone, 3ß-hydroxylup-20(29)-ene-27,28-dioic acid, and 2α,3ß-dihydroxylup-20(29)-ene-27,28-dioic acid, and three phytosteroids: stigmasterol, sitosterol and campesterol, have been isolated from stem extracts of A. amazonicus Ducke. Their structures were characterized by spectral data including COSY and HMQC. In an in vitro biological screening of the isolated compounds, 3ß-hydroxylup-20(29)-ene-27,28-dioic acid was cytotoxic against the SKBR-3 human adenocarcinoma cell line (1 to 10 mg/mL), while 2α,3ß-dihydroxylup-20(29)-ene-27,28-dioic acid exhibited cytotoxicity against both SKBR-3 human adenocarcinoma and C-8161 human melanoma tumor cell lines (>0.1 mg/mL). In the present study, different extracts and some fractions of this plant were also investigated for trypanocidal activity due to the presence of pentacyclic triterpenes. The triterpene classes are potent against Trypanosoma cruzi. The bioassays were carried out using blood collected from Swiss albino mice by cardiac puncture during the parasitemic peak (7th day) after infection with the Y strain of T. cruzi. The results obtained showed that A. amazonicus is a potential source of bioactive compounds since its extracts and fractions isolated from it exhibited in vitro parasite lysis against trypomastigote forms of T. cruzi at concentrations >100 µg/mL. Fractions containing mainly betulin, lupenone, 3ß-hydroxylup-20(29)-ene-27,28-dioic acid, and 2α,3ß-dihydroxylup-20(29)-ene-27,28-dioic acid showed more activity than crude extracts.

Evaluation of the bactericidal and trypanocidal activities of triterpenes isolated from the leaves, stems, and flowers of Lychnophora pinaster

“…Rutin, quercetin, isochlorogenic acid, caffeic acid, isovitexin, vitexin, sesquiterpene derivatives (Alcântara et al, 2005;Leite et al, 2008), and the triterpenes lupeol, a mixture of α-and β-amyrin, and friedelin were previously isolated from its aerial parts. Although several studies have lately related triterpenes to treatment of the trypanosomiases (Rosas et al, 2007;Leite et al, 2006;Cunha et al, 2006) and bactericidal activity (Al-Fatimi et al, 2010), no data are available about the trypanocidal and bactericidal activities of triterpenes isolated from Lychnophora species. The present work describes an investigation of the chemistry of leaves, stems, and flowers of L. pinaster for triterpenes, which were tested for antibacterial and trypanocidal activities.…”

In vitro trypanocidal activity of the Egyptian plant Schinopsis lorentizii against trypomastigote and amastigote forms of Trypanosoma cruzi

“…Their in vitro and in vivo trypanocidal potential has been extensively studied (Duarte et al, 2002;Rosas et al, 2007;Ferreira et al, 2013).…”

HPLC-DAD phenolic profile, cytotoxic and anti-kinetoplastidae activity ofMelissa officinalis

“…This can be considered significant, given that inhibition at concentrations 500 mg/mL, is regarded as clinically relevant. Anti-protozoan activity against the epimastigote form of T. cruzi was identified as moderate (Rosas et al 2007).…”