Croton cajucara crude extract and isolated terpenes: activity on Trypanosoma cruzi

Abstract

Croton cajucara is a plant found in the Amazon region and is known for its medicinal properties. The effects of the methanolic extract of the stem bark of C. cajucara (MCC) and of the isolated terpenes, trans-dehydrocrotonin (t-DCTN) and acetyl aleuritolic acid (AAA), were investigated using four isolates of Trypanosoma cruzi. In assays with trypomastigotes, the extract was more active than the isolated compounds, presenting IC(50) in the range of 10 to 50 μg/mL. The trypanocidal effect of MCC, AAA and benznidazole was significantly higher in the GLT291 and C45 strains, which were recently isolated from wild animals. MCC and AAA caused a dose-dependent inhibition of epimastigote proliferation. In assays using intracellular amastigotes, AAA and MCC reduced the percent of infection and the endocytic index after 96 h of treatment, at concentrations that were non-toxic to the host cells. MCC inhibited the trypanothione reductase pathway in both epimastigotes and trypomastigotes of all the subpopulations. The absence of AAA activity on the trypanothione reductase pathway in epimastigotes of Dm28c suggests heterogeneity of the biochemical profile between this clone and the three strains. Epimastigotes and trypomastigotes (GLT291) were treated for 24 h with MCC or AAA, and both induced alterations of the plasma membrane, while AAA-treated epimastigotes also displayed mitochondrial damage.

Chemical composition, antibacterial and modulatory action of the essential oil of Croton rhamnifolioides leaves Pax and Hoffman

“…For example, some species of the Croton genus can be cited, whose studies have confirmed its anti-inflammatory, anti-ulcerogenic, antimutagenic, anti-estrogenic and hypoglycemic (ROSA et al, 2003), antinociceptive (OLIVEIRA et al, 2001), antifungal (SOUZA et al, 2006), antibacterial RODRIGUES et al, 2009), anti-leishmaniosis (ROSA et al, 2003), anti-Trypanosoma cruzi (CAMPOS et al, 2010), larvicide (LIMA et al, 2006) and as a central nervous system depressor (LAZARINI et al, 2000).…”

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

“…Foram isolados ainda três esteróides e dois flavonóides com atividades farmacológicas, porém em concentrações minoritárias (Maciel et al, 2000). C. cajucara possui óleo volátil rico em linalol, além de já terem sido identificados para a espécie diterpenos e esteróis, o que explica a atividade anti-inflamatória, antinociceptiva, antifúngica (Souza et al, 2006), anti-leishmaniose (Rosa et al, 2003) e anti-Trypanossoma cruzzi (Campos et al, 2010).…”

“…Os esqueletos estruturais mais comuns são: labdanos, cauranos, seco-cauranos, cembranóides, clerodanos, neoclerodanos, halimanos, isopimaranos, traquilobanos e ésteres de forbol (Salatino et al, 2007) (Maciel et al, 1998;Grynberg, 1999;Campos et al, 2010). Outras espécies com clerodanos bioativos são C. lechleri -clerodanos com atividade antioxidante (De Marino, 2008), C. palanostigma -atividade antitumoral (Campos et al, 2010) e C. cajucara da qual foi isolada a trans-desidrocrotonina (DCTN) com atividade antitumoral (Grynberg, 1999).…”

“…Compostos considerados bioativos apresentam atividade insetífuga, antimicrobiana, antiviral, antiúlcera, gastroprotetora e antitumoral (Maciel et al, 1998;Fattorusso et al, 2002;Campos et al, 2010). Relatos sobre ocorrência de clerodanos em Croton (principalmente furano-clerodanos) são bastante comuns tendo registro em C. cajucara (Maciel et al, 1998;Grynberg et al, 1999;Souza et al, 2006;Campos et al, 2010), C. draco (Murillo et al, 2001;Deepika-Gupta et al, 2008), C. eluteria (Fattorusso et al, 2002), C lechleri (De Marino et al, 2008), C. membranaceous (Bayor et al, 2009), C. oblongifolius (Youngsa et al, 2007, C. palanostigma (Socorro et al, 2004;Brasil et al, 2009) e C. polyandrus (Araújo-Junior et al, 2005. Nos trabalhos realizados com C. cajucara, um dos diterpenos mais característico é a trans-crotonina, um furano-clerodano bioativo com atividades fungicida (Souza et al, 2006), anti-úlcera (Campos et al, 2010), antitumoral e anti-inflamatória (Grynberg et al, 1999).…”

“…eluteria -Fattorusso et al, 2002;C. palanostigma -Socorro et al, 2004;Campos et al, 2010;C. polyandrus -Araújo-Junior et al, 2005).…”