Constituents and antiproliferative activity of extracts from leaves of Croton macrobothrys

Abstract

Abstract:Croton macrobothrys Baill, Euphorbiaceae, is a tree from the Atlantic Forest in Southern Brazil, used in traditional medicine and popularly known as "dragon's blood" and "pau-sangue". Leaf n-hexane, dichloromethane and methanol extracts were analyzed by GC/MS and evaluated for their in vitro antiproliferative activity on cell lines 786-0 (kidney), HT-29 (colon), K562 (leukemia), NCI-ADR/ RES (drug resistant ovary), NCI-H460 (lung), MCF-7 (mammary), PC-3 (prostate), OVCAR-3 (ovary), U251 (glioma) and UACC-62 (melanoma). The dicloromethane extract exhibited activity against all cell lines at the concentration 25 µg/mL, in particular on cell lines NCI-H460 (GI50 0.33 μg/mL) and K5662 (GI50 0.91 μg/ mL). Relevant constituents in dichloromethane extract are the alkaloids corydine and salutaridine, as well as the diterpenes geranylgeraniol and crotonin-derived clerodanes.

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“…Corydine and salutaridine (both alkaloids) are important compounds in the dichloromethane extract, while stigmasterol and β-sitosterol are minor constituents. 73 …”

Alkaloids from Croton echinocarpus Baill.: Anti-HIV potential

“…Corydine was previously described in C. macrobothrys (Motta et al, 2011) and C. hemiargyreus var. hemiargyreus (Pereira et al, 1999).…”

“…In a recent study, it was found that the dichloromethane (CH 2 Cl 2 ) extract Croton macrobothrys Baill. leaves, composed by geranyl geraniol, corydine and clerodane diterpene derivatives, showed antiproliferative activity on tumor cell lines, particularly NCI-H460 (lung) and K562 (leukemia) (Motta et al, 2011).…”

Systematic Screening of Plant Extracts from the Brazilian Pantanal with Antimicrobial Activity against Bacteria with Cariogenic Relevance

“…3 ). Of the six compounds identified, five (scopoletin, ferulic acid, ent-18-hydroxy-trachyloban-3-one, crotonin and cajucarin B) were previously isolated from Croton species and one (malic acid) was observed in the Euphorbiaceae family [Craveiro and Silveira, 1982;Maciel et al, 1998;Zhang et al, 2001;Martinsen et al, 2010;Motta et al, 2011;Silva et al, 2011]. The investigation by ESI-MS/MS provided important information about the bioactive components present in these extracts.…”

“…The collision gas pressure was optimized to produce extensive fragmentation of the ion under investigation. The constituents were identified by comparing their ESI-MS/MS fragmentation spectra to the fragmentation spectra of authentic standard samples and literature data [Craveiro and Silveira, 1982;Maciel et al, 1998;Zhang et al, 2001;Martinsen et al, 2010;Motta et al, 2011;Pascoal et al, 2011;Silva et al, 2011].…”