Antiproliferative activity of extracts of Euphorbia tirucalli L (Euphorbiaceae) from three regions of Brazil

Purpose: To investigate Euphorbia tirucalli extract for probable geographic variations in its antiproliferative activity.Methods: The aerial parts of E. tirucalli were collected in the Brazilian states of Mato Grosso, Rio de Janeiro, Pará, Minas Gerais and Santa Catarina. The 70 % ethanol extract was obtained according to the procedure described in Brazilian Homeopathic Pharmacopeia. The antiproliferative activity of extracts, in concentrations of 62, 125, 250, and 500 μg mL-1, was tested against leukemia (HL-60), lymphoma (Daudi) and melanoma (B16F10) cell lines using methyl thiazol tetrazolium assay (MTT). Phytochemical analysis were carried out using High-performance liquid chromatography-diode array (HPLC-UV-DAD) and electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry (ESI(-) FT-ICR MS) assays.Results: There was significant regional variability in the cytotoxicity of E. tirucalli extracts in a dosedependent manner. The extracts had similar activity towards leukemia cell line HL-60, decreasing cell viability to about 60 – 70 %. The extract showed the presence of ellagitannins, flavonoids, veracylglucan, and acid triterpenes as the major compounds.Conclusion: While the results support the ethnopharmacological use of E. tirucalli throughout Brazil, regional quantitative differences found in some classes of secondary metabolites may explain the variations observed in antitumor activity.Keywords: Aveloz, Cancer, Cytotoxicity, Antiproliferative, Ethnopharmacological, Traditional medicin

Chemical composition and cytotoxic activity of Lepechinia speciosa (St. Hill) Epling

The cell viability of Lepechinia speciosa (St. Hill) Epling fractions was measured by cell membrane integrity (lactate dehydrogenase assay) on rat basophilic leukemia cells (RBL-2H3). All fractions and extract tested (100 μg/ml) increased the release of lactate dehydrogenase (LDH), being the ethyl acetate and dichloromethane fractions with LDH release of 94.5% and 91.2%, respectively. As these fractions showed decrease of cell viability, the antiproliferative activity on human breast adenocarcinoma cells (MCF-7) through sulphorhodamine B (SRB) assay was performed with them. The dichloromethane fraction (50 μg/ml) displayed the maximum activity (95% of inhibition) (IC50 = 1.99 ± 0.06 μg/ml). From this fraction was obtained a mixture containing two triterpenes (ursolic and oleanolic acids) and one fatty acid (palmitic acid), which were identified by gas chromatography coupled to mass spectrometry (GC-MS) and had their structures confirmed by 13C NMR. Rosmarinic acid and verbascoside were isolated from the ethyl acetate fraction and had their structures confirmed by 1H NMR.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Terpinen-4-ol is overproduced in tissue cultures of Alpinia zerumbet (Pers.) Burtt et Smith by induction of methyl jasmonate

Alpinia zerumbet (Zingiberaceae) presents a high medicinal value, in part by its production of volatile compounds. Organogenic in vitro cultures of A. zerumbet were treated with the elicitor methyl jasmonate (MeJA), a natural volatile signaling molecule in biotic and abiotic stress, and the effect was evaluated on the in vitro production of volatiles. Leaves of plantlets were subjected to simultaneous distillation-extraction (SDE), and sabinene, β-pinene, 1,8 cineole and terpinen-4-ol were the main volatiles detected. However, after exposure to a solution of of MeJA for 3 and 10 days, terpinen-4-ol showed a remarkable increase, corresponding to 18.01 and 14.75 %, respectively, when compared to control with ethanol. In contrast, exposure of plantlets to the addition of ethanol induced levels of sabinene and 1,8 cineole higher than those produced by MeJA.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Vasodilator activity of extracts of field Alpinia purpurata (Vieill) K: Schum and A. zerumbet (Pers.) Burtt et Smith cultured in vitro

Nowadays, the high blood pressure is one of the main causes of death and cardiovascular diseases. Vasodilator drugs are frequently used to treat arterial hypertension. Experiments were undertaken to determine whether hydroalcoholic extracts obtained from leaves of field-grown Alpinia purpurata and A. zerumbet cultured in vitro under different plant growth regulators induce a vasodilator effect on Wistar rat mesenteric vascular bed pre-contracted with norepinephrine. Plant extracts were able to induce a long-lasting endothelium-dependent vasodilation. Efficiency on activity of A. purpurata reached 87% at concentration of 60 μg. The extract of A. zerumbet maintained in medium containing IAA, induced the relaxation (17.4%) at 90 μg, as compared to the control (MS0) that showed a better vasodilator effect (60%). These results are in agreement with the quantification of phenolic compounds in the extracts, which were 50% lower for those plants cultured in IAA. A. purpurata was assayed for the first time in relation to its vasodilator activity. This paper showed a strong probability of correlation between the pharmacological activities of A. purpurata with their content in phenolic compounds.Atualmente, a hipertensão arterial é uma das maiores causas de morte e de doenças cardiovasculares. Os vasodilatadores são freqüentemente utilizados no tratamento da hipertensão. Extratos hidroalcoólicos de Alpinia purpurata de campo e de A. zerumbet cultivada in vitro sob diferentes reguladores de crescimento vegetal foram ensaiados no leito mesentérico de ratos Wistar. Os extratos de A. purpurata e A. zerumbet produziram efeito vasodilatador com padrão de resposta dose-dependente de duração prolongada. Extratos da espécie A. purpurata tiveram efeito vasodilatador de 87% na dose de 60 μg. O extrato obtido de folhas de A. zerumbet oriundas das culturas mantidas em meio contendo AIA (ácido indol acético) inibiu o relaxamento (17,4%) na dose de 90 μg em relação ao controle (MS0), com o qual foi verificado melhor efeito vasodilatador (60%). Estes resultados estão de acordo com a concentração de fenóis totais que foi 50% menor para os extratos de plantas cultivadas in vitro em AIA. A espécie A. purpurata foi pela primeira vez ensaiada quanto à atividade vasodilatadora. Os resultados obtidos indicaram a presença de substâncias fenólicas provavelmente correlacionadas à ação terapêutica de A. purpurata

Genotoxicity and mutagenicity of Echinodorus macrophyllus (chapéu-de-couro) extracts

Echinodorus macrophyllus, commonly known as chapéu-de-couro, is a medicinal plant used in folk medicine to treat inflammation and rheumatic diseases. In this work, we used short-term bacterial assays based on the induction of SOS functions to examine the genotoxicity and mutagenicity of an aqueous extract of E. macrophyllus leaves. Whole extract and an ethyl acetate fraction showed similar genotoxicity and caused an ~70-fold increase in lysogenic induction. The extract also gave a positive result in the SOS chromotest with an increase of 12-fold in β-Galactosidase enzymatic units. There was a strong trend towards base substitutions and frameshifts at purine sites in the mutations induced by the extract in Escherichia coli (CC103 and CC104 strains) and Salmonella typhimurium test strains (22-fold increase in histidine revertants in TA98 strain). Since reactive oxygen species may be implicated in aging process and in degenerative diseases, we used antioxidant compounds as catalase, thiourea and dipyridyl in the lysogenic induction test. All this compounds were able to reduce the induction factor observed in the treatment with chapéu-de-couro, thus suggesting that the genotoxicity and mutagenicity were attributable to the production of reactive oxygen species that targeted DNA purines

Production of rutin and Kaempferol-3-O-glucuronide by tissue cultures of Alpinia purpurata (Vieill) K. Schum

The accumulation of flavonoids was evaluated in organogenic cultures of Alpinia purpurata through HPLC analysis. Cultures were maintained in liquid MS medium in the following treatments: MS0 (control), TDZ, BAP and IAA + TDZ. Kaempferol-3-O-glucuronide content was higher than rutin for all in vitro treatments, except by control medium in which plants did not produce kaempferol-3-O-glucuronide. A remarkable increase in kaempferol-3-O-glucuronide content was verified using BAP 2 mg.l-1 (0.027 mg/100 mg dried extract) and IAA 2 mg.l-1 + TDZ 2 mg.l-1 (0.030 mg/100 mg dried extract) treatments. With the addition of 2 mg.l-1 BAP, rutin concentration also increased in the proportion 1:4 compared to control.Colegio de Farmacéuticos de la Provincia de Buenos Aire

PHYTOCHEMICAL AND PHYLOGENETIC ANALYSIS OF Spondias

<p>This paper describes the correlation between the phenolic composition and the molecular phylogenetic reconstruction of five <italic>Spondias</italic> species (Anacardiaceae). Two of these species (<italic>S. venulosa</italic> and <italic>Spondias</italic> sp.) occur in rainforest areas and the other three are widely distributed in Brazil (<italic>S. dulcis</italic>, <italic>S.mombin</italic>, and <italic>S. purpurea</italic>). The flavonoid enriched fraction of the <italic>S. venulosa</italic> leaf extract also underwent a chemical study. The results indicate that the presence of flavonol 3-<italic>O</italic>-glycosides are a synapomorphic character of the studied American <italic>Spondias</italic> and the production of rhamnetin 3-<italic>O</italic>-rutinoside is a synapomorphy of the Atlantic forest species. This is the first report of flavonoids in <italic>S. venulosa</italic>, an endemic species from the Brazilian Atlantic rainforest.</p