A chemical investigation of Anaxagorea dolichocarpa Sprague & Sandwith, a member of Annonaceae family, was carried out. The ethanolic extract from the roots of this plant led, by chromatography tecniches, to isolation of the new azaphenanthrene alkaloids dolichocarpine (1) and 9-methoxyeupolauramine (2), besides the known alkaloids eupolauramine (3), 3-methoxyeupolauridine (4), eupolauramine (5) and 4-methylsampangine (6). The structures of isolated compounds were established by 1D and 2D NMR, HRESIMS, tandem MSn and IR data. The cytotoxicity of compounds 1 - 5 was evaluated against HCT-116 (human colorectal carcinoma) and L929 (murine fibroblast) cell lines.

In this study, inductively coupled plasma optical emission spectrometry (ICP OES) was used for multi-element analysis in five multimineral preparations from a dissolution test, in accordance with the United States Pharmacopeia (USP 34 method): apparatus 1, 75 rpm and 900 mL of 0.1 mol L-1 HCl. Element releases in all samples (minimum-maximum in %) were: Ca (14.5-28.2), Cr (54.5-68.0), Cu (2.9-10.0), Fe (4.0-34.3), Mg (6.0-25.2), Mn (2.6-51.2), V (0.0-51.4) and Zn (1.5-107.3). The concentrations of Al, Ba, Cd, Co, Mo, Pb and Se were below the limit of detection of ICP OES. Accuracy was assessed by microwave digestion and recovery values of 94-102%. USP 34 method indicates that not less than 75% of the elements described on the product label must be dissolved in 1 h. Only the release of Zn met the recommendations. The results indicated the need for greater quality control in multivitamin preparations. The dissolution test was validated in order to contribute to Brazilian and other pharmacopoeias.

In this study, the elemental composition of nine medicinal plants and phytomedicines was evaluated by using axial view inductively coupled plasma optical emission spectrometry (ICP OES) after three digestion procedures: dry ashing (DA) and two wet digestions with a mineral acid (HNO3/H2O2) mixture on a conventional hot plate (CD), besides microwave digestion (MW). Accuracy was assessed from spinach leaves (CRM 1570a) and recovery values were in the range of 82 to 113.8%. Precisions, such as relative standard deviation (RSD), below 10% were reached. The MW procedure was preferred for its accuracy (recovery values of 94 to 102%), reduced contamination, increase in the efficiency of the decomposition process, lower residual acidity and reduced time required for digestion. The concentrations of analytes in the samples (minimum-maximum in μg g-1) were: Ca (100.71-462.20), Co (0.54-0.85), Cu (0.32-7.82), Fe (2.74-18.03), Mg (18.40-521.28), Mn (0.17-55.14), Ni (0.56-1.25) and Zn (2.96-20.92). The levels of Al, Ba, Cd, Cr, Mo, Pb, Se and V in all investigated samples were found to be below the limit of detection of ICP OES. The multielement analysis by ICP OES showed that the method is simple, fast and reliable for the multielement determination in medicinal plants and phytomedicines.

O presente estudo descreve a acentuada atividade citotóxica da nor-β-lapachona, seus derivados arilamino substituídos, naftoquinonas iodadas e metilada, além de nor-β-lapachonas 1,2,3-triazólicas, contra quatro linhagens de células de leucemia humana (HL-60, K562, Molt-4 e Jurkat). Nor-β-lapachonas arilamino substituídas foram identificadas com potente atividade, revelando-se como potenciais protótipos contra as linhagens tumorais descritas. Estudos utilizando o ensaio cometa evidenciaram danos ao ácido desoxirribonucleico (ADN) causado pelos derivados arilamino substituídos devido o aumento dos níveis intracelulares de espécies reativas de oxigênio (ERO's). Células de HL-60 foram selecionadas para a continuidade dos estudos de mecanismos moleculares subjacentes e apoptose induzida pelos derivados quinoidais foi observada por análise de citometria de fluxo. Cepas de Saccharomyces cerevisiae foram utilizadas para uma investigação preliminar sobre o mecanismo de ação em topoisomerases de ADN. Os estudos sugerem que, aparentemente, a citotoxidade dos compostos não envolve a inibição de topoisomerases, mas que o tratamento prejudica a atividade de reparação do ADN, provocando assim a morte celular. A capacidade em induzir apoptose e aberrações cromossômicas em fibroblastos de pulmão de hamster chinês (células V79) também foi investigada. Núcleos apoptóticos foram observados e nossos estudos indicam uma correlação entre dano ao ADN e apoptose.

The current study describes that nor-β-lapachone and its arylamino derivatives, iodinated and methylated naphthoquinones and nor-β-lapachone-based 1,2,3-triazoles exhibited pronounced cytotoxic effects against four human leukemia cell lines (HL-60, K562, Molt-4 and Jurkat). Nor-β-lapachones arylamino substituted with potent activity were identified, revealing themselves as potential prototypes against tumor cell lines. Moreover, cells treated with these compounds showed DNA damage according to the standard comet assay, a finding that was, at least in part, due to increased intracellular levels of ROS. HL-60 cells were chosen to study the underlying molecular mechanisms of cytotoxicity. Drug-induced apoptosis in HL-60 cells was observed by flow cytometry analyses. Strains of Saccharomyces cerevisiae were used for a preliminary investigation into the mechanism of drug action on DNA topoisomerases. These results suggested that the cytotoxicity of these compounds apparently does not involve topoisomerase inhibition, but that treatment impairs DNA repair activity, thus triggering cell death. Considering their pro-oxidant properties, we investigated the ability of these compounds to induce apoptosis and chromosomal aberrations as micronuclei in Chinese hamster lung fibroblasts (V79 cells). Morphological apoptotic nuclei and micronuclei induction following drug treatment were observed, suggesting a correlation between DNA damage and apoptosis.

Cytotoxic activity of eight plant extracts, native from the Mid-West of Brazil comprising Cerrado, Pantanal and semideciduous forest, was evaluated for MDA-MB-435, SF-295, and HCT-8 cancer cell strains. A single 100 µg.mL-1 dose of each extract was employed with 72 h of incubation for all tests. Doxorubicin (1 µg.mL-1) was used as the positive control and the MTT method was used to detect the activity. Cytotoxicity of distinct polarities was observed in thirty extracts (46%), from different parts of the following species: Tabebuia heptaphylla (Vell.) Toledo, Bignoniaceae, Tapirira guianensis Aubl., Anacardiaceae, Myracrodruon urundeuva Allemão, Anacardiaceae, Schinus terebinthifolius Raddi, Anacardiaceae, Gomphrena elegans Mart., Amaranthaceae, Attalea phalerata Mart. ex Spreng., Arecaceae, Eugenia uniflora L., Myrtaceae, and Annona dioica A. St.-Hil., Annonaceae. Extracts of at least two tested cell strains were considered to be highly active since their inhibition rate was over 75%.

Phytochemical investigation of heartwood of Auxemma glazioviana (Boraginaceae) has led to the isolation of three benzoquinones, one hydroquinone identified as: oncocalyxone A (1), oncocalyxone C (2), glazioviana A (3), glaziovianol (4) besides allantoin (5) α-bisabolol (6) and α-cadinol (7). Their structures were determined based on spectral analysis, including 2D NMR experiments. Essential oil obtained from heartwood by hydrodistillation was analyzed by GC/MS. The major constituents were identified as α-bisabolol and α-cadinol. The oil was active against larvae of dengue (Aedes aegypti ) with DL50 2.98 ppm.