Cytotoxic Guanidine Alkaloids from Pterogyne nitens

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Human ABCB1 confers cells resistance to cytotoxic guanidine alkaloids from Pterogyne nitens

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Alkaloids extracted from Pterogyne nitens induce apoptosis in malignant breast cell line

In the present study, two alkaloids isolated from Pterogyne nitens, a plant native to Brazil, have been shown to induce apoptosis in human breast cancer cells. These compounds, pterogynine (PGN) and pterogynidine (PGD), were tested for their effect on a human infiltrating ductal carcinoma cell line (ZR-7531). The cell line was treated with each alkaloid at several concentrations. Time-dependence (with or without recuperation time) and concentration-dependence (in the range 0.25-10 mM) were investigated in cytotoxicity and apoptosis assays. The annexin assay indicated an apparently higher percentage of death by necrosis of malignant cells after 24 h exposure to both P. nitens extracts than the Hoechst assay. Thus, our results in the two tests demonstrated that the Hoechst assay can discriminate between late apoptotic cells and necrosis, whereas the flow cytometry-based annexin V assay cannot. We concluded that PGN and PGD have effective antineoplastic activity against human breast cancer cells in vitro, by inducing programmed cell death.

Sinalização celular para apoptose em linhagem celular de adenocarcinoma (MCF-7) e carcinoma ductal invasivo de mama (ZR 7531) tratados com alcalódes isolados de Pterogyne nitens

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Bioatividade da solamargina e solasodina para diferentes sistemas celulares após metabolização in vitro por fração microssomal hepática

Pós-graduação em Biociências e Biotecnologia Aplicadas à Farmácia - FCFAR

Bioactive guanidine alkaloids from Pterogyne nitens

Bioactivity-guided fractionation of a methanolic CHCl 3 extract of the leaves of Pterogyne nitens afforded the known guanidine alkaloid pterogynidine [2] and three new guanidine alkaloids, nitensidines A [3], B [4], and C [5], all of which exhibited selective activity towards the DNA repair-deficient yeast mutant RS 321 (IC 12=9.3-20.0 μg/ml); 3,4, and 5 were moderately cytotoxic to CHO Aux B 1 cells (IC 50=8.5-13.0 μg/ml).

Leishmanicidal activity of the crude extract, fractions and major piperidine alkaloids from the flowers of Senna spectabilis

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Antiophidic Solanidane Steroidal Alkaloids from Solanum campaniforme

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Antimicrobial and Cytotoxic Activity of Fruit Extract from Syzygium cumini (L.) Skeels

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Immunostimulatory and cytotoxic activities of Indigofera suffruticosa (Fabaceae)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Cytotoxic and mutagenic evaluation of extracts from plant species of the Miconia genus and their influence on doxorubicin-induced mutagenicity: An in vitro analysis

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

A new cytotoxic naphthoquinone from Paepalanthus latipes

Quinones constitute an important class of naturally occurring compounds. They are found in plants, fungi and bacteria. Large number of quinones has been associated with antitumor, antibacterial, antimalarial and antifungal activities. In this work we describe the isolation, structure determination and the cytotoxic index of a new 1,4-naphthoquinone isolated from the capitula of Paepalanthus latipes.

Cytotoxic lignans from the stems of Styrax camporum (Styracaceae)

An ethanolic extract from the stems of Styrax camporum Pohl (Styracaceae), a plant traditionally used for gastrointestinal diseases, was fractionated and subjected to flash chromatography and afforded two benzofuran lignans, egonol and homoegonol, and one furofuran lignan, (+/-) syringaresinol, which were identified by spectral data interpretation. Their cytotoxic activities against Hep-2 (larynx epidermoid carcinoma), HeLa (human cervix carcinoma) and C6 (rat glioma) cell lines were evaluated using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) assay at several concentrations for 24 h. Activities could be observed for egonol against C6 (IC50 = 3.2 mu g/mL) and Hep-2 (IC50 = 3.6 mu g/mL) cell lines, and for homoegonol against C6 (IC50 = 4.9 mu g/mL) and HeLa (IC50 =- 5.3 mu g/mL) cells.

Mutagenic and cytotoxic effect of planifolin: A naphthopyranone dimer isolated from Paepalanthus planifolius

A naphthopyranone dimer, named planifolin, was isolated from a methylene chloride extract of the capitula of Paepalanthus planifolius Koern. The molecule (C31H26O10) appeared to be made up of two monomeric portions, semi-vioxanthin and paepalantine (an isocoumarin), linked by an ether bond, and it may possess several kinds of biological activity that can be related to its polyphenolic structure. Short-term tests that detect genetic damage can afford the information needed to evaluate carcinogenic risks of chemicals to humans. The Ames test, recommended for testing the mutagenicity of chemical compounds with potential pharmacological application, was used in the present study. The mutagenic activity was evaluated in Salmonella typhimurium strains TA100, TA98, TA102 and TA97a and the cytotoxic effect in McCoy cells. The in vitro cytotoxicity of planifolin to McCoy cells, tested in microculture with neutral red, showed a significant cytotoxic index (CI50) of 12.83 mu g/mL. Planifolin showed mutagenic activity for TA100, TA98 and TA97a. The results indicate that this new naphthopyranone dimer causes mutations by substitution and by addition and deletion of bases in the sequence of DNA. Moreover, its mutagenic potential was increased by metabolic activation. (c) 2005 Elsevier Ltd. All rights reserved.

Anxiolytic-like effects of erythrinian alkaloids from erythrina suberosa

Two alkaloids, erysodine (1) and erysothrine (2) were isolated from the flowers of a Pakistani medicinal plant, Erythrina suberosa. These compounds were investigated for anxiolytic properties, and the results showed significant effect, in an acute oral treatment with 1-2, which were suspended in saline (NaCl 0.9%) plus DMSO 1%, and evaluated in 122 Swiss male mice exposed to two tests of anxiety - the elevated plus-maze (EPM) and the light/dark transition model (LDTM).