Antiophidic Solanidane Steroidal Alkaloids from Solanum campaniforme

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

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).

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.

Quinolizidine alkaloids in Ormosia arborea seeds inhibit predation but not hoarding by agoutis (Dasyprocta leporina)

Quinolizidine alkaloids (QAs) are secondary compounds found in seeds of many species of plants, possibly protecting them against pathogens and seed predators. QAs were isolated from Ormosia arborea seeds and bioassayed against red-rumped agoutis (Dasyprocta leporina, Rodentia: Caviomorpha) to verify if they inhibit seed predation and food hoarding (seed dispersal). Three treatments were used: (1) seeds of O. arborea, (2) palatable seeds of Mimusops coriacea (Sapotaceae) treated with MeOH, and (3) seeds of M. coriacea treated with QAs dissolved in MeOH in similar concentration to that present in O. arborea. Palatable seeds were significantly more preyed upon than seeds treated with QAs and Ormosia seeds, but QAs did not influence hoarding behavior. QAs in O. arborea may have a strong effect in avoiding seed predation by rodents, without reducing dispersal.

CNS-selective noncompetitive cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline

LASSBio-767 [(-)-3-O-acetyl-spectaline] and LASSBio-822 [(-)-3-O-tert-Boc-spectaline] were recently described as cholinesterase inhibitors derived from the natural piperidine alkaloid (-)-spectaline, obtained from the flowers of Senna spectabilis (Fabaccae). We investigated their mechanism of inhibition of acetylcholinesterase and their efficacy in reversing scopolamine-induced amnesia. Competition assays with the substrate acetylthiocholine showed a concentration-dependent reduction in rat brain cholinesterase V-max without changes in apparent K-m. The kinetic data for LASSBio-767 and LASSBio-822 were best fit by a model of simple linear noncompetitive inhibition with K-i of 6.1 mu M and 7.5 mu M, respectively. A dilution assay showed a fast and complete reversal of inhibition, independent of incubation time. Simulated docking of the compounds into the catalytic gorge of Torpedo acetylcholinesterase showed interactions with the peripheral anionic site, but not with the catalytic triad. Anti-amnestic effects in mice were assessed in a step-down passive avoidance test and in the Morris water maze 30 min after injection of scopolamine (1 mg/kg i.p.). Saline, LASSBio-767, or LASSBio-822 was administered 15 min before scopolamine. Both compounds reversed the scopolamine-induced reduction in step-down latency at 0.1 mg/kg i.p. LASSBio-767 reversed scopolamine-induced changes in water maze escape latency at 1 mg/kg i.p. or p.o., while its cholinergic side effects were absent or mild up to 30 mg/kg i.p. (LD50 above 100 mg/kg i.p.). Thus, the (-)-spectaline derivatives are potent cholinergic agents in vivo, with a unique profile combining noncompetitive cholinesterase inhibition and CNS selectivity, with few peripheral side effects. (C) 2007 Elsevier B.V. All rights reserved.

Pyridine Alkaloids from Senna multijuga As Acetylcholinesterase Inhibitors

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

Antiprotozoal Sesquiterpene Pyridine Alkaloids from Maytenus ilicifolia

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

Cytotoxic Guanidine Alkaloids from Pterogyne nitens

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

Aporphine and bisaporphine alkaloids from Aristolochia lagesiana var. intermedia

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

Dimeric alkaloids and flavonoids from Aristolochia ridicula

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

Acetylcholinesterase Inhibitory Pyridine Alkaloids of the Leaves of Senna multijuga

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

An LC-DAD Fingerprinting Method for Alkaloids, Flavonoids and Styrylpyrones from Cryptocarya mandioccana

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

Alkaloids from Stems of Esenbeckia leiocarpa Engl. (Rutaceae) as Potential Treatment for Alzheimer Disease

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

Biological Activity of Quinoline Alkaloids from Raulinoa echinata and X-ray Structure of Flindersiamine

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