Venom peptide analysis of Vipera ammodytes meridionalis (Viperinae) and Bothrops jararacussu (Crotalinae) demonstrates subfamily-specificity of the peptidome in the family Viperidae

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

Triacontyl p-coumarate: An inhibitor of snake venom metalloproteinases

Snake venom metalloproteinases (SVMPs) participate in a number of important biological, physiological and pathophysiological processes and are primarily responsible for the local tissue damage characteristic of viperid snake envenomations. The use of medicinal plant extracts as antidotes against animal venoms is an old practice, especially against snake envenomations. Such plants are sources of many pharmacologically active compounds and have been shown to antagonize the effects of some venoms and toxins. The present study explores the activity of triacontyl p-coumarate (PCT), an active compound isolated from root bark of Bombacopsis glabra vegetal extract (Bg), against harmful effects of Bothropoides pauloensis snake venom and isolated toxins (SVMPs or phospholipase A2). Before inhibition assays, Bg or PCT was incubated with venom or toxins at ratios of 1:1 and 1:5 (w/w; venom or isolated toxins/PCT) for 30 min at 37 °C. Treatment conditions were also assayed to simulate snakebite with PCT inoculated at either the same venom or toxin site. PCT neutralized fibrinogenolytic activity and plasmatic fibrinogen depletion induced by B. pauloensis venom or isolated toxin. PCT also efficiently inhibited the hemorrhagic (3MDH-minimum hemorrhagic dose injected i.d into mice) and myotoxic activities induced by Jararhagin, a metalloproteinase from B. jararaca at 1:5 ratio (toxin: inhibitor, w/w) when it was previously incubated with PCT and injected into mice or when PCT was administered after toxin injection. Docking simulations using data on a metalloproteinase (Neuwiedase) structure suggest that the binding between the protein and the inhibitor occurs mainly in the active site region causing blockade of the enzymatic reaction by displacement of catalytic water. Steric hindrance may also play a role in the mechanism since the PCT hydrophobic tail was found to interact with the loop associated with substrate anchorage. Thus, PCT may provide a alternative to complement ophidian envenomation treatments. © 2012 Elsevier Ltd. All rights reserved.

Effect of propolis, some isolated compounds and its source plant on antibody production

Propolis is a beehive product with a very complex chemical composition, widely used in folk medicine because of its several therapeutic activities. Its biological properties and chemical composition may vary according to the geographic location and to the different plant sources. The possible mechanism of action of propolis as well as of its active compounds has been the subject of researchers in recent years. In this work, first we reported the results of our study on the seasonal effect of the immunomodulatory action of propolis on antibody production in bovine serum albumin (BSA)-immunized rats. Then, we compared the effect of Brazilian and Bulgarian propolis, some isolated compounds and Baccharis extract on anti-BSA antibody levels. Based on the results, we conclude that propolis stimulates antibody production, independently of the season and geographic origin. Caffeic acid, quercetin and Baccharis extract had no effect on antibody production, although the importance of isolated compounds is well reported in other biological assays. Propolis action is a consequence of plant-derived products with synergic effects. while isolated compounds or extracts from its plant sources had no effect in this assay. (c) 2005 Elsevier B.V.. All rights reserved.

Anticholinesterasic, Nematostatic and Anthelmintic Activities of Pyridinic and Pyrazinic Compounds

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

Cytotoxicity of Active Ingredients Extracted from Plants of the Brazilian "Cerrado"

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

Amoebicidal compounds from medicinal plants.

A series of the natural constituents with amoebicidal activity isolated from several medicinal plants is shown. A list of the medicinal plants potentially active as amoebicide and/or against dysentery also is demonstrated. The present data grouping of the natural compounds and medicinal plants can be an important source of information for the selection of research plant material by the investigators interested in the discovery of new biologically active compounds as amoebicide.

Antiulcer effects of Ethyl acetate fraction of Carpolobia lutea leaf

Carpolobia lutea leaves (CLL) (Polygalaceae) were earlier screened and the antiulcer ethnomedicinal claim established. This article seeks to quantitatively isolate, elucidate the active compounds from most active CLL fraction. Fractionation was by semi-preparative HPLC; the active fraction was subjected to radical scavenging assays (RSA) and quantification of the total phenolic content (TPC) were also executed. Results: Ethyl acetate fraction (EAF) was observed to be the most pharmacologically active antiulcer fraction when screened using acute ulcer models induced in rodents. The EAF demonstrated significant (p < 0.05-0.001) antiulcer activity in various in vivo induced ulceration models by reducing the ulcer index and increasing the preventive ratio. The EAF demonstrated > 70% in TPC and < 20 % in RSA. Cinnamic and coumaric acids derivatives were isolated from EAF. Cinnamic acids have been implicated and patented as antiulcer agent. Isolated compounds could in part mediate the observed pharmacological activities which lend credence to its ethnobotanical uses.

ANTIDIARRHEAL MECHANISM AND IONIC PROFILE OF CARPOLOBIA LUTEA ETHANOLIC STEM-BARK EXTRACT IN RATS

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

Use of Guanidine Compounds in the Treatment of Neglected Tropical Diseases

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

Zeyheria montana Mart. (Bignoniaceae) as source of antioxidant and immunomodulatory compounds with beneficial effects on intestinal inflammation

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Farmacocinética e farmacodinâmica de derivado ftalimídico planejado para o tratamento da anemia falciforme

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

Activity of Ricinus communis (Euphorbiaceae) and ricinine against the leaf-cutting ant Atta sexdens rubropilosa (Hymenoptera : Formicidae) and the symbiotic fungus Leucoagaricus gongylophorus

The focus of this study was the identification of compounds from plant extracts for use in crop protection. This paper reports on the toxic activity of fractions of leaf extracts of Ricinus communis L (Euphorbiaceae) and isolated active compounds in the leaf-cutting ant Atta sexdens rubropilosa Forel and its symbiotic fungus Leucoagaricus gongylophorus (Singer) Moller. The main compounds responsible for activity against the fungus and ant in leaf extracts of R communis were found to be fatty acids for the former and ricinine for the ants. (C) 2004 Society of Chemical Industry.

Sesquiterpene lactones as allelochemicals

Six new sesquiterpene lactones, annuolide H ( 3), helivypolides F, H-J ( 4, 11-13), and helieudesmanolide A ( 6), together with known compounds, were isolated from polar bioactive fractions of Helianthus annuus cv. SH-222 and Stella fresh leaf water extracts. Spectroscopic analysis of the new data for 1,2-anhydroniveusin A and 1-methoxy-4,5-dihydroniveusin A corrects some previous assignments. The compounds were tested using the etiolated wheat coleoptile bioassay, and the most active compounds were assayed in standard target species ( STS) ( Lepidium sativum, Allium cepa, Lactuca sativa, Lycopersicon esculentum, and Triticum aestivum) from 5 x 10(-4) to 10(-5) M. The most phytotoxic compounds were helivypolide F and 15-hydroxy-3-dehydrodeoxyfruticin, both of which have a carbonyl group at C-3 conjugated with two double bonds.

Agronomical and phytochemical aspects of fafia

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)