Rosmarinic acid, a new snake venom phospholipase A(2) inhibitor from Cordia verbenacea (Boraginaceae): antiserum action potentiation and molecular interaction

Many plants are used in traditional medicine as active agents against various effects induced by snakebite. The methanolic extract from Cordia verbenacea (Cv) significantly inhibited paw edema induced by Bothrops jararacussu snake venom and by its main basic phospholipase A(2) homologs, namely bothropstoxins I and II (BthTXs). The active component was isolated by chromatography on Sephadex LH-20 and by RP-HPLC on a C18 column and identified as rosmarinic acid (Cv-RA). Rosmarinic acid is an ester of caffeic acid and 3,4-dihydroxyphenyllactic acid [2-O-cafeoil-3-(3,4-di-hydroxy-phenyl)-R-lactic acid]. This is the first report of RA in the species C. verbenacea ('baleeira', 'whaler') and of its anti-inflammatory and antimyotoxic properties against snake venoms and isolated toxins. RA inhibited the edema and myotoxic activity induced by the basic PLA(2)s BthTX-I and BthTX-II. It was, however, less efficient to inhibit the PLA(2) activity of BthTX-II and, still less, the PLA(2) and edema-inducing activities of the acidic isoform BthA-1-PLA(2), from the same venom, showing therefore a higher inhibitory activity upon basic PLA(2)s. RA also inhibited most of the myotoxic and partially the edema-inducing effects of both basic PLA(2)s, thus reinforcing the idea of dissociation between the catalytic and pharmacological domains. The pure compound potentiated the ability of the commercial equine polyvalent antivenom in neutralizing lethal and myotoxic effects of the crude venom and of isolated PLA(2)s in experimental models. CD data presented here suggest that, after binding, no significant conformation changes occur either in the Cv-RA or in the target PLA(2). A possible model for the interaction of rosmarinic acid with Lys49-PLA(2) BthTX-I is proposed. (c) 2005 Elsevier Ltd. All rights reserved.

Gastroprotective and ulcer healing effects of essential oil from Hyptis spicigera Lam. (Lamiaceae)

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Cytotoxic constituents of propolis inducing anticancer effects: a review

Objectives Propolis is a honeybee product used extensively in traditional medicine for its antioxidant, anti-inflammatory, immunomodulatory and anticancer effects. Propolis exhibits a broad spectrum of biological activities because it is a complex mixture of natural substances. In this review, the antitumour effects of propolis extracts and its constituents (e. g. flavonoids, terpenes and caffeic acid phenethyl ester) are discussed.Key findings The effect of propolis on experimental carcinogenesis is discussed, as well as its possible mechanisms of action against tumours, involving apoptosis, cell cycle arrest and interference on metabolic pathways. Propolis seems to be efficient against different tumour cells both in vitro and in vivo, which suggests its potential in the development of new anticancer drugs.Summary Propolis extracts may be important economically and would allow a relatively inexpensive cancer treatment. Preclinical investigations are needed to further elucidate the benefits of propolis and its antitumour properties.

Uncaria tomentosa Aqueous-ethanol Extract Triggers an Immunomodulation toward a Th2 Cytokine Profile

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

Chemical and Antidiarrheal Studies of Plinia cauliflora

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

Patents of drugs extracted from Brazilian medicinal plants

Background: Plants synthesise a vast repertoire of chemicals with various biological activities. Brazilian enormous botanical diversity facilitates the development of novel ethical drugs for the treatment of diseases in humans. Objective: To present therapeutic patent applications comprising Brazilian native plants published in the 2003 - 2008 period in light of legal aspects of patentability of biodiversity and public health concerns. Methods: Therapeutic patent applications related to Brazilian medicinal plants available at both the European Patent Office and the Brazilian National Institute of industrial Property databases were reviewed. Results/conclusion: Twenty-five patents are presented, most of which concern inflammatory, allergic, parasitic, infectious or digestive diseases, including extracts from Carapa guianensis, Copaifera genus, Cordia verbenacea, Erythrina mulungu, Physalis angulata and other pharmaceutical compositions with antileishmanial, antimalarial or trypanocidal activity. Brazilian research centres and universities are responsible for most of these inventions.

Ação de fitorreguladores no crescimento da erva-cidreira-brasileira

Lippia alba, espécie brasileira da família Verbenaceae, é plantada e usada em todo o Brasil por suas atividades farmacológicas como analgésica, antiespasmódica, calmante, sedativa e citostática. Popularmente a Lippia é denominada de alecrim, cidreira falsa ou falsa melissa. O trabalho visou testar o efeito das aplicações de GA3, ethephon e CCC sobre o crescimento de Lippia alba (Mill.) N.E.Br. - Verbenaceae, em diferentes épocas do ano. O experimento foi instalado na Fazenda São Manuel, pertencente à UNESP em Botucatu, de dezembro/95 a dezembro/96. O mesmo consistiu de sete tratamentos e três repetições em blocos inteiramente casualizados, com os tratamentos aplicados nas parcelas e as colheitas nas subparcelas. Os tratamentos incluíram o controle, ácido giberélico (GA3 50 e 100 mg.L-1), ácido 2-cloroetil-fosfônico (ethephon- 100 e 200 mg.L-1) e cloreto de 2-cloroetil-trimetil amônio (CCC 1000 e 2000 mg.L-1). Os reguladores vegetais foram aplicados em duas épocas, aos quarenta e cem dias da implantação do experimento no campo e o crescimento das plantas foi avaliado em seis épocas. Após a primeira aplicação as plantas foram coletadas em intervalos de 14 dias. Os fitorreguladores GA3, e CCC tenderam a elevar os resultados das características, matéria seca de caule, folhas, flores e total, porém sempre permaneceram menores ou iguais ao controle.

Neo-clerodane diterpenoid, a new metalloprotease snake venom inhibitor from Baccharis trimera (Asteraceae): anti-proteolytic and anti-hemorrhagic properties

Many plants are used in traditional medicine as active agents against various effects induced by snakebite. Few attempts have been made however to identify the nature of plain natural products with anti-ophidian properties. Baccharis trimera (Less) DC (Asteraceae), known in Brazil as carqueja. has been popularly used to treat liver diseases. rheumatism. diabetes, as well as digestive, hepatic and renal disorders. The active component was identified as 7alpha-hydroxy-3,13-clerodadiene-16,15:18,19-diolide, C20H28O5, (clerodane diterpenoid, Bt-CD). We report now the anti-proteolytic and anti-hemorrhagic propenies against snake venoms of a Bt-CD inhibitor from B. trimera. Bt-CD exhibited full inhibition of hemorrhage and proteolytic activity caused by Bothrops snake venoms. The inhibitor was able to neutralize the hemorrhagic, fibrinogenolytic and caseinolytic activities of class P-I and III metalloproteases isolated from B. neuwiedi and B. jararacussu venoms. No inhibition of the coagulant activity was observed. Bt-CD also partially inhibited the edema induced by other crude venoms, metallopronteases, basic and acidic phospholipases A(2). To further elucidate the inhibitory specificity of Bt-CD against metalloproteases isolated from snake venoms, a deeper understanding of its Structure and function is necessary. Furthermore, the potential use of these inhibitors to complement anti-venom as an alternative treatment of snakebite envenomations needs to be evaluated in future Studies. (C) 2004 Elsevier B.V.. All rights reserved.

Application of low-pressure gas chromatography-ion-trap mass spectrometry to the analysis of the essential oil of Turnera diffusa (Ward.) Urb.

Turnera diffusa Willd. var. afrodisiaca (Ward) Urb. (syn. T. aphrodisiaca) belongs to the family of Turneraceae and is an aromatic plant growing wild in the subtropical regions of America and Africa. It is widely used in the traditional medicine as e.g. anti-cough, diuretic, and aphrodisiac agent. This work presents a 3 min chromatographic analysis using low-pressure (LP) gas chromatography (GC)-ion-trap (IT) mass spectrometry (MS). The combination of a deactivated 0.6 m x 0.10 mm i.d., restrictor with a wide-bore CP-Wax 52 capillary column (10 m x 0.53 mm i.d., 1 mum) reduces the analysis time by a factor of 3-7 in comparison to the use of a conventional narrow bore column. Chromatographic conditions have been optimized to achieve the fastest separation with the highest signal/noise ratio in MS detection. These results allow fast and reliable quality control of the essential oil to be achieved. (C) 2003 Elsevier B.V. All rights reserved.

First record of L-quebrachitol in Allophylus edulis (Sapindaceae)

Allophylus edulis, commonly called 'Chal chal', is a member of the Sapindaceae occurring in the Uruguayan and Brazilian native flora. During the phytochemical analysis of two Chal chal specimens from two welldifferentiated geographical zones (Assis, São Paulo, Brazil, and Santa Lucia, Canelones, Uruguay), considerable amounts of L-quebrachitol were isolated from both samples. The isolation was carried out from the ethanolic twig extracts obtained by maceration of both vegetal samples. White easily distinguishable crystals were mechanically separated, washed, and characterized by 1D and 2D NMR experiments and by MS data. Such techniques confirmed that the crystals isolated from sources collected in both countries resulted in the same compound, L-quebrachitol, a natural product not previously reported for this species and one that has been investigated as a sugar substitute for diabetics. Worthy of note, the content of L-quebrachitol in A. edulis may be the chemical basis to explain its ethnobotanical uses, since infusions of this plant are used to treat diabetes in the practice of local traditional medicine. (c) 2008 Elsevier Ltd. All rights reserved.

Atividade antimicrobiana de extratos brutos de Petiveria alliacea L.

"Antimicrobial activity of crude extratcs of Petiveria alliacea L.". Petiveria alliacea L. (Phytolaccacea) is an herbaceous plant of great importance in traditional medicine. This species have been widely used in several applications such as antirheumatic, anticarcinogenic, anti-flu, antitussive, analgesic, insecticidal, acaricidal, as well as bactericide and fungicide. Currently, the pathogenic microorganisms are acquiring resistence against the traditional antibiotics, and the search for new herbal antimicrobial agents has been intensified. The objective of this study was to evaluate the antifungal and antibacterial activity of several leaf crude extracts of P. alliacea against several strains of bacterias and yeasts namely Bacilus subtilis, Pseudomonas aeruginosa, Escherichia coli, Streptococcus mutans, Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Candida parapsilosis, Candida kefyr and Candida albicans, using microdilution method. Promising results were observed for the 70% v/v ethanolic extract which presented minimum inhibitory concentration (MIC) from 250 to 760 mu g/mL for yeast. For the bacteria strains tested the MIC ranged between 240 to 3960 mu g/mL, depending of the extractive solution tested.

Antioxidant Action of Mangrove Polyphenols against Gastric Damage Induced by Absolute Ethanol and Ischemia-Reperfusion in the Rat

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

Toxicologic evaluation of acute and subacute oral administration of Cucurbita maxima seed extracts to rats and swine

The extract prepared from dried seeds of Cucurbita maxima was administered to rats and pigs. Following a single dose or 4 weeks of daily oral administration, the extract produced no changes in serum glucose, urea, creatinine, total protein, uric acid, GOT, GPT, LDH or blood counts. Urine analysis (urea, uric acid, creatinine, total protein, Na and K), as well as histopathological investigation, showed no abnormalities. These results taken as a whole indicate that the seeds of C. maxima as used in Brazilian folk medicine are not toxic for rats and swine.