Phenolic derivatives from Baccharis retusa DC. (Asteraceae)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Universidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 São Paulo, BrazilUniv Presbiteriana Mackenzie, Ctr Ciencias & Humanidades, BR-01302907 São Paulo, BrazilUniv Presbiteriana Mackenzie, Ctr Ciencias Biol & Saude, BR-01302907 São Paulo, BrazilUniversidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 São Paulo, BrazilWeb of Scienc

In vitro antileishmanial and antitrypanosomal activities of flavanones from Baccharis retusa DC. (Asteraceae)

Leishmaniasis and Chagas' are parasitic protozoan diseases that affect the poorest population in the world, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, novel, safe and more efficacious drugs are essential. in this work, the CH2Cl2 phase from MeOH extract from the leaves of Baccharis retusa DC. (Asteraceae) was fractioned to afford two flavonoids: naringenin (1) and sakuranetin (2). These compounds were in vitro tested against Leishmania spp. promastigotes and amastigotes and Ttypanosoma cruzi trypomastigotes and amastigotes. Compound 2 presented activity against Leishmania (L) amazonensis, Leishmania (V.) braziliensis, Leishmania (L) major, and Leishmania (L) chagasi with IC50 values in the range between 43 and 52 mu g/mL and against T. cruzi trypomastigotes (IC50= 20.17 mu g/mL). Despite of the chemical similarity, compound 1 did not show antiparasitic activity. Additionally, compound 2 was subjected to a methylation procedure to give sakuranetin-4'-methyl ether (3), which resulted in an inactive compound against both Leishmania spp. and T. cnizi. the obtained results indicated that the presence of one hydroxyl group at C-4' associated to one methoxyl group at C-7 is important to the antiparasitic activity. Further drug design studies aiming derivatives could be a promising tool for the development of new therapeutic agents for Leishmaniasis and Chagas' disease. (C) 2011 Elsevier Inc. All rights reserved.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Pesquisa e DesenvolvimentoUniversidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Diadema, SP, BrazilInst Adolfo Lutz Registro, Dept Parasitol, São Paulo, BrazilUniv Fed ABC, Ctr Ciencias Nat & Humanas, Santo Andre, SP, BrazilUniv Presbiteriana Mackenzie, Ctr Ciencias & Humanidades, São Paulo, BrazilUniversidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Diadema, SP, BrazilFAPESP: 06/57626-5FAPESP: 08/11496-9Conselho Nacional de Pesquisa e Desenvolvimento: 473405/2008-3Conselho Nacional de Pesquisa e Desenvolvimento: 477422/2009-8Web of Scienc

Combined treatment with caffeic and ferulic acid from Baccharis uncinella C. DC. (Asteraceae) protects against metabolic syndrome in mice

Fractionation of the EtOH extract from aerial parts of Baccharis uncinella C. DC. (Asteraceae) led to isolation of caffeic and ferulic acids, which were identified from spectroscopic and spectrometric evidence. These compounds exhibit antioxidant and anti-inflammatory properties and have been shown to be effective in the prevention/treatment of metabolic syndrome. This study investigated whether the combined treatment of caffeic and ferulic acids exhibits a more significant beneficial effect in a mouse model with metabolic syndrome. The combination treatment with caffeic and ferulic acids was tested for 60 days in C57 mice kept on a high-fat (40%) diet. The data obtained indicated that treatment with caffeic and ferulic acids prevented gain in body weight induced by the high-fat diet and improved hyperglycemia, hypercholesterolemia and hypertriglyceridemia. The expression of a number of metabolically relevant genes was affected in the liver of these animals, showing that caffeic and ferulic acid treatment results in increased cholesterol uptake and reduced hepatic triglyceride synthesis in the liver, which is a likely explanation for the prevention of hepatic steatosis. In conclusion, the combined treatment of caffeic and ferulic acids displayed major positive effects towards prevention of multiple aspects of the metabolic syndrome and liver steatosis in an obese mouse model.CAPESFAPESPMackPesquisaUniv Presbiteriana Mackenzie, Programa Posgrad Disturbios Desenvolvimento, Ctr Ciencias Biol & Saude, Sao Paulo, SP, BrazilUniv Fed Sao Paulo, Dept Med Translac, Escola Paulista Med, Sao Paulo, SP, BrazilUniv Fed ABC, Ctr Ciencias Nat & Humanas, Sao Paulo, SP, BrazilEscola Ciencias Med, Dept Ciencias Patol, Sao Paulo, SP, BrazilUniv Presbiteriana Mackenzie, Escola Engn, Sao Paulo, SP, BrazilUniv Fed Sao Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Sao Paulo, SP, BrazilRush Univ & Med Ctr, Dept Internal Med, Div Endocrinol & Metab, Chicago, IL 60612 USAUniv Fed Sao Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Sao Paulo, SP, BrazilFAPESP: 2011/21847-6Web of Scienc

Serge Romoff - temoin inconnu

En mai 1921 et à Paris depuis une quinzaine d’années, Serge Romoff est appelé comme témoin au procès fictif de Maurice Barrès monté par les Dadaïstes et les Surréalistes. Bien qu’il soit presque certain qu’il connaissait plusieurs membres des deux groupes, il n’y a aucune trace de sa participation au cours des années précédentes ni à leurs activités ni à leurs publications. Qui donc était Serge Romoff?? La documentation manque, mais il semble qu’à partir de 1920 il joue un rôle de plus en plus important dans le monde culturel et surtout dans celui des artistes émigrés russes dans le quartier de Montparnasse. Il travaille dans l’imprimerie, fait quelques traductions, collabore à plusieurs revues culturelles, organise des expositions et écrit des articles de presse, notamment pour L’Humanité. En 1928 il retourne à Moscou où il continue à faire des conférences, probablement sur la littérature française et l’art. Il est mort en février 1939, une des victimes peut-être des purges staliniennes

Tris(3,7-dihydroxyflavonolate-κO3,O4)chromium(III) Complex

The complex [Cr(3,7diHF)3]·3H2O (3,7diHF is the monoanion of flavonoid 3,7-dihydroxyflavone) was synthetized and characterized by mass spectrometry, thermogravimetry, UV-Vis and FTIR spectroscopies. The data indicated that the coordination of the chromium(III) ion to the flavonoid increased its thermal stability

Antinociceptive and anti-inflammatory effects of Lantana camara L. extract in mice

ABSTRACT:he Lantana camara L. belongs to the family Verbenaceae, which contains several active compounds in leaves and roots and which are reported to have medicinal and insecticidal properties. Studies of plants within the same family show the existence of anti-inflammatory activity in paw edema induced by carrageenan, serotonin and histamine and analgesic activity in the acetic acid writhing and tail-flick tests. The present study investigated whether the L. camara extract (ACE) also exerts these effects. The ACE toxicity was studied in male mice, and the percentage of mortality recorded 7 days after treatment was assessed. The ACE was evaluated as an antinociceptive agent in the hot plate, tail-flick and acetic acid writhing tests at a nontoxic dose of 1.0 g/Kg. The results showed that 1.5 g/Kg of ACE was not able to cause death, and doses of 3.0 and 4.0 g/Kg caused 50% and 60% death, respectively, in male mice. In all of the antinociceptive tests, 1 g/Kg of ACE markedly reduced responses to pain. Our findings suggest that ACE may have active anti-inflammatory and antinociceptive properties in much smaller doses than toxic

A Trinuclear Oxo-Chromium(III) Complex Containing the Natural Flavonoid Primuletin: Synthesis, Characterization, and Antiradical Properties

A new trinuclear oxo-centered chromium(III) complex with formula [Cr3O(CH3CO2)6(L)(H2O)2] (L = 5-hydroxyflavone, known as primuletin) was synthetized and characterized by ESI mass spectrometry, thermogravimetry, and 1H-NMR, UV-Vis, and FTIR spectroscopies. In agreement with the experimental results, DFT calculations indicated that the flavonoid ligand is coordinated to one of the three Cr(III) centers in an O,O-bidentate mode through the 5-hydroxy/4-keto groups. In a comparative study involving the uncoordinated primuletin and its corresponding complex, systematic reactions with the free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) showed that antiradical activity increases upon complexation

An Evaluation Of 3-rhamnosylquercetin, A Glycosylated Form Of Quercetin, Against The Myotoxic And Edematogenic Effects Of Spla 2 From Crotalus Durissus Terrificus

This paper shows the results of quercitrin effects on the structure and biological activity of secretory phospholipase (sPLA2) from Crotalus durissus terrificus, which is the main toxin involved in the pharmacological effects of this snake venom. According to our mass spectrometry and circular dichroism results, quercetin was able to promote a chemical modification of some amino acid residues and modify the secondary structure of C. d. terrificus sPLA2. Moreover, molecular docking studies showed that quercitrin can establish chemical interactions with some of the crucial amino acid residues involved in the enzymatic activity of the sPLA2, indicating that this flavonoid could also physically impair substrate molecule access to the catalytic site of the toxin. Additionally, in vitro and in vivo assays showed that the quercitrin strongly diminished the catalytic activity of the protein, altered its Vmax and Km values, and presented a more potent inhibition of essential pharmacological activities in the C. d. terrificus sPLA2, such as its myotoxicity and edematogenic effect, in comparison to quercetin. Thus, we concluded that the rhamnose group found in quercitrin is most likely essential to the antivenom activities of this flavonoid against C. d. terrificus sPLA2. © 2014 Daniela de Oliveira Toyama et al