Quick preparative separation of natural naphthopyranones with antioxidant activity by high-speed counter-current chromatography

The natural naphthopyranones paepalantine (1), paepalantine-9O-β-D-glucopyranoside (2) and paepalantine-9-O-β-D-allopyranosyl-(1→6)-O-β-D-glucopyranoside (3) were separated in a preparative scale from the ethanolic extract of the capitula of Paepalanthus bromelioides by high-speed counter-current chromatography (HSCCC). The solvent system used was composed of water-ethanol-ethyl acetate-hexane (10:4:10:4, v/v/v/v). This technique led to the separation of the three different naphthopyranone glycosides in pure form in approximately 7 hours. Paepalantine showed a good antioxidant activity when assayed by the DPPH radical spectrophotometric assay.

Análise conformacional dos petídeos protonectina e protonectina (1-6), isolados e em associação, em mistura TFE-água

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Cristalização e resolução de estrutura das proteínas Canavalia gladiata lectin (CGL) e Canavalia marítima lectin (CML) complexadas ao açúcar manose 1-6 manose

Pós-graduação em Biofísica Molecular - IBILCE

Intoxicação experimental de cães com folhas verdes de Nerium oleander e uso da frutose 1,6 difosfato e da glicose como tratamentos

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Acaricidal effects of fluazuron (2.5 mg/kg) and a combination of fluazuron (1.6 mg/kg) + ivermectin (0.63 mg/kg), administered at different routes, against Rhipicephalus (Boophilus) microplus parasitizing cattle

The present study aimed to evaluate the acaricidal efficacy of fluazuron (2.5 mg/kg), administered as a pour-on, in comparison to an injectable formulation containing fluazuron (1.6 mg/kg) + ivermectin (0.63 mg/kg), against Rhipicephalus (Boophilus) microplus in naturally and experimentally infested cattle. Two studies were conducted with different tick strains, one with artificial infestations (Stall Test, using leight animals per group) and one with natural infestations (utilizing ten animals per group): In both studies, the animals were randomized, according to average tick counts performed on days -3, -2 and -1, into four groups: T01, negative control (saline solution); T02, pour-on fluazuron (2.5 mg/kg); T03: subcutaneous fluazuron (1.6 mg/kg) + ivermectin (0.63 mg/kg); and T04 subcutaneous ivermectin (0.63 mg/kg). Based on obtained results, and considering the utilized tick strains, it was possible to conclude that the pour-on fluazuron (2.5 mg/kg) formulation demonstrated high acaricidal efficacy, with protection periods ranging from 49 to 77 days against Rhipicephalus (Boophilus) microplus. On the other hand, for the injectable fluazuron (1.6 mg/kg) + ivermectin (0.63 mg/kg) formulation, it was not possible to observe elevated anti-R. (B.) microplus effect on both artificial and experimental infestation studies. Results observed for this combination were similar or inferior to those obtained by subcutaneous ivermectin (0.63 mg/kg). Future studies with this formulation containing fluazuron (1.6 mg/kg) + ivermectin (0.63 mg/kg), regarding pharmacokinetic and/or bioavailability profiles, or even studies analyzing both this active principles separately, are needed, seeking to better understand the effects of such combination against Rhipicephalus (Boophilus) microplus parasitizing cattle. (C) 2015 Elsevier Inc. All rights reserved.

In vitro effect of caffeic acid phenethyl ester on matrix metalloproteinases (MMP-1 and MMP-9) and their inhibitor (TIMP-1) in lipopolysaccharide-activated human monocytes

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

(1→6)- and (1→3)(1→6)-β-glucans from Lasiodiplodia theobromae MMBJ: structural characterization and pro-inflammatory activity

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

2,3-Divinyl- und 2-Aryl-3-vinylindole als Bausteine zu Carbazolen und Versuche zur photochemischen und Ultraschall-induzierten 1,6-Elektrocyclisierung

Es wurden neue funktionalisierte Carbazole und anellierte Benzo[a]carbazole als potentielle pharmakologische Therapeutika durch 1,6-pi-Elektrocyclisierung auf photo-chemischem, thermischem und sonochemischem Weg synthetisiert und die Synthesemethoden der 1,6-pi-Elektrocyclisierung sowie der 2,3-Divinylindole und der 2-Aryl-3-vinylindole als entsprechende Ausgangsprodukte validiert und evaluiert. Es gelang weder das nach den Woodward-Hoffmann-Regeln erwartete primäre Cyclisierungsprodukt mit Indolochinodimethanstruktur noch die Existenz des in einer photochemischen Abfangreaktion daraus resultierenden Cycloprodukts NMR-spektroskopisch nachzuweisen, um den stereochemischen Verlauf der Cyclisierung vorherzusagen. Ergebnisse der quantenchemischen Berechnungen der Eduktmoleküle (AO-Koeffizienten der MO's, HOMO/LUMO-Energien) sowie der Übergangszustandsgeometrien der Cyclisierungen decken sich mit den experimentellen Daten. Divinyl- und 2-Aryl-3-vinylindole sind als Systeme mit Hexatriensymmetrie aufzufassen, deren Cyclisierungsverhalten sich mit den Woodward-Hoffmann-Regeln beschreiben läßt. Im Vergleich der verschiedenen 1,6-pi-Elektrocyclisierungsmethoden zeigte sich, daß die photochemische Variante eine elegante Synthesemethode darstellt, um funktionalisierte Carbazole und Benzo[a]carbazole mit unterschiedlichen pharmakologischen Aktivitäten unter schonenden Reaktionsbedingungen mit den vergleichbar höchsten Ausbeuten zu erhalten. Demgegenüber lieferten die Ultraschallreaktionen keine nachweisbaren Cyclisierungsprodukte. Die thermische Cyclisierung führte zur Gruppe der 1,2-Dihydrocarbazole. Sie bildeten sich in einer Folgereaktion durch [1,5s]-H-Verschiebung aus dem primär entstandenen Woodward-Hoffmann-Cyclisierungsprodukt. In abschließenden DNA-Bindestudien mit verschiedenen Testsystemen zeigte keine der synthetisierten Testsubstanzen DNA-Bindungsaktivität.

Studio ed ottimizzazione di un turbocompressore per un motore avio V6 da 1.6 l

In questo elaborato vengono studiati e dimensionati due elementi fondamentali di un compressore: la girante e il diffusore.

Synthesis of 1,1'-(Hexane-1,6-Diyl)Bis(5-Oxopyrrolidine-3-Carboxylic Acid) as a Monomer for a Polyanhydride Drug Delivery System

Polyanhydrides have been given much attention in the literature recently because of their desirable properties as controlled drug delivery solutions. Drug therapies could be loaded into a polyanhydride matrix and protected from denaturation and removal from the body while being slowly eluted as the polyanhydride degraded yielding a tailorable concentration profile in the bloodstream at therapeutic levels. To that end, this report discusses the synthesis of a novel monomer for polyanhydride synthesis: 1,1'-(hexane-1,6-diyl)bis(5-oxopyrrolidine-3-carboxylic acid) henceforth known as CPyH monomer for (carboxypyrrolidone)hexane monomer.