Abstract Phytochemical studies of Cespedesia spathulata (Ochnaceae) leaves using 1H, 13C NMR, and GC-MS have led to the isolation of some metabolites identified for the first time in these species such as cathechin, epicatechin, vitexin, orientin, 6’’-O-acetyl-vitexin, sitosterol, stigmasterol, phytol, 4,5-dihydrovomifoliol and a mixture of aliphatic methyl esters, together with ochnaflavone, which was previously isolated from this plant. The modulating activity of some fractions and compounds from Cespedesia spathulata towards tyrosinase enzyme was assayed by spectroscopic and theoretical means/experiments. The dichloromethane fraction (133 μg mL-1) and ochnaflavone (333 μM) inhibited tyrosinase activity by 20 % and 2.0 %, respectively, whereas the ethyl acetate fraction (666 μg mL-1) and ±catechins (catechin and epicatechin - 800 μM) activated it by 104 % and 384 %, respectively. Quantum chemical calculations suggested that catechin and epicatechin are better activators than L-DOPA by interacting with Cu (II) ions. Molecular docking results suggested that hydrogen bonding and hydrophobic interactions are the main binding forces between each tyrosinase activator and the amino acid residues inside the active protein binding pocket.

Abstract Leiomyomas are the most common benign tumors in women. Many of them are associated with significant morbidity. The present study aimed to analyze histomorphological and histochemical characteristics and immunoexpression of Cripto-1 in oral leiomyomas (OL), uterine leiomyomas (UL), and normal myometrium (NM). Sample was composed of ten OL, 11 UL and 11 NM. Histomorphological characteristics were analyzed at 100 and 400x magnifications with HE staining. The immunoexpression of Cripto-1 was analyzed in five high-power fields. Statistical analysis considered a significant difference when p<0.05. Six OL disclosed moderate/intense inflammatory infiltrate, while ten UL exhibited mild infiltrate (p=0.024). When analyzing all leiomyomas together, 20 exhibited hyalinization, whereas no NM exhibited this alteration (p<0.001). There was no statistical difference in the distribution of mast cells among the lesions. The median Cripto-1 was higher in UL (9.0), followed by OL and NM (4.0). Associations of the Cripto-1 expression between leiomyomas (separately and together) and NM were statistically significant (p<0.001). These results indicate that OL and UL exhibit similar histomorphological and histochemical characteristics, as well as differences to NM. The higher immunoexpression of Cripto-1 in leiomyomas compared to NM suggests that this protein may influence cell proliferation and tissue architecture of oral and uterine leiomyomas.

OBJECTIVE: We aimed to assess the effects of diazoxide on the mortality, pancreatic injury, and inflammatory response in an experimental model of acute pancreatitis. METHODS: Male Wistar rats (200-400 g) were divided randomly into two groups. Fifteen minutes before surgery, animals received physiological (0.9%) saline (3 mL/kg) (control group) or 45 mg/kg diazoxide (treatment group) via the intravenous route. Acute pancreatitis was induced by injection of 2.5% sodium taurocholate via the biliopancreatic duct. Mortality (n=38) was observed for 72 h and analyzed by the Mantel-Cox Log-rank test. To study pancreatic lesions and systemic inflammation, rats (10 from each group) were killed 3 h after acute pancreatitis induction; ascites volume was measured and blood as well as pancreases were collected. Pancreatic injury was assessed according to Schmidt’s scale. Cytokine expression in plasma was evaluated by the multiplex method. RESULTS: Mortality at 72 h was 33% in the control group and 60% in the treatment group (p=0.07). Ascites volumes and plasma levels of cytokines between groups were similar. No difference was observed in edema or infiltration of inflammatory cells in pancreatic tissues from either group. However, necrosis of acinar cells was lower in the treatment group compared to the control group (3.5 vs. 3.75, p=0.015). CONCLUSIONS: Treatment with diazoxide can reduce necrosis of acinar cells in an experimental model of acute pancreatitis, but does not affect the inflammatory response or mortality after 72 h.

Abstract The aim of the current study is to evaluate the effect of Acmella oleracea (L.) R.K. Jansen, Asteraceae, methanolic extract, hexane (84.28% spilanthol) and dichloromethane (approximately 100% spilanthol) fractions on the tyrosinase enzyme. The dehydrated jambu extract was obtained through maceration using methanol. The extract residue was solubilized in MeOH/H2O (8:2) and subjected to liq.–liq. partition in organic solvents. Both the extraction and the partition procedures were conducted with three replicates. The analyses were performed using GC–MS, 1H and 13C NMR. The hexane fraction provided samples containing 84.28, 82.91 and 62.83% spilanthol in repetitions 1, 2 and 3, respectively. The dichloromethane fraction showed 88.55% spilanthol in repetition 1, and approximately 100% spilanthol in repetitions 2 and 3. The jambu extract as well as the hexane fraction (84.28% spilanthol) were able to activate the oxidizing activity of the tyrosinase enzyme for L-DOPA. The dichloromethane fraction (approximately 100% spilanthol) showed stronger inhibition effect on the tyrosinase enzyme in the first 10 min. The results raise the interest in study in spilanthol formulations for topical use, since it may prevent and/or slow skin hyperpigmentation or depigmentation processes. Furthermore, spilanthol may be used to control the enzymatic browning in fruits and vegetables.

O principal objetivo do presente trabalho foi o estudo de bromofenóis (2bromofenol, 4bromofenol, 2,4dibromofenol,2,6dibromofenol and 2,4,6tribromofenol), no músculo e estômago de duas espécies de peixes da Familia Lutjanidae: Lutjanus synagris e Ocyurus chrysurus. Os bromofenóis foramextraídos através de destilação por arraste a vapor com pentanoéter (7:3 v/v), analisados por Cromatografia Líquida de AltaEficiência e quantificados por padronização externa. As concentrações totais de bromofenóis no músculo de ambas as espécies foram similares e estiveram na faixa de 36 ng g¹ a349 ng g¹. As concentrações totais de bromofenóis no estômago (na faixa de 12 ng g¹ a 586 ng g¹) foram mais altas queno músculo. A presença de bromofenóis no músculo das espécies estudadas pode ter origem na dieta. Os resultados destetrabalho contribuirão para o melhor entendimento das rotas deabsorção de bromofenóis nos peixes.

The main objective of this work is to evaluate the occurrence of bromophenols (2bromophenol, 4bromophenol, 2,4dibromophenol, 2,6dibromophenol and 2,4,6tribromophenol), in the flesh and guts in two species of the LutjanidaeFamily: Lutjanus synagris and Ocyurus chrysurus. The bromophenols were extracted by steam distillation with pentaneether (7:3 v/v), identified by reverse phase High Performance Liquid Chromatography (HPLCUV), and quantified bythe externalstandard method. Total bromophenol concentrations were similar in the muscle of both species, rangingfrom 36 ng g¹ to 349 ng g¹. The total bromophenol concentrations in stomach (ranging from 12 ng g¹ to 586 ng g¹)were slightly higher than in muscle. The presence of bromophenol in the muscles of the species under study may occuras a result of their diet. The results of this work are therefore expected to contribute toward a better understanding ofthe path of bromophenol absorption from the fish's stomach to the rest of its body.