Evaluation of the toxicity of Virola sebifera crude extracts, fractions and isolated compounds on the nest of leaf-cutting ants

The phytochemical study of Virola sebifera leaves led to the isolation of three lignans: (+)-sesamin, (-)-hinokinin, and (-)-kusunokinin and three flavonoids: quercetin-3-O - L-rhamnoside, quercetin-3-O - D-glucoside, and quercetin-3-methoxy-7-O - D-glucoside by using techniques as high-speed counter-current chromatography and high-performance liquid chromatography. The crude extracts, fractions, and isolated compounds were evaluated for their insecticidal and fungicidal potential against Atta sexdens rubropilosa and its symbiotic fungus Leucoagaricus gongylophorus. The bioassay results showed a high insecticidal activity for the methanol crude extract of the leaves of V. sebifera and its n-hexane, dichloromethane and ethyl acetate fractions. The fungicidal bioassay revealed high toxicity of the lignans against L. gongylophorus. © 2012 Keylla Utherdyany Bicalho et al.

High Content Screening of a Kinase-Focused Library Reveals Compounds Broadly-Active against Dengue Viruses

Dengue virus is a mosquito-borne flavivirus that has a large impact in global health. It is considered as one of the medically important arboviruses, and developing a preventive or therapeutic solution remains a top priority in the medical and scientific community. Drug discovery programs for potential dengue antivirals have increased dramatically over the last decade, largely in part to the introduction of high-throughput assays. In this study, we have developed an image-based dengue high-throughput/high-content assay (HT/HCA) using an innovative computer vision approach to screen a kinase-focused library for anti-dengue compounds. Using this dengue HT/HCA, we identified a group of compounds with a 4-(1-aminoethyl)-N-methylthiazol-2-amine as a common core structure that inhibits dengue viral infection in a human liver-derived cell line (Huh-7.5 cells). Compounds CND1201, CND1203 and CND1243 exhibited strong antiviral activities against all four dengue serotypes. Plaque reduction and time-of-addition assays suggests that these compounds interfere with the late stage of viral infection cycle. These findings demonstrate that our image-based dengue HT/HCA is a reliable tool that can be used to screen various chemical libraries for potential dengue antiviral candidates. © 2013 Cruz et al.

Synthesis, characterization and thermal behavior of solid state compounds of heavy trivalent lanthanide succinates

Solid-state Ln-L compounds, where Ln stands for heavy trivalent lanthanides or yttrium(III) (Tb-Lu, Y) and L is succinate, have been synthesized. Simultaneous thermogravimetry and differential thermal analysis (TG-DTA), differential scanning calorimetry (DSC), infrared spectroscopy, TG-DTA coupled to FTIR, elemental analysis, X-ray powder diffractometry and complexometry were used to characterize and study the thermal behavior of these compounds. For the terbium to thulium and yttrium compounds, the dehydration, as well the thermal decomposition of the anhydrous compound occurs in two consecutive steps, while ytterbium and lutetium the dehydration occurs in a single step. The results also led to information about the ligand's denticity, thermal stability and thermal decomposition of these compounds. © 2013 Elsevier B.V.

Thermal behaviour of α-hydroxyisobutyric acid, sodium α-hydroxyisobutyrate and its compounds with some bivalent transition metal ions

Synthesis, characterization and thermal decomposition of bivalent transition metal α-hydroxyisobutyrates, M(C4H7O 3)2·nH2O (M = Mn(II), Fe(II), Co(II), Ni(II), Cu(II), Zn(II)), as well as the thermal behaviour of α-hydroxyisobutyric acid and its sodium salt were investigated employing simultaneous thermogravimetry and differential scanning calorimetry (TG-DSC), infrared spectroscopy (FTIR), TG-DSC coupled to FTIR, elemental analysis and complexometry. All the compounds were obtained as dihydrated, except the copper one which was obtained in the anhydrous state. The thermal decomposition of the anhydrous compounds occurs in a single or two steps and the final residue up to 235 C (Mn), 300 C (Fe), 305 C (Co), 490 C (Ni), 260 C (Cu) and 430 C (Zn) is Mn2O3, Fe2O3, Co3O 4, NiO, CuO and ZnO, respectively. The results also provided information concerning the ligand's denticity and identification of the gaseous products evolved during the thermal decomposition of these compounds. Copyright © 2013 Published by Elsevier B.V. All rights reserved.

Synthesis, characterization and thermal behaviour of solid-state compounds of folates with some bivalent transition metals ions

Solid-state M-L compounds, where M stands for bivalent Mn, Co, Ni, Cu and Zn and L is folate (C19H17N7O6), have been synthesized. Simultaneous thermogravimetry and differential scanning calorimetry (TG-DSC), X-ray powder diffractometry, infrared spectroscopy (FTIR), TG-DSC coupled to FTIR, elemental analysis and high-resolution continuum source flame atomic absorption spectrometry technique (HR-CS FAAS) were used to characterize and to study the thermal behaviour of these compounds. The results provided information concerning the composition, dehydration, thermal stability and thermal decomposition. © 2013 Akadémiai Kiadó, Budapest, Hungary.

Fatty acids and some antioxidant compounds of Psidium guajava seed oil

Physico-chemical characteristics, fatty acid and tocopherol compositions, total phenolic content and antioxidant activity of crude oil extracted from guava (Psidium guajava var. pomifera) seeds were investigated. Oil yield from the seeds was 14.0%. Data obtained for the analytical indexes compared well with those of others edible oils. The oil showed high levels of unsaturated fatty acids (88.1%), mainly linoleic acid (78.4%). The tocopherol and total phenolic contents in the oil amounted to 29.2 and 92.3 mg/100 g, respectively. The guava seed oil exhibited a great DPPH · scavenging activity showing EC₅₀ of 12.9 g oil/g [DPPH · ] -1 and antiradical efficiency of 7.9×10 -2 . Therefore, the potential utilization of the guava seed oil as a raw material of food, chemical and pharmaceutical industries appears to be favourable and provides the use of a renewable resource, adding value to agricultural products.

Bioactive compounds present in the Mediterranean sofrito

Sofrito is a key component of the Mediterranean diet, a diet that is strongly associated with a reduced risk of cardiovascular events. In this study, different Mediterranean sofritos were analysed for their content of polyphenols and carotenoids after a suitable work-up extraction procedure using liquid chromatography/electrospray ionisation-linear ion trap quadrupole-Orbitrap-mass spectrometry (LC/ESI-LTQ-Orbitrap- MS) and liquid chromatography/electrospray ionisation tandem triple quadrupole mass spectrometry (LC/ESI-MS-MS). In this way, 40 polyphenols (simple phenolic and hydroxycinnamoylquinic acids, and flavone, flavonol and dihydrochalcone derivatives) were identified with very good mass accuracy (<2 mDa), and confirmed by accurate mass measurements in MS and MS2 modes. The high-resolution MS analyses revealed the presence of polyphenols never previously reported in Mediterranean sofrito. The quantification levels of phenolic and carotenoid compounds led to the distinction of features among different Mediterranean sofritos according to the type of vegetables (garlic and onions) or olive oil added for their production. © 2013 Elsevier Ltd. All rights reserved.

Extrusion of flavored corn grits: Structural characteristics, volatile compounds retention and sensory acceptability

The effects of the moisture content of the raw material, extrusion temperature and screw speed on flavor retention, sensory acceptability and structure of corn grits extrudates flavored with isovaleraldehyde, ethyl butyrate and butyric acid were investigated. Higher temperature resulted in more expanded extrudates with lower density and cutting force, while higher moisture content increased ethyl butyrate retention. The most acceptable extrudates were those obtained with low moisture content, under conditions of high extrusion temperature and high screw speed, or low screw speed and low extrusion temperature, whereas the aroma intensity closest to the ideal was observed under conditions of low extrusion temperature and low moisture content of the raw material. © 2013 Elsevier Ltd.

Cytotoxic study of organometallic compounds of palladium (II) in mice peritoneal macrophages

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Compounds used to produce cloned animals are genotoxic and mutagenic in mammalian assays in vitro and in vivo

The compounds 6-dimethylaminopurine and cycloheximide promote the successful production of cloned mammals and have been used in the development of embryos produced by somatic cell nuclear transfer. This study investigated the effects of 6-dimethylaminopurine and cycloheximide in vitro, using the thiazolyl blue tetrazolium bromide colorimetric assay to assess cytotoxicity, the trypan blue exclusion assay to assess cell viability, the comet assay to assess genotoxicity, and the micronucleus test with cytokinesis block to test mutagenicity. In addition, the comet assay and the micronucleus test were also performed on peripheral blood cells of 54 male Swiss mice, 35 g each, to assess the effects of the compounds in vivo. The results indicated that both 6-dimethylaminopurine and cycloheximide, at the concentrations and doses tested, were cytotoxic in vitro and genotoxic and mutagenic in vitro and in vivo, altered the nuclear division index in vitro, but did not diminish cell viability in vitro. Considering that alterations in DNA play important roles in mutagenesis, carcinogenesis, and morphofunctional teratogenesis and reduce embryonic viability, this study indicated that 6-dimethylaminopurine and cycloheximide utilized in the process of mammalian cloning may be responsible for the low embryo viability commonly seen in nuclear transfer after implantation in utero.

Diurnal and nocturnal measurements of PAH, nitro-PAH, and oxy-PAH compounds in atmospheric particulate matter of a sugar cane burning region

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

Thermal behaviour of nicotinic acid, sodium nicotinate and its compounds with some bivalent transition metal ions

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

Electrochemical Determination of Organic Compounds in Automotive Fuels

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Antifungal activity of flavonoids from Heteropterys byrsonimifolia and a commercial source against Aspergillus ochraceus: In silico interactions of these compounds with a protein kinase

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Identification of Novel Compounds Inhibiting Chikungunya Virus-Induced Cell Death by High Throughput Screening of a Kinase Inhibitor Library

Chikungunya virus (CHIKV) is a mosquito-borne arthrogenic alphavirus that causes acute febrile illness in humans accompanied by joint pains and in many cases, persistent arthralgia lasting weeks to years. The re-emergence of CHIKV has resulted in numerous outbreaks in the eastern hemisphere, and threatens to expand in the foreseeable future. Unfortunately, no effective treatment is currently available. The present study reports the use of resazurin in a cell-based high-throughput assay, and an image-based high-content assay to identify and characterize inhibitors of CHIKV-infection in vitro. CHIKV is a highly cytopathic virus that rapidly kills infected cells. Thus, cell viability of HuH-7 cells infected with CHIKV in the presence of compounds was determined by measuring metabolic reduction of resazurin to identify inhibitors of CHIKV-associated cell death. A kinase inhibitor library of 4,000 compounds was screened against CHIKV infection of HuH-7 cells using the resazurin reduction assay, and the cell toxicity was also measured in non-infected cells. Seventy-two compounds showing >= 50% inhibition property against CHIKV at 10 mu M were selected as primary hits. Four compounds having a benzofuran core scaffold (CND0335, CND0364, CND0366 and CND0415), one pyrrolopyridine (CND0545) and one thiazol-carboxamide (CND3514) inhibited CHIKV-associated cell death in a dose-dependent manner, with EC50 values between 2.2 mu M and 7.1 mu M. Based on image analysis, these 6 hit compounds did not inhibit CHIKV replication in the host cell. However, CHIKV-infected cells manifested less prominent apoptotic blebs typical of CHIKV cytopathic effect compared with the control infection. Moreover, treatment with these compounds reduced viral titers in the medium of CHIKV-infected cells by up to 100-fold. In conclusion, this cell-based high-throughput screening assay using resazurin, combined with the image-based high content assay approach identified compounds against CHIKV having a novel antiviral activity -inhibition of virus-induced CPE - likely by targeting kinases involved in apoptosis.