ABSTRACT We present a linear-time algorithm that computes in a given real interval the number of eigenvalues of any symmetric matrix whose underlying graph is unicyclic. The algorithm can be applied to vertexand/or edge-weighted or unweighted unicyclic graphs. We apply the algorithm to obtain some general results on the spectrum of a generalized sun graph for certain matrix representations which include the Laplacian, normalized Laplacian and signless Laplacian matrices.

Abstract The present work aims to study the photocatalytic degradation of three organophosphate esters considered environmental emerging contaminants by the UV/H2O2 system with the use of 31P NMR spectroscopy to investigative their removal after the treatment. Results demonstrated the efficiency of the oxidation system in removing the esters tris(2-butoxyethyl) phosphate (TBEP), tris(2-chloroethyl) phosphate (TCEP) and tri-butyl phosphate (TBP) from aqueous solutions when they were individually present and mixed. High levels of degradation of these chemicals were achieved, in addition to the good performance of the analytical technique applied in the study, which represents some advantages in comparison with other techniques reported in the literature. An increase in the 31P NMR signal removal could also be observed when the oxidizing agent concentration increases. Decreases in solution acute toxicity were also verified for both TBP and TBEP treated samples when compared with the samples before the treatment.

RESUMO Sementes de Acacia farnesiana são comumente vendidas em feiras locais no nordeste do Brasil como agente terapêutico. O presente trabalho objetivou avaliar as atividades antiinflamatória e antinociceptiva de proteínas obtidas de sementes de A. farnesiana. Cinco frações protéicas distintas (albuminas, globulinas, prolaminas, glutelinas ácidas e básicas) foram obtidas e investigadas quanto o perfil de proteínas, presença de atividade hemaglutinante e proteolítica. A fração globulina (GLB) também foi avaliada quanto a presença de atividade antiinflamatória e analgésica. Globulinas reduziram o edema de pata induzido por carragenina de modo dependente da dose que foi acompanhada da redução da atividade da mieloperoxidase (p < 0,05). Em adição, GLB reduziu a migração de neutrófilos para cavidade peritoneal induzida por carragenina. Entretanto, GLB não foi capaz de inibir o edema induzido por dextrana. O pré-tratamento com globulinas reduziu as contorções abdominais induzidas por ácido acético, bem como o tempo de lambedura da pata induzida por formalina (69.1% na primeira fase). Por outro lado, GLB não produziu um efeito antinociceptivo significante no teste de placa quente (55-56 °C). O pré-tratamento de GLB com calor (100 °C por 30 min) aboliu sua atividade anti-edematogênica e hemaglutinante. Nossos resultados mostraram que sementes de A. farnesiana são fonte de proteínas com propriedades antiinflamatórias e analgésicas.

ABSTRACT Seeds of Acacia farnesiana are commonly sold in the local markets of northeastern Brazil as a therapeutic agent. The present work aimed to evaluate the anti-inflammatory and analgesic activities of proteins obtained from A. farnesiana seeds. Five different protein fractions (albumin, globulin, prolamin, acidic and basic glutelins) were obtained and investigated for the protein pattern, the presence of hemagglutinating and proteolytic activities. The globulin fraction (GLB) was also evaluated for anti-inflammatory and analgesic activities. Globulins reduced the paw edema induced by carrageenan in a dose-dependent manner, which was accompanied by a reduction of myeloperoxidase activity (p < 0.05). Additionally, GLB reduced the neutrophil peritoneal migration induced by carrageenan. However, GLB was not able to inhibit the edema triggered by dextran. Pre-treatment with globulins reduced the abdominal constrictions induced by acetic acid as well as the paw licking time induced by formalin (69.1% at first phase). However, it did not produce a significant antinociceptive effect in the hot plate test (55-56 °C). Treating the GLB with heat (at 100 °C for 30 min) abolished its anti-edematogenic and hemagglutinating activities. Our results showed that seeds from A. farnesiana are a source of proteins with anti-inflammatory and analgesic properties.

This study aimed to estimate the absorption, distribution, metabolism and excretion (ADME) properties and safety of LDT5, a lead compound for oral treatment of benign prostatic hyperplasia that has previously been characterized as a multi-target antagonist of α1A-, α1D-adrenoceptors and 5-HT1A receptors. The preclinical characterization of this compound comprised the evaluation of its in vitro properties, including plasma, microsomal and hepatocytes stability, cytochrome P450 metabolism and inhibition, plasma protein binding, and permeability using MDCK-MDR1 cells. De-risking and preliminary safety pharmacology assays were performed through screening of 44 off-target receptors and in vivo tests in mice (rota-rod and single dose toxicity). LDT5 is stable in rat and human plasma, human liver microsomes and hepatocytes, but unstable in rat liver microsomes and hepatocytes (half-life of 11 min). LDT5 is highly permeable across the MDCK-MDR1 monolayer (Papp ∼32×10-6 cm/s), indicating good intestinal absorption and putative brain penetration. LDT5 is not extensively protein-bound and is a substrate of human CYP2D6 and CYP2C19 but not of CYP3A4 (half-life >60 min), and did not significantly influence the activities of any of the human cytochrome P450 isoforms screened. LDT5 was considered safe albeit new studies are necessary to rule out putative central adverse effects through D2, 5-HT1A and 5-HT2B receptors, after chronic use. This work highlights the drug-likeness properties of LDT5 and supports its further preclinical development.

Our objective was to investigate the protective effect of Lawesson's reagent, an H2S donor, against alendronate (ALD)-induced gastric damage in rats. Rats were pretreated with saline or Lawesson's reagent (3, 9, or 27 µmol/kg, po) once daily for 4 days. After 30 min, gastric damage was induced by ALD (30 mg/kg) administration by gavage. On the last day of treatment, the animals were killed 4 h after ALD administration. Gastric lesions were measured using a computer planimetry program, and gastric corpus pieces were assayed for malondialdehyde (MDA), glutathione (GSH), proinflammatory cytokines [tumor necrosis factor (TNF)-α and interleukin (IL)-1β], and myeloperoxidase (MPO). Other groups were pretreated with glibenclamide (5 mg/kg, ip) or with glibenclamide (5 mg/kg, ip)+diazoxide (3 mg/kg,ip). After 1 h, 27 µmol/kg Lawesson's reagent was administered. After 30 min, 30 mg/kg ALD was administered. ALD caused gastric damage (63.35±9.8 mm2); increased levels of TNF-α, IL-1β, and MDA (2311±302.3 pg/mL, 901.9±106.2 pg/mL, 121.1±4.3 nmol/g, respectively); increased MPO activity (26.1±3.8 U/mg); and reduced GSH levels (180.3±21.9 µg/g). ALD also increased cystathionine-γ-lyase immunoreactivity in the gastric mucosa. Pretreatment with Lawesson's reagent (27 µmol/kg) attenuated ALD-mediated gastric damage (15.77±5.3 mm2); reduced TNF-α, IL-1β, and MDA formation (1502±150.2 pg/mL, 632.3±43.4 pg/mL, 78.4±7.6 nmol/g, respectively); lowered MPO activity (11.7±2.8 U/mg); and increased the level of GSH in the gastric tissue (397.9±40.2 µg/g). Glibenclamide alone reversed the gastric protective effect of Lawesson's reagent. However, glibenclamide plus diazoxide did not alter the effects of Lawesson's reagent. Our results suggest that Lawesson's reagent plays a protective role against ALD-induced gastric damage through mechanisms that depend at least in part on activation of ATP-sensitive potassium (KATP) channels.

A densidade de parasitoides por hospedeiro influencia nas suas principais características biológicas. Assim, o objetivo desse trabalho foi avaliar o desenvolvimento do parasitoide Palmistichus elaeisis Delvare & LaSalle, 1993 (Hymenoptera: Eulophidae) em pupas de Anticarsia gemmatalis Hübner, 1818 (Lepidoptera: Noctuidae) expostas nas densidades de 1:1, 2:1, 4:1, 6:1, 8:1, 10:1 ou 12:1 parasitoides/hospedeiro, respectivamente. Os parasitoides permaneceram em contato com as pupas por 24 horas em tubos de vidro (14,0 x 2,2 cm), acondicionadas em câmara climatizada a 25 ± 1º C, 70 ± 10% de UR e fotofase de 14 horas. Observou-se 54,54 e 90,90% de pupas parasitadas nas densidades de 1:1 e 2:1, respectivamente, e 100,00% nas demais densidades com melhor índice de emergência (72,72%) na densidade 6:1. A duração do ciclo de vida (ovo-adulto) decresceu com o aumento da densidade de fêmeas e variou de 20 a 22 dias. A progênie variou de 16 a 225 descendentes por pupa, com melhor resultado na densidade 8:1. A razão sexual do parasitoide variou de 0,95 ± 0,00 a 0,97 ± 0,01, sem diferença significativa e o comprimento do corpo de fêmeas e de machos variou de 1,95 ± 0,02 a 2,22 ± 0,03 mm e de 1,49 ± 0,02 a 1,87 ± 0,01 mm, respectivamente. Seis a oito fêmeas de P. elaeisis por pupa de A. gemmatalis proporcionam maior emergência e progênie do parasitoide, viabilizando sua criação massal.

The density of parasitoids per host affects their biological characteristics. The present study aimed to evaluate the development of Palmistichus elaeisis Delvare & LaSalle, 1993 (Hymenoptera: Eulophidae) in Anticarsia gemmatalis Hübner, 1818 (Lepidoptera: Noctuidae) pupae exposed to 1:1, 2:1, 4:1, 6:1, 8:1, 10:1 or 12:1 females/ host, respectively. The parasitoid remained in contact with pupae for 24 h in glass tubes (14.0 x 2.2 cm), packed in a climate controlled chamber regulated at 25 ± 1ºC, 70 ± 10% relative humidity and photophase of 14 hours. We observed 54.54 and 90.90% of pupae parasitized at densities of 1:1 and 2:1, respectively, and 100.00% in the other densities with a better emergence index (72.72%) at a density of 6:1. The duration of the (egg-adult) life cycle decreased with increasing density of females and varied from 20 to 22 days. The offspring varied from 16 to 225 descendants per A. gemmatalis pupae with best results at the density 8:1. The sex ratio of the parasitoid varied from 0.95 ± 0.00 to 0.97 ± 0.01 without significant differences, and the body length of females and of males varied from 1.95 ± 0.02 to 2.22 ± 0.03 mm and 1.49 ± 0.02 to 1.87 ± 0.01 mm, respectively. Six to eight of P. elaeisis females per A. gemmatalis pupae provide more emergence and offspring of the parasitoid, allowing for its mass rearing.