ABSTRACT Natural products and their derivatives have been sources of search and research for new drugs for the treatment of neglected diseases. Naphthoquinones, a special group of quinones, are products of natural metabolites with a wide spectrum of biological activities and represent a group of interesting molecules for new therapeutic propositions. Among these compounds, lapachol stands out as a molecule from the heartwood of Tabebuia sp. whose structural changes resulted in compounds considered promising, such as epoxy-a-lapachone (ELAP). The biological activity of ELAP has been demonstrated, so far, for parasitic protozoa such as Leishmania spp., Trypanosoma cruzi and Plasmodium spp., species causing diseases needing new drug development and adequate health policy. This work gathers in vitro and in vivo studies on these parasites, as well as the toxicity profile, and the probable mechanisms of action elucidated until then. The potential of ELAP-based technology alternatives for a further drug is discussed here.

Sesquiterpene lactones are an important class of secondary metabolites frequently isolated from Vernonanthura genus that present a variety of biological properties, including antiproliferative activity. Due to the limitation of pharmacological studies on Vernonanthura nudiflora, the aim of this work was to investigate their antioxidant potential and antiproliferative activity against human tumor cells, as well as to isolate and identify the chemical constituents present in their aerial parts. The phytochemical investigation resulted in the isolation of the sesquiterpene lactones piptocarphins A, B, D, and a new hirsutinolide derivative, 8α-tigloyloxy-10α-hydroxy-hirsutinolide, besides triterpenes, glycosylated steroids, flavonoids, and one chlorogenic acid derivative. Also, other sesquiterpene lactones were identified by ultra-high performance liquid chromatography-high resolution tandem mass spectrometry (UHPLC-HRMS/MS) from dichloromethane fraction. This fraction showed activity against the tumor cells tested, mainly against leukemia, glioma, ovarian and kidney, with growth inhibitory activity (GI50) less than 0.80 µg mL-1. Piptocarphins A and B, in mixture, showed strong activity against all human cancer cell lines tested, with GI50 values ≤ 0.15 µg mL-1. Piptocarphin D was selective for glioma and resistant ovarian cell lines. The new hirsutinolide derivative showed potent activity against breast (GI50= 0.96 µg mL-1) and resistant ovarian (GI50 = 3.60 µg mL-1) cell lines.

BACKGROUND Trichomonas vaginalis is the aetiological agent of human trichomoniasis, which is one of the most prevalent sexually transmitted diseases in humans. Iron is an important element for the survival of this parasite and the colonisation of the host urogenital tract. OBJECTIVES In this study, we investigated the effects of iron on parasite proliferation in the dynamics of pseudocyst formation and morphologically characterised iron depletion-induced pseudocysts. METHODS We performed structural and ultrastructural analyses using light microscopy, scanning electron microscopy and transmission electron microscopy. FINDINGS It was observed that iron depletion (i) interrupts the proliferation of T. vaginalis, (ii) induces morphological changes in typical multiplicative trophozoites to spherical non-proliferative, non-motile pseudocysts, and (iii) induces the arrest of cell division at different stages of the cell cycle; (iv) iron is the fundamental element for the maintenance of typical trophozoite morphology; (v) pseudocysts induced by iron depletion are viable and reversible forms; and, finally, (vi) we demonstrated that pseudocysts induced by iron depletion are able to interact with human epithelial cells maintaining their spherical forms. MAIN CONCLUSIONS Together, these data suggest that pseudocysts could be induced as a response to iron nutritional stress and could have a potential role in the transmission and infection of T. vaginalis.

Nos últimos anos, visando a garantir a efetividade da justiça, iniciou-se o processo de reforma do judiciário brasileiro. Se, por um lado, as mudanças têm sido significativas e positivas, por outro pouco se sabe dos impactos das transformações sobre o trabalhador. A fim de dar visibilidade aos efeitos destas transformações, com base no referencial teórico da ergonomia da atividade, o objetivo desta pesquisa foi avaliar o Contexto de Trabalho e o Custo Humano no Trabalho em um órgão do Poder Judiciário brasileiro. Utilizaram-se a Escala de Avaliação do Contexto de Trabalho (EACT) e a Escala de Custo Humano no Trabalho (ECHT), ambas componentes do Inventário sobre Trabalho e Risco de Adoecimento (ITRA). Participaram deste estudo 383 servidores de diferentes lotações, sendo 58% do sexo feminino, 62,7% com curso de pós-graduação completo, 59,3% casados e 53% com idade entre 21 e 40 anos. Os resultados apontam, na EACT, para avaliações tendendo a críticas nos fatores Organização do Trabalho e Relações Socioprofissionais. No caso da ECHT, os fatores Custo Afetivo e Custo Cognitivo tiveram avaliação de moderada a crítica. A ANOVA evidenciou diferenças de percepções relacionadas a algumas variáveis sociodemográficas.

In recent years, in order to ensure the effectiveness of justice, the process of reform of the Brazilian Judiciary began. If, on the one hand, the changes have been significant and positive, on the other, little is known about the impact of the changes on the worker. In order to give visibility to the effects of these changes, based on the theory of the ergonomics of the activity, the scope of this research was to evaluate the Work Context and the Human Cost of Work in a Brazilian Judiciary Organ. The Assessment Scale of Work Context (ASWC) and the Scale of Human Cost of Work (SHCW) were used, as they are both components of the Inventory on Work and Risk - IWR. The study included 383 staff in different locations: 58% female, 62.7% with postgraduate qualifications, 59.3% married and 53% between 21 and 40 years of age. The results in ASWC reveal critical factors in work organization and socio-professional relations. In the case of SHCW, Affective Cost and Cognitive Cost factor assessments were moderate to critical. The ANOVA revealed differences in perceptions related to some socio-demographic variables.

Nos últimos anos, visando a garantir a efetividade da justiça, iniciou-se o processo de reforma do judiciário brasileiro. Se, por um lado, as mudanças têm sido significativas e positivas, por outro pouco se sabe dos impactos das transformações sobre o trabalhador. A fim de dar visibilidade aos efeitos destas transformações, com base no referencial teórico da ergonomia da atividade, o objetivo desta pesquisa foi avaliar o Contexto de Trabalho e o Custo Humano no Trabalho em um órgão do Poder Judiciário brasileiro. Utilizaram-se a Escala de Avaliação do Contexto de Trabalho (EACT) e a Escala de Custo Humano no Trabalho (ECHT), ambas componentes do Inventário sobre Trabalho e Risco de Adoecimento (ITRA). Participaram deste estudo 383 servidores de diferentes lotações, sendo 58% do sexo feminino, 62,7% com curso de pós-graduação completo, 59,3% casados e 53% com idade entre 21 e 40 anos. Os resultados apontam, na EACT, para avaliações tendendo a críticas nos fatores Organização do Trabalho e Relações Socioprofissionais. No caso da ECHT, os fatores Custo Afetivo e Custo Cognitivo tiveram avaliação de moderada a crítica. A ANOVA evidenciou diferenças de percepções relacionadas a algumas variáveis sociodemográficas.

In recent years, in order to ensure the effectiveness of justice, the process of reform of the Brazilian Judiciary began. If, on the one hand, the changes have been significant and positive, on the other, little is known about the impact of the changes on the worker. In order to give visibility to the effects of these changes, based on the theory of the ergonomics of the activity, the scope of this research was to evaluate the Work Context and the Human Cost of Work in a Brazilian Judiciary Organ. The Assessment Scale of Work Context (ASWC) and the Scale of Human Cost of Work (SHCW) were used, as they are both components of the Inventory on Work and Risk - IWR. The study included 383 staff in different locations: 58% female, 62.7% with postgraduate qualifications, 59.3% married and 53% between 21 and 40 years of age. The results in ASWC reveal critical factors in work organization and socio-professional relations. In the case of SHCW, Affective Cost and Cognitive Cost factor assessments were moderate to critical. The ANOVA revealed differences in perceptions related to some socio-demographic variables.

O estudo fitoquímico das folhas de Calycorectes psidiiflorus (O. Berg) Sobral, Myrtaceae, resultou no isolamento e identificação de: sesquiterpeno [8-hidroxicalameneno (1)], triterpenos [α-amirina (2a) e β-amirina (2b)], flavonóide [3-O-α-ramnopiranosil-7-O-bglucopiranosil canferol (3)], e alcalóide [1,2,3,4-tetraidro-1-metil-β-carbolina (4)]. As estruturas das substâncias isoladas foram elucidadas com base nos seus dados de RMN em comparação com os da literatura. A substância 8-hydroxicalameneno apresentou atividade antibacteriana (MIC = 7,8 µg/mL) e antifúngica (MIC = 15,6 µg/mL).

The phytochemical study of Calycorectes psidiiflorus (O. Berg) Sobral leaves resulted in isolation and identification of the sesquiterpene 8-hydroxycalamenene (1), triterpenes α-amyrin (2a) and β-amyrin (2b), flavonoid 3-O-α-rhamnopyranosyl-7-O-β-glucopyranosyl kaempferol (3), and of the alkaloid 1,2,3,4-tetrahydro-1-methyl-β-carboline (4). The structures of the isolated compounds were elucidated based on their spectroscopic NMR data and comparison with those reported in literature. Substance 1 presented antibacterial (MIC = 7.8 µg/mL) and antifungal (MIC = 15.6 µg/ mL) activities.

Extratos de Croton fluribundus (Euphorbiaceae), ácido caurenóico e dois derivados do ácido caurenóico foram avaliados como moluscicida, cercaricida e também foi verificada a letalidade destas amostras frente a larvas de Artemia salina Leach. Nestes ensaios foram observadas significantes atividades moluscicida e cercaricida associadas a uma reduzida toxicidade frente ao camarão de água salgada.

Lethality of the extracts of Croton floribundus (Euphorbiaceae), a medicinal plant from south Brazil, and of the kaurenoic acid, an isolated compound, and two of its derivatives against adult Biomphalaria glabrata snails, Schistosoma mansoni cercariae and Artemia salina Leach. brine shrimp larvae are reported. Both extracts and the isolated compound showed significant molluscicidal and cercaricidal activities and reduced toxicity in brine shrimp assays.

Um novo triterpeno caracterizado como ácido 6alfa-hidroxibetulínico foi isolado das folhas e caule da planta, vulgarmente conhecida no Brasil como Cambuí, Eugenia moraviana (Myrtaceae), juntamente com três outras substâncias conhecidas, identificadas como ácido platânico, ácido betulínico e beta-sitosterol. Através da análise de espectros incluindo NOE e experimentos de RMN em duas dimensões foi realizada a atribuição inequívoca dos deslocamentos químicos de ¹H e de 13C do ácido 6alfa-hidroxibetulínico(ácido-3beta,6alfa-diidróxi-20(29)-lupen-28-óico) e do ácido platânico.

A novel triterpene, characterized as 6alpha-hydroxybetulinic acid, was isolated from the leaves and stems of Eugenia moraviana (Myrtaceae), known in Brazil as Cambuí, together with three known compounds, platanic acid, betulinic acid and beta-sitosterol. Unequivocal ¹H and 13C assignments of 6alpha-hydroxybetulinic acid (3beta,6alpha-dihydroxy-20(29)-lupen-28-oic acid) and platanic acid were undertaken by spectral analysis including NOE and 2 D NMR experiments.