Phenolic derivatives from Baccharis retusa DC. (Asteraceae)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Universidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 São Paulo, BrazilUniv Presbiteriana Mackenzie, Ctr Ciencias & Humanidades, BR-01302907 São Paulo, BrazilUniv Presbiteriana Mackenzie, Ctr Ciencias Biol & Saude, BR-01302907 São Paulo, BrazilUniversidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 São Paulo, BrazilWeb of Scienc

In vitro antileishmanial and antitrypanosomal activities of flavanones from Baccharis retusa DC. (Asteraceae)

Leishmaniasis and Chagas' are parasitic protozoan diseases that affect the poorest population in the world, causing a high mortality and morbidity. As a result of highly toxic and long-term treatments, novel, safe and more efficacious drugs are essential. in this work, the CH2Cl2 phase from MeOH extract from the leaves of Baccharis retusa DC. (Asteraceae) was fractioned to afford two flavonoids: naringenin (1) and sakuranetin (2). These compounds were in vitro tested against Leishmania spp. promastigotes and amastigotes and Ttypanosoma cruzi trypomastigotes and amastigotes. Compound 2 presented activity against Leishmania (L) amazonensis, Leishmania (V.) braziliensis, Leishmania (L) major, and Leishmania (L) chagasi with IC50 values in the range between 43 and 52 mu g/mL and against T. cruzi trypomastigotes (IC50= 20.17 mu g/mL). Despite of the chemical similarity, compound 1 did not show antiparasitic activity. Additionally, compound 2 was subjected to a methylation procedure to give sakuranetin-4'-methyl ether (3), which resulted in an inactive compound against both Leishmania spp. and T. cnizi. the obtained results indicated that the presence of one hydroxyl group at C-4' associated to one methoxyl group at C-7 is important to the antiparasitic activity. Further drug design studies aiming derivatives could be a promising tool for the development of new therapeutic agents for Leishmaniasis and Chagas' disease. (C) 2011 Elsevier Inc. All rights reserved.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Pesquisa e DesenvolvimentoUniversidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Diadema, SP, BrazilInst Adolfo Lutz Registro, Dept Parasitol, São Paulo, BrazilUniv Fed ABC, Ctr Ciencias Nat & Humanas, Santo Andre, SP, BrazilUniv Presbiteriana Mackenzie, Ctr Ciencias & Humanidades, São Paulo, BrazilUniversidade Federal de São Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Diadema, SP, BrazilFAPESP: 06/57626-5FAPESP: 08/11496-9Conselho Nacional de Pesquisa e Desenvolvimento: 473405/2008-3Conselho Nacional de Pesquisa e Desenvolvimento: 477422/2009-8Web of Scienc

Biseugenol Exhibited Anti-Inflammatory and Anti-Asthmatic Effects in an Asthma Mouse Model of Mixed-Granulocytic Asthma

In the present work, the anti-inflammatory and antiasthmatic potential of biseugenol, isolated as the main component from n-hexane extract from leaves of Nectandra leucantha and chemically prepared using oxidative coupling from eugenol, was evaluated in an experimental model of mixed-granulocytic asthma. Initially, in silico studies of biseugenol showed good predictions for drug-likeness, with adherence to Lipinski’s rules of five (RO5), good Absorption, Distribution, Metabolism and Excretion (ADME) properties and no alerts for Pan-Assay Interference Compounds (PAINS), indicating adequate adherence to perform in vivo assays. Biseugenol (20 mg·kg−1) was thus administered intraperitoneally (four days of treatment) and resulted in a significant reduction in both eosinophils and neutrophils of bronchoalveolar lavage fluid in ovalbumin-sensitized mice with no statistical difference from dexamethasone (5 mg·kg−1). As for lung function parameters, biseugenol (20 mg·kg−1) significantly reduced airway and tissue damping in comparison to ovalbumin group, with similar efficacy to positive control dexamethasone. Airway hyperresponsiveness to intravenous methacholine was reduced with biseugenol but was inferior to dexamethasone in higher doses. In conclusion, biseugenol displayed antiasthmatic effects, as observed through the reduction of inflammation and airway hyperresponsiveness, with similar effects to dexamethasone, on mixed-granulocytic ovalbumin-sensitized miceFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)FAPESP: 2018/06088-

Perspectivas de adolescentes em conflito com a lei sobre o delito, a medida de internação e as expectativas de futuro

O objetivo desse estudo foi investigar as avaliações que os adolescentes em conflito com a lei fazem sobre o cometimento do delito, a medida socioeducativa e as perspectivas futuras. Os dados foram coletados por meio dos prontuários dos internos e de entrevistas semiestruturadas realizadas com nove adolescentes que cumpriam medida de internação em um centro de atendimento socioeducativo. Os resultados retrataram um perfil permeado por pobreza, baixa escolaridade, falta de rede familiar, uso de drogas e reiterações nos delitos. Embora os adolescentes tenham avaliado negativamente o ato cometido, destacaram os benefícios secundários que o delito pode proporcionar. A privação de liberdade foi considerada negativa mas, ao mesmo tempo, foi avaliada como uma possibilidade de proteção das vulnerabilidades a que estavam expostos. As perspectivas futuras estiveram voltadas para o estudo e o trabalho, no entanto, não descartam a possibilidade de vir a cometer novos delitos. Tais dados promovem uma reflexão quanto ao caráter educativo e ressocializador da medida de internação para os adolescentes em conflito com a lei.The aim of this study was to investigate youth offender perceptions about their youth criminal behavior, educative measure and future prospects. The data were ollected from records and semistructured interviews. Interviews were conducted with nine adolescents who were imprisoned in educational center for young offenders. Results indicated poverty, low education, lack of family network, drug use, and youth criminal behavior. They evaluated their youth criminal behavior as a negative act, but they highlighted the financial advantages from their offense. The deprivation of freedom was considered negative, but at the same time, they evaluate the imprisonment as an opportunity to protect them. Future prospects were related to work and study; however, they didn’t discard the possibility of committing new criminal acts. These results promote a reflection about educational and social aspect of imprisonment for young offenders

Regenerative and Protective Effects on Dental Tissues of a Fluoride–Silicon-Rich Toothpaste Associated with a Calcium Booster: An <i>In Vitro</i> Study

Calcium boosters have been used as a supplement for fluoride toothpastes to repair the dental tissues and reduce dentin permeability. This in vitro study aimed to characterize the regenerative and protective effects of the treatment of dental tissues with a fluoride–silicon-rich toothpaste associated with a calcium booster. Bovine enamel and dentin blocks (n = 5) were obtained (4 × 4 × 6 mm). A fluoride–silicon-rich toothpaste and a calcium booster were used to brush the enamel and dentin both immediately and five days afterwards. The outcomes were then compared to those of the untreated control group. After that, the specimens were cross-sectioned. SEM was used to evaluate the micromorphology of the surface and cross-section. Energy-dispersive X-ray spectroscopy (EDS) was used to determine the elemental analyses (weight%). After treatment for 5 days with a booster/silicon-rich toothpaste, EDS analysis demonstrated that it induced a significant mineral change. It was also able to form a protective silicon-enriched mineral layer on both enamel and dentin surfaces. It was demonstrated in vitro that a fluoride–silicon-rich toothpaste associated with a calcium booster regenerates the dental tissues, remineralizing the enamel structure and occluding the dentin tubules

Treatment with triterpenic fraction purified from Baccharis uncinella leaves inhibits Leishmania (Leishmania) amazonensis spreading and improves Th1 immune response in infected mice

The current medications used to treat leishmaniasis have many side effects for patients; in addition, some cases of the disease are refractory to treatment. Therefore, the search for new leishmanicidal compounds is indispensable. Recently, it was demonstrated that oleanolic- and ursolic-containing fraction from Baccharis uncinella leaves eliminated the promastigote and amastigote forms of Leishmania (Leishmania) amazonensis and L. (Viannia) braziliensis without causing toxic effects for J774 macrophages. Thus, the aim of the present work was to characterize the therapeutic effect of the triterpenic fraction in L. (L.) amazonensis-infected BALB/c mice. Oleanolic- and ursolic acid-containing fraction was extracted from B. uncinella leaves using organic solvents and chromatographic procedures. L. (L.) amazonensis-infected BALB/c mice were treated intraperitoneally with triterpenic fraction during five consecutive days with 1.0 and 5.0 mg/kg of triterpenic fraction, or with 10.0 mg/kg of amphotericin B drug. Groups of mice treated with the triterpenic fraction, presented with decreased lesion size and low parasitism of the skin-both of which were associated with high amounts of interleukin-12 and interferon gamma. the curative effect of this fraction was similar to amphotericin B-treated mice; however, the final dose, required to eliminate amastigotes, was lesser than amphotericin B. Moreover, triterpenic fraction did not cause microscopic alterations in liver, spleen, heart, lung, and kidney of experimental groups. This work suggests that this fraction possesses compounds that are characterized by leishmanicidal and immunomodulatory activities. From this perspective, the triterpenic fraction can be explored as a new therapeutic agent for use against American Tegumentar Leishmaniasis.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Univ São Paulo, Fac Med, Dept Patol, Lab Patol Molestias Infeciosas, BR-01246000 São Paulo, BrazilUniversidade Federal de São Paulo, Dept Ciencias Exatas & Terra, BR-09972270 São Paulo, BrazilUniv Fed ABC, Ctr Ciencias Nat & Humanas, BR-09210180 São Paulo, BrazilUniversidade Federal de São Paulo, Dept Ciencias Exatas & Terra, BR-09972270 São Paulo, BrazilFAPESP: 2012/03903-9: HCFMUSP-LIM50Web of Scienc