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Volpato A.,Santa Catarina State University | Grosskopf R.K.,Santa Catarina State University | Santos R.C.,Centro Universitario Franciscano | Vaucher R.A.,Centro Universitario Franciscano | And 5 more authors.
Journal of Essential Oil Research | Year: 2015

The aim of this study was to verify in vitro the influence of rosemary, andiroba, and copaiba essential oils on different stages of the cattle tick Rhipicephalus microplus. Female ticks were collected from naturally infected cows and treated in vitro with these essential oils at concentrations of 5% and 10%. All tests were performed in triplicate using positive (amitraz 10%) and negative (untreated) controls. It was possible to observe that rosemary, andiroba, and copaiba essential oils inhibited female reproduction at concentrations of 5% (45.0%, 77.5%, and 71.6%, respectively) and 10% (55.7%, 92.0,% and 86.7%, respectively) compared with amitraz (72.9%). Additionally, andiroba (10%) and copaiba (5% and 10%) oil solutions also had an acaricidal effect (100%), similarly to the positive control. The andiroba and copaiba oils showed an ovicidal effect, which effected hatchability. Rosemary oil showed neither acaricidal nor ovicidal effect. Therefore, based on these results, we were able to show that all oils and concentrations tested may affect tick reproduction by inhibiting tick oviposition and hatchability. In addition, andiroba and copaiba oils exhibited ovicidal and acaricidal effects. © 2015 Taylor & Francis.


Pazinato R.,Santa Catarina State University | Klauck V.,Santa Catarina State University | Volpato A.,Santa Catarina State University | Tonin A.A.,Federal University of Santa Maria | And 10 more authors.
Experimental and Applied Acarology | Year: 2014

The aim of this study was to verify the influence of tea tree oil (TTO) (Melaleuca alternifolia) tested in its pure and nanostructured (TTO nanoparticles) forms on the reproduction of female Rhipicephalus microplus. For our purpose, female ticks were collected from naturally infected animals and treated in vitro with TTO (1, 5, and 10 %) and TTO nanoparticles (0.075, 0.375, and 0.75 %). In order to validate the tests, they were performed in triplicate using positive (amitraz) and negative (untreated) controls. It was possible to observe that pure TTO (5 and 10 %) and TTO nanoparticles (0.375 and 0.75 %) showed 100 % reproductive inhibition on female ticks. Additionally, pure TTO (1 %) also showed an acaricide effect (70 %), similarly to the positive control (78.3 %). This is the first study demonstrating the activity of pure TTO and TTO nanoparticles on female ticks. Therefore, based on these results, we were able to show that both forms and all concentrations of M. alternifolia affected tick reproduction by inhibiting egg laying and hatching. We were also able to show that TTO nanoparticles potentiated the inhibitor effect of pure TTO on the reproduction of R. microplus. © 2013 Springer Science+Business Media Dordrecht.


The present invention relates to a method of treatment of a mucopolysaccharidosis with 4-methyl-2-oxo-2H-1-benzopyran-7-yl-5-thio--D-xylopyranoside.


Santos R.C.V.,Centro Universitario Franciscano | Santos R.C.V.,Laboratorio Of Nanotecnologia | Lopes L.Q.S.,Centro Universitario Franciscano | Lopes L.Q.S.,Laboratorio Of Nanotecnologia | And 14 more authors.
Journal of Asia-Pacific Entomology | Year: 2014

Paenibacillus larvae and Melissococcus plutonius are the primary bacterial pathogens of honeybees and the causative agents of American and European foulbrood disease (AFB and EFB) respectively. Such diseases have been gaining importance since there are few therapeutic options beyond the reporting of microorganisms resistant to conventional antibiotics. Due to the inefficiency and/or low efficacy of some antibiotics, researches with nanotechnology represent, possibly, new therapeutic strategies. Nanostructured drugs have presented some advantages over the conventional medicines, such as slow, gradual and controlled release, increased bioavailability, and reduced side-effects, among others. In this study, in vitro antimicrobial activity of tea tree oil (TTO) nanoparticles against Paenibacillus species, including P. larvae and M. plutonius strains was evaluated. Minimal inhibitory concentration (MIC) in Mueller-Hinton or KSBHI broth by the microdilution method was assessed. TTO registered MIC values of 0.18-6.25%, while the MIC values obtained for the TTO nanoparticle were of 0.01-0.93%. The possible toxic effect of TTO and TTO nanoparticle has been assessed by the spraying application method in the concentrations higher than the MICs. Bee mortality was evident only in treatment with TTO and the TTO nanoparticles show no toxic effects after 7. days of observation. Our results showed for the first time that TTO nanoencapsulation presented a high activity against Paenibacillus species and M. plutonius strains showing that the use of nanotechnology may represent one alternative way for the treatment or prevention of AFB and EFB. •TTO nanoencapsulation presented a high activity against Paenibacillus species and M. plutonius strains showing that the use of nanotechnology may represent one alternative way for the treatment or prevention of AFB and EFB. © 2014 Korean Society of Applied Entomology, Taiwan Entomological Society and Malaysian Plant Protection Society.


George D.M.,AbbVie Bioresearch Center | Breinlinger E.C.,AbbVie Bioresearch Center | Friedman M.,AbbVie Bioresearch Center | Zhang Y.,WuXi AppTec | And 11 more authors.
Journal of Medicinal Chemistry | Year: 2015

Protein kinase Cθ (PKCθ) regulates a key step in the activation of T cells. On the basis of its mechanism of action, inhibition of this kinase is hypothesized to serve as an effective therapy for autoimmune diseases such as rheumatoid arthritis (RA), inflammatory bowel disease (IBD), and psoriasis. Herein, the discovery of a small molecule PKCθ inhibitor is described, starting from a fragment hit 1 and advancing to compound 41 through the use of structure-based drug design. Compound 41 demonstrates excellent in vitro activity, good oral pharmacokinetics, and efficacy in both an acute in vivo mechanistic model and a chronic in vivo disease model but suffers from tolerability issues upon chronic dosing. © 2014 American Chemical Society.

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