Magnetic nanosystem for cancer therapy using oncocalyxone A, an antitomour secondary metabolite isolated from a Brazilian plant

none14siThis paper describes the investigation and development of a novel magnetic drug delivery nanosystem (labeled as MO-20) for cancer therapy. The drug employed was oncocalyxone A (onco A), which was isolated from Auxemma oncocalyx, an endemic Brazilian plant. It has a series of pharmacological properties: antioxidant, cytotoxic, analgesic, anti-inflammatory, antitumor and antiplatelet. Onco A was associated with magnetite nanoparticles in order to obtain magnetic properties. The components of MO-20 were characterized by XRD, FTIR, TGA, TEM and Magnetization curves. The MO-20 presented a size of about 30 nm and globular morphology. In addition, drug releasing experiments were performed, where it was observed the presence of the anomalous transport. The results found in this work showed the potential of onco A for future applications of the MO-20 as a new magnetic drug release nanosystem for cancer treatment.openBarreto, Antônio C.H.; Santiago, Vivian R.; Freire, Rafael M.; Mazzetto, Selma E.; Denardin, Juliano C.; Mele, Giuseppe; Cavalcante, Igor M.; Ribeiro, Maria E.N.P.; Ricardo, Nágila M.P.S.; Gonçalves, Tamara; Carbone, Luigi; Lemos, Telma L.G.; Pessoa, Otília D.L.; Fechine, Pierre B.A.*Barreto, Antônio C. H.; Santiago, Vivian R.; Freire, Rafael M.; Mazzetto, Selma E.; Denardin, Juliano C.; Mele, Giuseppe; Cavalcante, Igor M.; Ribeiro, Maria E. N. P.; Ricardo, Nágila M. P. S.; Gonçalves, Tamara; Carbone, Luigi; Lemos, Telma L. G.; Pessoa, Otília D. L.; Fechine, Pierre B. A

Coccidioidal pericarditis: a rapid presumptive diagnosis by an in-house antigen confirmed by mycological and molecular methods

Coccidioidal pericarditis is a condition found in approximately 1-5% of patients infected by Coccidioides species. It is associated with widely diverse clinical symptoms. This paper reports a case of coccidioidal pericarditis diagnosed by an in-house Coccidioides posadasii antigen and confirmed with mycological and molecular methods. From February to September 2005, the patient suffered from fever, weight loss, a non-productive cough, thoracic pain and tachycardia. He received a positive diagnosis of coccidioidal pericarditis only in October 2005. the macromorphological examination of the culture showed a whitish felt-like colony, which became brownish with age. Preparations in lactophenol cotton blue stain showed hyaline septate hyphae with fragmentation and thin arthroconidia-like structures. Pericardial fluid and sera samples were positive for Coccidioides antibodies by immunodiffusion and ELISA with a C. posadasii in-house antigen preparation. the C. posadasii identification was confirmed by nested PCR of the antigen 2/proline-rich antigen (Ag2/PRA) encoding gene.Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Univ Fed Ceara, Specialized Med Mycol Ctr, Fortaleza, Ceara, BrazilUniv Fed Ceara, Postgrad Program Med Sci, Fortaleza, Ceara, BrazilUniv Fed Ceara, Postgrad Program Med Microbiol, Fortaleza, Ceara, BrazilUniv Estadual Ceara, Dept Biol Sci, Fortaleza, Ceara, BrazilUniv Estadual Ceara, Postgrad Program Vet Sci, Fortaleza, Ceara, BrazilUniv Fed Ceara, Dept Clin & Toxicol Anal, Fortaleza, Ceara, BrazilUniversidade Federal de São Paulo, Dept Microbiol Immunol & Parasitol, São Paulo, BrazilUniversidade Federal de São Paulo, Dept Microbiol Immunol & Parasitol, São Paulo, BrazilCNPq: 150984/2005-7CNPq: 620161/2006-0FAPESP: 4/14270-0Web of Scienc

Ethyl butyrate synthesis catalyzed by lipases A and B from candida antarctica immobilized onto magnetic nanoparticles. Improvement of biocatalysts’ performance under ultrasonic irradiation

The synthesis of ethyl butyrate catalyzed by lipases A (CALA) or B (CALB) from Candida antarctica immobilized onto magnetic nanoparticles (MNP), CALA-MNP and CALB-MNP, respectively, is hereby reported. MNPs were prepared by co-precipitation, functionalized with 3-aminopropyltriethoxysilane, activated with glutaraldehyde, and then used as support to immobilize either CALA or CALB (immobilization yield: 100 ± 1.2% and 57.6 ± 3.8%; biocatalysts activities: 198.3 ± 2.7 Up-NPB/g and 52.9 ± 1.7 Up-NPB/g for CALA-MNP and CALB-MNP, respectively). X-ray diffraction and Raman spectroscopy analysis indicated the production of a magnetic nanomaterial with a diameter of 13.0 nm, whereas Fourier-transform infrared spectroscopy indicated functionalization, activation and enzyme immobilization. To determine the optimum conditions for the synthesis, a four-variable Central Composite Design (CCD) (biocatalyst content, molar ratio, temperature and time) was performed. Under optimized conditions (1:1, 45 °C and 6 h), it was possible to achieve 99.2 ± 0.3% of conversion for CALA-MNP (10 mg) and 97.5 ± 0.8% for CALB-MNP (12.5 mg), which retained approximately 80% of their activity after 10 consecutive cycles of esterification. Under ultrasonic irradiation, similar conversions were achieved but at 4 h of incubation, demonstrating the efficiency of ultrasound technology in the enzymatic synthesis of esters.This research was funded by Fundação Cearense de Apoio ao Desenvolvimento Científico e Tecnológico (FUNCAP), grant numbers BP3-0139-00005.01.00/18 and PNE-0112-00048.01.00/16, Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), grant numbers 422942/2016-2, 409058/2015-5 and 408790/2016-4, Coordenação de Aperfeiçoamento de Ensino Superior (CAPES-Finance Code 001) and MICIU, grant number CTQ2015-68951-C3-3-R.Peer reviewe

Immobilization of lipase a from candida antarctica onto chitosan-coated magnetic nanoparticles

In this communication, lipase A from Candida antarctica (CALA) was immobilized by covalent bonding on magnetic nanoparticles coated with chitosan and activated with glutaraldehyde, labelled CALA-MNP, (immobilization parameters: 84.1% ± 1.0 for immobilization yield and 208.0 ± 3.0 U/g ± 1.1 for derivative activity). CALA-MNP biocatalyst was characterized by X-ray Powder Diffraction (XRPD), Fourier Transform Infrared (FTIR) spectroscopy, Thermogravimetry (TG) and Scanning Electron Microscope (SEM), proving the incorporation of magnetite and the immobilization of CALA in the chitosan matrix. Besides, the immobilized biocatalyst showed a half-life 8–11 times higher than that of the soluble enzyme at pH 5–9. CALA showed the highest activity at pH 7, while CALA-MNP presented the highest activity at pH 10. The immobilized enzyme was more active than the free enzyme at all studied pH values, except pH 7.This research was funded by Fundação Cearense de Apoio ao Desenvolvimento Científico e Tecnológico (FUNCAP), grant numbers BP3-0139-00005.01.00/18 and PNE-0112-00048.01.00/16, Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), grant numbers 422942/2016-2, 409058/2015-5 and 408790/2016-4, Coordenação de Aperfeiçoamento de Ensino Superior (CAPES-Finance Code 001) and MICIU, grant number CTQ2015-68951-C3-3-R.Peer reviewe

Polymorphism evaluation in generic tablets containing mebendazole by dissolution tests

This study evaluates the incidence of the polymorphic forms of mebendazole (MBZ) in tablets within the Brazilian market by dissolution tests. The indicated dissolution medium by the USP 30 (United States Pharmacopoeia) and a proposed modified medium were duly compared in order to verify whether they are able to discriminate the polymorph A from polymorph C in commercial tablets. Dissolution assay tests of physical mixtures in raw materials of polymorph A and polymorph C, as well as of nine tablets of MBZ (available in the Brazilian market), were properly performed. For the dissolution tests, the USP 30 medium (I) and a modified medium (II) were used. The modified medium allowed a reproducible and reliable quality control of MBZ polymorphism in commercial tablets

Optimization of the production of enzymatic biodiesel from residual babassu oil (Orbignya sp.) via RSM

This article belongs to the Special Issue Application of Immobilized Enzyme as Catalysts in Chemical Synthesis.Residual oil from babassu (Orbignya sp.), a low-cost raw material, was used in the enzymatic esterification for biodiesel production, using lipase B from Candida antarctica (Novozym® 435) and ethanol. For the first time in the literature, residual babassu oil and Novozym® 435 are being investigated to obtain biodiesel. In this communication, response surface methodology (RSM) and a central composite design (CCD) were used to optimize the esterification and study the effects of four factors (molar ratio (1:1–1:16, free fatty acids (FFAs) /alcohol), temperature (30–50 °C), biocatalyst content (0.05–0.15 g) and reaction time (2–6 h)) in the conversion into fatty acid ethyl esters. Under optimized conditions (1:18 molar ratio (FFAs/alcohol), 0.14 g of Novozym® 435, 48 °C and 4 h), the conversion into ethyl esters was 96.8%. It was found that after 10 consecutive cycles of esterification under optimal conditions, Novozym® 435 showed a maximum loss of activity of 5.8%, suggesting a very small change in the support/enzyme ratio proved by Fourier Transform Infrared (FTIR) spectroscopy and insignificant changes in the surface of Novozym® 435 proved by scanning electron microscopy (SEM) after the 10 consecutive cycles of esterification.This research was funded by Fundação Cearense de Apoio ao Desenvolvimento Científico e Tecnológico (FUNCAP), grant numbers BP3-0139-00005.01.00/18 and PNE-0112-00048.01.00/16, Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), grant numbers 422942/2016-2, 409058/2015-5, 408790/2016-4, and 311062/2019-9. Coordenação de Aperfeiçoamento de Ensino Superior (CAPES-Finance Code 001)

Histoplasmosis in HIV-positive patients in Ceara, Brazil: clinical-laboratory aspects and in vitro antifungal susceptibility of Histoplasma capsulatum isolates

This study contains a descriptive analysis of histoplasmosis in AIDS patients between 2006 and 2010 in the state of Ceara, Brazil. Additionally, the in vitro susceptibility of Histoplasma capsulatum isolates obtained during this period was assessed. We report 208 cases of patients with histoplasmosis and AIDS, describing the epidemiological, clinical, laboratory and therapeutic aspects. the in vitro antifungal susceptibility test was carried out by the microdilution method, according to Clinical and Laboratory Standards Institute, with H. capsulatum in the filamentous and yeast phases, against the antifungals amphotericin B, fluconazole, itraconazole, voriconazole and caspofungin. in 38.9% of the cases, histoplasmosis was the first indicator of AIDS and in 85.8% of the patients the CD4 cell count was lower than 100 cells/mm(3). the lactate dehydrogenase levels were high in all the patients evaluated, with impairment of hepatic and renal function and evolution to death in 42.3% of the cases. the in vitro susceptibility profile demonstrated there was no antifungal resistance among the isolates evaluated. There was a significant increase in the number of histoplasmosis cases in HIV-positive patients during the period surveyed in the state of Ceara, northeastern Brazil, but no antifungal resistance among the recovered isolates of H. capsulatum. (C) 2012 Royal Society of Tropical Medicine and Hygiene. Published by Elsevier B.V. All rights reserved.Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Univ Fed Ceara, Specialized Med Mycol Ctr, Fortaleza, Ceara, BrazilUniv Fed Ceara, Postgrad Program Med Microbiol, Fortaleza, Ceara, BrazilUniv Fed Ceara, Postgrad Program Med Sci, Fortaleza, Ceara, BrazilUniv Estadual Ceara, Postgrad Program Vet Sci, Fortaleza, Ceara, BrazilUniv Fed Ceara, Dept Stat & Appl Math, Fortaleza, Ceara, BrazilHosp Sao Jose, Fortaleza, Ceara, BrazilUniversidade Federal de São Paulo, São Paulo, BrazilUniversidade Federal de São Paulo, São Paulo, BrazilCNPq: 562296/2010-7CNPq: 552161/2011-0CNPq: 304779/2011-3CAPES: 2103/2009Web of Scienc