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Friedelin, a pentacyclic triterpene found in the leaves of the Celastraceae species, demonstrates numerous biological activities and is a precursor of quinonemethide triterpenes, which are promising antitumoral agents. Friedelin is biosynthesized from the cyclization of 2,3-oxidosqualene, involving a series of rearrangements to form a ketone by deprotonation of the hydroxylated intermediate, without the aid of an oxidoreductase enzyme. Mutagenesis studies among oxidosqualene cyclases (OSCs) have demonstrated the influence of amino acid residues on rearrangements during substrate cyclization: loss of catalytic activity, stabilization, rearrangement control or specificity changing. In the present study, friedelin synthase from Maytenus ilicifolia (Celastraceae) was expressed heterologously in Saccharomyces cerevisiae. Site-directed mutagenesis studies were performed by replacing phenylalanine with tryptophan at position 473 (Phe473Trp), methionine with serine at position 549 (Met549Ser) and leucine with phenylalanine at position 552 (Leu552Phe). Mutation Phe473Trp led to a total loss of function, mutants Met549Ser and Leu552Phe interfered with the enzyme specificity leading to enhanced friedelin production, in addition to α-amyrin and β-amyrin. Hence, these data showed that methionine 549 and leucine 552 are important residues for the function of this synthase.

Made available in DSpace on 2018-12-11T17:36:22Z (GMT). No. of bitstreams: 0 Previous issue date: 2018-05-01. Added 1 bitstream(s) on 2019-10-09T18:33:08Z : No. of bitstreams: 1 S0103-50532018000501105.pdf: 2907602 bytes, checksum: ef8123c16f0caba93af7dd13a547df64 (MD5) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Département Caractérisation et Élaboration des Produits Issus de l’Agriculture, Institut National de la Recherche Agronomique Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Piper gaudichaudianum Kunth (Piperaceae) accumulates gaudichaudianic acid, a prenylated benzopyran, as its major component. Interestingly, this trypanocidal compound occurs as a racemic mixture. Herein, transcriptomic investigations of Piper gaudichaudianum using the RNA-seq approach are reported, and from the analysis of the transcripts expressed it was possible to propose a complete biosynthetic pathway for the production of gaudichaudianic acid, including the steps that originate its precursor, p-hydroxybenzoic acid. Peperomia obtusifolia (L.) A. Dietr. (Piperaceae) also accumulates racemic benzopyrans, however, its chromanes originate from the polyketide pathway, while the chromenes from Piper derives from the shikimate pathway. Recent transcriptomic and proteomic studies of the former species did not identify polyketide synthases involved in the production of the benzopyran moiety, but revealed the expression of tocopherol cyclase, which may be responsible for the cyclization of the 3,4-dihydro-2H-pyran ring. The analysis of the enzymes involved in the secondary metabolism of Piper gaudichaudianum and the comparison with the data previously obtained from Peperomia obtusifolia can provide valuable information on how these compounds are biosynthesized. Instituto de Química Universidade Estadual Paulista (UNESP) Departamento de Química Universidade Federal de São Carlos (UFSCar) Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista (UNESP) Instituto de Química Universidade de São Paulo (USP) Instituto de Química Universidade Estadual Paulista (UNESP) Faculdade de Ciências Farmacêuticas Universidade Estadual Paulista (UNESP) FAPESP: 2013/07600-3 Département Caractérisation et Élaboration des Produits Issus de l’Agriculture, Institut National de la Recherche Agronomique: 2014/25222-9 Département Caractérisation et Élaboration des Produits Issus de l’Agriculture, Institut National de la Recherche Agronomique: 2014/50316-7 Département Caractérisation et Élaboration des Produits Issus de l’Agriculture, Institut National de la Recherche Agronomique: 2015/07089-2 FAPESP: 2011/01003-8

Equisetum hyemale species is considered a medicinal plant used in the form of infusions to combat infectious or inflammation diseases and also diuretic effects, presenting several compounds related to these actions. In previous studies different species of Equisetum showed several phenolic compounds. The objective of this study was, for the first time, based on phytochemistry analysis to evaluate the antioxidant and antimicrobial activity. The 70% ethanolic and methanolic extracts of E. hyemale were characterized by spectrophotometric and high-performance liquid chromatography with pulsed amperometric detector analyses, as well as its antioxidant potential based on the scavenger activity of 2,2-diphenyl-1-picrylhydrazyl (DPPH). In addition was verified the antimicrobial activity by broth microdilution technique against bacteria and fungi. The extracts showed phytochemical similarity, which demonstrated the presence of phenolic compounds, the scavenging activity for free radicals was about 30% and was observed better antifungal activity against dermatophyte fungi, with minimum inhibitory concentration and minimum fungicidal concentration of 0.62 mg/mL to Trichophyton rubrum and Microsporum canis. The extracts exhibits great potential to therapeutic applications or product development, since both possess antifungal activity and antioxidant action associated with little difference in their phytochemical composition.

Made available in DSpace on 2018-12-11T17:24:03Z (GMT). No. of bitstreams: 0 Previous issue date: 2018-04-05 Plinia cauliflora is a plant species with edible fruits but its chemical composition is not totally known yet although former studies showed its potential as antifungal agent. This work aimed the chemical analysis of the leaves, the activity against fungi species and evaluated cytotoxicity. Extract was obtained with 70% ethanol. An ethyl acetate fraction was obtained and glycosylated quercetin and myricetin were isolated. Samples were tested against Candida species, dermatophytes and entomopathogenic fungi. Cytotoxicity was evaluated against fibroblast cells. Extract showed good activity against C. albicans (minimum inhibitory concentration at 156 μg/mL), C. parapsilosis (78 μg/mL), C. krusei (19 μg/mL), Trichophyton rubrum (78 μg/mL) and Microsporum canis (156 μg/mL). Isolated compounds were more active against C. krusei and T. rubrum. The extract, which was the more active sample, demonstrated low cytotoxic effect and encourage more studies against rising non-albicans species and dermatophyte T. rubrum. Department of Drugs and Medicines, São Paulo State University-UNESP, Araraquara, Brazil Department of Organic Chemistry, São Paulo State University-UNESP, Araraquara, Brazil

Made available in DSpace on 2018-12-11T17:21:52Z (GMT). No. of bitstreams: 0 Previous issue date: 2018-08-01 A complexity of pathway expression in yeast compared to prokaryotes is the need for separate promoters and terminators for each gene expressed. Single transcript expression and separated protein production is possible via the use of 2A viral peptides, but detailed characterization to assess their suitability and applications is needed. The present work aimed to characterize multiple 2A peptide sequences to determine suitability for metabolic engineering applications in Saccharomyces cerevisiae. We screened 22 peptides placed between fluorescent protein sequences. Cleaving efficiency was calculated by western blot intensity of bands corresponding to the cleaved and uncleaved forms of the reporter. Three out of the 22 sequences showed high cleavage efficiency: 2A peptide from Equine rhinitis B virus (91%), Porcine teschovirus-1 (85%) and Operophtera brumata cypovirus-18 (83%). Furthermore, expression of the released protein was comparable to its monocistronic expression. As a proof-of-concept, the triterpene friedelin was successfully produced in the same yeast strain by expressing its synthase with the truncated form of HMG1 linked by the 2A peptide of ERBV-1, with production titers comparable to monocistronic expression (via separate promoters). These results suggest that these peptides could be suitable for expression and translation of multiple proteins in metabolic engineering applications in S. cerevisiae. Department of Organic Chemistry São Paulo State University (UNESP), Rua Prof. Francisco Degni, 55 Department of Biology and Biological Engineering Chalmers University of Technology, Kemivägen 10 Department of Biological Sciences São Paulo State University (UNESP), Rod. Araraquara-Jau km 1 Novo Nordisk Foundation Center for Biosustainability Chalmers University of Technology Novo Nordisk Foundation Center for Biosustainability Technical University of Denmark Biopetrolia AB, Kemivägen 10 Department of Organic Chemistry São Paulo State University (UNESP), Rua Prof. Francisco Degni, 55 Department of Biological Sciences São Paulo State University (UNESP), Rod. Araraquara-Jau km 1

Peperomia obtusifolia, an ornamental plant from the Piperaceae family, accumulates a series of secondary metabolites with interesting biological properties. From a biosynthesis standpoint, this species produces several benzopyrans derived from orsellinic acid, which is a polyketide typically found in fungi. Additionally, the chiral benzopyrans were reported as racemic and/or as diastereomeric mixtures, which raises questions about the level of enzymatic control in the cyclization step for the formation of the 3,4-dihydro-2H-pyran moiety. Therefore, this article describes the use of shotgun proteomic and transcriptome studies as well as phytochemical profiling for the characterization of the main biosynthesis pathways active in P. obtusifolia. This combined approach resulted in the identification of a series of proteins involved in its secondary metabolism, including tocopherol cyclase and prenyltransferases. The activity of these enzymes was supported by the phytochemical profiling performed in different organs of P. obtusifolia. However, the polyketide synthases possibly involved in the production of orsellinic acid could not be identified, suggesting that orsellinic acid may be produced by endophytes intimately associated with the plant. Fil: Batista, Andrea N. L.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil Fil: Dos Santos Pinto, José Roberto A.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil Fil: Batista, Joao M.. Universidade Federal do São Carlos; Brasil Fil: Souza Moreira, Tatiana M.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil Fil: Santoni, Mariana M.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil Fil: Zanelli, Cleslei F.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil Fil: Kato, Massuo J.. Universidade de Sao Paulo; Brasil Fil: López, Silvia Noelí. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Química Orgánica. Área Farmacognosia; Argentina Fil: Palma, Mario S.. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil Fil: Furlan, Maysa. Universidade Estadual Paulista Julio de Mesquita Filho; Brasil

Made available in DSpace on 2020-12-12T01:41:02Z (GMT). No. of bitstreams: 0 Previous issue date: 2019-11-01 Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) Objective: The aim of this study was to investigate the functionality of ATC/TTC (Hap-1) and ATT/TTC (Hap-2) Interleukin (IL) 8 gene haplotypes in the response of neutrophils to Gram-negative bacteria associated with periodontitis. Design: Neutrophils were isolated by gradient centrifugation from whole peripheral blood of systemically healthy individuals presenting the two IL8 gene haplotypes. Neutrophils were stimulated with P. gingivalis, A. actinomycetemcomitans and PMA/ionomycin. Cytokine gene expression (RT-qPCR) and migration/chemotaxis (boyden chamber assay) were compared according to the presence of Hap-1 or Hap-2 haplotypes. Protein production was also evaluted in the multiplex assay using the mixed population of leukocytes present in the whole blood from the same individuals. The influence of these two haplotypes on the IL8 promoter activity was assessed in gene-reporter experiments. Results: Hap-1 haplotype in neutrophils and leukocytes exacerbated the response to stimulation with Gram-negative bacteria, with higher levels of TNF-α (mRNA and protein), IL-1β, IL-2R and IFN-γ (protein) and with increased chemotaxis. Presence of the T allele at the rs4071 polymorphism (alias -251) was associated with increased activity of IL8 proximal promoter. Conclusions: Neutrophils and leukocytes carrying the Hap-1 haplotype (ATC/TTC) in the IL8 gene present an enhanced response to stimulation with Gram-negative bacteria associated with periodontitis. Presence of the T allele (rs4073) in the IL8 proximal promoter increases transcription activity. Department of Oral Diagnosis and Surgery School of Dentistry at Araraquara UNESP- São Paulo State University Department of Clinics and Surgery School of Dentistry Alfenas Federal University (UNIFAL-MG) Department of Biological Sciences School of Pharmaceutical Sciences UNESP- São Paulo State University Department of Microbiology Institute of Biomedical Sciences University of São Paulo Department of Morphology School of Dentistry at Araraquara UNESP- São Paulo State University Department of Oral Diagnosis and Surgery School of Dentistry at Araraquara UNESP- São Paulo State University Department of Biological Sciences School of Pharmaceutical Sciences UNESP- São Paulo State University Department of Morphology School of Dentistry at Araraquara UNESP- São Paulo State University CNPq: #141787/2014-7

Rhipicephalus sanguineus, commonly known as the brown dog tick, is one of the most widely distributed species of tick. In dogs, it can cause anemia and provide the transmission of pathogenic microorganisms such as Babesia canis, Ehrlichia canis, Hepatozoon canis, Anaplasma platys, and Mycoplasma haemocanis. To man, it can transmit the intracellular parasites Rickettsia rickettsii and Rickettsia conorii, the causative agents of the Rocky Mountain spotted fever in the Americas and Mediterranean and spotted fever in Europe and North Africa. Its control is performed by applying synthetic formulations composed of pyrethroids; however, continued use of these products results in environmental damage and acquisition of resistance. Alternatively, studies with botanical insecticides have been increasingly recurrent. Therefore, this study aimed to test the efficacy of essential oil of Tagetes patula, a ruderal species widely described in the literature for its insecticidal properties, in engorged females of R. sanguineus by the adults immersion test (AIT) and impregnated paper disk test (IPDT). The essential oil used, through gas chromatography coupled to mass spectrometry, revealed the presence of 55 compounds, being the 4-vinyl guaiacol and gamma terpinene the majority ones. The AIT compared to the IPDT was more efficient in inhibiting oviposition of tick; however, the eggs laid by the females submitted to saturated atmosphere with essential oil, from IPDT, not hatched, interrupted their development cycle. Besides being a pioneer work, the results presented here contributes to new researches, aiming the incorporation of essential oil in an acaricide for use in the environment.

Made available in DSpace on 2018-12-11T17:23:17Z (GMT). No. of bitstreams: 0 Previous issue date: 2016-11-22 Among the biologically active triterpenes, friedelin has the most-rearranged structure produced by the oxidosqualene cyclases and is the only one containing a cetonic group. In this study, we cloned and functionally characterized friedelin synthase and one cycloartenol synthase from Maytenus ilicifolia (Celastraceae). The complete coding sequences of these 2 genes were cloned from leaf mRNA, and their functions were characterized by heterologous expression in yeast. The cycloartenol synthase sequence is very similar to other known OSCs of this type (approximately 80% identity), although the M. ilicifolia friedelin synthase amino acid sequence is more related to β-amyrin synthases (65-74% identity), which is similar to the friedelin synthase cloned from Kalanchoe daigremontiana. Multiple sequence alignments demonstrated the presence of a leucine residue two positions upstream of the friedelin synthase Asp-Cys-Thr-Ala-Glu (DCTAE) active site motif, while the vast majority of OSCs identified so far have a valine or isoleucine residue at the same position. The substitution of the leucine residue with valine, threonine or isoleucine in M. ilicifolia friedelin synthase interfered with substrate recognition and lead to the production of different pentacyclic triterpenes. Hence, our data indicate a key role for the leucine residue in the structure and function of this oxidosqualene cyclase. Instituto de Química Univ. Estadual Paulista UNESP, Rua Prof. Francisco Degni 55 Centro de Pesquisa e Inovaçaõ em Biodiversidade e Fármacos Instituto de Física de Saõ Carlos Universidade de Saõ Paulo Faculdade de Ciências Farmaceûticas Univ. Estadual Paulista-UNESP, Rod. Araraquara-Jaú km 1 Faculdade de Ciências Farmaceûticas Universidade de Saõ Paulo, Avenida do Café s/n Instituto de Química Univ. Estadual Paulista UNESP, Rua Prof. Francisco Degni 55 Faculdade de Ciências Farmaceûticas Univ. Estadual Paulista-UNESP, Rod. Araraquara-Jaú km 1

Plinia cauliflora (Mart.) Kausel, widespread in South America, has edible fruits, and its bark is commonly used against diarrhea and other disorders, on account of its astringency. Because diarrhea is still one of the most important causes of illness and death among children in developing countries, where the population turns to traditional medicine for its treatment, the present study determined the composition of fruit and leaf extracts of P. cauliflora, analyzed the activity against diarrhea by antimicrobial and gastrointestinal motility, and evaluated the cytotoxicity of the extracts. Chemical composition was determined by high-performance liquid chromatograpy-ultraviolet/photodiode array detection. Antimicrobial activity was analyzed by agar diffusion and the microdilution method against etiological agents of diarrhea. The effect on gastrointestinal motility was analyzed using an experimental model in mice. Cytotoxicity was evaluated in vitro with the fibroblast cell line SIRC CCL 60, and leaf extract showed a 50% inhibitory concentration of 0.48 μg/mL. Gallic acid, ellagic acid, and flavonoid derivatives were detected in the extracts. It was observed that fruit and leaf extracts showed some activity against Enterococcus faecalis, Escherichia coli, Salmonella sp., and Shigella sp. However, neither extract had any effect on gastrointestinal motility.

Submitted by Guilherme Lemeszenski (guilherme@nead.unesp.br) on 2013-08-22T18:45:13Z No. of bitstreams: 1 S1984-82502011000300010.pdf: 315527 bytes, checksum: d2b61515500c132321b3c00d4a660ce0 (MD5) Made available in DSpace on 2013-08-22T18:45:14Z (GMT). No. of bitstreams: 1 S1984-82502011000300010.pdf: 315527 bytes, checksum: d2b61515500c132321b3c00d4a660ce0 (MD5) Previous issue date: 2011-09-01 Made available in DSpace on 2013-09-30T19:34:03Z (GMT). No. of bitstreams: 2 S1984-82502011000300010.pdf: 315527 bytes, checksum: d2b61515500c132321b3c00d4a660ce0 (MD5) S1984-82502011000300010.pdf.txt: 38085 bytes, checksum: 18232721cba4db7fd049bb28127136e4 (MD5) Previous issue date: 2011-09-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T15:09:15Z No. of bitstreams: 2 S1984-82502011000300010.pdf: 315527 bytes, checksum: d2b61515500c132321b3c00d4a660ce0 (MD5) S1984-82502011000300010.pdf.txt: 38085 bytes, checksum: 18232721cba4db7fd049bb28127136e4 (MD5) Made available in DSpace on 2014-05-20T15:09:15Z (GMT). No. of bitstreams: 2 S1984-82502011000300010.pdf: 315527 bytes, checksum: d2b61515500c132321b3c00d4a660ce0 (MD5) S1984-82502011000300010.pdf.txt: 38085 bytes, checksum: 18232721cba4db7fd049bb28127136e4 (MD5) Previous issue date: 2011-09-01 Programa de Apoio ao Desenvolvimento Científico da Faculdade de Ciências Farmacêuticas da UNESP (PADC) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) As folhas da espécie brasileira Plinia cauliflora foram utilizadas a fim de se obter um extrato hidroalcoólico e frações ativas proporcionando o desenvolvimento de eficazes formulações farmacêuticas antissépticas. A composição química do extrato etanólico 70%, fração aquosa e acetato de etila foi analisada por cromatografia em camada delgada e teor de fenóis. A atividade antimicrobiana foi testada frente a Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Lactobacillus acidophilus e Candida albicans por difusão em ágar e a concentração inibitória mínima foi determinada por microdiluição. A qualidade microbiológica do extrato foi avaliada para evitar a contaminação das formulações. Foram desenvolvidos um enxaguatório bucal e um creme tópico contendo o extrato sendo que a atividade antisséptica foi ensaiada por difusão em ágar. A estabilidade sensorial e físico-química foram testadas. A cromatografia indicou a presença de terpenos, flavonóides e taninos no extrato e frações, observando-se alto teor de fenóis totais. As amostras vegetais foram ativas contra todos os micro-organismos testados, exceto Lactobacillus acidophilus. Ambas as formulações apresentaram atividade antisséptica e estabilidade. Desta forma, infere-se que as formulações desenvolvidas podem ser utilizadas como antissépticas em infecções de pele, podendo ser mais eficazes no tratamento de candidíase. The leaves of the Brazilian species Plinia cauliflora were used to obtain active hydroalcoholic extract and fractions enabling the development of efficient antiseptic pharmaceutical formulations. A chemical composition of 70% ethanol extract, aqueous and ethyl acetate fractions was analyzed by thin-layer chromatography and for phenol content. Antimicrobial activity was tested against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Lactobacillus acidophilus and Candida albicans by the agar diffusion method and the minimum inhibitory concentration was assayed by broth microdilution. Extract microbiological quality was tested to avoid contamination in the formulations. A mouthwash and a topical cream containing the extract were developed and antiseptic activity was assessed by agar diffusion. Sensory and physicochemical stability of the formulations were assayed. Chromatography indicated the presence of terpenes, flavonoids and tannins in the extract and fractions and total phenol content were found to be high. The plant samples were active against all the microorganisms tested, except for Lactobacillus acidophilus. Both topical formulations showed antiseptic activity and stability. Thus, these may be used as antimicrobials in skin infections, but would be more useful in the treatment of candidiasis. University Center of Araraquara Faculty of Pharmacy UNESP Faculty of Pharmaceutical Sciences UNESP Faculty of Pharmaceutical Sciences

Foram revisados todos os protocolos de exames histopatológicos, arquivados no Laboratório de Patologia Veterinária da Universidade Federal de Santa Maria (LPV-UFSM), realizados entre janeiro de 2000 e março de 2010, na busca de casos de sarcoide equino. Quarenta casos foram selecionados com o objetivo de determinar os aspectos epidemiológicos e a distribuição anatômica das diferentes formas clínicas deste tumor em equinos no Rio Grande do Sul. Dos casos que tiveram suas idades anotadas nos protocolos, 73,0% (27/37) eram de equinos entre 1 e 5 anos de idade. Múltiplos sarcoides foram observados na maioria dos equinos afetados (29/40 [72,5%]). A forma clínica mais observada foi a fibroblástica, que ocorreu em 42,2% (27/64) dos casos. Em mais da metade dos casos (22/40 [55,0%]), os sarcoides tinham distribuição multifocal. Equinos que apresentavam tumores nos membros totalizaram 22 dos 40 (55%) casos analisados.The files of histopathological exams carried out by the Laboratório de Patologia Veterinária of the Universidade Federal de Santa Maria (LPV-UFSM), between January 2000 and March 2010, were reviewed in search of cases of equine sarcoid. Forty cases were selected to determine epidemiological aspects and anatomical distribution of the various clinical forms of these neoplasms in horses from Rio Grande do Sul. Out of the cases in which the ages were registered in the histopathological reports, 73.0% (27/37) were 1 to 5-year-old horses. Multiple sarcoids were observed in most of the affected horses (29/40 [72.5%]). The fibroblastic form was most frequently observed and occurred in 42.2% (27/64) of the cases. In more than half of the cases (22/40 [55.0%]), sarcoids had a multifocal distribution. Twenty two (55%) out of the 40 horses evaluated had the tumors in the limbs.

Made available in DSpace on 2022-04-28T19:01:45Z (GMT). No. of bitstreams: 0 Previous issue date: 2015-01-01 Lycopene is a carotenoid found in tomatoes with potent antioxidant activity. The aim of the study was to obtain an extract containing lycopene from four types of tomatoes, validate a quantification method for the extracts by HPLC, and assess its antioxidant activity. Results revealed that the tomatoes analyzed contained lycopene and antioxidant activity. Salad tomato presented the highest concentration of this carotenoid and antioxidant activity. The quantification method exhibited linearity with a correlation coefficient of 0.9992. Tests for the assessment of precision, accuracy, and robustness achieved coefficients with variation of less than 5%. The LOD and LOQ were 0.0012 and 0.0039 μg/mL, respectively. Salad tomato can be used as a source of lycopene for the development of topical formulations, and based on performed tests, the chosen method for the identification and quantification of lycopene was considered to be linear, precise, exact, selective, and robust. University of São Paulo State Faculty of Pharmaceutical Sciences, Araraquara-Jau Highway, Km 1

Licopeno é um carotenóide com potente atividade antioxidante encontrado em grande quantidade no tomate e usado no combate a diversas doenças como doenças cardiovasculares e diferentes tipos de cânceres, incluindo o câncer de próstata. O objetivo desse trabalho foi desenvolver uma emulsão contendo extrato de licopeno obtido do tomate salada e avaliar a citotoxicidade do extrato, a estabilidade, o comportamento reológico, atividade antioxidante e permeação do fitocosmético. O cosmético foi desenvolvido utilizando fase oleosa contendo derivados de Karité e submetido à avaliação da estabilidade físico-química, espalhabilidade, análise térmica, comportamento reológico, qualidade microbiológica, citotoxicidade, atividade antioxidante e testes de permeação e retenção cutânea. Os resultados demonstraram que o fitocosmético é estável, apresenta comportamento reológico desejável para uma formulação tópica e é um produto promissor para ser utilizado no combate à aceleração do envelhecimento cutâneo. Lycopene, a carotenoid and potent antioxidant is found in large quantities in tomatoes. Lycopene combats diseases, such as cardiovascular disease and different types of cancer, including prostate cancer. However, its topical use in emulsion form for the combat of skin aging is under-explored. The aim of the present study was to develop an emulsion containing lycopene extracted from salad tomatoes and evaluate its cytotoxicity, stability, rheological behavior, antioxidant activity and phytocosmetic permeation. The developed cosmetic comprised an oil phase made up of shea derivatives and was evaluated in terms of its physiochemical stability, spreadability, thermal analysis, rheological behavior, microbiological quality, cytotoxicity, antioxidant activity, cutaneous permeation and retention. The results demonstrate that this phytocosmetic is stable, exhibits satisfactory rheological behavior for a topical formula and is a promising product for combating skin aging.

Casos de tripanossomíase por Trypanosoma evansi foram diagnosticados em eqüinos no Rio Grande do Sul entre 2003 e 2004. Em uma propriedade (Propriedade A) com 125 eqüinos, 52 morreram. A Propriedade A recebeu ao redor de 80 éguas de outras propriedades para cobertura. Dessas, 66 adoeceram e 56 morreram após voltarem para suas propriedades de origem. A doença clínica observada em 21 eqüinos caracterizava-se por emagrecimento (apesar de apetite voraz), letargia, incoordenação e instabilidade dos membros pélvicos, atrofia das grandes massas musculares dos membros pélvicos, fraqueza muscular e palidez das mucosas. Exemplares de T. evansi foram observados na corrente sangüínea de 4 eqüinos. Anemia normocítica normo-crômica, com hematócritos que variavam de 15-31%, e leuco-citose por linfocitose associada à presença de linfócitos atípicos foram observadas em vários eqüinos. Altos níveis de anticorpos contra T. evansi foram detectados em 6 eqüinos da Propriedade A. Oito eqüinos desenvolveram um quadro neurológico encefálico caracterizado por andar em círculos, ataxia, cegueira, hiperexcitabilidade, quedas, embotamento, déficits proprioceptivos e desvio da cabeça. Um eqüino desenvolveu "posição de cão sentado". Nas 13 necropsias, havia espleno-megalia, linfadenomegalia, hiperplasia linfóide no baço e linfo-nodo, atrofia das grandes massas musculares dos membros pélvicos, edema e malacia na substância branca e cinzenta do encéfalo. Histologicamente, uma panencefalite devastadora foi observada nos 7 casos e caracterizada por marcado edema, desmielinização, necrose e infiltrado perivascular de 6-10 camadas de células linfoplasmocitárias afetando tanto a substância branca quanto a cinzenta. Muitos plasmócitos do infiltrado inflamatório continham numerosos grânulos eosinofílicos no citoplasma (células de Mott). Lesões semelhantes foram observadas na medula espinhal do eqüino que desenvolveu "posição de cão sentado". Os encéfalos de 5 eqüinos com quadro encefálico foram submetidos à técnica de imunoistoquímica estrepto-avidina-biotina; em todos eles observou-se a marcação de números moderados ou elevados de espécimes de T. evansi pelo anticorpo específico nos espaços intravasculares e na neurópila. Os aspectos epidemiológicos, clínicos, hematológicos e patológicos da tripanossomíase por T. evansi em eqüinos são discutidos.Cases of trypanosomiasis by Trypanosoma evansi were diagnosed in horses in the state of Rio Grande do Sul, Brazil, between 2003 and 2004. In one stud farm (Farm A) with 125 horses, 52 died. Additionally, around 80 mares were sent to Farm A to be bred. Of those, 66 became ill and 56 died after being returned to their farms of origin. Twenty one horses clinically affected by the disease were observed. Clinical signs included loss of weight (despite voracious appetite), lethargy, incoordination and instability of hindlimbs, atrophy of the large muscles of the hindlimbs, muscle weakness and paleness of mucosae. Specimens of T. evansi were detected in the blood drawn from four affected horses. Normocytic normochromic anemia with PCVs ranging from 15 to 31%, leucocytosis due to lymphocytosis associated to large atypical lymphocytes was observed in several affected horses. High levels of antibodies against T. evansi were detected in the serum of six horses from Farm A. Eight horses presented encephalic neurological signs such as circling, ataxia, blindness, excitation, falls, listlessness, proprioception deficits and head tilt. One horse assumed a "dog-seating position". Necropsy findings included muscle atrophy, enlargement and lymphoid hyperplasia of the spleen and lymphnodes, edema and softening of the white and grey matter of the brain. Histologically, an overwhelming necrotizing panencephalitis was observed in the seven horses with encephalic signs. This panencephalitis was characterized by marked edema, demyelination and necrosis and perivascular infiltrates of 6-10 layers of lymphocytes and plasm cells affecting both the white and gray matter. Several plasm cells in the inflammatory infiltrate contained numerous eosinophilic globules in their cytoplasm (Mott cells). Similar histological lesions were observed in the spinal cord of the horse with the "dog-seating position". The brains of five horses with the encephalic signs were submitted to immunohistochemistry stain by the streptavidin-biotin technique. In all of those five brains moderate to abundant specimens of T. evansi in the perivascular spaces and neuropile were marked by the specific antibody. Epidemiological, clinical, hematological, and pathological aspects of equine trypanosomiasis caused by T. evansi are discussed.

The growing list of drug-resistant microorganisms and the persistence of deaths due to diarrhea are compelling reasons to study plants in search of new therapeutic agents. The chemical constitution and popular use of the edible fruits of Campomanesia xanthocarpa O. Berg motivated this study to assess the antimicrobial and antidiarrheal properties of the fruits. An extract in 70% ethanol was prepared, and its antimicrobial activity was tested against several strains of bacteria by the agar diffusion and microdilution methods. Antidiarrheal activity was analyzed by testing intestinal motility in an animal model. Preliminary phytochemical study indicated the presence of flavonoids, saponins, and tannins in the hydroalcoholic extract. Antimicrobial activity was significant, but the minimum inhibitory concentration proved to be higher than the maximum extract concentration tested. The extract did not show significant activity for intestinal motility. Although this fruit extract did not show great results as an antimicrobial or antidiarrheal agent, the study contributes to the search for new plant agents and could be referred to as a research protocol by investigators in this area.

Submitted by Guilherme Lemeszenski (guilherme@nead.unesp.br) on 2013-08-22T18:57:48Z No. of bitstreams: 1 S0102-695X2010000300023.pdf: 674638 bytes, checksum: 61ca55c32d25b8981ecd6e767e09c8cd (MD5) Made available in DSpace on 2013-08-22T18:57:48Z (GMT). No. of bitstreams: 1 S0102-695X2010000300023.pdf: 674638 bytes, checksum: 61ca55c32d25b8981ecd6e767e09c8cd (MD5) Previous issue date: 2010-07-01 Made available in DSpace on 2013-09-30T19:52:53Z (GMT). No. of bitstreams: 2 S0102-695X2010000300023.pdf: 674638 bytes, checksum: 61ca55c32d25b8981ecd6e767e09c8cd (MD5) S0102-695X2010000300023.pdf.txt: 27564 bytes, checksum: 76aa514e07e29f5a3cc3dbce9c0a006b (MD5) Previous issue date: 2010-07-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T13:24:42Z No. of bitstreams: 2 S0102-695X2010000300023.pdf: 674638 bytes, checksum: 61ca55c32d25b8981ecd6e767e09c8cd (MD5) S0102-695X2010000300023.pdf.txt: 27564 bytes, checksum: 76aa514e07e29f5a3cc3dbce9c0a006b (MD5) Made available in DSpace on 2014-05-20T13:24:42Z (GMT). No. of bitstreams: 2 S0102-695X2010000300023.pdf: 674638 bytes, checksum: 61ca55c32d25b8981ecd6e767e09c8cd (MD5) S0102-695X2010000300023.pdf.txt: 27564 bytes, checksum: 76aa514e07e29f5a3cc3dbce9c0a006b (MD5) Previous issue date: 2010-07-01 Atualmente, as plantas medicinais movem altos valores financeiros em todo o mundo e representam o tipo de tratamento mais acessível para cerca de 80% da população, principalmente entre os países em desenvolvimento. Entretanto, existe ainda uma falta de conhecimento sobre propriedades químicas, farmacológicas e toxicológicas a fim de assegurar a eficácia e segurança das plantas medicinais. Os critérios de eficácia e segurança de plantas medicinais estão relacionados a qualidade, isto é, as plantas necessitam ser corretamente identificadas, cultivadas e coletadas, devem estar livres de material estranho, partes de outras plantas e contaminações inorgânicas e/ou microbianas. O objetivo deste estudo foi o de elucidar os diferentes processos e padronizações sobre o controle de drogas vegetais, principalmente no Brasil. Nowadays medicinal plants move high financial values at the world and represent a type of treatment more accessible for about 80% of people, mainly among developing countries. However, there is a lack of knowledge about chemical, pharmacological and toxicological properties towards ensure their efficacy and safety. Efficacy and safety criteria of medicinal plants are related to quality, that is, the plants need to be correctly identified, cultivated and harvested, they must be free of strange material, part of other plants and inorganic and/or microorganisms contamination. The aim of this study was to elucidate different process and standardizations about quality control of vegetal drugs mainly in Brazil. Universidade Estadual Paulista Júlio de Mesquita Filho Faculdade de Ciências Farmacêuticas Pós-graduação em Ciências Farmacêuticas Universidade Estadual Paulista Júlio de Mesquita Filho Faculdade de Ciências Farmacêuticas Pós-graduação em Ciências Farmacêuticas

Background Cellulose is a homopolysaccharide composed of extracellular D-glucose monomers connected by glycosidic linkages in b-1,4 conformation which can be synthesized by a variety of living organisms, possessing numerous applications in food, pharmaceutical, medical area, etc.[1][2]. In 1990, cellulose synthase operon encoding four proteins required for bacterial cellulose (BC) biosynthesis by Gluconacetobacter hansenii was isolated. It was demonstrated that these genes bcsA, bcsB, bcsC and bcsD were, together, required for maximum production of celulose [3]. Later, researches identified other relevant regions for bacterial cellulose biosynthesis that occur upstream (cmcax and ccpAx genes) and downstream of the operon (bglx gene) [4]. In this study, we aimed to clone the most important genes related to the BC synthesis. With the purpose of cloning those genes, the genomic DNA of the mentioned microorganism was extracted and proceeded with the amplification of cmcax, ccpAx and cellulose synthase operon genes. Later, the genes were ligated to a cloning vector, transformed in Escherichia coli and the identity of the clones was confirmed by sequencing and comparing with the GenBank using Blastn tool. The cloning achievement of the operon and upstream genes from G. hansenii and their overexpression will enable studies on BC synthesis improvement.

In this work, chemical and biological activities of crude extracts obtained with 50% ethanol, 70% ethanol, acetone:water (7:3; v/v) and chloroform of Plinia cauliflora (DC.) Kausel, Myrtaceae, leaves, a native tree from several regions of Brazil, was investigated. Histochemical and phytochemical screenings were done according to characterization reactions and thin layer chromatography. To assist in extracts standardization, total phenol and flavonoids content spectrophotometric was performed. Antioxidant activity was analyzed by percentage of radical scavenging using DPPH solution. Antimicrobial activity was evaluated against Gram-positive, Gram-negative pathogenic bacteria and species of Candida using agar diffusion and minimal inhibitory concentration (MIC) determination methods according to standard methods. The leaves presented lipids at secretory cavity and phenols, mainly tannins, in nervures and palisade parenchyma. Polar extracts showed flavonoids, tannins and high content of phenols and flavonoids. The extracts showed great antioxidant activity and antimicrobial activity was better against Candida species than against bacteria.