Brazilian Green Propolis: Effects In Vitro and In Vivo on Trypanosoma cruzi

The composition of a Brazilian green propolis ethanolic extract (Et-Bra) and its effect on Trypanosoma cruzi trypomastigotes and other pathogenic microorganisms have already been reported. Here, we further investigated Et-Bra targets in T. cruzi and its effect on experimental infection of mice. The IC50/4 days for inhibition of amastigote proliferation was 8.5 ± 1.8 μg mL−1, with no damage to the host cells. In epimastigotes Et-Bra induced alterations in reservosomes, Golgi complex and mitochondrion. These effects were confirmed by flow cytometry analysis. In trypomastigotes, Et-Bra led to the loss of plasma membrane integrity. The in vitro studies indicate that Et-Bra interferes in the functionality of the plasma membrane in trypomastigotes and of reservosomes and mitochondrion in epimastigotes. Acutely infected mice were treated orally with Et-Bra and the parasitemia, mortality and GPT, GOT, CK and urea levels were monitored. The extract (25–300 mg kg−1 body weight/day for 10 days) reduced the parasitemia, although not at significant levels; increased the survival of the animals and did not induce any hepatic, muscular lesion or renal toxicity. Since Et-Bra was not toxic to the animals, it could be assayed in combination with other drugs. Et-Bra could be a potential metacyclogenesis blocker, considering its effect on reservosomes, which are an important energy source during parasite differentiation

Tendinopathy of the anterior compartment of the ankle

OBJETIVO: Análise retrospectiva da etiopatogenia, diagnóstico e opções de tratamento nos casos de tendinopatias do compartimento anterior do tornozelo (TCAT). MÉTODO: No período de setembro de 1998 a fevereiro de 2009, 13 pacientes foram operados por tendinopatia do compartimento anterior do tornozelo. A casuística constou de 10 pacientes do sexo masculino e três do feminino. O lado direito foi acometido em 12 pés e um do esquerdo. A média de idade foi de 35 anos (15-67). A etiologia foi traumática em oito pacientes e em cinco, degenerativa (atraumática). O tempo médio do diagnóstico ao tratamento foi de 19 meses (1-60) e o seguimento foi de 34 meses (4-127). O diagnóstico foi feito através da história e exame clínico. A ressonância magnética foi realizada em nove pacientes para estadiamento e planejamento. O tratamento cirúrgico foi personalizado para cada caso (sinovectomia, ressecção de ventre muscular, solidarização com o tendão adjacente e enxerto livre de tendão semitendíneo). Para a avaliação dos resultados foram utilizadas as escalas: 1) graduação subjetiva de satisfação, 2) AOFAS e 3) Maryland. RESULTADO: Em relação à escala de graduação subjetiva de satisfação, 12 pacientes satisfeitos e um paciente insatisfeito. A média da escala AOFAS foi de 80 pontos, a média da escala Maryland foi de 86 pontos. CONCLUSÃO: O tratamento cirúrgico é eficaz para recuperação funcional. As técnicas cirúrgicas devem ser personalizadas. A opção do enxerto livre de tendão semitendíneo é eficiente nas falhas maiores que cinco centímetros.OBJECTIVE: To carry out a retrospective analysis of the etiopathogeny, diagnosis and therapeutic options in cases of tendinopathies of the anterior compartment of the ankle. METHOD: 13 patients underwent surgery between September 1998 and February 2009; ten men and three women. The right side was involved in twelve patients and the left in one. The averaging age was 35 years of age (15-67). The etiology was traumatic in eight patients and degenerative (non-traumatic) in five. The average time to diagnosis was 19 months (1 - 60) and the average follow-up time was 34 months (4 - 127). The diagnosis was made by anamnesis and clinical findings. Magnetic resonance imaging was performed in nine patients, for staging and planning. The surgical treatment was personalized in each case (debridement, resection of the muscle, grafting with the adjacent tendon, and free graft of the semitendinosus tendon). The following scales were used for the evaluation: 1) subjunctive satisfaction scale, 2) AOFAS and 3) Maryland. RESULTS: In relation to the subjective satisfaction scale, 12 patients were satisfied and one was dissatisfied. The average AOFAS scale was 80 points, and the average Maryland scale was 86 points. CONCLUSION: Surgical treatment is effective for restoring function. The surgical techniques must also be personalized. The free graft of the semitendinosus tendon option is effective for gaps larger than five centimeters

Gum of Terminalia argentea Mart. Et. Zucc. (Combretaceae) as a Resource in Biotechnology Processes: Chemistry and Toxicity

Biodegradable polymers are in areas such as pharmaceutical, food and bioremediation processes. Isolation, characterization (SEM, FTIR, TGA, Monosaccharide Composition, Zeta Potential), antimicrobial activity and toxicity to Artemia salina and Allium cepa L. from the in natura gummy exudate of Terminalia argentea (GTa) are presented herein. The data show irregular morphology and depressions, bands in 1770, 2112, 1354 cm-1, indicating groups of polysaccharides, amphiphilic character, thermo-degradation above 300 ° C and low water activity (0.6). The assays were negative for S. aureus and E. coli, nontoxic against the bioindicators tested. GTa presented low cost, extracted and isolated in a sustainable way, with possibility of commercial exploitation by communities, since these biopolymers present possibilities of applications as agents in the support of immobilization of enzymes, as sensors in diagnostics, encapsulating material in processes of microencapsulation of drugs and additives in food industries.Polímeros biodegradáveis estão em áreas como a farmacêutica, alimentos e processos de bioremediação. O isolamento, a caracterização (MEV, FTIR, TGA, Composição de monossacarídeos, Potencial Zeta), atividade antimicrobiana e toxicidade frente a Artemia salina e Allium cepa L. do exsudato gomoso in natura de Terminalia argentea (GTa) são aqui apresentados. Os dados mostram morfologia irregular e depressões, bandas em 1770, 2112, 1354 cm-1, indicando grupamentos de polissacarídeos, caráter anfiflitico, termodegradação acima de 300°C e baixa atividade de água (0.6). Os ensaios foram negativos para S. aureus e E. coli, atóxicos frente aos bioindicadores testados. O GTa apresentou-se de baixo custo, extraído e isolado de forma sustentável, com possibilidade de exploração comercial por comunidades, uma vez que estes biopolímeros apresentam possibilidades de aplicações como agentes no suporte de imobilização de enzimas, como sensores em diagnósticos, material encapsulante em processos de microencapsulação de fármacos e aditivos em indústrias de alimentos

Tendinopathy of the anterior compartment of the ankle

Análise retrospectiva da etiopatogenia, diagnóstico e opções de tratamento nos casos de tendinopatias do compartimento anterior do tornozelo (TCAT). No período de setembro de 1998 a fevereiro de 2009, 13 pacientes foram operados por tendinopatia do compartimento anterior do tornozelo. A casuística constou de 10 pacientes do sexo masculino e três do feminino. O lado direito foi acometido em 12 pés e um do esquerdo. A média de idade foi de 35 anos (15-67). A etiologia foi traumática em oito pacientes e em cinco, degenerativa (atraumática). O tempo médio do diagnóstico ao tratamento foi de 19 meses (1-60) e o seguimento foi de 34 meses (4-127). O diagnóstico foi feito através da história e exame clínico. A ressonância magnética foi realizada em nove pacientes para estadiamento e planejamento. O tratamento cirúrgico foi personalizado para cada caso (sinovectomia, ressecção de ventre muscular, solidarização com o tendão adjacente e enxerto livre de tendão semitendíneo). Para a avaliação dos resultados foram utilizadas as escalas: 1) graduação subjetiva de satisfação, 2) AOFAS e 3) Maryland. Em relação à escala de graduação subjetiva de satisfação, 12 pacientes satisfeitos e um paciente insatisfeito. A média da escala AOFAS foi de 80 pontos, a média da escala Maryland foi de 86 pontos. O tratamento cirúrgico é eficaz para recuperação funcional. As técnicas cirúrgicas devem ser personalizadas. A opção do enxerto livre de tendão semitendíneo é eficiente nas falhas maiores que cinco centímetros452141147To carry out a retrospective analysis of the etiopathogeny, diagnosis and therapeutic options in cases of tendinopathies of the anterior compartment of the ankle. 13 patients underwent surgery between September 1998 and February 2009; ten men and three women. The right side was involved in twelve patients and the left in one. The averaging age was 35 years of age (15-67). The etiology was traumatic in eight patients and degenerative (non-traumatic) in five. The average time to diagnosis was 19 months (1 - 60) and the average follow-up time was 34 months (4 - 127). The diagnosis was made by anamnesis and clinical findings. Magnetic resonance imaging was performed in nine patients, for staging and planning. The surgical treatment was personalized in each case (debridement, resection of the muscle, grafting with the adjacent tendon, and free graft of the semitendinosus tendon). The following scales were used for the evaluation: 1) subjunctive satisfaction scale, 2) AOFAS and 3) Maryland. In relation to the subjective satisfaction scale, 12 patients were satisfied and one was dissatisfied. The average AOFAS scale was 80 points, and the average Maryland scale was 86 points. Surgical treatment is effective for restoring function. The surgical techniques must also be personalized. The free graft of the semitendinosus tendon option is effective for gaps larger than five centimeter

Experimental Chemotherapy for Chagas Disease: A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma cruzi Targets of Amidines Derivatives and Naphthoquinones

Chagas disease (CD), caused by Trypanosoma cruzi, affects approximately eight million individuals in Latin America and is emerging in nonendemic areas due to the globalisation of immigration and nonvectorial transmission routes. Although CD represents an important public health problem, resulting in high morbidity and considerable mortality rates, few investments have been allocated towards developing novel anti-T. cruzi agents. The available therapy for CD is based on two nitro derivatives (benznidazole (Bz) and nifurtimox (Nf)) developed more than four decades ago. Both are far from ideal due to substantial secondary side effects, limited efficacy against different parasite isolates, long-term therapy, and their well-known poor activity in the late chronic phase. These drawbacks justify the urgent need to identify better drugs to treat chagasic patients. Although several classes of natural and synthetic compounds have been reported to act in vitro and in vivo on T. cruzi, since the introduction of Bz and Nf, only a few drugs, such as allopurinol and a few sterol inhibitors, have moved to clinical trials. This reflects, at least in part, the absence of well-established universal protocols to screen and compare drug activity. In addition, a large number of in vitro studies have been conducted using only epimastigotes and trypomastigotes instead of evaluating compounds' activities against intracellular amastigotes, which are the reproductive forms in the vertebrate host and are thus an important determinant in the selection and identification of effective compounds for further in vivo analysis. In addition, due to pharmacokinetics and absorption, distribution, metabolism, and excretion characteristics, several compounds that were promising in vitro have not been as effective as Nf or Bz in animal models of T. cruzi infection. In the last two decades, our team has collaborated with different medicinal chemistry groups to develop preclinical studies for CD and investigate the in vitro and in vivo efficacy, toxicity, selectivity, and parasite targets of different classes of natural and synthetic compounds. Some of these results will be briefly presented, focusing primarily on diamidines and related compounds and naphthoquinone derivatives that showed the most promising efficacy against T. cruzi

Brazilian Propolis: Correlation Between Chemical Composition and Antimicrobial Activity

The chemical composition of ethanol extracts from samples of Brazilian propolis (EEPs) determined by HPLC and their activity against Trypanosoma cruzi, Staphylococcus aureus, Streptococcus pneumoniae, Klebisiella pneumoniae, Candida albicans, Sporothrix schenckii and Paracoccidioides brasiliensis were determined. Based on the predominant botanical origin in the region of samples' collection, the 10 extracts were separated into three groups: A (B. dracunculifolia + Auraucaria spp), B (B. dracunculifolia) and C (Araucaria spp). Analysis by the multiple regression of all the extracts together showed a positive correlation, higher concentrations leading to higher biological effect, of S. aureus with p-coumaric acid (PCUM) and 3-(4-hydroxy-3-(oxo-butenyl)-phenylacrylic acid (DHCA1) and of trypomastigotes of T. cruzi with 3,5-diprenyl-4-hydroxycinnamic acid derivative 4 (DHCA4) and 2,2-dimethyl-6-carboxyethenyl-2H-1-benzopyran (DCBEN). When the same approach was employed for each group, due to the small number of observations, the statistical test gave unreliable results. However, an overall analysis revealed for group A an association of S. aureus with caffeic acid (CAF) and dicaffeoylquinic acid 3 (CAFQ3), of S. pneumoniae with CAFQ3 and monocaffeoylquinic acid 2 (CAFQ2) and of T. cruzi also with CAFQ3. For group B, a higher activity against S. pneumoniae was associated DCBEN and for T. cruzi with CAF. For group C no association was observed between the anitmicrobial effect and any component of the extracts. The present study reinforces the relevance of PCUM and derivatives, especially prenylated ones and also of caffeolyquinic acids, on the biological activity of Brazilian propolis

Aferição do pH de diferentes agentes clareadores indicados para o clareamento intracoronário

Objective: to measure pH values of bleaching agents that are indicated to intracoronal bleaching technique in different time intervals. Methods: Each group (G) received five samples (n=5): G1 – distilled water (AD); G2 – hydrogen peroxide (H2O2) 30%; G3 – sodium perborate (PbS) + AD; G4 – PbS + H2O2 30%; G5 – sodium percarbonate (PcS) + AD; and G6 – PcS + H2O2 30%. pH values were stated using a digital pHmeter, in different time intervals: immediately after handling (T0), 24 hours (T1) and 168 hours after handling (T2). The results were submitted to statistical analysis through Kruskal-Wallis and Mann Whitney tests, in this order, allowing multiple comparisons among the groups. To verify the effect of time in each group, Friedman test was applied. Results: In the evaluation of the effect of time in each group, it was observed that G2 presented acid behavior, while the other groups exhibited values close to neutrality or alkaline. Conclusions: H2O2 30% was the only agent that showed acidic behavior in every evaluation time. Meanwhile, PcS + H2O had the highest pH values.Objetivo: Aferir os valores de pH de diferentes produtos clareadores indicados para uso na técnica intracoronária em diferentes intervalos de tempo. Materiais e métodos: Para cada grupo experimental (G), foram preparadas cinco amostras (n=5): G1 – água destilada (AD); G2 – peróxido de hidrogênio (H2O2) a 30%; G3 – perborato de sódio (PbS) + AD; G4 – PbS + H2O2 a 30%; G5 – percarbonato de sódio (PcS) + AD; e G6 – PcS + H2O2 a 30%. O pH foi determinado por um pHmetro digital, em diferentes intervalos de tempo: imediatamente após a manipulação (T0), 24 horas (T1) e 168 horas após a manipulação (T2). Os dados obtidos foram submetidos à análise estatística por meio do teste de Kruskal-Wallis, seguido pelo teste de Mann Whitney para comparações múltiplas entre os grupos. Para verificar o efeito do tempo em cada grupo, foi aplicado o teste de Friedman. Resultados: Na avaliação do efeito do tempo em cada grupo, observou-se que G2 apresentou comportamento ácido, enquanto os demais grupos exibiram valores de pH próximos da neutralidade ou alcalinos. Conclusão: H2O2 30% foi o único agente que apresentou comportamento ácido em todos os tempos de avaliação, e a mistura PcS + H2O foi a que apresentou os maiores valores de pH