Azathioprine is an immunosuppressive drug for several inflammatory disorders. Due to its clinical relevance, to explore the solid-state properties for excipient compatibility in the product quality review process is essential. Fourier transform infrared spectroscopy, powder X-ray diffraction and thermal analysis (thermogravimetry/derivative thermogravimetry (TG/DTG), differential thermal analysis (DTA), and differential scanning calorimetry (DSC)) were applied. The compatibility studies evidenced that starch pregelatinized, colloidal silicon dioxide, and talc are fully compatible with azathioprine. However, stearic acid, magnesium stearate, and mannitol are incompatible after heat supply at temperatures easily reached by industrial processing. The nonlinear Vyazovkin isoconversional treatment performed the kinetic study of the thermal degradation. The activation energies were determined to clarify the influence of each excipient on the thermal drug stability, an essential procedure in the pharmaceutical development, and all over the commercial live span, in Good Manufacturing Practices.

Abstract Anticarsia gemmatalis Hübner, 1818 (Lepidoptera) is a major pest of soybean in the Brazil. It is known that the reduction of proteolytic activity by the ingestion of protease inhibitors reduces digestion and larval development of the insects. Control via inhibition of the digestive enzymes necessitates deeper knowledge of the enzyme kinetics and the characterization of the inhibition kinetics of these proteases, for better understanding of the active centers and action mechanisms of this enzyme. Trypsin-like proteases found in the gut of Anticarsia gemmatalis were purified in a p-aminobenzamidine agarose column. Kinetic characterization showed KM 0.503 mM for the L-BApNA substrate; Vmax= 46.650 nM s-1; Vmax/[E]= 9.256 nM s-1 mg L-1 and Vmax/[E]/KM= 18.402 nM s-1 mg L-1 mM. The Ki values for the inhibitors benzamidine, berenil, SKTI and SBBI were 11.2 µM, 32.4 µM, 0.25 nM and 1.4 nM, respectively, and all revealed linear competitive inhibition. The SKTI showed the greatest inhibition, which makes it a promising subject for future research to manufacture peptide mimetic inhibitors.

Abstract: Twig girdlers have a short adult life and a long larval stage (up to one year in some species). This fact, together with lack of morphological traits to identify the species from the larval stage, poses obstacles for the taxonomic identification and characterization of the many twig girdlers found in the wild. To solve this matter, Random Amplified Polymorphic DNA (RAPD) molecular markers have been applied to identify some insect species and to determine species boundaries. The aim of this study was to identify three species of Oncideres using the RAPD technique. Adults and larvae of O. saga, O. ocularis and O. ulcerosa were collected in Minas Gerais, Brazil. Two RAPD primers were used (OPA-05 and OPB-13), which produced different electrophoretic profiles that were used to construct a UPGMA phenogram. Three groups identified in the analyses accurately separated the three species, based on individuals in two different stages of development (adults and larvae): I: O. saga, II: O. ulcerosa, and III: O. ocularis. Molecular markers, such as RAPD, are valuable tools that help taxonomists in species identification.

Abstract The response of plants to grazing includes the production of chemical defense compounds such as proteases inhibitors and secondary metabolites as flavonoids, which makes them less palatable to feeding and negatively affecting the physiology of insects. The aim of this study was to evaluate the phytochemical response of soybean cultivars (Glycine max (L.) Merrill) resistant (IAC-17, IAC-24) and susceptible (IAC-P1) to insects after mechanical damage. These cultivars were mechanically injured, and after 24 hours samples of these plants were analyzed by HPLC to identify and quantify flavonoids. The flavonoids daidzein, quercetin, and rutin were quantified, with the highest concentration of daidzin in soybean cultivars after mechanical damage. Rutin was biosynthesized by IAC-24. The cultivars IAC-PL1, IAC-17, and IAC-24 did not show a flavonoid response to mechanical damage. The soybean cultivars are not dependent on mechanical damage to produce flavonoids.

Abstract The recognition of protease inhibitors with insecticidal activity is important as a basis for the development of mimetic peptides with potential use as biorational insecticides. We sprayed benzamidine on soybean plants and assessed whether this potent synthetic trypsin-inhibitor has protease inhibitory, insecticidal and deterrent effects on the velvetbean caterpillar Anticarsia gemmatalis Hübner (Lepidoptera: Erebidae). Activity of trypsin inhibition in soybean leaves was increased and total proteolytic activity in the midgut extract from larvae fed on these leaves was reduced by benzamidine. Different concentrations of benzamidine sprayed on the plant caused approximately 50 % of larval mortality, and larval choice and moth preference and oviposition were all negatively affected. Low concentrations of benzamidine increased mortality and hindered insect choice and oviposition as well as higher doses. Since many synthetic protease inhibitors are usually expensive, small doses of benzamidine may be effective to protect soybean against A. gemmatalis attack. Our results highlight the potential of synthetic protease inhibitors for insecticidal and deterrent purposes in insect pest management.

Duguetia furfuracea (St. Hil.) Benth & Hook f. (1862), popularmente conhecida como "sofre-do-rim-quem-quer" e "araticum-seco", é um arbusto da família Annonaceae que ocorre em várias regiões do Brasil. Na medicina popular a infusão de suas folhas e galhos é usada no tratamento de reumatismo e cólica renal, enquanto que o pó da semente é misturado com água para o tratamento de pediculose. Estudos anteriores têm descrito atividades biológicas desta planta com ação citotóxica, antitumoral, tripanomicida, leishmanicida, antiplasmódica e antiprotozoárica. No presente trabalho, a genotoxicidade e citotoxicidade do extrato liofilizado de folhas de Duguetia furfuracea foram avaliadas pelo teste de indução profago λ (Induteste-SOS) e pelo teste do micronúcleo em medula óssea de camundongos. Nossos resultados mostraram que o extrato liofilizado de folhas Duguetia furfuracea não apresentou um aumento na indução do profago λ (P>0,05) no Induteste-SOS e também não foi observado aumento do número de eritrócitos policromáticos micronucleados (P>0,05), no Teste do Micronúcleo, sugerindo ausência de genotoxicidade em ambos os testes. Por outro lado, uma diminuição significativa no número de bactérias, (P<0,05), bem como uma diminuição significativa na relação entre eritrócitos policromáticos e eritrócitos normocromáticos, (P<0,05), foram observadas, mostrando ação citotóxica do extrato liofilizado de folhas de Duguetia furfuracea. Assim, Duguetia furfuracea não apresentou ação genotóxica, mas mostrou um efeito citotóxico em ambos os testes utilizados no presente trabalho.

Duguetia furfuracea (St. Hil.) Benth & Hook f. (1862), popularly known as "sofre-do-rim-quem-quer" and "araticum-seco", is a shrub of the Annonaceae family that occurs in several regions of Brazil. In folk medicine the infusion of its leaves and twigs is used to treat rheumatism and renal colic, whereas the seed powder is mixed with water to treat pediculosis. Previous studies have described biological activities of this plant with cytotoxic, antitumoral, trypanocidal, leishmanicidal, antiplasmodial and antiprotozoal effects. In the present work, genotoxicity and cytotoxicity of Duguetia furfuracea lyophilized leaf extract were evaluated using the prophage λ induction test (SOS-Inductest) and mouse bone marrow micronucleus test. Our results showed that Duguetia furfuracea lyophilized leaf extract did not present an increase either in the induction of prophage λ (P>0.05) using the SOS-inductest or in the micronucleated polychromatic erythrocytes (P>0.05) using the micronucleus test, suggesting absence of genotoxicity in both tests. On the other hand, a significant decrease in the number of bacteria, (P<0.05), as well as a significant decrease in the polychromatic erythrocytes and normochromatic erythrocytes ratio, (P<0.05), were observed, showing the cytotoxic action of Duguetia furfuracea lyophilized leaf extract. Thus, Duguetia furfuracea did not present the genotoxic action, but showed a cytotoxic effect in both assays utilized in the present work.

A seca-da-mangueira, causada pelo fungo Ceratocystis fimbriata, é uma doença endêmica no município de São Fidelis, no norte do Estado do Rio de Janeiro. Ceratocystis fimbriata foi encontrado associado a árvores de pinha (Annona squamosa) apresentando sintomas de seca dos ramos. Isolados obtidos de pinha e manga, originários da mesma região, apresentaram a mesma morfologia e sequências espaçadoras ITS do rDNA similares. Estas seqüências foram também similares a de outros isolados brasileiros de C. fimbriata sensu stricto. Inoculações cruzadas dos isolados de pinha e manga resultaram no desenvolvimento de sintomas em ambas espécies de plantas. Este é o primeiro relato de A. squamosa como hospedeira de C. fimbriata.

Mango branch blight disease, caused by Ceratocystis fimbriata, is endemic to the municipality of São Fidelis in northern Rio de Janeiro State. In addition to mango, C. fimbriata was found associated with sugar apple trees (Annona squamosa) showing symptoms of branch blight in São Fidelis. Sugar apple and mango isolates from the same region had the same morphology and showed similar ITS-rDNA sequences. These sequences were also similar to other Brazilian isolates of C. fimbriata sensu stricto. Cross inoculation of such isolates obtained from diseased sugar apple and mango resulted in diseased symptoms on both plant species. This is the first record of A. squamosa as a host for C. fimbriata.

Tricorynus herbarius (Gorham) é uma potencial praga de livros, especialmente em obras raras devido à composição do papel destas. Há carência de trabalhos referentes à sua biologia, principalmente por se tratar de um inseto que apresenta vários hábitos alimentares, sendo esse estudo uma etapa fundamental para o controle do inseto. Assim, a biologia de T. herbarius foi estudada em insetos mantidos em duas dietas diferentes: papel mata-borrão e farelo de trigo mais levedura de cerveja. Quatro ínstares foram obtidos em ambas dietas. A duração do período larval e a longevidade dos adultos foram mais curtas e a duração do período pupal foi maior quando os insetos foram mantidos em papel mata-borrão. Em ambas dietas a mortalidade foi alta, sempre acima de 50%. A fecundidade observada para as fêmeas foi de 3,3 ± 3,93 ovos/fêmea em papel mata-borrão e 12,1 ± 12,61 em farelo de trigo. A razão sexual foi 0,5 para ambas dietas. A dieta de farelo de trigo mais levedura de cerveja mostrou-se a mais adequada para criação de T. herbarius.

Tricorynus herbarius (Gorham) is a potential bibliophagous insect, especially for rare books due to paper constituents of them. There are few studies with regards to the biology of this insect, perhaps because T. herbarius feeds on different resources, being this study an important feature to control the pest. The biological parameters of T. herbarius were studied in two different diets: blotting paper and wheat meal plus yeast extract. Four instars were obtained on both diets. The length of the larval period and adult longevity were shorter while the pupal period was longer when the insects fed on blotting paper. In both diets mortality was high, over 50%. Female fecundity was 3.3 ± 3.93 eggs per female for blotting paper and 12.1 ± 12.61 for wheat meal plus yeast extract. The sex rate was 0.5 for both diets. Wheat meal plus yeast extract is the best diet for rearing the book borer T. herbarius.