Manilkara subsericea (Mart.) Dubard (Sapotaceae) is popularly known in Brazil as “guracica.” Studies with Manilkara spp indicated the presence of triterpenes, saponins, and flavonoids. Several activities have been attributed to Manilkara spp such as antimicrobial, antiparasitic and antitumoral, which indicates the great biological potential of this genus. In all, 87.19% of the hexanic extract from fruits relative composition were evaluated, in which 72.81% were beta- and alpha-amyrin esters, suggesting that they may be chemical markers for M. subsericea. Hexadecanoic acid, hexadecanoic acid ethyl ester, (E)-9-octadecenoic acid ethyl ester, and octadecanoic acid ethyl ester were also identified. Ethanolic crude extracts from leaves, stems, and hexanic extract from fruits exhibited antimicrobial activity against Staphylococcus aureus ATCC25923. These extracts had high IC50 values against Vero cells, demonstrating weak cytotoxicity. This is the first time, to our knowledge, that beta- and alpha-amyrin caproates and caprylates are described for Manilkara subsericea.

Myrciaria floribunda (H. West ex Willd.) O. Berg, Myrtaceae, is a native plant species of the Atlantic Rain Forest, from north to south of Brazil. The lyophilized ethyl acetate extract from the leaves of M. floribunda was investigated for its antiproliferative activity in tumor cell lines, antioxidant capacity and its total phenolic, flavonoid and tannin contents. Antiproliferative activity was tested in vitro against seven human cancer cells and against immortalized human skin keratinocytes line (HaCat, no cancer cell). Antioxidant activity was determined using 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging and oxygen radical absorbing capacity (ORAC) assays and total phenolic, flavonoid and tannin contents were determined by spectrophotometric techniques. Ethyl acetate extract of M. floribunda exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 69.70 and 172.10 µg/mL. For HaCat cell, TGI value was 213.60 µg/mL. M. floribunda showed a strong antioxidant potential: EC 50 of 45.89±0.42 µg/mL and 0.55±0.05 mmol TE/g for DPPH and ORAC, respectively. Total phenolic content was 0.23±0.013g gallic acid equivalents (GAE)/g extract and exhibited 13.10±1.60% of tannins content. The content of flavonoid was 24.08±0.44% expressed as rutin equivalents. These results provide a direction for further researches about the antitumoral potential of M. floribunda.

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Monoclonal antibodies (mAb) are high added value glycoproteins recommended for immunotherapy, diagnosis, and also for the treatment of bacterial infections resistant to multiple drugs such as Methicillin Resistant Staphylococcus aureus (MRSA). In addition to environmental conditions related to cell cultures, the intrinsic characteristics of hybridoma cells, like the secretion stability of monoclonal antibodies by the cells through successive subcultures, are relevant for the characterization of cell lines related to the productivity of mAb. The rate of mAb production differs significantly between different cell lines and different passage numbers, and it is an important variable in characterization of cell lines. In order to find a more robust, fastergrowing, and higher-productivity cell line of hybridoma, cultivations in 24-well plates were performed in different subculture periods, or cell passages (P), of hybridoma cells producing MRSA anti-PBP2a monoclonal antibodies ]. The objective of this study was to study the effects of cell growth and production of MRSA-antiPBP2a mAb secreted by murine hybridoma cells grown in different passages as well as determine the which passages the hybridomas can be cultivated without harming their growth and productivity. So, cell growth profiles of hybridomas secreting MRSA-antiPBP2a (mAb) and the production of MRSA-antiPBP2a mAb in different subculture periods or cell passages (P) were studied. Cell growth tests, monoclonal antibody productivity, and metabolite characteristics revealed substantial differences in those cells kept between P10 and P50. Similarities in the secretion of monoclonal antibody, growth, and metabolic profiles, were noted in the MRSA-antiPBP2a mAb producing hybridoma cells kept between P10 and P20. Also, glucose consumption (g/L) and lactate production (g/L) in the latter cell cultures were monitored daily through biochemical analyzer. As of P30, it was observed a 4.4 times reduction in productivity, a 13 % reduction in metabolic yield, and a significant change in cell growth. Secretion of MRSA-antiPBP2a mAb should be obtained through the culture of hybridomas up to P20 in order to keep its stability.

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The Dysdercus peruvianus Guérin-Méneville is commonly known as the cotton stainer bug. In this study, it was evaluated the insecticide activity and mode of action of the essential oil from leaves of Ocotea elegans Mez and its nanoemulsion against D. peruvianus. Leaves of O. elegans were extracted by hydrodistillation. The essential oil obtained was analyzed by gas chromatography coupled with electron impact mass spectrometry and flame ionization detector. The essential oil toxicity measured by lethal dose 50 (LD50) and survival rate of insects were recorded. Lastly, an assay was carried out to assess the inhibition of the enzyme acetylcholinesterase to determine a possible mechanism of action of insecticidal activity. The sesquiterpene sesquirosefuran was the major compound detected and corresponds to 92% of the components of the essential oil. The nanoemulsion more stable showed hydrophilic lipophilic balance (HLB 11.74), droplet size 92±1.80 nm, and polydispersity index (PDI of 0.215±0.015). After the topical application of the O. elegans essential oil, significant decreases in the survival of D. peruvianus occurred in a dose-response manner with LD50 = 162.18 μg and the survival rate of the nanoemulsion in D. peruvianus was 10.0±5.47, a better value than in pure essential oil. The acetylcholinesterase inhibition presented inhibition concentration (IC50 = 1.37mg/mL) and mixed type of inhibition. This indicates that the essential oil of leaves from O. elegans and its nanoemulsion are promising candidates for use in integrated pest management programs.

Neste trabalho, verificou-se a aplicabilidade de uma metodologia computacional para se predizer a estrutura de compostos orgânicos com atividade biológica. Para isso, selecionaramse três floroglucinóis, e compararam-se suas conformações obtidas por modelagem molecular e por difração de raios X. Os resultados mostraram que as conformações obtidas por análise conformacional com o método AM1 seguidas de otimização de geometria utilizando o método DFT (B3LYP/6-31G(d,p)) estão em boa concordância com os dados obtidos experimentalmente por difração de raios X, indicando que a metodologia empregada parece ser uma ótima ferramenta para predizer preferências conformacionais desta classe de compostos.In this work we intend to verify the applicability of a computational methodology to predict structural features of organic compounds with biological activity. We selected three phloroglucinols and compared their calculated conformational data with their X-ray crystallographic structure. The results showed that conformations obtained by conformational analysis with the AM1 method followed by geometry optimization by using the DFT B3LYP/6-31 G(d,p) basis set are in very good agreement with X-ray data, indicating that the methodology employed here seems to be a very useful tool in order to predict the conformational preference for this class of compounds.Keywords: conformational analysis, X-ray, molecular modeling, phloroglucinols IntroductionDespite the development of organic synthesis, biotechnology and combinatorial chemistry, natural plants are still a great source of bioactive compounds. However, just 8% of the Brazilian flora has been already studied in the search for new bioactive substances. 1,2 In the last decades several antibacterial compounds are being less effective in the treatment of infectious diseases due to multi-resistant bacteria.3 In this context medicinal plants are extremely important in the search of new molecules as therapeutic alternatives. The genus Hypericum seems to be a good choice for this problem. It is constituted by flavonoids, xantones and phloroglucinols with considerable pharmacological and biological effects.4,5 Phloroglucinol derivatives have been described in the literature as promising substances with Conformational Analysis of Phloroglucinols from Hypericum Brasiliense J. Braz. Chem. Soc. 838 high antibacterial activity. [6][7][8][9] The Hypericum brasiliense presents three phloroglucinols in its constitution and they are active against bacteria.10,11 These phloroglucinols are the japonicin A, the uliginosin B and the isouliginosin B (Figure 1).The study of conformations of bioactive compounds is very important in the design of new drugs, since that conformational profile may have direct implications in their activity. When the conformational properties of a drug are known to play an important role in establishing its therapeutic value, any newly designed analogue should have similar conformational properties to enhance the probability that it will bind to the receptor target.Nowada...