Acyclic Sesquiterpenes from the Fruit Pericarp of Sapindus saponaria

Previous studies reported antiprotozoal activities of Sapindus saponaria L. The aim of this work was the evaluation of antileishmanial activity and mechanism of action of extract and fractions of S. saponaria L. Hydroethanolic extract (EHA) obtained from fruit pericarps was fractionated using solid-phase extraction in a reversed phase, resulting in fractions enriched with saponins (SAP fraction) and acyclic sesquiterpene oligoglycosides (OGSA fraction). The activities of EHA, SAP, and OGSA were evaluated by antiproliferative assays with promastigote and intracellular amastigote forms. Cytotoxicity on macrophages and hemolytic activity were also analyzed. Morphological and ultrastructural changes in Leishmania amazonensis promastigotes were evaluated by electron microscopy. Flow cytometry was used to investigate mitochondrial dysfunction and phosphatidylserine exposure. OGSA was more selective for parasites than mammalian J774A1 macrophage cells, with selectivity indices of 3.79 and 7.35, respectively. Our results showed that only the OGSA fraction did not present hemolytic activity at its IC50 for promastigote growth. Electron microscopy revealed changes in parasite flagellum, cell body shape, and organelle size, mainly mitochondria. Flow cytometry analysis indicated mitochondrial membrane and cell membrane dysfunction. OGSA showed antileishmanial activity, resulting in several changes to protozoa cells, including mitochondrial depolarization and early phosphatidylserine exposure, suggesting a possible apoptotic induction

Microdialysis Study of Imipenem Distribution in Skeletal Muscle and Lung Extracellular Fluids of Acinetobacter baumannii-Infected Rats

The aim of this study was to investigate imipenem distribution in muscle and lung interstitial fluids of rats with Acinetobacter baumannii pulmonary infection. By combining microdialysis in blood and tissues, it was possible to demonstrate that free imipenem concentrations were virtually identical in blood, muscle, and lung

Antibacterial activity of extracts and neolignans from Piper regnellii (Miq.) C. DC. var. pallescens (C. DC.) Yunck

The evaluation of the activity of the aqueous and ethyl acetate extracts of the leaves of Piper regnellii was tested against gram-positive and gram-negative bacteria. The aqueous extractdisplayed a weak activity against Staphylococcus aureus and Bacillus subtilis with minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of 1000 µg/ml. The ethyl acetate extract presented a good activity against S. aureus and B. subtilis with MIC and MBC at 15.62 µg/ml. In contrast to the relative low MICs for gram-positive bacteria, gram-negative bacteria were not inhibited by the extracts at concentrations < 1000 mg/ml. The ethyl acetate extract was fractionated on silica gel into nine fractions. The hexane and chloroform fractions were active against S. aureus (MIC at 3.9 µg/ml) and B. subtilis (MIC at 3.9 and 7.8 µg/ml, respectively). Using bioactivity-directed fractionation, the hexane fraction was rechromatographed to yield the antimicrobial compounds 1, 2, 5, and 6identified as eupomatenoid-6, eupomatenoid-5, eupomatenoid-3, and conocarpan, respectively. The pure compounds 1 and 2 showed a good activity against S. aureus with MIC of 1.56 µg/ml and 3.12 µg/ml, respectively. Both compounds presented MIC of 3.12 µg/ml against B. subtilis. The pure compound 6 named as conocarpan was quite active against S. aureus and B. subtilis with MIC of 6.25 µg/ml. The antibacterial properties of P. regnellii justify its use in traditional medicine for the treatment of wounds, contaminated through bacteria infections

Pharmacognostic analysis of Piper regnellii (Miq.) C. DC. var. pallescens (C. DC.) Yunck: botanical aspects and preliminary physical-chemical analysis

Piper regnellii (Miq.) C. DC. var. pallescens (C. DC.) Yunck. (pariparoba), uma planta medicinal que ocorre no Brasil, é popularmente utilizada em casos de ulcerações e irritação da pele. Dados farmacognósticos insuficientes e a grande semelhança entre as espécies de Piper levaram a realização desde trabalho, para o estabelecimento de parâmetros de analise botânica e físico-química da referida espécie. A descrição anatômica foi realizada através de lâminas permanentes e semi-permanentes do caule, folhas e raízes, corados com azul de astra e safranina. Testes histoquímicos e farmacopéicos realizados mostraram a presença de células oleíferas e determinaram os parâmetros para avaliação da qualidade e pureza.Piper regnellii (Miq.) C. DC. var. pallescens (C. DC.) Yunck. (pariparoba), a folk plant of occurrence in Brazil, is popularly used in several cases of ulceration and skin irritation. Owed to insufficient pharmacognostic data about the species and its similarity with other Piper species, the purpose of this work was to establish the botanical aspects and preliminary analysis of physical-chemical parameters. Anatomical description was undertaken by the analysis of semi-permanent and permanent slides made with different sections of leaves, stem and roots, stained with safranin and astra blue. The histochemical and pharmacopoeial tests demonstrated the presence of cells with lipophilic content and determined the parameters than can be used for quality control and purity degree.Colegio de Farmacéuticos de la Provincia de Buenos Aire