Pectis brevipedunculata is native species and widely available in dry and semi-arid ecosystems showing high biotechnological potential. The objective of this study was to evaluate the circadian and seasonal chemical variation of the essential oil (EO) of P. brevipedunculata, as well as its acaricide effect on Rhipicephalus microplus larvae. Aerial parts were collected and submitted to the hydrodistillation process, and the chemical composition was determined by gas chromatography mass spectrometry (GC-MS). For the assays with R. microplus, the larval immersion test was performed. The main constituents were citral (75% of the EO), followed by α-pinene and limonene. In the seasonality analysis, the highest yields were in the months of April (2.08%) and August (2.05%), while in the study of circadian rhythm, the percentage was 2.0% at 6 p.m. in the rainy season, and 1.2%, dry season at 6 p.m. Concerning acaricidal activity (50% lethal concentration (LC50)), the April (1.17 mg mL-1), March (1.28 mg mL-1), June (1.37 mg mL-1), and October (1.27 mg mL-1) oils obtained were the most active and assays performed with circadian rhythm revealed in the rain season (April) at 6 p.m. and dry season (September) at 12 a.m. LC50 values of 1.75 and 1.75 mg mL-1, respectively. Additionally, this EO is selective to non-target organisms, i.e., ladybeetles and lacewing.

Essential oils from the leaves, stems, flowers and fruits of Melaleuca leucadendra growing in the state of Pernambuco, Brazil, were analyzed using gas chromatography-mass spectrometry (GC-MS). The effects of the oils and their major constituent were evaluated on the agricultural pests Tetranychus urticae and Plutella xylostella in different stages of development. The analysis revealed a M. leucadendra chemotype rich in (E)-nerolidol (81.78 ± 0.90 to 95.78 ± 1.20%). P. xylostella was more susceptible to the oils and major constituent than T. urticae. The fruit oil was 1.5-fold more toxic than the leaf oil to T. urticae eggs. (E)-Nerolidol was 5.5-fold and 4.5-fold more toxic to T. urticae adults than the leaf and fruit oils, respectively. Azamax® used as the positive control was more efficient than the oils and (E)-nerolidol against T. urticae. However, the oils and (E)-nerolidol were more toxic to P. xylostella than Azamax®.

Melissopalynological, physicochemical analysis, mineral content, antiradical activity and profile of compounds by Ultra-Performance Liquid Chromatography coupled with a Diode Array Detector and quadrupole Time of Flight Mass Spectrometry (UPLC-DAD-qTOF-MS/MS) of Frieseomelitta doederleini honeys from semiarid region of the Northeast of Brazil are presented. The melissopalynological analysis showed two principal pollen types of Mimosa tenuiflora (jurema preta) and Shinus sp (aroeira). The chemical profile data obtained by UPLC-DAD-qTOF-MS/MS of the Mimosa tenuiflora flowers (principal pollen of honey) and the five samples of F. doederleini honeys both flowers and honey showed similar profile. Abelha branca honeys samples had similar characteristic profile of phenolic compounds (flavonoids), and also antiradical activity. The main flavonoids identified in the honey samples in the jurema preta flowers were flavonols/flavone and flavanols/flavanones aglycones. All the flavonoids identified showing that the nectar collected by the bees may be from this plant species. The antiradical activity of the honey samples strongly correlated with their phenolic content. Among the minerals analyzed, potassium was the most abundant, followed by magnesium.

A modified and efficient Knoevenagel condensation procedure was developed to synthesize the title compounds using β-alanine and acetic acid as catalysts, showing good to excellent yields. We used lawsone with suitable aliphatic aldehydes including isobutyraldehyde, 3-methyl-butyraldehyde, 2-ethylbutyraldehyde, phenylacetaldehyde, 2-phenyl-propionaldehyde, among others. These compounds were submitted to cytotoxic screening against three tumor cell lines presenting good to excellent cytotoxic profiles.

Uma série de derivados 2,3-diino-1,4-naftoquinona foi sintetizada a partir do 2,3-dibromo1,4-naftoquinona e diversos alquinos terminais funcionalizados usando a reação de acoplamento de Sonogashira catalisada por paládio. Os compostos foram submetidos à avaliação do potencial citotóxico em três linhagens de células tumorais, OVCAR-8 (ovário), PC-3M (próstata) e NCI-H358M (pulmão), apresentando, no geral, resultados satisfatórios para inibição do crescimento celular.

A series of 2,3-diyne-1,4-naphthoquinone derivatives was synthesized from 2,3-dibromo1,4-naphthoquinone and various functionalized terminal alkynes using palladium-catalyzed Sonogashira cross-coupling reaction. The diynes were evaluated as potential cytotoxic agents against three tumor cell lines: human ovarian adenocarcinoma (OVCAR-8), human metastatic prostate cancer (PC-3M) and human bronchoalveolar lung carcinoma (NCI-H358M), presenting, in general, satisfactory results for inhibition of cell growth.

O lapachol, α e β-lapachona são naftoquinonas obtidas de espécies de Tabebuia, apresentam propriedades antiinflamatória, antibacteriana, anticâncer e tripanossomicida. O objetivo deste trabalho foi investigar um possível efeito espasmolítico destas naftoquinonas em íleo de cobaia, uma vez que, outras naftoquinonas inibem a atividade contrátil de músculos lisos. O lapachol, α e β-lapachona inibiram as contrações fásicas induzidas tanto por carbacol (CI50 = 1,5 ± 0,2 x 10-4; 7,3 ± 0,9 x 10-5 e 3,2 ± 0,5 x 10-5 M, respectivamente) quanto por histamina (CI50 = 3,6± 0,5; 3,6 ± 0,7 e 3,3 ± 0,6 x 10-5 M, respectivamente). Estes compostos também relaxaram o íleo pré-contraído com KCl (CE50 = 1,2 ± 0,4; 4,3 ± 0,8 e 2,7 ± 0,2 x 10-5 M, respectivamente); carbacol (CE50 = 2,6 ± 0,7; 3,5 ± 0,5 e 2,2 ± 0,7 x 10-5 M, respectivamente) ou histamina (CE50 = 3,0 ± 0,8; 1,1 ± 0,3 e 3,3 ± 0,6 x 10-5 M, respectivamente) de maneira dependente de concentração. Este efeito é provavelmente devido à inibição do influxo de Ca2+ através dos canais de Ca2+ dependentes de voltagem (CaV). β-lapachona antagonizou (pD'2 = 5,73 ± 0,12; "slope" = 1,51 ± 0,05) as contrações induzidas por CaCl2 em meio despolarizante nominalmente sem Ca2+. O achado de que a β-lapachona inibiu as contrações tônicas induzidas por S-(-)-Bay K8644 (CE50 = 1,4 ± 0,1 x 10-5 M) é sugestivo que o CaV envolvido é o do tipo L. Em conclusão, lapachol, α e β-lapachona apresentam atividade espasmolítica não seletiva em íleo de cobaia, e β-lapachona exerce este efeito pelo bloqueio dos canais CaV tipo L.

Lapachol, α and β-lapachone are naphthoquinones extracted from species of Tabebuia that have shown antiinflammatory, antibacterial, anticancer and trypanosomicidal properties. The aim of this work was to investigate the spasmolytic effect of these naphthoquinones on the guinea-pig ileum, since other naphthoquinones are known to depress the contractile activity of smooth muscles. Lapachol, α and β-lapachone inhibited the phasic contractions induced by both carbachol (IC50 = 1.5 ± 0.2 x 10-4; 7.3 ± 0.9 x 10-5 and 3.2 ± 0.5 x 10-5 M, respectively) and histamine (IC50 = 3.6± 0.5; 3.6 ± 0.7 and 3.3 ± 0.6 x 10-5 M, respectively). These compounds also relaxed the ileum pre-contracted with KCl (EC50 = 1.2 ± 0.4; 4.3 ± 0.8 and 2.7 ± 0.2 x 10-5 M, respectively); carbachol (EC50 = 2.6 ± 0.7; 3.5 ± 0.5 and 2.2 ± 0.7 x 10-5 M, respectively) or histamine (EC50 = 3.0 ± 0.8; 1.1 ± 0.3 and 3.3 ± 0.6 x 10-5 M, respectively) in a concentration-dependent manner. This effect is probably due to inhibition of calcium influx through voltage-gated calcium channels (Ca v). β-lapachone antagonized (pD'2 = 5.73 ± 0.12; slope = 1.51 ± 0.05) CaCl2-induced contractions in depolarizing medium nominally without Ca2+. The finding that β-lapachone inhibited the tonic contractions induced by S-(-)-Bay K8644 (EC50 = 1.4 ± 0.1 x 10-5 M) is suggestive that the L-type CaV is involved. In conclusion, lapachol, α and β-lapachone showed non-selective spasmolytic activity in guinea-pig ileum, and β-lapachone exerts this effect by to blockade of L-type CaV channels.

Diante da problemática da resistência microbiana as pesquisas apontam para o uso de novos antibióticos que sejam eficazes ante os patógenos emergentes. Este trabalho objetiva testar frente a bactérias gram-positivas (Staphylococcus aureus), bactérias gram-negativas (Escherichia coli e Pseudomonas aeruginosa) e fungos leveduriformes (Candida albicans), a atividade antimicrobiana e a concentração inibitória mínima (CIM) de fitoconstituintes de Ocotea duckei Vattimo, do lapachol, seus derivados semi-sintéticos, alfa-lapachona, beta-nor-lapachona, beta-lapachona, alfa-nor-lapachona, beta-3-iodo-lapachona e alfa-3-iodo-lapachona, assim como 07 derivados nitrogenados obtidos a partir do lapachol por semi-síntese e de imidas cíclicas similares ao alcalóide filantimida. Os resultados obtidos estimulam o aprofundamento dos estudos para algumas dessas substâncias a exemplo do lapachol e seus análogos que demonstraram atividade antimicrobiana, de modo que os produtos que se apresentaram ativos para S. aureus, foram lapachol e o extrato etanólico de Ocotea duckei, para E. coli foi a iangambina e para a Candida albicans foram as imidas. As demais substâncias não apresentaram atividade antimicrobiana para as cepas testadas.

Regarding the problem of microbial resistance, the researches point to the use of new antibiotic which can be active against the emergent pathogens. This work aims to test the activity against Gram-positive bacteria (Staphylococcus aureus), Gram-negative bacteria (Escherichia coli e Pseudomonas aeruginosa) and leveduriform fungi (Candida albicans), and also the Minimum Inhibitory Concentration (MIC) of the constituent of Ocotea duckei Vattimo, lapachol and its synthetic derivatives alpha-lapachone, beta-nor-lapachone, beta-lapachone, alpha-nor-lapachone, beta-3-iodin-lapachone and alpha-3-iodin-lapachone, as well as seven nitrogenated derivatives of lapachol obtained through semi synthesis. The achieved results stimulate the deepening of the studies for some of theses substances such as lapachol and its analogous which demonstrated antimicrobial activity. The substances which were active against S. aureus, were lapachol and the ethanolic extract of Ocotea duckei Vattimo, against Escherichia coli iangambin and against C. albicans the imides. The other substances did not show any activity against the tested bacteria.

Foi realizado o isolamento do vírus rábico em morcego insetívoro Nyctinomops macrotis capturado próximo à represa Billings e à mata Atlântica, no Município de Diadema, SP (Brasil). A pesquisa do antígeno rábico no tecido cerebral do morcego apresentou resultado positivo na reação de imunofluorescência direta. O isolamento do vírus rábico no tecido cerebral e nas glândulas salivares do morcego foi obtido através da inoculação intracerebral em camundongos. O Município de Diadema não apresentava casos de raiva animal desde 1982, sendo este o primeiro relato da presença do vírus rábico em morcego insetívoro.

The rabies virus was isolated from an insectivorous bat, Nyctinomops macrotis, trapped in Diadema, SP, Brazil, in a public building near a water supply reservoir. Fluorescent antibodies against rabies virus were detected in cerebral tissue and the viral isolation was made after the inoculation of cerebral tissue and salivary gland suspension in mice. There have been no recorded cases of animal rabies in Diadema since 1982, and this is the first isolation of the rabies virus in an insectivorous bat in the city.

Foi realizado o isolamento do vírus rábico em morcego insetívoro Nyctinomops macrotis capturado próximo à represa Billings e à mata Atlântica, no Município de Diadema, SP (Brasil). A pesquisa do antígeno rábico no tecido cerebral do morcego apresentou resultado positivo na reação de imunofluorescência direta. O isolamento do vírus rábico no tecido cerebral e nas glândulas salivares do morcego foi obtido através da inoculação intracerebral em camundongos. O Município de Diadema não apresentava casos de raiva animal desde 1982, sendo este o primeiro relato da presença do vírus rábico em morcego insetívoro.

The rabies virus was isolated from an insectivorous bat, Nyctinomops macrotis, trapped in Diadema, SP, Brazil, in a public building near a water supply reservoir. Fluorescent antibodies against rabies virus were detected in cerebral tissue and the viral isolation was made after the inoculation of cerebral tissue and salivary gland suspension in mice. There have been no recorded cases of animal rabies in Diadema since 1982, and this is the first isolation of the rabies virus in an insectivorous bat in the city.