Abstract Remifentanil is a modern fentanyl analogue with ultrashort-action granted by an esterase-labile methyl propanoate chain. Here, we present the development of a continuous flow methodology for the key N-alkylation step of remifentanil preparation in a biphasic, “slug-flow” regime. We screened parameters under microwave-assisted reactions, translated conditions to flow settings, and obtained remifentanil under 15-min residence time in a 1-mL microreactor, with a space-time yield of 89 mg/mL·h and 94% yield.

RESUMO Bemisia tabaci (Hemiptera: Aleyrodidae) é um inseto polífago que causa danos diretos e indiretos na cultura do tomateiro. A pulverização com inseticidas sintéticos é um dos principais métodos de controle, porém, o uso abusivo dessa ferramenta pode impactar o ambiente e os seres humanos. Este estudo avaliou a bioatividade de extratos de plantas das famílias Asteraceae e Meliaceae sobre B. tabaci biótipo B em tomateiro. Um ensaio preliminar avaliou os efeitos dos extratos a 2% (p/v) sobre a infestação e oviposição dessa mosca-branca. Os efeitos ninficida e ovicida do extrato clorofórmico de Trichilia pallida - TP-Cl em seis concentrações foram avaliados. Finalmente, a TP-Cl CL50 foi estimada. Todos os extratos foram repelentes para a mosca-branca, com exceção de T. pallida (etanólico) e Melia azedarach (hexânico), considerados neutros em 24 h. Todos os extratos causaram deterrência para oviposição. Todas as concentrações de TP-Cl apresentaram atividade ninficida e as maiores promoveram as menores médias de viabilidade de ovos. A CL50 foi de 0,0955%. Os resultados evidenciaram o potencial dos extratos para serem usados como agentes alternativos de controle de B. tabaci biótipo B em tomateiro.

ABSTRACT Bemisia tabaci (Hemiptera: Aleyrodidae) is a polyphagous insect that causes direct and indirect damage on tomato. Spraying with synthetic insecticides is one of the main control tools for the whitefly; however, the abusive use of this tool can impact the environment and human beings. In this study we evaluated the bioactivity of extracts from plant species from Asteraceae and Meliaceae families on B. tabaci biotype B in tomato. A preliminary bioassay evaluated the effects of the extracts at 2% (w/v) on infestation and oviposition of this whitefly. Then, the nymphicidal and ovicidal effects of the chloroformic extract of Trichilia pallida - TP-Cl at six concentrations were performed. Finally, the TP-Cl LC50 was estimated. All extracts were repellent to the whitefly, except that ones from T. pallida (ethanolic) and Melia azedarach (hexanic), considered neutral at 24 h. All the extracts caused deterrence of oviposition. All concentrations of TP-Cl revealed nymphicidal activity and the highest ones provided the lowest egg viability averages. The estimated LC50 was 0.0955%. These results provide evidence for the potential of the extracts to be used as alternative control agents of B. tabaci biotype B in tomatoes.

Abstract Methanolic extracts of the Brazilian endemic ascidian Eudistoma vannamei have been extensively studied for their cytotoxic activity against several human cancer cell lines. Previous work reported the occurrence of purine derivatives and staurosporine alkaloids as the major nitrogen-containing compounds. In this study, we report the occurrence of three pyrimidine alkaloids in addition to cholesterol, sitosterol and stigmasterol.

ABSTRACTThe genus Erythrina, Fabaceae, is widely distributed in tropical and subtropical regions. Their flowers, fruits, seeds and bark are frequently used in folk medicine for its effects on the central nervous system such as anticonvulsant, antidepressant, analgesic, sedative, and hypnotic effects. Erythraline has been reported as one of the active compounds from Erythrina, but until now there are no pharmacokinetics data about this compound and only few results showing a putative metabolism were reported. To improve the information about erythraline metabolism, this article reports and discusses, for the first time, the in vitrometabolism biotransformation of erythraline by cytochrome P450 enzymes.

Four goyazensolide-type sesquiterpene lactones - lychnofolide, centratherin, goyazensolide and goyazensolide acetate - were thoroughly studied by NMR experimental techniques. ¹H NMR, 13C NMR {¹H}, COSY, HMQC, HMBC, J-res. and NOE experiments were performed to provide the needed structural information. Complete and unequivocal assignment, including the determination of all multiplicities, was obtained for each structure and the data collections are presented in tables.

The species Eremanthus mattogrossensis, known as "veludo do cerrado" (cerrado velvet), is native to the Brazilian Cerrado. Because the amount of metabolites present in plants may be influenced by biological and environmental factors, here we conducted an HPLC-DAD-MS/MS investigation of the metabolite concentrations found in the MeOH/H2O extract of the leaves of this species. The main compounds were identified and quantified, and the metabolites were grouped by chemical class (caffeoylquinic acids, flavonoids, and sesquiterpene lactone). Statistical analysis indicated a straight correlation between the quantity of metabolites and seasonality, suggesting that environmental properties elicit important metabolic responses.

Erythrina verna is a medicinal plant used to calm agitation popularly known as mulungu. We purchased the barks of E. verna from a commercial producer and analyzed the alkaloid fraction of the bark by CG-MS and HRESI-MS. Five erythrinian alkaloids were identified: erysotrine, erythratidine, erythratidinone, epimer, and 11-hydroxieritratidinone. Here we report the compound 11-hydroxieritratidinone for the first time as a natural product.

This work reviews the current literature about the chemical constituents and the biological activities of the subtribe Lychnophorinae (Vernonieae, Asteraceae). The notable secondary metabolites are sesquiterpene lactones of furanoheliangolide (goyazensolide and eremantholide types) and flavonoids. Some of its most investigated activities include its anti-inflammatory, analgesic, antimicrobial and cytotoxic activities, specially for the Lychnophora and Eremanthus species. The data presented on this paper not only displayed the role played by the Lychnophorinae species as a source of bioactive compounds, but also reinforced the need of further studies involving the species of such subtribe.

Chemical investigation of the methanolic extract of the ascidian Didemnum psammatodes has led to the identification of the nucleosides 2'-deoxyuridine (1), thymidine (2), 2'-deoxyinosine (3) and 2'-deoxyguanosine (4), the steroids cholestanol, cholestanone and stigmasterol in mixture and batyl alcohol plus two analogs, 1-heptadecyloxy-2,3-propanediol and 1-nonadecyloxy-2,3-propanediol in mixture. Their structures were proposed by NMR, MS and comparison with literature data and GC-MS analysis.

An overview of the current literature on the chemical processes involved in the ion formation from low molecular weight organic compounds by electrospray ionization mass spectrometry is given.

Some informations about the sesquiterpene lactones isolated from Brazilian species of Vernonia are described, as well the results of tests developed with such compounds with respect to their anti-feedant, molluscicide, antimicrobial and analgesic properties.