RESUMOOs objetivos desta pesquisa foram a obtenção e caracterização do óleo essencial de folhas de pimenta longa Piper hispidinervum, e avaliação de seu efeito no comportamento e/ou mortalidade da lagarta-do-cartucho do milho Spodoptera frugiperda. O óleo essencial foi obtido pela técnica "arraste a vapor d'água", utilizando-se de um aparelho de Clevenger modificado, e posteriormente submetido, à análise por CG-EM e CG. Foram realizados testes de ingestão e contato tópico em lagartas de 1° e 3° ínstar. Os resultados constataram que o óleo essencial de pimenta-longa possui atividade inseticida sobre S. frugiperda, causando redução alimentar e mortalidade, sendo o safrol (82%) seu constituinte majoritário. Verificou-se mortalidade no teste de ingestão em lagartas de 1° ínstar com CL 50 = 16,2 mg/mL e para lagartas de 3° ínstar a CL 50 = 9,4 mg/mL com redução alimentar CD 50 = 0,72 mg/mL; e de toxicidade aguda no teste de contato tópico com DL 50 = 277,91 μg/lagarta, após o intervalo de tempo de 96 horas, sendo também observados sintomas de neurotoxicidade, como o efeito knock-down. PALAVRAS-CHAVE:Lagarta-do-cartucho, Safrol, Manejo integrado de pragas.Insecticidal Activity of Long-pepper essential oil (Piper hispidinervum C. DC.) on fall armyworm Spodoptera frugiperda (J. E. Smith, 1797) (Lepidoptera: Noctuidae) ABSTRACT The objectives of this research were to evaluate the chemical composition and bioactivity of the essential oil from the longpepper leaves (Piper hispidinervum) and its effect on the comportment and/or mortality of the fall armyworm (Spodoptera frugiperda). The essential oil was obtained by steam stream distillation, using the modified Clevenger apparatus, the chemical composition was analyzed by GC-MS and GC. Tests of ingestion and topical application in fall armyworm of 1 st and 3 rd ínstar were made. The results showed that the long-pepper essential oil has insecticide activity on S. frugiperda, causing mortality and food reduction, and safrole (82%) as its majority constituent. Mortality was found in the ingestion test in larvae of 1 st ínstar LC 50 = 16.2 mg/mL for larvae of 3 rd ínstar LC 50 = 9.4 mg/mL, with reduced food CD 50 = 0.72 mg/mL; and acute toxicity test of the contact topic with LD 50 = 277.91 μg/larvae, after an interval of 96 hours, neurotoxicity symptoms were also observed, as knock-down effect.

The chemical composition of Lippia sidoides essential oils obtained by hydrodistillation was characterized and quantified by GC/MS and their insecticidal activity by fumigation test was assayed against Tenebrio molitor. Moreover, the toxicity of monoterpenes carvacrol, 1,8-cineol and thymol were also evaluated when applied alone or in binary (1:1) or tertiary (1:1:1) mixture. The essential oil of L. sidoides has as major constituents carvacrol (31.68%), -cymene (19.58%), 1,8-cineole (9.26%) and -terpinene (9.21%), from a 21 compounds identified, being 92.53% of total. Both compounds have insecticidal activity against T. molitor, being the degree of toxicity of carvacrol > 1,8-cineole > L. sidoides essential oil > thymol, and its respectively LC 50 at 24h were 5.53; 5.71; 8.04 and 14.71 µL/L air. When the different mixture of carvacrol, 1,8-cineole and thymol was assayed against T. molitor, the synergism among them was observed. For the mixture of carvacrol:1,8-cineole LC 50 was 5.34 µL/L air; carvacrol:thymol 7.67 µL/L air; 1,8-cineole:thymol 7.51 µL/L air and carvacrol:1,8-cineole:thymol 6.34 µL/L air. Mainly, the monoterpene thymol had a synergic effect, which increased the toxicity of carvacrol and 1,8-cineole, both in binary mixture like carvacrol:thymol and 1,8-cineole:thymol.Index terms: "Alecrim pepper", mealworm, natural compound, toxicity, synergism. RESUMOA composição química do óleo essencial de Lippia sidoides obtido por hidrodestilação foi caracterizada e quantificada por GC/MS, bem como sua atividade inseticida por teste de fumigação foi avaliada sobre Tenebrio molitor. Além disso, a toxicidade dos monoterpenos carvacrol, 1,8-cineol e timol, também foi avaliada quando esses compostos foram aplicados isoladamente, ou em misturas binárias (1:1), ou terciárias (1:1:1). O óleo essencial de L. sidoides tem como principais constituintes o carvacrol (31,68%), ñ-cimeno (19,58%), 1,8-cineol (9,26%) e -terpineno (9,21%), em 21 compostos identificados, sendo 92,53% do total. Termos para indexação: Alecrim pimenta, bicho-da-farinha, produto natural, toxicidade, sinergismo.

Mayaro fever, caused by Mayaro virus (MAYV) is a sub-lethal disease with symptoms that are easily confused with those of dengue fever, except for polyarthralgia, which may culminate in physical incapacitation. Recently, outbreaks of MAYV have been documented in metropolitan areas, and to date, there is no therapy or vaccine available. Moreover, there is no information regarding the three-dimensional structure of the viral proteins of MAYV, which is important in the search for antivirals. In this work, we constructed a three-dimensional model of protein C of MAYV by homology modelling, and this was employed in a manner similar to that of receptors in virtual screening studies to evaluate 590 molecules as prospective antiviral agents. In vitro bioassays were utilized to confirm the potential antiviral activity of the flavonoid epicatechin isolated from Salacia crassifolia (Celastraceae). The virtual screening showed that six flavonoids were promising ligands for protein C. The bioassays showed potent antiviral action of epicatechin, which protected the cells from almost all of the effects of viral infection. An effective concentration (EC) of 0.247 μmol/mL was observed with a selectivity index (SI) of 7. The cytotoxicity assay showed that epicatechin has low toxicity, with a 50% cytotoxic concentration (CC) greater than 1.723 µmol/mL. Epicatechin was found to be twice as potent as the reference antiviral ribavirin. Furthermore, a replication kinetics assay showed a strong inhibitory effect of epicatechin on MAYV growth, with a reduction of at least four logs in virus production. Our results indicate that epicatechin is a promising candidate for further testing as an antiviral agent against Mayaro virus and other alphaviruses.

Recebido em 3/10/11; aceito em 26/2/12; publicado na web em 2/7/12The phytochemical study of hexane/ethyl ether (1:1) extract of the roots of M. imbricata, Celastraceae, resulted in the isolation and characterization of six known triterpenes: 11α-hydroxylup-20(29)-en-3-one, previously isolated from this species besides, 3β,11α-di-hydroxylup-20(29)-ene, 3,7-dioxofriedelane, 3-oxo-29-hydroxyfriedelane, tingenone and 6-oxo-tingenol. The chemical structures of these triterpenes were established by spectrometric data (IR, 1 H and 13 C NMR) and through comparison with literature data. The hexane/ethyl ether (1:1), ethyl acetate and methanol extracts, and 11α-hydroxylup-20(29)-en-3-one, tingenone and 6-oxo-tingenol, showed antimicrobial properties on in vitro assays. All extracts and triterpenes, except 3β,11α-di-hydroxylup-20(29)-ene, presented toxicity demonstrated by the larvicidal effect test using Artemia salina.

No abstract

Plants belonging to the genus Maytenus are routinely used in folk medicine for the treatment of pain diseases. Our previous phytochemical study of the roots of Maytenus imbricata resulted in the isolation and characterization of tingenone, a pentacyclic triterpene. Natural triterpenoids are of growing interest because they have several biological activities, including analgesic properties. The present study assessed the involvement of the opiodergic pathway in the tingenone-induced antinociceptive effect against hyperalgesia induced by prostaglandin E2 (2 µg) in the peripheral pathway. We evaluated the effect of several antagonists to opioid receptors using the mouse paw pressure test. Tingenone administered into the right hind paw induced a local antinociceptive effect that was antagonized by naloxone, a nonselective antagonist to opioid receptors. Clocinnamox, naltrindole, and nor-binaltorphimine are selective antagonists to µ, δ, and κ receptors, respectively, which reverted the peripheral antinociception induced by tingenone. Bestatine acts as an inhibitor of aminopeptidase, an enzyme that degrades endogenous opioid peptides, and was shown to intensify the antinociceptive effect of tingenone. The results suggest that the opioidergic system participates in the peripheral antinociception induced by tingenone.

The results showed that PvHE has beneficial effects and may treat inflammatory and metabolic dysfunction induced by HC diet, that are associated to a negative modulation of the inflammatory process at systemic and local levels.

Substances derived from plants play an important role in the development of new analgesic drugs, among them, triterpenoids. The connection between the participation of L-arginine/NO/cGMP pathway and the activation of ATP-sensitive K(+) channels (KATP) has been established on the peripheral antinociception induced by various drugs. The study assessed the involvement of L-arginine/NO/cGMP/KATP pathway in the antinociceptive effect induced by tingenone, from Maytenus imbricata, against the hyperalgesia evoked by prostaglandin E2 (PGE2) in peripheral pathway. The paw pressure test was used, with hyperalgesia induced by intraplantar injection of PGE2 (2 μg). Tingenone (200 µg/paw) administered into the right hind paw induced a local antinociceptive effect, that was antagonized by l-NOArg, nonselective nitric oxide synthase (NOS) inhibitor and by L-NPA, selective neuronal NOS (nNOS) inhibitor. The L-NIO, selective inhibitor of endothelial (eNOS), and the L-NIL, selective inhibitor of inducible (iNOS), did not alter the peripheral antinociceptive effect of the tingenone. The ODQ, selective soluble guanylyl cyclase inhibitor, prevented the antinociceptive effect of tingenone, and zaprinast, inhibitor of the phosphodiesterase that is cyclic guanosine monophosphate (cGMP) specific, intensified the peripheral antinociceptive effect of the smaller dose of tingenone. Glibenclamide, ATP-sensitive K(+) channels (KATP) blocker, but not tetraethylammonium chloride, voltage-dependent K(+) channel blocker; dequalinium dichloride, blocker of the small conductance Ca(2+)-activated K(+) channel, and paxilline, a potent blocker of high-conductance Ca(2+)-activated K(+) channels, respectively, prevented the peripheral antinociceptive effect of tingenone. The results demonstrate that tingenone induced a peripheral antinociceptive effect by L-arginine/NO/cGMP/KATP pathway activation, with potential for a new analgesic drug.