Abstract: As a part of our continuing search for insect and arthropod development regulators from Brazilian restinga vegetation of the Rio de Janeiro State, crude extracts, purified fractions and essential oils were submitted to screening tests seeking for biological activities on the development of the insects Rhodnius prolixus, Dysdercus peruvianus, Oncopeltus fasciatus and Rhipicephalus (Boophilus) microplus. Up to now, 102 secondary metabolites have been detected in the fractions, among them monoterpenes, sesquiterpenes and two triterpenes which were obtained from the species, Eugenia sulcata, Pilocarpus spicatus, Manilkara subsericea, Myrciaria floribunda and Zanthoxylum caribaeum. These secondary plant metabolites are considered of interest for the use of studies related to arthropod endocrinology, vector-parasite interaction system, and population control of vector insect and agricultural pest. The observed biological activities were surprisingly high, involving increased mortality, molting and metamorphosis inhibition, paralysis, corporeal deformities, apparition of permanent nymphs, of adultoids and juvenoids, partial or total inhibition of oviposition and egg hatching. These compounds are now being studied further to determine if they may or may not be useful in controlling insect populations and/or interfere with the life cycle and vector transmission of parasites to animal and human populations.

Visando a radioproteção ambiental, baseada no conceito de limite de taxa de dose absorvida, foi desenvolvida uma metodologia de conversão da concentração de atividade de radionuclídeos (Bq kg-1) em taxa de dose absorvida (Gy a-1). O modelo considera apenas a taxa de dose absorvida interna. Essa metodologia foi aplicada ao peixe vermelho-caranho (Lutjanus cyanopterus, Cuvier, 1828) capturado na costa do Ceará e aos radionuclídeos naturais: urânio-238, rádio-226, chumbo-210, tório-232 e rádio-228. As taxas de dose absorvidas foram calculadas por radionuclídeo e por tipo de radiação emitida. A taxa de dose média devida a esses radionuclídeos foi de 5.36 µGy a-1, valor seis ordens de grandeza menor que o valor de limite de taxa de dose absorvida utilizada no presente trabalho (3.65 10³ mGy a-1), e similar ao encontrado na literatura para peixes bentônicos. Ra-226 e U-238 contribuíram com 67% e 22% da taxa de dose absorvida, seguidos de Th-232 com 10%. Já Ra-228 e Pb-210 respondem por menos de 1% da taxa de dose absorvida. Essa distribuição é um pouco diferente do relatado na literatura, onde Ra-226 responde por 86% da taxa de dose absorvida.

A methodology was developed for converting the activity concentration of radionuclides (Bq kg-1) into absorbed dose rate (Gy y-1), aiming an approach to environmental radioprotection based on the concept of standard dose limit. The model considers only the internal absorbed dose rate. This methodology was applied to the cubera snapper fish (Lutjanus cyanopterus, Cuvier, 1828) caught off the coast of Ceará. The natural radionuclides considered were uranium-238, radium-226, lead-210, thorium-232 and radium-228. The absorbed dose rates were calculated for individual radionuclides and the type of emitted radiation. The average dose rate due to these radionuclides was 5.36 µGy y-1, a value six orders of magnitude smaller than the threshold value of absorbed dose rate used in this study (3.65 10³ mGy y-1), and similar to that found in the literature for benthic fish. Ra-226 and U-238 contributed 67% and 22% of the absorbed dose rate, followed by Th-232 with 10%. Ra-228 and Pb-210, in turn, accounted for less than 1% of the absorbed dose rate. This distribution is somewhat different from that reported in the literature, where the Ra-226 accounts for 86% of the absorbed dose rate.

Os extratos brutos e as frações obtidas das sementes de Melia azedarach L. (Meliaceae) foram testados em Musca domestica Linnaeus, 1758 (Diptera: Muscidae). Os bioensaios mostraram inibição no desenvolvimento pós-embrionário das moscas e um significativo aumento do período larva recém eclodida- adulto. Além disso, o peso pupal foi reduzido e a proporção sexual alterada. Foi observada toxicidade para os ovos das moscas.

Crudes extracts and fractions from seeds of Melia azedarach L. (Meliaceae) have been assayed on Musca domestica Linnaeus, 1758 (Diptera: Muscidae). Thus, the post-embryonic development of the flies was reduced and the delay from newly hatched larvae to adults had significant increase. In addition, the pupal weights were reduced and the sexual ratio altered. Toxicity to fly eggs was also observed.

Bioensaios contra ninfas de 5º estádio de Rhodnius prolixus foram conduzidos utilizando-se óleo essencial de Pilocarpus spicatus extraído por hidrodestilação. Os principais resultados podem ser resumidos como se segue: (i) altos níveis de toxicidade e paralisia associados à discreta inibição da muda foram induzidos pela aplicação tópica de 0,5 µL ou 1,0 µL do óleo essencial por inseto; (ii) fagoinibição parcial, altos níveis de inibição da muda, período intermuda prolongado e alto número de insetos paralisados mas ausência de toxicidade foram observados após tratamento oral com 5,0 µL ou 10 µL de óleo essencial de P. spicatus por mL de sangue ingerido. A importância destes resultados em relação a eventos biológicos relevantes em R. prolixus é aqui discutida.

Bioassays against fifth-instar nymphae of Rhodnius prolixus were conducted with essential oil of Pilocarpus spicatus extracted by hydrodistillation. The main results may be summarized as follows: (i) high levels of toxicity and paralysis together with discrete moulting inhibition were caused by topical application of either 0.5 µL or 1.0 µL per insect of the crude essential oil; (ii) partial fagoinhibition, high moulting inhibition, prolonged intermoulting period and high number of paralyzed insects, but no toxicity were observed after oral treatment using either 5 µL or 10 µL of Pilocarpus spilcatus essential oil per mL of ingested blood meal. The importance of these results in relation to the relevant biological events in R. prolixus is herein discussed.

Os glicosídeos cianogênicos são substâncias de defesa encontradas em alguns vegetais, capazes de liberar ácido cianídrico por meio de reações de hidrólise. O presente estudo teve como objetivo avaliar a ocorrência da cianogênese em esporófitos de pteridófitas num afloramento rochoso localizado no Parque Estadual da Serra da Tiririca, Rio de Janeiro, Brasil. Foram analisadas mensalmente durante um ano, folhas férteis, estéreis, jovens (báculos) e caules de 19 espécies de pteridófitas, distribuídas em 13 gêneros e nove famílias. A cianogênese foi caracterizada pelo teste do papel de filtro gotejado com ácido pícrico. Das pteridófitas estudadas, 14 foram pela primeira vez analisadas e 14 espécies apresentaram resultado positivo para a cianogênese. Os resultados encontrados demonstraram haver variação na liberação do ácido cianídrico nas espécies em diferentes partes do vegetal ao longo do período analisado. Microgramma vacciniifolia (Langsd. & Fisch.) Copel. (Polypodiaceae) e Pteridium aquilinum (L.) Kuhn var. arachnoideum (Kaulf.) Brade (Dennstaedtiaceae) mostraram-se cianogênicas durante todo o período analisado.

Cyanogenic glycosides are defense substances found in some plants that are able to produce cyanhydric acid on hydrolysis. The present work aimed to study the occurrence of cyanogenesis in pteridophytes of rocky areas of Pedra de Itacoatiara, State Park of Serra da Tiririca, Rio de Janeiro State. Nineteen species, distributed in 13 genera and nine families have been analyzed monthly, during one year. In each species, the analysis was carried out on fertile leaves, sterile ones, young leaves (croziers) and stems. Cyanogenesis was evidenced using filter paper embedded with picric acid. Among studied species, 14 were analysed here for the first time, and 14 gave a positive picric test. Our results showed variation along time in the production of cyanhydric acid in the vegetal species and parts. The species, Microgramma vacciniifolia (Langsd. & Fisch.) Copel. (Polypodiaceae) and Pteridium aquilinum (L.) Kuhn var. arachnoideum (Kaulf.) Brade (Dennstaedtiaceae) were cyanogenic all along the studied period.

A vegetação fluminense, em particular aquela proveniente da Restinga de Jurubatiba, foi investigada por um grupo multidisciplinar de botânicos, químico, radiobiólogo, fisiologistas de insetos e geneticista. Amostras de 564 espécimes foram coletadas, identificadas, organizadas em herbário e um banco de dados está sendo elaborado contendo, além das clássicas informações botânicas, dados químicos e indicações quanto ao uso econômico potencial destas plantas, em paisagismo, como alimentos alternativos ou como plantas medicinais. Estudos fitoquímicos da Guttiferae, Clusia hilariana, forneceram ácido oleanólico e nemorosona. Estes metabólitos foram ensaiados no barbeiro Rhodnius prolixus, vetor da doença de Chagas. Por fim, observou-se que plantas aquáticas apresentaram teores muito altos do radionuclídeo natural, polônio-210, fato este que parece estar relacionado mais com as condições de solo do que com um aporte atmosférico.

The fluminense vegetation, more specifically the flora from the Jurubatiba restinga has been investigated by a multidisciplinary team of botanists, chemist, radiobiologist, insect physiologists and geneticist. Vouchers of 564 specimens have been collected, identified, organized in an herbarium, and a database is being build up containing, in addition to classical botanical data, chemical data and information on the potential economic use either for landscape gardening, alternative foods or as medicinal plants. Phytochemical studies of the Guttiferae, Clusia hilariana, yielded oleanolic acid and nemorosone. Their biological activities against the haematophagous insect Rhodnius prolixus vector of Chagas disease have been investigated. Finally, it has been observed that aquatic plants possessed high levels of the natural radionuclide polonium-210, which seems to be originated mainly from soil rather than from atmospheric supply.

Após 40 anos de intensos esforços, a química de produtos naturais do mar tornou-se um campo maduro. Desde 1995, existem sinais de queda de interesse pela busca de novos metabólitos a partir das fontes tradicionais como macroalgas e octocorais, e uma estabilização do número anual de trabalhos sobre esponjas marinhas. Em franca expansão estão as pesquisas com microorganismos, devido em grande parte às suspeitas de que muitos dos metabólitos de algas e invertebrados poderiam ser produzidos, de fato, pelos microorganismos associados. Estudam-se bactérias e fungos, isolados da água do mar, de sedimentos, algas, peixes e principalmente de invertebrados marinhos como esponjas, moluscos, tunicados, celenterados e crustáceos. Embora seja cedo ainda para definir tendências, pode-se dizer que, na maioria dos casos, os microorganismos produzem metabólitos e até classes de metabólitos bem diferentes daqueles encontrados nos invertebrados hóspedes. Analisando as rotas biogenéticas, observa-se predominância de substâncias nitrogenadas, muitos derivados da via do acetato e poucos terpenóides. Estes são representados por sesquiterpenos, diterpenos e alguns carotenos. Substâncias nitrogenados incluem principalmente amidas, peptídeos cíclicos e alcalóides indólicos.

After 40 years of intensive research, chemistry of marine natural products has become a mature field. Since 1995, there are signals of decreased interest in the search of new metabolites from traditional sources such as macroalgae and octocorals, and the number of annual reports on marine sponges stabilized. On the contrary, metabolites from microorganisms is a rapidly growing field, due, at least in part, to the suspicion that a number of metabolites obtained from algae and invertebrates may be produced by associated microorganisms. Studies are concerned with bacteria and fungi, isolated from seawater, sediments, algae, fish and mainly from marine invertebrates such as sponges, mollusks, tunicates, coelenterates and crustaceans. Although it is still to early to define tendencies, it may be stated that the metabolites from microorganisms are in most cases quite different from those produced by the invertebrate hosts. Nitrogenated metabolites predominate over acetate derivatives, and terpenes are uncommon. Among the latter, sesquiterpenes, diterpenes and carotenes have been isolated; among nitrogenated metabolites, amides, cyclic peptides and indole alkaloids predominate.

210Po concentrations have been determined in one green alga and in five freshwater plants grown in a pond of the Carapebus restinga (State of Rio de Janeiro). The alga Chara sp showed elevated concentration of 210Po, similar to that observed for marine algae. All the other plants had the lowest concentration of 210Po in the stems and the highest in the roots. Intermediate values were observed in the leaves. The unexpected high concentration of 210Po in the roots, even superior to reported values for roots of plants from high radioactive background areas, must be due to the elevated levels of this radionuclide in associated soils that are known to be rich in humic organic material. There seem to have been no translocation of this radionuclide from the roots to the other parts of the plants.

Descreve-se as sínteses de 23 produtos naturais marinhos, realizadas no Brasil ou por químicos brasileiros.

Syntheses of 23 marine natural products carried out in Brazil or by Brazilian chemists are comprehensively reviewed.

A study of the phagoinhibitor and anti-moulting activities of the Brazilian Melia azedarach, collected in the state of Rio de Janeiro, Brazil, allowed the isolation of four lignanes identified as pinoresinol, bis-epi-pinoresinol, the hemicetal and the diacid. These substances are devoid of anti-moulting activity.

This paper recalls the outcoming of marine natural products research and reviews a selection of marirne bioactive metabolites in current use together with promising trends in marine pharmacology.