ABSTRACT
Perforalactoneâ A (1), a new 20S quassinoid with a unique cagelike 2,4-dioxaadamantane ring system and a migrated side chain, was isolated from the plant Harrisonia perforata together with two biosynthetically related new quassinoids. The structures of these natural products were elucidated by NMR spectroscopy, X-ray diffraction analysis, computational modeling, and the CD excitation chirality method. The compounds exhibited notable biological properties, including insecticidal activity against Aphis medicaginis Koch and antagonist activity at the nicotinic acetylcholine receptor of Drosophila melanogaster. The structural features of these compounds may be related to their promising biological characteristics. Their biosynthesis and an alternative origin of quassinoid-type natural products are also discussed.
Subject(s)
Biological Products/pharmacology , Coleoptera/drug effects , Insecticides/pharmacology , Quassins/pharmacology , Receptors, Nicotinic/metabolism , Simaroubaceae/chemistry , Animals , Biological Products/chemistry , Biological Products/metabolism , Dose-Response Relationship, Drug , Drosophila melanogaster/chemistry , Drosophila melanogaster/metabolism , Insecticides/chemistry , Insecticides/metabolism , Molecular Conformation , Quassins/biosynthesis , Quassins/chemistry , Simaroubaceae/metabolism , Structure-Activity RelationshipABSTRACT
RESUMO A susceptibilidade dos conceptos a agentes químicos varia muito em cada estágio do desenvolvimento. Devido a isto, a maioria dos países passou a exigir a análise do potencial para afetar todos os aspectos da reprodução (espermatogênese, acasalamento, prenhez, parto e lactação) para o desenvolvimento de novos medicamentos e fitoterápicos. O presente trabalho objetivou avaliar o efeito do extrato hidroetanólico de Simaba ferruginea St. Hil (calunga) (EHSF) v.o., em ratas da linhagem Wistar tratadas durante a prenhez e verificar a interferência no desenvolvimento intra-uterino da prole. As ratas foram tratadas com EHSF 50 e 100 mg Kg-1 ou água destilada, do seguinte modo: a) do 1º ao 6º dia de prenhez (período da formação do blastocisto e implantação); b) do 8º ao 16º dia de prenhez (fase embrionária de organogênese); c) do 15º ao 19º dia de prenhez (fase do desenvolvimento fetal). O tratamento do 1º ao 6º dia, mostrou redução no número de fetos com ambas doses e não alterou o peso do útero / ovário nem peso corporal das mães. Quando as ratas foram tratadas na fase da organogênese verificou-se, redução estatisticamente significante do número de fetos vivos com a dose 50 mg Kg-1, e o aparecimento de fetos mortos em 30% das fêmeas tratadas com EHSF 50 mg Kg-1 e em 20% nas fêmeas tratadas com a dose de 100 mg Kg-1, não houve alteração no peso do útero / ovário nem no peso corporal das matrizes. Finalmente, o tratamento no período fetal não afetou o número de filhotes vivos, não provocou malformações anatômicas visíveis a olho nu, nem reabsorção fetal; porém, observou-se que 10% das mães tratadas com 50 mg Kg-1 apresentaram 2 fetos mortos e 20% das mães tratadas com 100 mg Kg-1 apresentaram, em média, 4 fetos mortos. Com estes dados, pode ser concluído que o EHSF apresenta baixa ou nenhuma toxicidade materna para ratas Wistar, embora seja letal para alguns descendentes, independente da fase da prenhez em que foram realizados os tratamentos ...
ABSTRACT The susceptibility of concepts to chemical agents varies a lot at each development stage. Because of that, most countries started requiring the analysis of potential to affect all aspects of reproduction (spermatogenesis, mating, pregnancy, birth and lactation) for the development of new drugs and herbal medicines. This study aimed to evaluate the effect of the hydroethanolic extract of Simaba ferruginea St. Hil ("calunga") (EHSF) on female Wistar rats treated during pregnancy in order to check the interference on the intrauterine development of the offspring. The rats were treated with EHSF 50 and 100 mg/kg-1or distilled water, as follows: a) from day 1 to day 6 of pregnancy (period of blastocytes formation and implantation); b) from day 8 to day 16 of pregnancy (embryonic phase of organogenesis); c) from day 15 to day 19 of pregnancy (fetal development phase). The treatment from day 1 to day 6 showed reduction on the amount of fetuses with both doses and it did not alter neither the weight of the uterus / ovary nor the body weight of the mothers. When the female rats were treated in the organogenesis phase, it was verified both statistical significant decrease on the number of live fetuses for the 50 mg / Kg-1, and also appearance of dead fetuses in 30% of the female rats treated with EHSF 50 mg / Kg-1. In 20% of the female rats treated with 100 mg / Kg-1, there was no alteration neither in the weight of the uterus / ovary or in the body weight of the matrixes. Finally, the treatment in the fetal period did not affect the number of live descendants, or caused anatomical malformations visible to naked eye and fetal reabsorption. However, 10% of the mothers treated with 50 mg / Kg-1presented 2 dead fetuses and 20% of the mothers who had 100 mg / Kg-1showed, on average, 4 dead fetuses. With this data, we can conclude that EHSF presents low maternal toxicity for Wistar rats, although being fatal to some descendants, not mattering in which pregnancy phase the treatments have been performed, being more evident in the earlier phases. For this reason, it is recommended to avoid the use of this plant in pregnancy case.
Subject(s)
Animals , Female , Rats , Rats, Wistar/classification , Simaroubaceae/metabolism , Organogenesis , Reproduction , Pregnancy , Pregnancy, Animal/metabolismABSTRACT
Storage carbon (C) pools are often assumed to contribute to respiration and growth when assimilation is insufficient to meet the current C demand. However, little is known of the age of stored C and the degree to which it supports respiration in general. We used bomb radiocarbon ((14)C) measurements to determine the mean age of carbon in CO2 emitted from and within stems of three tropical tree species in Peru. Carbon pools fixed >1 year previously contributed to stem CO2 efflux in all trees investigated, in both dry and wet seasons. The average age, i.e., the time elapsed since original fixation of CO2 from the atmosphere by the plant to its loss from the stem, ranged from 0 to 6 years. The average age of CO2 sampled 5-cm deep within the stems ranged from 2 to 6 years for two of the three species, while CO2 in the stem of the third tree species was fixed from 14 to >20 years previously. Given the consistency of (14)C values observed for individuals within each species, it is unlikely that decomposition is the source of the older CO2. Our results are in accordance with other studies that have demonstrated the contribution of storage reserves to the construction of stem wood and root respiration in temperate and boreal forests. We postulate the high (14)C values observed in stem CO2 efflux and stem-internal CO2 result from respiration of storage C pools within the tree. The observed age differences between emitted and stem-internal CO2 indicate an age gradient for sources of CO2 within the tree: CO2 produced in the outer region of the stem is younger, originating from more recent assimilates, whereas the CO2 found deeper within the stem is older, fueled by several-year-old C pools. The CO2 emitted at the stem-atmosphere interface represents a mixture of young and old CO2. These observations were independent of season, even during a time of severe regional drought. Therefore, we postulate that the use of storage C for respiration occurs on a regular basis challenging the assumption that storage pools serve as substrates for respiration only during times of limited assimilation.