This extensive review covers research published between 2010 and 2012 regarding new compounds derived from marine sponges, including 62 species from 60 genera belonging to 33 families and 13 orders of the Demospongia class (Porifera). The emphasis is on the cytotoxic activity that bioactive metabolites from sponges may have on cancer cell lines. At least 197 novel chemical structures from 337 compounds isolated have been found to support this work. Details on the source and taxonomy of the sponges, their geographical occurrence, and a range of chemical structures are presented. The compounds discovered from the reviewed marine sponges fall into mainly four chemical classes: terpenoids (41.9%), alkaloids (26.2%), macrolides (8.9%) and peptides (6.3%) which, along with polyketides, sterols, and others show a range of biological activities. The key sponge orders studied in the reviewed research were Dictyoceratida, Haplosclerida, Tetractinellida, Poecilosclerida, and Agelasida. Petrosia, Haliclona (Haplosclerida), Rhabdastrella (Tetractinellida), Coscinoderma and Hyppospongia (Dictyioceratida), were found to be the most promising genera because of their capacity for producing new bioactive compounds. Several of the new compounds and their synthetic analogues have shown in vitro cytotoxic and pro-apoptotic activities against various tumor/cancer cell lines, and some of them will undergo further in vivo evaluation.

The study of chemistry of naturally occurring compounds and the synthesis of their derivatives is fundamentally important for the development of new drugs. In this work, dehydrodieugenol (DHDE) was obtained through oxidative coupling of eugenol, promoted by an aqueous mixture of potassium ferricyanide (K3 [Fe(CN)6 ]) and NH3  · H2 O. The partial methoxylation of DHDE with MeI and K2 CO3 mainly resulted in the molecular-shaped monomethyl ether (DHDE-1MeO) and its dimethyl ether derivative (DHDE-2MeO). The products from the reactions were characterized by (1) H- and (13) C-NMR spectroscopy. Additionally, these studies have reported the antileishmanial activity of DHDE against Leishmania amazonensis (IC50 value of 42.20 μg ml(-1) ) and shown that partial methoxylation of DHDE results in a significant increase in its antiparasitic activity (IC50 value of 13.68 μg ml(-1) ). Based on in vitro bioassays, DHDE-1MeO has shown the highest leishmanicidal activity in promastigota form. Production by direct one-step synthesis of this monomethoxylated compound can be considered to be a cost-effective and environmentally friendly method with a short reaction time.

Abstract:The capacity of simple coconut water, which contains natural peroxidases, to act as a biocatalyst for the oxidative coupling-cyclization of p-(OH)-phenylpropanoids, was evaluated in this work. As a result, dimeric forms of isoeugenol (licarin A) and methyl p-coumarate (methyl dehydrodicoumarate) were obtained. The products of the reactions were characterized by optical rotatory dispersion, and 1 H-NMR and 13 C-NMR spectroscopy. The oxidative coupling-cyclization mechanism for coniferyl alcohol is proposed.

Using classical reactions, the synthesis of seven natural esters was described, including for the first time the synthesis of four natural phenylpropanoid esters proven by preliminary studies using samples obtained from natural sources. Applying the Wittig reaction, trans-bornyl ferulates were obtained, in an unusual manner, which established an alternative for the preparation of phenylpropanoid esters, especially in the synthesis of phenolic esters of tertiary alcohols such as the trans-caffeate. The compounds obtained were identified and characterized by spectroscopy.

Objetivo: Investigar a substância GA-4, quanto a ser um potente candidato a antidepressivo, além de identificar seu possível mecanismo de ação através de docking. Métodos: Foram realizados ensaios psicofarmacológicos in vivo, devidamente autorizado pelo Comitê de ética no uso de animais, utilizando camundongos Swiss, sendo através de testes do campo aberto nas doses de 50, 100 e 200 mg/Kg, analisando os parâmetros: Rearing, Grooming, Número de cruzamentos, micções e bolos fecais. Além do teste do nado forçado, sendo avaliado o tempo de imobilidade dos animais nas mesmas doses do teste de campo aberto. A modelagem molecular foi realizada através de programas computacionais. Resultados: Os resultados mostraram que a substância GA-4 apresenta atividade antidepressiva, tendo em vista que reduziu o tempo de imobilidade no teste do nado forçado e não alterou a atividade locomotora no teste de campo aberto. No estudo de docking, a substância GA-4 teve afinidade com o receptor α2- adrenérgico e se ligou no mesmo sítio de ativação da ioimbina, mostrando ser um possível antagonista dos receptores α2- adrenérgico Conclusão: Diante dos resultados obtidos, podemos concluir que a substância GA-4 é um potencial candidato a medicamento antidepressor. Possivelmente por antagonizar os receptores α2- adrenérgico.