Fabiane M. Farias

Anticancer, antichemotactic and antimicrobial activities of marine sponges collected off the coast of Santa Catarina, southern Brazil

Abstract This study reports the in vitro screening of 10 marine sponges (Porifera) collected from the coastline of Santa Catarina, southern Brazil, in the search for novel pharmaceuticals. Organic and aqueous extracts were tested for anticancer, antibacterial, antifungal and antichemotactic activities. Eight of the ten species tested demonstrated activity in one or more of the bioassays. Organic extracts of Polymastia janeirensis Boury-Esnauls, 1973, Haliclona aff tubifera George and Wilson, 1919, Mycale arcuiris Lerner and Hajdu, 2002 and Raspailia ( syringella ) sp. each demonstrated cytotoxicity at 100 μg/ml in an in vitro screening assay against the HT29 colorectal tumour cell line. Further analysis against three human tumour cell lines (HT29, U373 and NCI-H460) demonstrated IC 50 concentrations ranging from 25 to 50 μg/ml. Aqueous extracts of six species P. janeirensis , M. arcuiris , Raspailia ( syringella ) sp., Guitarra sp., Tedania ignis Duchassaing and Michelotti, 1864 and Pseudaxinella reticulata Ridley and Dendy, 1886 each significantly ( p ≤0.05) retarded the migration of polymorphonuclear (PMN) leukocytes in a chemotactic assay. In antibacterial assays, only H. aff tubifera (four of five bacterial strains) and Axinella corrugata George and Wilson, 1919 (one of five bacterial strains) demonstrated activity. None of the 10 species demonstrated measurable antifungal activity. These extracts are currently undergoing further analysis to identify the active constituents.

Brachycerine, a novel monoterpene indole alkaloid from Psychotria brachyceras

Brachycerine (1), an unusual alkaloid from the leaves of Psychotria brachyceras, was characterized through spectroscopic data interpretation and its stereochemistry established by NOE difference techniques. Brachycerine (1) was found to be restricted to shoots in rooted cuttings of P. brachyceras (0.018 +/- 0.004% dry weight), and accumulation was unaffected by root induction treatment with auxin.

Essential Oil of Myrrhinium atropurpureum Schott (Myrtaceae) Leaves

Abstract Essential oil obtained by hydrodistillation from the leaves of Myrrhinium atropurpureum (Myrtaceae) growing in southern Brazil were analyzed by GC and GC/MS. Twenty compounds (99.3%) have been identified of which α-pinene (12.2%), limonene (35.0%) and 1,8-cineole (23.4%) were the major components.

Química combinatória: moderna ferramenta para a obtenção de candidatos a protótipos de novos fármacos

Nowadays, Combinatorial Chemistry is one of the most promising tools used in the design and discovery of new molecules potentially useful in the therapeutics. In this methodology, the reaction products are synthesized simultaneously and can be evaluated once, either in a complex mixture or as isolated compounds. The main aim of this new approach is the time for the development of new drugs. The synthesis of combinatorial libraries can be performed using either insoluble or soluble polymers and also by the traditional organic synthesis in solution. Each one of these approaches presents features that may be advantageous depending on the final objective of the synthetic process. The development of high throughput screening (HTS) assays takes much time, which makes the synthesis of small and well designed combinatorial libraries the most recommended strategy.