Abstract
This paper reports the in vitro antiproliferative effects, antiprotozoal, anti-herpes and antimicrobial activities of 32 organic extracts of 14 marine sponges and 14 corals collected in northeast Brazilian coast. The ethanolic extracts of the sponges Amphimedon compressa and Tedania ignis, and the acetone extract of Dysidea sp. showed relevant results concerning the antiproliferative effects against A549, HCT-8, and PC-3 cell lines by sulforhodamine B assay, but also low specificity. Concerning the antiprotozoal screening, the ethanolic extract of Amphimedon compressa and the acetone and ethanolic extracts of Dysidea sp. were the most active against Leishmania amazonensis and Trypanosoma cruzi expressing β-galactosidase in THP-1 cells. In the preliminary anti-HSV-1 (KOS strain) screening, the ethanolic extracts of the sponges Amphimedon compressa, Haliclona sp. and Chondrosia collectrix inhibited viral replication by more than 50%. The most promising anti-herpes results were observed for the ethanolic extract of Haliclona sp. showing high selective indices against HSV-1, KOS and 29R strains (SI> 50 and >79, respectively), and HSV-2, 333 strain (IS>108). The results of the antibacterial screening indicated that only the ethanolic extract of Amphimedon compressa exhibited a weak activity against Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli by the disk diffusion method. In view of these results, the extracts of Amphimedon compressa, Tedania ignis and Dysidea sp. were selected for further studies aiming the isolation and identification of the bioactive compounds with antiproliferative and/or antiprotozoal activities. The relevant anti-herpes activity of the ethanolic extract of Haliclona sp. also deserves special attention, and will be further investigated.
Highlights
Most of the natural products used in therapeutics come from terrestrial organisms
The analysis, which compared molecular scaffolds reported in the Dictionary of Natural Products (DNM) to those in the Dictionary of Marine Natural Products (DMNP), showed that approximately 71% of the molecular scaffolds in the DMNP were exclusively found in marine organisms (Kong et al, 2010)
The collection range of these organisms on the Brazilian coast is concentrated in the south and southeast regions of the country (Seleghim et al, 2007; Monks et al, 2002; Rangel et al, 2001). Based on these data and the urgent requirement to discover new molecules for the treatment of neglected tropical diseases, such as Chagas disease and leishmaniasis, we evaluated the in vitro antiproliferative, antiprotozoal, anti-herpes, and antimicrobial activities of 32 organic extracts obtained from 14 marine sponges and 14 coral species from the northeastern Brazilian coast
Summary
Most of the natural products used in therapeutics come from terrestrial organisms. the marine environment allowed a new approach for the discovery of chemical molecules and biological activities. A comparative analysis performed by Kong and coworkers showed that marine natural products are superior to terrestrial natural products in terms of chemical novelty and significant bioactivity. Despite the large number of natural products isolated from marine sources in the last decade that show high bioactivity for a variety of diseases, only few have the chance to get to the end of drug discovery pipeline (Blunt et al, 2010, 2017). Worldwide bioprospecting efforts have not ceased, and marine invertebrates are amongst the top group of organisms that have contributed for this fact with a larger number of new molecules entries in Natural Products libraries (Jha and Xu, 2004; Blunt et al, 2008). Leal and coworkers showed that between 2000 and 2009, a great number of natural products from marine invertebrates was isolated from the phyla Porifera (47%) and Cnidaria (33%) (Leal et al, 2012)
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