The hexane extracts of Dictyota ciliolata Sonder ex Kützing (Dictyotaceae), Padina sanctae-crucis Børgesen (Dictyotaceae), and Turbinaria tricostata E.S. Barton (Sargassaceae) were found to exhibit cytotoxic and antiproliferative activities in vitro. Bioactive compounds responsible for these activities have not been studied in detail for these species and phytochemical studies are very limited. Isolate, evaluate, and elucidate the bioactive constituents of D. ciliolata, P. sanctae-crucis, and T. tricostata. Bioassay-guided cytotoxicity fractionations using the Hep-2 cell line of the hexane extracts from these brown algae were analyzed using various chromatographic techniques. Cytotoxic and antiproliferative activities of all isolated compounds were also evaluated on a panel of cell lines (KB, Hep-2, MCF-7, and SiHa). Furthermore, their selectivity index, the ratio of cytotoxicity on normal cells to cancer cells, was evaluated using the HEK-293 cell line. Four compounds were isolated from studied species: two sterol, fucosterol (1) and 24ξ-hydroperoxy-24-vinylcholesterol (2); and two diterpenes, pachydictyol A (3) and dictyol B acetate (4). The major bioactive components of the hexane extracts of T. tricostata and P. sanctae-crucis were compounds 1 and 2 (with CC50 varying around 3.1-25.6 µg/mL) on cell lines tested. Whereas compounds 1, 3, and 4 showed cytotoxic activity against cancer cell lines (CC50 varying between 14.8 and 41.2 µg/mL) and were major bioactive constituents of hexane extract of D. ciliolata. Compounds 1 and 4 showed antiproliferative activity on MCF-7 (IC50 = 43.3 µg/mL for compound 1 and 38.3 µg/mL for compound 2) and SiHa (IC50 = 43.3 µg/mL for compound 1 and 38.3 µg/mL for compound 2) cell lines. This study is the first investigation on the bioactive components of D. ciliolata, P. sanctae-crucis, and T. tricostata. Although compounds 1-3 were described previously, the pharmacological activity of compound 4 is presented here for the first time.
The plant Aeschynomene fascicularis (Fabaceae) has been used in Mayan traditional medicine in the Yucatan peninsula. However, the compounds present in the plant responsible for its curative properties have not yet been investigated. Aeschynomene fascicularis root bark was extracted with 100% methanol to obtain a crude extract. The methanol extract was partitioned successively with solvents with increasing polarity to obtain the corresponding hexane (Hx), dichloromethane (DCM) and ethyl acetate fractions (EtOAc), as well as a residual water-alcoholic fraction. These fractions were tested for their cytotoxic activities using an MTT assay against Hep-2 cancer cell lines. The Hx fraction led to the isolation of spinochalcone C (1), spinochalcone A (2), isocordoin (3) and secundiflorol G (4). Their structures were identified based on spectroscopic evidence and chemical properties. All compounds were subjected to cytotoxicity and antiproliferative assays against a panel of seven cell lines, including one normal-type cell line. Spinochalcone A (2) exhibited cytotoxic activity against DU-145 cell line and antiproliferative activity against the KB cell line. Secundiflorol G (4) showed strong cytotoxic activity towards KB and Hep-2 cell lines. In addition, isocordoin (3) showed moderate activity on KB, Hep-2 and DU-145 cell lines. The active Compounds 2, 3 and 4 are potential therapeutic entities against cancer.
Polysaccharides extracted from Rhodymenia pseudopalmata, Solieria filiformis, Hydropuntia cornea (Rhodophyta) and Sargassum fluitans (Phaeophyceae) were evaluated for its cytotoxic and antiviral activities against Herpes simplex virus (HSV-Type 1). Chemical structures were characterized by FT-IR spectroscopy and 13C-NMR analyses. Polysaccharides from Sargassum fluitans (EC50 = 42.8 μg/ml) and Solieria filiformis (EC50 = 136.0 μg/ml) showed antiviral activity against herpes simplex virus type-I in vitro at a multiplicity of infection (MOI) of 0.01 ID50/cells without cytotoxicity (1–200 μg/mL). The activity observed suggests that sulphation, molecular weight and carbohydrate nature of these polysaccharides may be involved in this activity. To better understand the antiviral activity of the polysaccharides evaluated, it seems important to study the mechanism of action involved. These polysaccharides could be studied further to evaluate their potential use as antiviral drugs.