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Filipendula ulmaria (L.) Maxim (meadowsweet) is a popular medicinal species that can be found throughout most Europe and Asia. The plant is known for its rich antioxidants content, having compounds such as flavonoids and ascorbic acid. Therefore, the aim of

Marine organisms are a prolific source of drug leads in a variety of therapeutic areas. In the last few years, biomedical, pharmaceutical and nutraceutical industries have shown growing interest in novel compounds from marine organisms, including macroalgae. Cystoseira is a genus of Phaeophyceae (Fucales) macroalgae known to contain bioactive compounds. Organic extracts (hexane, diethyl ether, ethyl acetate and methanol extracts) from three Cystoseira species (C. humilis, C. tamariscifolia and C. usneoides) were evaluated for their total phenolic content, radical scavenging activity against DPPH and ABTS radicals, and antiproliferative activity against a human hepatocarcinoma cell line (HepG2 cells). C. tamariscifolia had the highest TPC and RSA. The hexane extract of C. tamariscifolia (CTH) had the highest cytotoxic activity (IC50=2.31 µg/mL), and was further tested in four human tumor (cervical adenocarcinoma HeLa; gastric adenocarcinoma AGS; colorectal adenocarcinoma HCT-15; neuroblastoma SH-SY5Y), and two non-tumor (murine bone marrow stroma S17 and human umbilical vein endothelial HUVEC) cell lines in order to determine its selectivity. CTH strongly reduced viability of all tumor cell lines, especially of HepG2 cells. Cytotoxicity was particularly selective for the latter cells with a selectivity index = 12.6 as compared to non-tumor cells. Incubation with CTH led to a 2-fold decrease of HepG2 cell proliferation as shown by the BrdU incorporation assay. CTH-treated HepG2 cells presented also pro-apoptotic features, such as increased Annexin V/PI binding and dose-dependent morphological alterations in DAPI-stained cells. Moreover, it had a noticeable disaggregating effect on 3D multicellular tumor spheroids. Demethoxy cystoketal chromane, a derivative of the meroditerpenoid cystoketal, was identified as the active compound in CTH and was shown to display selective in vitro cytotoxicity towards HepG2 cells.

The in vitro anticancer activity of the crude extract of the sponge-associated fungus Eurotium cristatum and its secondary metabolites ABSTRACT Background: Marine natural products has captivated many researchers over the years and there is always a need for sources of diverse and pharmacologically active leads in the area of anticancer drugs. Materials and Methods: The ethyl acetate extract of the fungus Eurotium cristatum (ECE), isolated from the marine sponge Mycale sp., furnished 2-(2', 3-epoxy-1',3'-heptadienyl)-6-hydroxy-5-(3-methyl-2-butenyl) benzaldehyde (1), 1,8-dihydroxy-6-methoxy-3-methyl-9,10-anthracenedione (physcion, 2), and the dioxopiperazine alkaloid echinulin (3). The structures of the compounds were established by Nuclear Magnetic Resonance (NMR) spectral analysis (1H, 13C, DEPT, COSY, HSQC, and HMBC). The ECE and its metabolites were evaluated for their growth inhibitory activity on the following three human tumor cell lines: breast adenocarcinoma (MCF-7), non-small lung cancer (NCI-H460), and melanoma (A375-C5). Results: The results showed that the ECE was active in all the three cell lines, with the values of GI50 = 44.3 ± 1.2, 45.5 ± 7.5, and 71.3 ± 2.1 μg/ml for MCF-7, NCI-H460, and A375-C5, respectively. Compound 1 also exhibited moderate growth inhibitory activity against all the three cell lines (GI50 = 58.3 ± 1.2, 46.0 ± 5.5, and 116.7 ± 7.2 μM for MCF-7, NCI-H460, and A375-C5, respectively), whereas compound 3 showed only weak inhibition against MCF-7 (GI50 = 109.7 ± 0.3 μM) and NCI-H460 (GI50 = 96.7 ± 1.5 μM) but was inactive against A375-C5 (GI50 >150 μM). On the contrary, compound 2 was inactive in all the three cell lines at the highest concentration tested (150 μM). Furthermore, ECE was investigated for its effect on the cell cycle in the NCI-H460 cells. Analysis of the cell cycle profile showed that ECE was able to cause a slight cell arrest in the G1 phase, with a corresponding decrease of cells in the S and G2/M phases. Conclusion: The secondary metabolites isolated [Compound 1] from the crude ethyl acetate extract of the culture of the marine fungus E. cristatum were found as the most potent compound regarding cell growth inhibition.

Tuberaria lignosa (Sweet) Samp. is found in European regions, and has antioxidant properties due to its composition in ascorbic acid and phenolic compounds. Given its traditional use and antioxidant properties, the tumor cell growth inhibitory potential of aqueous extracts from T. lignosa (prepared by infusion and decoction) was investigated in three human tumor cell lines: MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), and HCT-15 (human colorectal adenocarcinoma). Both extracts inhibited the growth of these cell lines; the most potent one being the T. lignosa extract obtained by infusion in the NCI-H460 cells (GI 50 of approximately 50 µg/mL). Further assays were carried out with this extract in NCI-H460 cells. At 100 µg/mL or 150 µg/mL it caused an increase in the percentage of cells in the G0/G1 phase and a decrease of cells in S phase of the cell cycle. Additionally, these concentrations caused an increase in the percentage of apoptotic cells. In agreement, a decrease in total poly (ADP-ribose) polymerase (PARP) and pro-caspase 3 levels was found. In conclusion, the T. lignosa extract obtained by infusion was more potent in NCI-H460 cells, altering the cell cycle progression and inducing apoptosis. This work highlights the importance of T. lignosa as a source of bioactive compounds with tumor cell growth inhibitory potential.