Characterization and Bioactivity of Polysaccharides Separated through a (Sequential) Biorefinery Process from Fucus spiralis Brown Macroalgae.

Marine macroalgae biomass is a valuable renewable resource that can be used for the development of bioeconomy through the valorisation of valuable compounds. The aim of the current study is separate macroalgal polysaccharides with bioactive properties from brown macroalgae Fucus spiralis based on a designed biocascading biorefinery approach. Thus, we applied an integrated processing method for the separation of fucoidan and alginate, in addition to characterization through IR spectroscopy and 1H NMR. The bioactivity potential (antioxidant activity using superoxide anion and DPPH radical scavenging analysis) of the two polysaccharides was evaluated, together with DNA binding studies performed though voltametric techniques and electronic spectroscopy titration. In terms of results, functional groups S=O (1226 cm-1), N=S=O (1136 cm-1) and C-O-SO3 (1024 cm-1), which are characteristic of fucoidan, were identified in the first polysaccharidic extract, whereas guluronic units (G) (1017 cm-1) and mannuronic units (M) (872 and 812 cm-1) confirmed the separation of alginate. The DNA binding studies of the isolated polysaccharides revealed an electrostatic and an intercalation interaction of DNA with fucoidan and alginate, respectively. Both antioxidant activity assays revealed improved antioxidant activity for both fucoidan and alginate compared to the standard α-tocopherol.

In Vitro and In Silico Determination of Some N-ferrocenylmethylaniline Derivatives as Anti-Proliferative Agents Against MCF-7 Human Breast Cancer Cell Lines.

BACKGROUND: Since the binding of estradiol to its receptor promotes breast cancer cell proliferation (in the ER+ tumours), many molecules targeting this protein have been synthesized to counteract the estradiol action. Ferrocene derivatives have proved their efficiency against hormone-dependent breast cancer cells (MCF-7). OBJECTIVE: In this study, we aimed to find new ferrocene derivatives having pharmacochemistry properties as potential drugs against human breast cancer cells. METHODS: A series of 29 N-ferrocenylmethylaniline derivatives A0-A28 were synthesised, and their anti-proliferative activity against both hormone-dependent (MCF-7) and independent (MDA-MB 231) human breast cancer cell lines were performed using the MTT test. Molecular docking and drug-likeness prediction were also performed for the five most active derivatives towards MCF-7. A QSAR model was also developed for the perdition of the anti-proliferative activity against MCF-7 cell lines using molecular descriptors and MLR analysis. RESULTS: All studied derivatives demonstrated better cytotoxicity against MCF-7 compared to the MDA-MB-231 cell lines, and compounds A2, A9, A14, A17 and A27 were the most potent ones but still less active than the standard anticancer drug, crizotinib. The QSAR study revealed good predictive ability, as shown by R2 cv = 0.848. CONCLUSION: In vitro and in silico results indicated that derivatives A2, A9, A14, A17, and A27 possess the highest anti-proliferative activity; these results can be used to design more potent N-ferrocenylmethylaniline derivatives as anti-proliferative agents.