Co-Encapsulation of Lycopene and Resveratrol in Polymeric Nanoparticles: Morphology and Lycopene Stability.

Lycopene and resveratrol are well-known for their high bioactivity, anti-inflammatory effects, and strong antioxidant properties. The combination of lycopene and resveratrol was synergistic in the potentializing immunity of the mammal body. In this study, the scalable co-encapsulation of lycopene and resveratrol into polymeric nanoparticles was performed using lycopene extracted from ripe gac fruit. These nanoparticles exhibited excellent water dispersion and spherical morphology with average particle diameters of 66.102 nm. The particle size was proportional to the lycopene/resveratrol ratio. The combinative use of lecithin and Tween® as surfactants and the use of a polylactide-polyethylene glycol copolymer as an encapsulation agent generated well-defined lycopene/resveratrol nanoparticles although the total content of these active compounds reached 12%. The stability of lycopene was enhanced when combined with resveratrol and antioxidants such as vitamin E and butylated hydroxytoluene. After 3 months of storage at -16 °C, the lycopene content in the lycopene/resveratrol nanopowder remained at ∼95%.

Synthesis, structure and in vitro cytotoxicity testing of some 2-aroylbenzofuran-3-ols.

Five 2-aroyl-5-bromobenzo[b]furan-3-ol compounds (two of which are new) and four new 2-aroyl-5-iodobenzo[b]furan-3-ol compounds were synthesized starting from salicylic acid. The compounds were characterized by mass spectrometry and 1H NMR and 13C NMR spectroscopy. Single-crystal X-ray diffraction studies of four compounds, namely, (5-bromo-3-hydroxybenzofuran-2-yl)(4-fluorophenyl)methanone, C15H8BrFO3, (5-bromo-3-hydroxybenzofuran-2-yl)(4-chlorophenyl)methanone, C15H8BrClO3, (5-bromo-3-hydroxybenzofuran-2-yl)(4-bromophenyl)methanone, C15H8Br2O3, and (4-bromophenyl)(3-hydroxy-5-iodobenzofuran-2-yl)methanone, C15H8BrIO3, were also carried out. The compounds were tested for their in vitro cytotoxicity on the four human cancer cell lines KB, Hep-G2, Lu-1 and MCF7. Six compounds show good inhibiting abilities on Hep-G2 cells, with IC50 values of 1.39-8.03 µM.

Synthesis and Cytotoxic Evaluation of Artemisinin-triazole Hybrids.

Dihydroartemisinin was converted to its corresponding alkyne-functionalized esters, which were subsequently deployed as substrates for a 'click' chemistry-mediated coupling-with 3'-azido-3'-deoxythydimine (AZT) to furnish novel triazole-artesunate-AZT hybrid compounds. Moreover, various substituted triazole-artemisinin :hybrids were synthesized based on 'click' chemistry between propargyl-substituted derivatives and artemisinin containing a 2-hydroxypropane unit. Fourteen new hybrids were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity of four triazole-artemisinin derivative hybrids in KB and HepG2 cancer cell lines.