Proapoptotic Effect and Molecular Docking Analysis of Curcumin–Resveratrol Hybrids in Colorectal Cancer Chemoprevention

Different hybrids based on curcumin and resveratrol were previously synthesized and characterized by spectroscopic techniques. The most active molecules (3a, 3e, 3i, and 3k) were evaluated in vitro as an approach to determine the possible mechanism of action of the hybrids. The results indicated that the evaluated curcumin/resveratrol hybrids induce mitochondrial instability in SW620 and SW480 cells. Moreover, these molecules caused a loss in membrane integrity, suggesting an apoptotic process mediated by caspases after the treatment with compounds 3i (SW480) and 3k (SW620). In addition, the results suggest that the mechanism of action of the hybrids could be independent of the p53 status. Furthermore, hybrids 3e and 3i caused G0/G1 phase arrest, which highlights the potential of these molecules not only as cytotoxic but also as cytostatic compounds. Hybrids 3e and 3i caused a negative modulation of the matrix metalloproteinase 7 (MMP7) on SW480 cells. These curcumin resveratrol hybrids could be potential candidates for further investigations in the search for potential chemopreventive agents, even in those cases with resistance to conventional chemotherapy because of the lack of p53 expression or function. Molecular docking simulations showed that compounds 3e, 3i, and 3k bind efficiently to proapoptotic human caspases 3/7 proteins, as well as human MMP-7 and p53, which, in turn, could explain at the molecular level the in vitro cytotoxic effect of these compounds in SW480 and SW620 colon cancer cell lines.     

Polymer modification to achieve novel properties

Polymers have been modified, by subjecting them to reactions in solution, in the melt and in the solid state. Novel polymers with improved and optimized properties have also been created by copolymerization, chain transfer or by the design of chain termination. Even by manipulating the initiation step in polymerizations, functional and reactive groups have been introduced at the head of the polymer chain. Polymer properties have been modified by influencing physical properties of polymers by orienting, annealing and blending.     

Organische Chemie 2002

Die enantioselektive Synthese bleibt zentrales Thema in metallorganischen, metallfreien and bioorganischen Transformationen sowie in der industriellen organischen Chemie. Glanzpunkte zielmolekülorientierter Synthesechemie waren ein Zugang zu C₆₀, die Route zum Diazonamid A und die Totalsynthese von Vinblastin. Mit „Pyrrolysin”︁ wurde die 22. proteinogene Aminosäure entdeckt. Trotz der immer höheren Zahl an Testsubstanzen besteht in der medizinischen Chemie ein Engpass an klinisch erfolgreichen Wirkstoffen.     

ChemInform Abstract: Density Functional Calculation for Li2CuSn as an Electrode Material for Rechargeable Batteries.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.     

ChemInform Abstract: H2O Nucleation Around Au+

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.