The Synthesis and Antitumor Activity of the Sodium Salt and Copper (II) Complex of N-[(Trimethylamineboryl)-Carbonyl]-L-Phenylalanine Methyl Ester

Sodium N-[(trimethylamineboryl)-carbonyl]-L-phenylalanine 2 and {N-[(trimethylamineboryl)-carbonyl]-L-phenylalanyl- carbxylato}-bis-{N-[(trimethylaminebryl)-carbonyl]-L-phenylalanine} dicopper (II) 3 were successfully synthesized. The agents blocked L1210 leukemic cell DNA and RNA syntheses by inhibiting multiple enzyme activities for nucleic acid synthesis, e.g. PRPP amido transferase, IMP dehydrogenase, DNA polymerase α, thymidine kinase, and TMP kinase. The copper (II) complex 3 demonstrated improved ability to inhibit L1210 partially purified DNA topoisomerase II compared to the parent compound while the sodium salt was inactive at 100 μM

The Pharmacological Activities of the Metabolites of N-[(Trimethylamineboryl)-Carbonyl]-L-Phenylalanine Methyl Ester

The metabolites of N-[(trimethylamineboryl)-carbonyl]-L-phenylalanine methyl ester 1 proved to be active in a number of pharmacological screens where the parent had previously demonstrated potent activity. The proposed metabolites demonstrated significant activity as cytotoxic, hypolipidemic, and anti-inflammatory agents. In cytotoxicity screens several of the proposed metabolites afforded better activity than the parent compound against the growth of suspended and solid tumor cell lines. Evaluation of in vivo hypolipidemic activity demonstrated that the proposed metabolites of 1 were only moderately active and were generally less effective than the parent compound. Interestingly, L-phenylalanine methyl ester hydrochloride 3, which contains no boron atom, demonstrated equivalent hypolipidemic activity as the parent at 8 mg/kg/day in CF1 male mice. As anti-inflammatory agents the proposed metabolites demonstrated variable capacities to reduce foot pad inflammation. These compounds were similarly effective as the parent 1 at blocking local pain and were generally better than the parent at protecting CF1 male mice from LPS induced sepsis

Shaping children's healthy eating habits with food placements? Food placements of high and low nutritional value in cartoons, Children's BMI, food-related parental mediation strategies, and food choice

Research on media induced food choices of children has not sufficiently investigated whether food placements of snacks high in nutritional value can strengthen children's healthy eating behavior. Furthermore, we lack knowledge about the moderating role of children's individual characteristics such as parental food-related mediation or BMI. The current study combines data from an experiment involving children with a survey of their parents. We exposed children to a cartoon either containing no food placements, placements of mandarins (i.e., snack high in nutritional value), or placements of fruit gums (i.e., snack low in nutritional value). Afterwards, food consumption was measured by giving children the option to choose between fruit gums or mandarins. Children in both snack placement conditions showed stronger preference for the snack low in nutritional value (i.e., fruit gum) compared to the control group. Interestingly, neither restrictive nor active food-related mediation prevented the effects of the placements on children's choice of snacks low in nutritional value. Compared to children with a low BMI, children with high BMI levels had a stronger disposition to choose the fruit gums if a snack high in nutritional value (i.e., mandarin) was presented. Thus, making snacks high in nutritional attractive for children through media presentation might need stronger persuasive cues