For example, oleanolic acid, betulin or betulinic acid are more cytotoxic with a pronounced activity for tumor cells. GA, however, is easily to earn, cheap and shows apoptotic effects on tumor cells – like the other triterpenoic acids. These facts bring GA and derivatives in the focus of our scientific interest. Here we tried to improve the poor
cytotoxicity of GA by simple derivatization. Thus, we selected various glutamyl and aspartyl substituents for the synthesis of C(3) esters of GA methyl ester. A short (3-5 steps) synthesis was elaborated that allowed to access more effective compounds. One compound, methyl 30 3-(0-benzyl-L-glutamyl)-11-oxo-olean-12-en-30-oate (5), having a glutamyl substituent with a benzyl protected side chain showed up to 67-fold higher cytoxicity and an up to 140-fold better selectivity towards tumor JQEZ5 mw cells than parent GA. All compounds were evaluated by a sulforhodamine B assay as well as by
a trypan blue test and extra acridine orange/ethidium bromide tests for apoptosis.”
“The C5 and C6 sugars generated from sweet sorghum bagasse pretreated with five different chemical or physical schemes and then further hydrolyzed with a fibrolytic cocktail were determined. Hydrolysates were fermented with three yeast strains in order to determine which combination generated the highest amount of bioethanol. The bagasse only treated with the enzyme complex generated 50% of the total C5 and C6 sugars available. The pressure-cooked selleck chemical and extruded pretreatments further hydrolyzed with the enzymes generated 17% more sugars compared to the enzyme alone treatment. The enzyme increased the total sugar content
in approximately 40% in the three acid pretreated hydrolysates. STI571 in vitro Among the different pretreatments, only the extrusion process did not generate inhibitors acetic acid, furfural and 5-hydroxymethylfurfural. At 24 h fermentation, the strains Saccharomyces cerevisiae and Issatchenkia orientalis produced, respectively 183.9 and 209.2 mg ethanol/g dry bagasse previously treated with HCl and enzymes. (C) 2013 Elsevier Ltd. All rights reserved.”
“The claim that Grote-Hynes theory (GHT), when it provides accurate rates, is equivalent to multidimensional variational transition state theory (VTST) has been debated for decades with convincing arguments on both sides. For the two theories to be equivalent a perfect dividing surface with no recrossing must exist. We describe an easily implemented test employing deterministic microcanonical (NVE) trajectories which can identify situations where no perfect dividing surface exists and thereby potentially falsify the claim of equivalence. We use this test to reach data-supported conclusions about the relationship between GHT and VTST. (C) 2014 AIP Publishing LLC.”
“Epidermal growth factor receptor (EGFR)-targeted therapies have been effective in some cancers, but not in hepatocellular carcinoma (HCC).