New anticancer agents with lower toxicity have been always urged because of drug resistance associated with overused chemotherapy agents. In this study, steviol, a colonic metabolite of natural sweetener and also a component in leaves of stevia rebaudiana bertoni, was found to possess intensive anticancer activity on the human gastrointestinal cancer cells. Steviol inhibited six human gastrointestinal cancer cells intensively as 5-fluorouracil did at 100 μg/mL. The inhibition mechanism follows mitochondrial apoptotic pathway that was evidenced by increase of Bax/Bcl-2 ratio, activation of p21 and p53; and caspase 3-independent mechanism was also involved. These results are consistent with the miRNA expression analysis. The most regulated miRNAs in the steviol treated gastrointestinal cancer cells were miR-203a-3p (log2 =1.32) and miR-6088 (log2 =-2.54) in HCT-116, miR-1268b (log2 =19.85) and miR-23c (log2 =-2.05) in MKN-45. In view of the metabolic characteristics of steviol and its cytotoxicity on the cancer cells, steviol could be a chemotherapy agent potentially for cancer treatment.
Alizarin, a renewable natural ligand, was simply assembled with ZrCl4 to construct sustainable bifunctional catalysts (Zr–AZN) for highly efficient hydrogen transfer of biomass-derived oxygenates under mild conditions.
Although the conversion of furfural to formic acid oxidized by H2O2 in formic acid is very high, the molecular mechanism remains unknown. This work describes the entire reaction process of the condensation reaction based on the density functional theory (DFT). It is found that H acts as a shuttle throughout most of the basic reaction steps during this transformation. Besides, Baeyer–Villiger oxidation and Baeyer–Villiger rearrangement are also discovered during this process with the opening of furan ring following afterward. The reactants, products and intermediates in the reaction process are optimized; all possible reaction paths are considered as well as the energy barriers to be overcome at each step. Thermochemical data concerned with the conversion of furfural to maleic acid showed that the maximum energy barrier at 378.15[Formula: see text]K was 39.83[Formula: see text]kcal/mol. The results of this study do not only correspond with the existing conclusions about the reaction in question from previous research but also supplement to the study of the pathways and mechanisms of the reaction, which can provide reference and guidance for further research, both experimentally and theoretically.
Steviol glycosides, a natural sweetener, may perform bioactivities via steviol, their main metabolite in human digestion. The metabolising kinetics, i.e. glucuronidation kinetics and interaction between steviol glycosides or their metabolites and metabolising enzyme, are important for understanding the bioactivity and cytotoxicity. The present study investigated kinetics of steviol glucuronidation in human liver microsome and a recombinant human UDP-glucuronosyltransferases isomer, UGT2B7, along with molecular docking to analyse interaction between UGT2B7 and steviol or glucose. The active pocket of UGT2B7 is consisted of Arg352, Leu347, Lys343, Phe339, Tyr354, Lys355 and Leu353. The influence of stevioside, rebaudioside A, glucose and some chemotherapy reagents on the glucuronidation was also studied. The predicted hepatic clearence suggested that steviol could be classified as high-clearence drug. The steviol glycosides did not affect the glucuronidation of steviol notably.
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