Background Annonaceous acetogenins (ACGs) are secondary metabolites produced by the Annonaceae family and display potent anticancer activity against various cancer cell lines. Squamocin and bullatacin are two examples of ACGs that show promising antitumor activity; however, preclinical data are not sufficient partly due to their being highly lipophilic and poorly soluble in water. These compounds also display high toxicity to normal cells. Due to these disadvantageous properties, the therapeutic potential of squamocin and bullatacin as antitumor agents has not been fully evaluated.Methods In order to enhance their water solubility and potentially improve their cancer targeting, squamocin and bullatacin were conjugated to a glucose or galactose to yield glycosylated derivatives by direct glycosylation or the Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC) reaction (the click reaction). The synthesized compounds were evaluated for their anticancer property against HeLa, A549 and HepG2 cancer cell lines using MTT assay.Results Nine glycosyl derivatives were synthesized and structurally characterized. Most of them show comparable in vitro cytotoxicity against HeLa, A549 and HepG2 cancer cell lines as their parent compounds squamocin and bullatacin. It appears that the type of sugar residue (glucose or galactose), the position at which the sugar residue is attached, and whether or not a linking spacer is present do not affect the potency of these derivatives much. The solubility of galactosylated squamocin 13 in phosphate buffer saline (PBS, pH = 7) is greatly improved (1.37 mg/mL) in comparison to squamocin (not detected in PBS).Conclusion The conjugation of a glucose or galactose to squamocin and bullatacin yields glycosyl derivatives with similar level of anticancer activity in tested cell lines. Further studies are needed to demonstrate whether or not these compounds show reduced toxicity to normal cells and their therapeutic potential as antitumor agents.
The fruits of leguminous plants Cercis Chinensis Bunge are still overlooked although they have been reported to be antioxidative because of the limited information on the phytochemicals of C. chinensis fruits. A simple, rapid and sensitive HPLC-MS/MS method was developed for the identification and quantitation of the major bioactive components in C. chinensis fruits. Eighteen polyphenols were identified, which are first reported in C. chinensis fruits. Moreover, ten components were simultaneously quantified. The validated quantitative method was proved to be sensitive, reproducible and accurate. Then, it was applied to analyze batches of C. chinensis fruits from different phytomorph and areas. The principal components analysis (PCA) realized visualization and reduction of data set dimension while the hierarchical cluster analysis (HCA) indicated that the content of phenolic acids or all ten components might be used to differentiate C. chinensis fruits of different phytomorph.
Yuchen Zhang,Xigai Jia,Ziyang Kang,Xiaoxuan Kang,Ming Ge,Dongbin Zhang,Jilun Wei,Chongqing Wang,Zhangxing He
Tetracycline (TC) is a broad-spectrum antibiotic commonly, made use of in aquaculture and animal husbandry. After entering water bodies, it will represent a major threat to human health. In this study, sterculia foetida biochar (SFC) was readied by the combined hydrothermal pyrolysis (co-HTP) method with sterculia foetida as raw materials. Fen-SFC (Fe2-SFC, Fe3-SFC, and Fe4-SFC) was obtained by doping SFH with different concentrations of FeCl3. Finally, activation of peroxodisulfate (PDS) was achieved, using Fe3-SFC to degrade TC. The degradation of TC obeyed pseudo-second-order kinetics, and the constant of the reaction rate was 0.491 L mg−1min−1. Radical trapping experiments, EPR test and electrochemical tests evidenced that the high catalytic performance of the Fe3-SFC/PDS system was ascribed to free radical pathway (•OH and SO4•−) and non-radical pathway (1O2and electron transfer), in which the latter plays a dominant role. This research not only demonstrates a new kind of biochar as an effective catalyst for PS activation, but also offers an avenue for the value-added reuse of sterculia foetida.Keywords:peroxydisulfate activation;biochar;sterculia foetida;tetracycline wastewater;degradation
危险品化学品经营许可证（带存储）