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本期目录

    2020年, 第2卷, 第1期 刊出日期:2020-12-20 上一期   
    A review: anticancer activity of grape seed proanthocyanidins
    Fengjiao Zhang, Tingting Zhang, Jingyu Yang, Chunfu Wu
    2020 (1):  1-10. 
    摘要 ( 1376 )   PDF(1311KB) ( 859 )  
    Abstract For years, a great deal of work has been carried out on proanthocyanidins extracted from various kinds of plants, of which grape seed proanthocyanidins (GSPs) attract most attention due to their benefi cial roles in human health. Indeed, GSPs have demonstrated substantial health benefi ts for a variety of disorders such as cancer, atherosclerosis, and cardiovascular diseases, to just name a few. In particular, GSPs inhibit cell proliferation, migration and invasion, and induce apoptosis and cell cycle arrest in various human cancers, including head and neck carcinoma, gastrointestinal tumors, lung cancer, skin tumors, and reproductive tumors, which points them to be promising chemo-preventive and/or chemotherapeutic agents. In this setting, we summarized the eff ects of GSPs against various types of cancer with a focus on the detailed molecular mechanisms involving various signaling pathways of tumor cells, which may serve as a basis for development of improved chemo-preventive or therapeutic strategies for cancer
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    Structural composition of oligomeric and polymeric proanthocyanidins from diff erent parts of grape pomace
    Marta de Sá, Patrícia Martins, Baoshan Sun
    2020 (1):  11-23. 
    摘要 ( 757 )   PDF(1432KB) ( 512 )  
    Abstract Grape pomace is one of the most abundant solid by-products generated during winemaking, rich in bioactive compounds, i.e., proanthocyanidins. The major objective of this work was to characterize structurally oligomeric and polymeric proanthocyanidins of diff erent parts of grape pomace (seed, skin, and stem). Column chromatography techniques were used to isolate oligomeric and polymeric proanthocyanidins fractions from diff erent parts of grape pomace. The purifi ed grape seed proanthocyanidins were used to assess the effi ciency of the three most frequently-used acidic degradation methods, using benzyl mercaptan, phloroglucinol, and cysteamine as nucleophiles. The structural characterization of proanthocyanidins in the different parts of grape pomace was further performed by the phloroglucinolysis and ESI-MS analysis. The results showed signifi cant diff erences in the structural composition of proanthocyanidins among diff erent parts of pomace. A positive correlation was found between the mean degree of polymerization and percentage of galloylation, in both oligomeric and polymeric fractions. The results provided useful information for the preparation of diff erent proanthocyanidins products from grape pomace.
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    Eff ect of enzymatic extraction conditions on the yield and the polymerization degree of procyanidins
    Shijie Sun, Xiong Chen, Zhaoyang Pei, Lulu Xu, Cuiying Qin, Jing Han
    2020 (1):  24-34. 
    摘要 ( 843 )   PDF(1449KB) ( 378 )  
    Abstract Grape seeds are rich sources of procyanidin (PCs) known for potential health benefi ts. In this study, PCs were extracted from defatted grape seeds by enzymatic method in which pectinase and cellulase were used. The enzyme extraction process was further optimized by single factor experiment and response surface methodology. The optimal conditions were as follows: ethanol concentration of 70%, extraction time of 70 min, extraction temperature of 35 ℃, liquid/solid ratio of 103:1 (mL/g), pectinase/ cellulase ratio of 1:1, enzyme/solid ratio of 1:314 w/w. Under the above conditions, the extraction yields and mean degree of polymerisation (mDP) of PCs reached 47.18 mg/g dry material weight and 11.2, respectively. Compared with other extraction methods, enzyme extraction can obtain PCs with higher yield and lower mDP. According to the antioxidant activity test, PCs extracts with lower mDP showed better ability to clear 1,1-Diphenyl-2-picrylhydrazyl radical (DPPH). Enzymatic extraction was an effi cient method to obtain oligomeric procyanidin which has stronger antioxidant activity.
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    A concise total synthesis of natural flavonols
    Gaigai Liu, Shunqiang Gong, Zhan Li, Xingyi Du, Xiaolou Miao, Xuhong Ren
    2020 (1):  35-42. 
    摘要 ( 703 )   PDF(1149KB) ( 477 )  
    Abstract In this study, we designed a convenient method, to total synthesis of fl avonols especially for C-5 substituted ones and derivatives on a large scale. Beginning from the inexpensively available 2,4,6-trihydroxyacetophenone through Aldol condensation reaction, I2/DMSO cyclization reaction, Oxone “one pot” oxidation, kaempferol (1) and derivative (2) was obtained in an overall yield of 35%. The structures of the target compound and key intermediates were verifi ed by MS, IR, 1 H-NMR and 13C-NMR techniques, and the structure of 5a was further confi rmed by X-ray diff raction analysis.
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