番木瓜籽中异硫氰酸苄酯抗癌抑菌功能研究进展

番木瓜(Carica Papaya)是一种极具营养价值而被广泛种植的热带水果,其籽中含有苄基硫代葡萄糖苷(Glucosinolate,GS),约占番木瓜重量7%,是果肉加工的废弃物。GS主要存在于细胞空泡,当其接触到芥子酶就会被水解,生成异硫氰酸酯类(Isothiocyanates,ITCs)。ITCs是十字花科植物的次生代谢产物,是一类重要的有机合成中间体,公认具有防癌抗癌功效以及抑菌作用,异硫氰酸苄酯(Benzyl isothiocyanate,BITC)是ITCs中生物学效果最为明显的一种。BITC对许多癌症有明显的抑制作用,可以阻断癌细胞增殖分化;BITC对致病菌有抑制甚至杀死作用,这种抑菌活性可以作用于细菌和霉菌。本文结合国内外相关研究现状,综述BITC在防癌抗癌及抑菌方面的研究进展,为番木瓜籽副产物BITC更深一步的加工以及番木瓜综合利用率的提升提供一定的理论依据。     

红色LED光照下上海青采后硫代葡萄糖苷代谢的变化

为研究发光二极管（Light-Emitting Diodes，LED）处理对上海青采后硫代葡萄糖苷（简称硫苷）代谢的作用机理，该研究首先采用不同颜色和光密度的光照处理上海青，得出6.5 μmol/(m2•s)的红色LED光照处理可显著抑制上海青中叶绿素降解，延缓其黄化。在此基础上，研究了6.5 μmol/(m2•s)红色LED光照处理对贮藏期间上海青中硫苷代谢相关物质及基因表达水平的影响。结果表明，上海青叶柄中总硫苷和异硫氰酸酯含量分别为叶片的2.72倍和1.32倍；红色LED光照处理可显著上调上海青叶柄中脂肪族合成关键基因MYB28、CYP83A1、GSTF11等的表达水平，从而促进叶柄中主要硫苷物质3-丁烯基硫苷等的合成；由此，上海青叶柄中总硫苷含量在贮藏4~8 d期间为对照组的1.62~1.99倍；同时，该处理提升了上海青叶柄的黑芥子酶活性，从而促进了总异硫氰酸酯的积累，且在贮藏4~8 d期间，对照组上海青叶柄的总异硫氰酸酯含量为红光处理组的77.43%~91.98%。综上，红色LED光照处理通过调控硫苷合成关键基因和黑芥子酶活性来延缓上海青中硫苷物质和异硫氰酸酯的流失。     

Synthesis and Evaluation of Functionalized Aryl and Biaryl Isothiocyanates against Human MCF-7 Cells

Organic isothiocyanates (ITCs) are a class of anticancer agents which naturally result from the enzymatic degradation of glucosinolates produced by Brassica vegetables. Previous studies have demonstrated that the structure of an ITC impacts its potency and mode(s) of anticancer properties, opening the way to preparation and evaluation of synthetic, non-natural ITC analogues. This study describes the preparation of a library of 79 non-natural ITC analogues intended to probe further structure-activity relationships for aryl ITCs and second-generation, functionalized biaryl ITC variants. ITC candidates were subjected to bifurcated evaluation of antiproliferative and antioxidant response element (ARE)-induction capacity against human MCF-7 cells. The results of this study led to the identification of (1) several key structure-activity relationships and (2) lead ITCs demonstrating potent antiproliferative properties.