柯里拉京对顺铂抗卵巢癌Hey和SKOV3细胞的增敏作用

探讨柯里拉京(corilagin)与羟基喜树碱(HCPT)、顺铂(cDDP)单独及联合用药,体外抗卵巢癌细胞Hey,SKOV3的活性及与cDDP联用机制的初步研究.利用四唑盐(MTT)比色法检测柯里拉京,HCPT,cDDP在不同质量浓度下,单独及联合用药对卵巢癌细胞的增殖抑制率,并根据金氏公式计算其协同指数(Q),进而评价两药联用的增敏效果.通过形态学观察吖啶橙(AO)/溴化乙啶(EB)和Hoechst 33258染色及线粒体膜电位变化,探究其诱导机制.结果表明:柯里拉京对卵巢细胞Hey,SKOV3的半抑制浓度(IC₅₀值)分别为19.20,17.17 μmol·L^-1;柯里拉京与cDDP联合作用对于SKOV3,Hey两种细胞均有协同作用,与HCPT联用只对SKOV3细胞有协同作用,对Hey细胞仅是相加效应;联合用药组对卵巢癌细胞的抑制效果显著高于单独用药组;柯里拉京与cDDP联合用药对卵巢癌细胞的杀伤效果可能是通过诱导细胞凋亡实现的.     

不同产地、不同采收期及不同部位叶下珠药材柯里拉京含量的比较研究

对不同产地、不同采收期及不同部位叶下珠药材柯里拉京含量测定进行比较.分析采用Hypersil ODS2(250 mm×4.60 mm,5 um)色谱柱,以乙腈(A)-0.1%磷酸水溶液(B)二元系统梯度洗脱,柱温25℃,流量0.8 m L/min,检测波长280 nm.柯里拉京在0.458~4.580 mg/g(r=0.995 9)呈良好的线性关系,加样回收率(n=5)为97.98%.结果表明:不同产地叶下珠药材柯里拉京的含量有较大差异,广东中山的含量最高达4.224 mg/g;不同采收期叶下珠药材柯里拉京含量在10月5日达到最高,随后下降,建议叶下珠药材的采收期为每年的10月上旬;不同部位叶下珠药材柯里拉京含量差异较大,根含量很低,建议叶下珠药材只采收地上部分.本实验建立HPLC法测定叶下珠药材柯里拉京含量,该方法简便、准确、重现性好,可为叶下珠药材质量评价及质量控制提供依据.     

Searching for more effective HCV NS3 protease inhibitors via modification of corilagin

Corilagin was seperated from extract of Phyllanthus urinaria L. and used as the precursor of inhibitors of hepatitis C virus (HCV) NS3 serine protease. Six derivatives were obtained through the chemical modification of corilagin and their structures were elucidated by the spectra analysis. Bioassay of these compounds showed that two of them had improved inhibitory efficiency than the precursor, with IC₅₀ values of 2.28 μmol/L and 1.52 μmol/L, respectively. The binding mode of two active compounds with substrate binding site of HCV NS3 protease was also investigated by molecular docking method.