An electrochemical amino-azidation of 2-aminostyre ne with sodium azide(NaN3)was developed,which can be carried out smoothly in water under metal-free condition,affording a series of 3-azido indolines with high yields.
Azido-3′-deoxythymidine(AZT) was the first clinically approved drug against HIV infection, despite its undesirable side reactions, such as bone marrow suppression. In our aim to develop new chemical entity of anti-tu...Azido-3′-deoxythymidine(AZT) was the first clinically approved drug against HIV infection, despite its undesirable side reactions, such as bone marrow suppression. In our aim to develop new chemical entity of anti-tumor and anti-HIV, the H-phosphonate 6 of AZT conjugate with diosgenin was synthesized by a tandem transesterification reaction for the first time. There are the merits of easy operation and high yield in the reported method. It could be extended to synthesize other diosgenin phosphonate conjugates such as carbohydrate and peptide.展开更多
目的探讨小剂量三氧化二砷(arsenic trioxide,As_2O_3)联合3’-叠氮-3’-脱氧胸腺嘧啶核苷(3’-azido-3’-deoxythymidine,AZT)对人肝癌HepG2细胞自噬的影响及其可能存在的作用机制,为肝癌的治疗提供新思路。方法分别用As_2O_3(2μmol/L...目的探讨小剂量三氧化二砷(arsenic trioxide,As_2O_3)联合3’-叠氮-3’-脱氧胸腺嘧啶核苷(3’-azido-3’-deoxythymidine,AZT)对人肝癌HepG2细胞自噬的影响及其可能存在的作用机制,为肝癌的治疗提供新思路。方法分别用As_2O_3(2μmol/L)、AZT(20μmol/L)及两药联合处理人肝癌HepG2细胞,同时以未经任何药物处理的HepG2细胞作为空白对照组。药物作用24 h后,吖定橙染色法观察各组人肝癌HepG2细胞中酸性囊泡和自噬溶酶体的堆积情况;荧光定量PCR法检测各组人肝癌HepG2细胞的Beclin1、lc3和p62 m RNA的表达;蛋白质印迹法检测各组人肝癌HepG2细胞Beclin1、lc3Ⅱ、lc3Ⅱ/Ⅰ、p62蛋白的表达。结果吖啶橙染色法显示:联合用药组酸性囊泡和自噬溶酶体的堆积多于对照组及各单药组(P<0.01);荧光定量PCR法显示:联合用药组HepG2细胞的Beclin1、lc3 m RNA表达明显高于对照组及各单药组(P<0.01),p62 m RNA表达低于对照组及各单药组(P<0.01);蛋白质印迹法检测结果显示联合用药组HepG2细胞的Beclin1、lc3Ⅱ、lc3Ⅱ/Ⅰ蛋白表达量高于对照组及各单药组(P<0.01),p62蛋白表达低于对照组及各单药组(P<0.01)。结论 As_2O_3联合AZT促进人肝癌HepG2细胞自噬的作用明显强于各单药组,可能与两药联合导致Beclin1的表达上调有关。展开更多
基金financial support from the National Natural Science Foundation of China(Nos.21672200,21772185,21801233)the assistance of the product characterization from the Chemistry Experiment Teaching Center of University of Science and Technology of China+1 种基金supported by China Postdoctoral Science Foundation(No.2018M632532)the Strategic Priority Research Program of the Chinese Academy of Sciences(No.XDB20000000)。
文摘An electrochemical amino-azidation of 2-aminostyre ne with sodium azide(NaN3)was developed,which can be carried out smoothly in water under metal-free condition,affording a series of 3-azido indolines with high yields.
文摘Azido-3′-deoxythymidine(AZT) was the first clinically approved drug against HIV infection, despite its undesirable side reactions, such as bone marrow suppression. In our aim to develop new chemical entity of anti-tumor and anti-HIV, the H-phosphonate 6 of AZT conjugate with diosgenin was synthesized by a tandem transesterification reaction for the first time. There are the merits of easy operation and high yield in the reported method. It could be extended to synthesize other diosgenin phosphonate conjugates such as carbohydrate and peptide.
文摘目的探讨小剂量三氧化二砷(arsenic trioxide,As_2O_3)联合3’-叠氮-3’-脱氧胸腺嘧啶核苷(3’-azido-3’-deoxythymidine,AZT)对人肝癌HepG2细胞自噬的影响及其可能存在的作用机制,为肝癌的治疗提供新思路。方法分别用As_2O_3(2μmol/L)、AZT(20μmol/L)及两药联合处理人肝癌HepG2细胞,同时以未经任何药物处理的HepG2细胞作为空白对照组。药物作用24 h后,吖定橙染色法观察各组人肝癌HepG2细胞中酸性囊泡和自噬溶酶体的堆积情况;荧光定量PCR法检测各组人肝癌HepG2细胞的Beclin1、lc3和p62 m RNA的表达;蛋白质印迹法检测各组人肝癌HepG2细胞Beclin1、lc3Ⅱ、lc3Ⅱ/Ⅰ、p62蛋白的表达。结果吖啶橙染色法显示:联合用药组酸性囊泡和自噬溶酶体的堆积多于对照组及各单药组(P<0.01);荧光定量PCR法显示:联合用药组HepG2细胞的Beclin1、lc3 m RNA表达明显高于对照组及各单药组(P<0.01),p62 m RNA表达低于对照组及各单药组(P<0.01);蛋白质印迹法检测结果显示联合用药组HepG2细胞的Beclin1、lc3Ⅱ、lc3Ⅱ/Ⅰ蛋白表达量高于对照组及各单药组(P<0.01),p62蛋白表达低于对照组及各单药组(P<0.01)。结论 As_2O_3联合AZT促进人肝癌HepG2细胞自噬的作用明显强于各单药组,可能与两药联合导致Beclin1的表达上调有关。
