Lethal Effect of Benzene Nitrogen Mustard Glucoside Derivate on K562 Cells

IF 3.1 4区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
Tie-mei LIU , Guang-ze ZHU , Jin-song ZHOU , Zhi SUN , Feng XIE
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引用次数: 1

Abstract

A new synthesized benzene nitrogen mustard was converted into glycosyl donor-trichloroacetimidate that was glycosylated with p-nitrophenol(glycosyl donors) to form β-lactosyl p-nitrobenzene under the protection of acetyl in a stereoselective manner, was prepared and evaluated for its cytotoxicity towards cultured K562 cell line. Methylthiazoy tetrazolium(MTT) assay, transmission electron microscopy(TEM), flow cytometry(FCM) and immunohistochemistry were utilized to explore the mechanisms of how the compound arrests the growth of HCT-T cells. This new synthesed benzene nitrogen mustard glucoside derivate(BNMGD) presented a lower toxicity to normal cells, but is significantly more toxic to K562 cells compared with nitrogen mustard, meanwhile it can induce the apoptosis of K562 cells. These results indicate that the new synthesized BNMGD can inhibit the growth of K562 cells and induce the apoptosis, and its cytotoxicity towards cultured K562 cell line is much more effective than that of nitrogen mustard.

苯氮芥糖苷衍生物对K562细胞的杀伤作用
在乙酰基的保护下,合成了一种新的苯氮芥,将其转化为糖基供体-三氯乙酸酯与对硝基苯酚(糖基供体)糖基化形成β-乳糖基对硝基苯,并对培养的K562细胞株进行了细胞毒性评价。利用甲基噻唑四氮唑(MTT)测定、透射电镜(TEM)、流式细胞术(FCM)和免疫组织化学方法探讨该化合物抑制HCT-T细胞生长的机制。新合成的苯氮芥糖苷衍生物(BNMGD)对正常细胞的毒性较低,但对K562细胞的毒性明显高于氮芥,同时能诱导K562细胞凋亡。上述结果表明,新合成的BNMGD能抑制K562细胞的生长,诱导细胞凋亡,对培养的K562细胞株的细胞毒性远高于氮芥。
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来源期刊
CiteScore
5.30
自引率
6.50%
发文量
152
审稿时长
3.0 months
期刊介绍: The journal publishes research articles, letters/communications and reviews written by faculty members, researchers and postgraduates in universities, colleges and research institutes all over China and overseas. It reports the latest and most creative results of important fundamental research in all aspects of chemistry and of developments with significant consequences across subdisciplines. Main research areas include (but are not limited to): Organic chemistry (synthesis, characterization, and application); Inorganic chemistry (bio-inorganic chemistry, inorganic material chemistry); Analytical chemistry (especially chemometrics and the application of instrumental analysis and spectroscopy); Physical chemistry (mechanisms, catalysis, thermodynamics and dynamics); Polymer chemistry and polymer physics (mechanisms, material, catalysis, thermodynamics and dynamics); Quantum chemistry (quantum mechanical theory, quantum partition function, quantum statistical mechanics); Biochemistry; Biochemical engineering; Medicinal chemistry; Nanoscience (nanochemistry, nanomaterials).
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