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引用本文:杨旭超,王永波,木合布力·阿布力孜,西力扎提·阿不来提,任丙昭.查尔酮异甘草素类化合物的合成及其对子宫颈癌细胞的抑制作用[J].中国现代应用药学,2016,33(1):1-6.
YANG Xuchao,WANG Yongbo,MUHEBULI Abulizi,XILIZHATI Abulaiti,REN Bingzhao.Synthesis of Chalcone Isoliquiritigenin Compounds and Its Anti-cervical Cancer Activity[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(1):1-6.
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查尔酮异甘草素类化合物的合成及其对子宫颈癌细胞的抑制作用
杨旭超, 王永波, 木合布力·阿布力孜, 西力扎提·阿不来提, 任丙昭
新疆医科大学药学院药物化学有机教研室,乌鲁木齐 830011
摘要:
目的 设计并合成查尔酮异甘草素类化合物,并评价其抗子宫颈癌活性。方法 利用Claisen-Schmidt反应原理,通过微波固相合成5种目标化合物,并进行结构表征。以SiHa(人子宫颈鳞癌细胞)和HeLa(子宫颈癌细胞)细胞株作为体外模型,利用MTT法考察目标化合物对宫颈癌细胞增殖的抑制活性,利用流式细胞仪测定目标化合物对宫颈癌细胞促凋亡作用。结果与结论 快速高效合成了5个查尔酮异甘草素类化合物,其结构经1H-NMR、13C-NMR谱确认。目标化合物能有效抑制宫颈癌细胞增殖,促进宫颈癌细胞凋亡。
关键词:  查尔酮异甘草素  Claisen-Schmidt反应  微波固相反应  抗子宫颈癌活性
DOI:
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基金项目:国家自然科学基金(81260379);新疆研究生科研创新项目(XJGRI2014094)
Synthesis of Chalcone Isoliquiritigenin Compounds and Its Anti-cervical Cancer Activity
YANG Xuchao, WANG Yongbo, MUHEBULI Abulizi, XILIZHATI Abulaiti, REN Bingzhao
Department of Medicinal Chemistry, College of Pharmacy, Xinjiang Medical University, Urumqi 830011, China
Abstract:
OBJECTIVE To design and synthesis of chalcone isoliquiritigenin compounds, and evaluate its anti-cervical cancer activity. Methods Using Claisen-Schmidt reaction principle, by microwave solid-phase synthesis of 5 target compounds, and structural characterization. SiHa(human cervical squamous cell carcinoma) and HeLa(cervical cancer cells) cells as in vitro model, using MTT method to study the inhibitory activity of the target compounds on the proliferation of cervical cancer cells, promotion of the apoptosis of cervical cancer cells by flow cytometry. Results & conclusion Five chalcone isoliquiritigenin compounds were synthesized and characterized by 1H-NMR, 13C-NMR spectra. The target compound could inhibit the proliferation of cervical cancer cells effectively and promote the apoptosis of cervical cancer cells.
Key words:  chalcone isoliquiritigenin compound  Claisen-Schmidt reaction  microwave solid-phase synthesis  anti-cervical cancer activity
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