中国药师
中國藥師
중국약사
CHINA PHARMACIST
2015年
2期
194-196
,共3页
大黄素%希夫氏碱%衍生物%抗肿瘤活性
大黃素%希伕氏堿%衍生物%抗腫瘤活性
대황소%희부씨감%연생물%항종류활성
Emodin%Schiff base%Derivatives%Anti-tumor activity
目的：：合成大黄素10-位希夫氏碱衍生物并研究其抗肿瘤活性。方法：将大黄素与氨衍生物在无水乙醇中以醋酸催化而合成,用核磁共振氢谱、电子轰击质谱法进行结构表征；用四唑盐( MTT)比色法测定其对k562肿瘤细胞增殖抑制率并计算其IC50值。结果：合成了3个大黄素10-位希夫氏碱衍生物,对k562肿瘤细胞的IC50值分别是4.5,3.8,2.0μmol·L-1。结论：大黄素10位希夫氏碱衍生物提高了其母体化合物的抗肿瘤活性并增加了成药性,值得进一步研究。
目的：：閤成大黃素10-位希伕氏堿衍生物併研究其抗腫瘤活性。方法：將大黃素與氨衍生物在無水乙醇中以醋痠催化而閤成,用覈磁共振氫譜、電子轟擊質譜法進行結構錶徵；用四唑鹽( MTT)比色法測定其對k562腫瘤細胞增殖抑製率併計算其IC50值。結果：閤成瞭3箇大黃素10-位希伕氏堿衍生物,對k562腫瘤細胞的IC50值分彆是4.5,3.8,2.0μmol·L-1。結論：大黃素10位希伕氏堿衍生物提高瞭其母體化閤物的抗腫瘤活性併增加瞭成藥性,值得進一步研究。
목적：：합성대황소10-위희부씨감연생물병연구기항종류활성。방법：장대황소여안연생물재무수을순중이작산최화이합성,용핵자공진경보、전자굉격질보법진행결구표정；용사서염( MTT)비색법측정기대k562종류세포증식억제솔병계산기IC50치。결과：합성료3개대황소10-위희부씨감연생물,대k562종류세포적IC50치분별시4.5,3.8,2.0μmol·L-1。결론：대황소10위희부씨감연생물제고료기모체화합물적항종류활성병증가료성약성,치득진일보연구。
Objective: To synthesize 10-position schiff base derivatives of emodin and study the anti-tumor activity. Methods:The 10-position schiff base derivatives of emodin were synthesized through emodin reacting with ammonia derivatives in absolute alcohol with acetic acid as the catalytic agent. Their structures were characterized by 1 H-NMR and ESI-MS, and the anti-tumor activity on k562 cells was determined by MTT method. Results:Three 10-position schiff base derivatives were synthesized and the structures were confirmed, and the IC50 on k562 cells was 4. 5, 3. 8 and 2. 0 μmol·L-1 , respectively. Conclusion:The 10-position schiff base de-rivatives of emodin can improve the anti-tumor activity and druggability of the parent compound, which are worthy of further study.
