双(3-吗啉丙氧基)姜黄素抗肿瘤活性研究  

Antitumor Activity of Bis(3-morpholinopropoxy) Curcumin

作　　者：刘洋[1] 陈纯[2] 张志强[3] 许建华[3] 

机构地区：[1]福建医科大学药学院药物化学系 [2]福建医科大学药学院药理学系 [3]福建医科大学药学院新药研究所福建省高校天然药物药理学重点实验室,福州350108

出　　处：《天然产物研究与开发》2015年第4期695-698,共4页Natural Product Research and Development

基　　金：福建省科技厅项目(2011J01189);福建省教育厅项目(JA12138);国家自然科学基金(81173096)

摘　　要：合成双(3-吗啉丙氧基)姜黄素(PR1),研究PR1体内外抗肿瘤活性。姜黄素与N-(3-氯丙基)吗啉反应制备PR1,MTT法评价PR1体外对人肾癌细胞OS-RC-2、786-O和人慢性粒细胞白血病耐药细胞KA的抑制增殖活性,考察PR1体内抑制人结肠癌HT29裸鼠移植性肿瘤活性。PR1体外对肾癌细胞OS-RC-2和786-O抑制活性比姜黄素强,而对白血病耐药细胞KA抑制活性比姜黄素差。PR1体内对BALB/C-nu小鼠HT29皮下移植瘤的抑制作用明显,100 mg/kg·d灌胃的抑制率为55.7%,差别具有显著性(P<0.01),对裸鼠的体重无明显影响。PR1在体内外均有较强抗肿瘤活性。The objectives of this study were to synthesize bis （3-morpholinopropoxy）eurcumln （PR1） and to evaluate its antitumor activity. PR1 was synthesized from curcumln and N-（3-chlompropyl） morpholine. The in vitro antitumor activities of PR1 was evaluated through MTF assays against gastric carcinoma ceils （ OS-RC-2 and 786-O） and chronic myelogenous leukemia resistance cell （KA）. The in vivo antitumor activities of PR1 were evaluated by its growth inhibition of human colon cancer HT29 tumor xenograft in BALB/C-nu nude mice. Compared with curcumln, PR1 showed improved activities against OS-RC-2,786-0 ceUs, while less activities against KA cell. PR1 showed remarkable in vivo tumor growth inhibition activity. A dose of 100 mg/kg . d was able to inhibit the growth of HT29 xenograft in BALB/C-nu nude mice by 55.7%. No obvious decrease on the body weight of tested nude mice was observed. In concluslon,PR1 showed obvious antltumor activities both in vitro and in vivo.

关 键 词：姜黄素 姜黄素衍生物 双(3-吗啉丙氧基)姜黄素 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学]