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.
出处
《天然产物研究与开发》
CAS
CSCD
北大核心
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)