姜黄素衍生物FM0807体内外抗肿瘤作用研究_临床医学论文.docVIP

姜黄素衍生物FM0807体内外抗肿瘤作用研究_临床医学论文 姜黄素衍生物FM0807体内外抗肿瘤作用研究_临床医学论文 作者：叶丽香 张志强 刘洋 李鹏 许建华 【摘要】 　　目的 研究姜黄素衍生物FM0807的体内外抗肿瘤作用。 方法 应用四甲基偶氮唑蓝(MTT)法检测FM0807对多种肿瘤细胞生长的抑制作用；建立H22小鼠移植肿瘤模型进行体内实验，观察尾静脉、腹腔及口服给予FM0807后体内抗肿瘤活性。 结果 体外抗肿瘤研究表明，FM0807对K562，HL260，MGC，HepG2，Sw480等多种人肿瘤细胞均有生长抑制作用，IC50分别为5.21，6.25，7.37，24.72，9.72 μg/mL；体内抗肿瘤研究表明，尾静脉、腹腔及口服给予FM0807后对小鼠H22肿瘤生长均有明显抑制作用，抑制率分别达到69.0%，66.3%，52.5%。 结论 FM0807体内外均有较强抗肿瘤作用。 【关键词】 姜黄素； 抗肿瘤药； 肿瘤移植； 疾病模型，动物 　　Department of Pharmacology, School of Pharmacy, Fujian Medical University, Fuzhou 350004,China;New Drug Research Insititute of Fujian Medical University, Fuzhou 350004,China;Department of Medical Chemistry,School of Pharmacy, Fujian Medical University, Fuzhou 350004,China;Department of Pharmacology, School of Pharmacy, Fujian Medical University, Fuzhou 350004,China; 　　ABSTRACT: Objective To evaluate the antitumor effect of FM0807 in vitro and in vivo. Methods The MTT assay was used to examine the growth arrest of a variety of tumor cells by FM0807. The H22 mouse tumor xenograft models were established and antitumor effect of FM0807 given by tail vein injection, intraperitoneal injection and oral administration respectively was measured. Results FM0807 remarkably inhibited the proliferation of many kinds of tumor cells. The IC50 values to K562 , HL60，MGC803, HepG2 and SW480 were 5.21, 6.25, 7.37, 24.72 and 9.72 μg/mL respectively. FM0807 showed significant inhibitory effect on H22, the inhibitory rates of FM0807 given by tail vein injection, intraperitoneal injection and oral administration were 69.0%, 66.3%, 52.5%, respectively. Conclusion FM0807 was able to inhibit potently the growth of the tumor cells in vitro and in vivo. 　　KEY WORDS: CURCUMIN； antineoplastic agents； neoplasm transplantation； disease models, animal 　　姜黄素(Curcumin,Cur)是姜科植物姜黄（Curcuma Longa L.）的有效成分，具有抗肿瘤、抗炎、抗氧化、提高免疫力、抗胆结石等广泛的药理作用[l]。近年来，Cur在肿瘤预防和治疗方面的作用越来越引起重视[23]。但Cur水溶性差，水溶液易水解，首过消除现象明显，生物利用度低，成为限制其临床应用的主要因素和产业化的瓶颈，因此对Cur结构改造一直是该领域的研究热点[4。本课题组设计合成的Cur衍生物FM080