Wang Ai-Yun, Lu Yin, Zhu Hai-Liang, Jiao Qing-Cai
State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, P.R. China.
Oncol Lett. 2012 Feb;3(2):373-376. doi: 10.3892/ol.2011.474. Epub 2011 Nov 8.
Urea derivatives have been widely used in biology and medicine. The substituted urea derivative URD12 introduced in this study exhibits cytotoxic activity against the K562 human leukemia and KB human mouth epidermal carcinoma cell lines. To further study the bioactivity of URD12 and examine its feasibility as a new antitumor drug, we applied in vivo and in vitro assays to investigate the antitumor activity of URD12. URD12 was prepared and its cytotoxicity was evaluated using the BGC-823 human gastric carcinoma, MGC-803 human gastric carcinoma, SMMC-7721 human hepatoma and HepG2 human hepatocellular carcinoma cell lines using MTT assays. Antitumor activity in vivo was confirmed in mice bearing H22 hepatocellular carcinoma cells. Organ coefficient was used to further elucidate the cytotoxic mechanisms of URD12. URD12 inhibited the growth of tested tumor cell lines in vitro and the growth of H22 mouse hepatocellular carcinoma in vivo with no effects on the weight, spleen and thymus coefficient of tumor-bearing mice. In conclusion, our findings indicate that URD12 is an effective antitumor agent without evident immunosuppression effects.
尿素衍生物已在生物学和医学中得到广泛应用。本研究中引入的取代尿素衍生物URD12对K562人白血病细胞系和KB人口腔表皮癌细胞系具有细胞毒活性。为进一步研究URD12的生物活性并检验其作为新型抗肿瘤药物的可行性,我们应用体内和体外试验来研究URD12的抗肿瘤活性。制备了URD12,并使用MTT法以BGC - 823人胃癌细胞系、MGC - 803人胃癌细胞系、SMMC - 7721人肝癌细胞系和HepG2人肝癌细胞系评估其细胞毒性。在携带H22肝癌细胞的小鼠体内证实了其体内抗肿瘤活性。使用器官系数进一步阐明URD12的细胞毒性机制。URD12在体外抑制了受试肿瘤细胞系的生长,并在体内抑制了H22小鼠肝癌的生长,且对荷瘤小鼠的体重、脾脏和胸腺系数无影响。总之,我们的研究结果表明URD12是一种有效的抗肿瘤药物,且无明显的免疫抑制作用。