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共轭亚油酸-吉西他滨偶联物的体外抗肿瘤活性研究
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| 篇名： | 共轭亚油酸-吉西他滨偶联物的体外抗肿瘤活性研究 |
| TITLE： | |
| 摘要： | 目的：研究共轭亚油酸-吉西他滨偶联物（CLA-GEM）的体外抗肿瘤活性。方法：考察不同浓度（0.001～100 μmol/L）的CLA-GEM和吉西他滨（GEM）溶液分别与不同肿瘤细胞（乳腺癌MCF-7细胞、乳腺癌MDA-MB-231细胞、肺腺癌A549细胞、小细胞肺癌NCI-H446细胞、脑胶质瘤C6细胞）共同孵育72 h的半数抑制浓度（IC50）和与MCF-7细胞共同孵育24、48、72 h的细胞存活率。将核酸转运载体抑制剂NBMPR（100 μmol/L）和双嘧达莫（4 μg/ml）分别作用于MCF-7细胞和MDA-MB-231细胞，考察0.001～100 μmol/L的 CLA-GEM和GEM对核酸转运载体的依赖性（以IC50为指标）。考察1 μmol/L的CLA-GEM和GEM与MCF-7细胞共同孵育24 h的细胞周期变化。结果：与GEM比较，CLA-GEM孵育后对MCF-7、MDA-MB-231、NCI-H446细胞的IC50更低（P＜0.01），对A549、C6细胞的IC50差异无统计学意义（P＞0.05）。GEM孵育48 h后和CLA-GEM孵育24 h后MCF-7细胞存活率开始明显降低，GEM孵育72 h后细胞存活率最低为21％，而CLA-GEM能完全杀死肿瘤细胞。与GEM或CLA-GEM单用比较，经NBMPR、双嘧达莫处理的GEM对MCF-7和MDA-MB-231细胞的IC50明显升高（P＜0.01），而CLA-GEM对细胞的IC50差异无统计学意义（P＞0.05）。与GEM比较，CLA-GEM可使MCF-7细胞的S期延长约6％（P＜0.01）。结论：CLA-GEM较GEM的抗肿瘤活性更强、起效更快，且不受核酸转运载体的影响。 |
| ABSTRACT： | OBJECTIVE： To study in vitro anticancer activity of conjugated linoleic acid-gemcitabine conjugate （CLA-GEM）. METHODS： IC50 of different tumor cells （breast cancer MCF-7 cell， breast cancer MDA-MB-231 cell， lung cancer A549 cell， small cell lung cancer NCI-H446 cell， glioma C6 cell） were investigated after treated with different concentrations （0.001-100 μmol/L） of CLA-GEM and gemcitabine （GEM） for 72 h； survival rates of MCF-7 cell were investigated after treated with above solution for 24， 48 and 72 h. The dependence of 0.001-100 μmol/L CLA-GEM and GEM to nucleoside transporter was investigated （by IC50） through MCF-7 cells and MDA-MB-231 cells treated with nucleoside transporter inhibitors （NBMPR， 100 μmol/L） and dipyridamole （4 μg/ml）. The change of MCF-7 cell cycle was investigated after treated with 1 μmol/L CLA-GEM and GEM for 24 h. RESULTS： Compared with GEM， IC50 of MCF-7， MDA-MB-231 and NCI-H446 cells became lower after treated with CLA- GEM （P＜0.01）， there were no statistical significances in IC50 between A549 and C6 cells （P＞0.05）. Survival rate of MCF-7 cells decreased significantly after treated with GEM for 48 h and CLA-GEM for 24 h. Survival rate of MCF-7 cells was the lowest， being 21％ after treated with GEM for 72 h， while tumor cells were sacrificed by CLA-GEM completely. Compared with GEM or CLA-GEM， IC50 of MCF-7 and MDA-MB-231 cells increased significantly after treated with NBMPR， dipyridamole combined with GEM （P＜0.01）； there were no statistical significance in IC50 after treated with NBMPR， dipyridamole combined with CLA-GEM （P＞0.05）. Compared with GEM， CLA-GEM could prolong 6％ of S stage of MCF-7 cells （P＜0.01）. CONCLUSIONS： Compared with GEM， CLA-GEM exhibits significant antitumor activity and rapid action， and it isn’t influenced by nucleic acid transportation. |
| 期刊： | 2016年第27卷第25期 |
| 作者： | 陶小妹，顾红燕，李丽莉，陶巍巍 |
| AUTHORS： | TAO Xiaomei，GU Hongyan，LI Lili，TAO Weiwei |
| 关键字： | 共轭亚油酸-吉西他滨偶联物；抗肿瘤；核酸转运；细胞周期 |
| KEYWORDS： | Conjugated linoleic acid-gemcitabine conjugate； Anticancer； Nucleic acid transportation； Cell cycle |
| 阅读数： | 410 次 |
| 本月下载数： | 8 次 |
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