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两种5-乙酰氨基查尔酮对乳腺癌的体外和体内抗癌潜力评估

Evaluation of in vitro and in vivo anticancer potential of two 5-acetamido chalcones against breast cancer.

作者信息

Wankhede Sonal, Kumar Nitesh, Simon Lalitha, Biswas Subhankar, Gourishetti Karthik, Ramalingayya Grandhi Venkata, Joshi Mit, Rao C Mallikarjuna

机构信息

Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka-576104, India.

Department of Chemistry, Manipal Institute of Technology, Manipal University, Manipal, Karnataka-576104, India.

出版信息

EXCLI J. 2017 Oct 19;16:1150-1163. doi: 10.17179/excli2017-624. eCollection 2017.

DOI:10.17179/excli2017-624
PMID:29285012
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5735347/
Abstract

Two 5'acetamido chalcones, C1 and C2 were synthesized by Claisen-Schmidt condensation method and characterized by IR, LC-MS, H NMR and C NMR. These compounds were evaluated for anticancer activity in breast cancer cell lines (MCF-7 and MDA-MB-231) using MTT assay, anti-metastatic assay, apoptotic screening by AO/EB staining and in N-Methyl-N-nitrosourea (MNU) induced breast carcinoma model. Sprague-Dawley rats with developed tumors (50 mg/kg MNU ) were grouped in four, namely MNU control (0.25 % of CMC ), standard group (doxorubicin 2 mg/kg once in 4 days, ), C1 and C2 groups (50 mg/kg each). After 21 days of treatments, tumor volume and weight were assessed. Excised tumors were subjected to DNA fragmentation study. MTT assay showed IC values of 62.56 and 37.8 µM by for C1 and C2. Both compounds increased apoptotic bodies more than 3 fold compared to normal control in AO/EB staining. Antimetastatic (scratch wound) assay showed a significant (p<0.05) reduction in cell migration after 24 h and 48 h treatments compared to normal control. In studies, tumor weight and tumor volume were significantly (p<0.05) reduced in the doxorubicin group as well as in test groups compared to MNU control. DNA fragmentation assay showed an increase in the number of bands formed in C1 and C2 compared to normal control. Results obtained from and studies demonstrated the significant anticancer potentials of C1 and C2.

摘要

通过克莱森-施密特缩合方法合成了两种5'-乙酰氨基查尔酮C1和C2，并通过红外光谱（IR）、液相色谱-质谱联用（LC-MS）、氢核磁共振（H NMR）和碳核磁共振（C NMR）对其进行了表征。使用MTT法、抗转移试验、AO/EB染色凋亡筛选以及在N-甲基-N-亚硝基脲（MNU）诱导的乳腺癌模型中，对这些化合物在乳腺癌细胞系（MCF-7和MDA-MB-231）中的抗癌活性进行了评估。将患有肿瘤的斯普拉格-道利大鼠（50mg/kg MNU）分为四组，即MNU对照组（0.25%的羧甲基纤维素钠）、标准组（阿霉素2mg/kg，每4天一次）、C1组和C2组（每组50mg/kg）。治疗21天后，评估肿瘤体积和重量。对切除的肿瘤进行DNA片段化研究。MTT试验显示C1和C2的半数抑制浓度（IC）值分别为62.56和37.8μM。在AO/EB染色中，与正常对照相比，两种化合物使凋亡小体增加了3倍以上。抗转移（划痕伤口）试验显示，与正常对照相比，处理24小时和48小时后细胞迁移显著（p<0.05）减少。在研究中，与MNU对照组相比，阿霉素组以及试验组的肿瘤重量和肿瘤体积均显著（p<0.05）降低。DNA片段化试验显示，与正常对照相比，C1和C2中形成的条带数量增加。从和研究中获得的结果证明了C1和C2具有显著的抗癌潜力。

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