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Antiproliferative Activities of Cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornithine] and its in vitro anti-VEGFR-2 Inhibition
Journal of Scientific & Industrial Research ( IF 0.7 ) Pub Date : 2020-05-15
A E Amr, E A Elsayed, A A Almehizia, M A Wadaan, Nermien M Sabry, A Baabbad

Research is continuing for synthesizing new molecules with potent pharmacological effects against cancer. In the current work we prepared a new tripeptide and investigated its in vitro as well as in vivo antiproliferative effects. Firstly, cyclo (Nα-pyrido)-bis-[(L-valinyl)-L-ornithine] was prepared and then tested against 17 different cancer cell lines. Results showed that the prepared compound showed increased cytotoxic effects (in terms of decreased IC50 value), which reached about 20.3, 28.1, 18.3 and 72.3% against RKOP27, K561, GOTO, HT1080 cell lines, respectively, in comparison to standard positive controls. Furthermore, cancer cell viability was probably affected through VEGFR-2 kinase inhibition.

中文翻译:

环(Nα-吡啶基)-双-[[(L-缬氨酰基)-L-鸟氨酸]的抗增殖活性及其体外抗VEGFR-2抑制作用

合成具有抗药理作用强的新分子的研究仍在继续。在当前的工作中,我们制备了一种新的三肽并研究了其在体内以及体外的抗增殖作用。首先,环(Ñ α -吡啶) -双- [(L-缬氨酰基)-L-鸟氨酸]制备,然后与17个不同的癌细胞系进行测试。结果表明,与标准阳性对照相比,所制备的化合物对RKOP27,K561,GOTO,HT1080细胞系的细胞毒性作用增强(降低的IC50值),分别达到约20.3%,28.1%,28.1%,18.3%和72.3%。此外,癌细胞的生存能力可能受到了VEGFR-2激酶抑制的影响。
更新日期:2020-05-15
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