首页> 外国专利> POLYRGD PEPTIDES OBTAINED BY CHEMICAL AND BIOTECHNOLOGY METHODS WITH INJURY REDUCING AND/OR NEUROPROTECTIVE EFFECTS AND A KIT FOR THEIR ACTIVITY EVALUATION

POLYRGD PEPTIDES OBTAINED BY CHEMICAL AND BIOTECHNOLOGY METHODS WITH INJURY REDUCING AND/OR NEUROPROTECTIVE EFFECTS AND A KIT FOR THEIR ACTIVITY EVALUATION

机译:化学和生物技术方法获得的具有伤害减轻和/或神经保护作用的小肽,以及用于评估其活性的试剂盒

摘要

The present invention relates to chemical compounds with injury-reducing and/or neuroprotective properties, of the general formula:         A1-H2N-(RGD)n-amide-A2where n=1-10.The compounds are preferably selected from the group: RGD1; RGD2; RGD3; RGD4; AcRGDl; AcRGD3, RGD10-PM; RGD10-PS.;A subject of the invention is a method for the preparation of the compound RGD10-PS, and its derivatives, by biological means.;Moreover, a subject of the invention involves methodology for the evaluation of the injury-reducing and/or neuroprotective activity of chemical compounds on a cellular level, by in vitro analysis of six injury factors, namely glucose deprivation, sodium azide-induced inhibition of cellular respiration, acidosis induced by sodium lactate acidification at pH 6.35, excitotoxicity induced by NMDA, excitotoxicity induced by glutamic acid and excitotoxicity induced by kainic acid, in neural cells.;The present invention also includes also a setup for the evaluation of the neuroprotective activity of the aforementioned chemical compounds.
机译:本发明涉及具有减少伤害和/或神经保护特性的通式的化合物:A 1 -H 2 N-(RGD) n -酰胺-A 2 其中n = 1-10。所述化合物优选地选自:RGD1;或RGD1。 RGD2; RGD3; RGD4; AcRGDl; AcRGD3,RGD10-PM; RGD10-PS 。;本发明的主题是通过生物学手段制备化合物RGD10-PS及其衍生物的方法。此外,本发明的主题涉及评估减轻伤害和减轻伤害的方法。通过体外对六个损伤因子的体外/ I分析,确定化合物在细胞水平上的神经保护活性,这些损伤因子包括葡萄糖剥夺,叠氮化钠诱导的细胞呼吸抑制,乳酸钠在pH 6.35酸化引起的酸中毒在神经细胞中由NMDA引起的兴奋性毒性,由谷氨酸引起的兴奋性毒性和由海藻酸引起的兴奋性毒性。本发明还包括用于评估上述化合物的神经保护活性的装置。

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