[MORPHOFUNCTIONAL STATE OF BLOOD CELLS AFTER CHRONIC EXPOSURE OF THE PROTEIN KINASES INHIBITOR MALEIMIDE DERIVATIVE].

I. Byelinska, O. Lynchak, S. M. Tsyvinska, V. Rybalchenko
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引用次数: 6

Abstract

The effect of the protein kinases inhibitor maleimide derivative (MI-1, 1-(4-Cl-benzyl)-3-Cl-4-(CF3-phenylamino)-1H-pyrrole-2,5-dione), inhibitor of VEGF-R1,2,3, FGF-R1, EGF-R(h), PDK1, Src(h), Syk(h), YES, ZAP70 et al. with antineoplastic activity, on blood cells parameters of rats after chronic exposure has been studied. Administration of MI-1 at doses 0.027 and 2.7 mg/kg (suppress colon carcinogenesis) for 20 and 26 weeks does not affect the morphofunctional state of red blood cells in healthy rats. This is confirmed by the lack of differences in the concentration of hemoglobin in blood, red blood cells count, mean corpuscular hemoglobin and mean corpuscular hemoglobin concentration, hematocrit and mean corpuscular volume, and the number of reticulocytes in blood after 20 and 26 weeks of exposure compared with the control group. MI-1 at indicated doses does not influence total leukocytes count and content (eosinophilic and neutrophilic granulocytes, lymphocytes, monocytes) and does not inhibit thrombocytopoiesis (platelet count remains unchanged). No negative effect of MI-1 on hematopoiesis is not limited (by the hemopoietic system) use of this compound as a potential antitumor drug
[慢性暴露于蛋白激酶抑制剂马来酰亚胺衍生物后血细胞的形态功能状态]。
研究了具有抗肿瘤活性的蛋白激酶抑制剂马酰亚胺衍生物(mi - 1,1 -(4- cl -苄基)-3- cl -4-(cf3 -苯胺)- 1h -吡罗-2,5-二酮)、VEGF-R1、2,3、FGF-R1、EGF-R(h)、PDK1、Src(h)、Syk(h)、YES、ZAP70等抑制剂对慢性暴露大鼠血细胞参数的影响。以0.027和2.7 mg/kg(抑制结肠癌发生)剂量给药20周和26周对健康大鼠红细胞形态功能状态没有影响。暴露20周和26周后与对照组相比,血液中血红蛋白浓度、红细胞计数、平均红细胞血红蛋白和平均红细胞血红蛋白浓度、红细胞压积和平均红细胞体积、网状红细胞数量均无差异,证实了这一点。指定剂量的MI-1不影响白细胞总数和含量(嗜酸性粒细胞和嗜中性粒细胞、淋巴细胞、单核细胞),也不抑制血小板生成(血小板计数保持不变)。MI-1对造血没有负面影响,不受造血系统的限制,使用这种化合物作为潜在的抗肿瘤药物
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