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Alleviation of PEGylated Puerarin on Erythrocyte Hemolysis Induced by Puerarin in Glucose-6-phosphate Dehydrogenase-deficient Rats

机译:PEG化葛根素对6-磷酸葡萄糖脱氢酶缺乏症大鼠中葛根素引起的红细胞溶血的缓解

摘要

Objective To explore and analyze the reducing hemolytic effects of PEGylated puerarin (PEG-PUE) on erythrocytes induced by PUE in glucose-6-phosphate dehydrogenase (G6PD)-deficient rats. Methods The rat model with G6PD-deficiency was established via sc injecting 1% acetylphenyl-hydrazine. Then the G6PD-deficient erythrocyte suspension obtained from this rat model was used to evaluate the hemolytic effects of PUE and the reducing hemolytic effects of PEG-PUE via hemolytic activity and erythrocyte osmotic fragility assay. Results It was found that PUE could cause a serious hemolysis to the erythrocyte suspension with the increase of drug concentration and the prolongation of drug incubation time, the hemolytic rate of PUE was up to 40%, while the addition of PEG-PUE to the erythrocyte suspension revealed no significant hemolysis. Additionally, the result of erythrocyte osmotic fragility indicated that PEG-PUE exerted a slight effect on the erythrocyte membranes, and the NaCl concentration that induced 50% hemolysis (32 mmol/L) was about one-third PUE. Conclusion These results demonstrate that PEG-PUE could play a significant role in reducing the side effect of hemolysis induced by PUE. The low hemolytic activity of PEG-PUE makes it a favorable candidate for in vivo tests and PEG-PUE could also provide the useful insight for the further formulation development as an innovative drug.
机译:目的探讨并分析聚乙二醇化葛根素(PEG-PUE)对葡萄糖-6-磷酸脱氢酶(G6PD)乙型大鼠诱导红细胞诱导红细胞的溶血作用。方法通过喷射1%乙酰苯基 - 肼建立具有G6PD缺乏的大鼠大鼠模型。然后使用从该大鼠模型获得的G6PD缺陷的红细胞悬浮液来评估PUE的溶血作用和通过溶血活性和红细胞渗透脆性测定的降低PEG-PUE的溶血作用。结果发现,随着药物浓度的增加和药物孵化时间的延长,紫外线可能导致红细胞悬浮液中的严重溶血,紫水的溶血率高达40%,同时向红细胞添加PEG-Bue悬浮液显示没有显着的溶血。另外,红细胞渗透性脆性的结果表明,PEG-PUE对红细胞膜产生轻微影响,并且诱导50%溶血(32mmol / L)的NaCl浓度约为三分之一的灌注。结论这些结果表明,PEG-PUE可能在降低灌注诱导的溶血的副作用方面发挥重要作用。 PEG-PUE的低溶血活性使其成为体内测试的有利候选者,并且PEG-PUE还可以为进一步的配方开发作为一种创新药物提供有用的见解。

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