Alleviation of PEGylated Puerarin on Erythrocyte Hemolysis Induced by Puerarin in Glucose-6-phosphate Dehydrogenase-deficient Rats / 中草药·英文版

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. © 2013 Tianjin Press of Chinese Herbal Medicines.

Optimization of synthetic process of PEGylated puerarin by orthogonal test with multi-index / 中草药

Objective: To optimize the synthesis of PEGylated puerarin (PEG-PUE) by orthogonal test with multi-index evaluation. Methods: The research has focused on the optimized interacting factors of the synthetic process of PEG-PUE by HPLC, such as ratio of PEG and PUE, catalyst DMAP dosage, and reaction time, using the purity, drug loading, and yield of PEG-PUE as evaluation indexes. Results: The optimum synthesis conditions of PEG-PUE were as follows, PEG-EDC-PUE-DMAP (1 : 1.2 : 1.2 : 0.3) and reaction time 12 h. Conclusion: The optimum synthesis condition of PEG-PUE is reasonable, as well as feasible.