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Liposomal Drug with Carnosine and Lipoic Acid: Preparation, Antioxidant and Antiplatelet Properties
Biophysics Pub Date : 2021-07-02 , DOI: 10.1134/s0006350921020214
V. A. Shchelkonogov 1, 2, 3 , E. S. Darnotuk 1 , N. S. Shastina 1 , G. M. Sorokoumova 1 , A. V. Chekanov 2, 3 , O. A. Baranova 2, 3 , E. Yu. Solov’eva 2 , A. I. Fedin 2 , K. D. Kazarinov 3 , S. L. Stvolinsky 4 , T. N. Fedorova 4
Affiliation  

The conditions for producing phosphatidylcholine liposomes containing lipoic acid and carnosine together were determined. The obtained liposomes are 180–250-nm spherical particles with an efficiency of lipoic acid inclusion of 50–70% (for carnosine, 17–33%). Based on the model of the oxidation of phosphatidylcholine by hydrogen peroxide, an antioxidant effect of carnosine, lipoic acid or lipoic acid with carnosine together was demonstrated; it consisted in inhibition of lipid peroxidation process, which was manifested in a decrease in the formation of lipid peroxidation products that react with thiobarbituric acid. It was established that lipoic acid (5 mM) and carnosine (0.1–10 mM) in liposomes exhibit an antioxidant effect. At the same time, it was demonstrated that the content of the appropriate lipid peroxidation products in liposomes with antioxidants (lipoic acid + carnosine) was 15 times lower than in control liposomes (without antioxidants). The effect of the obtained liposomal drugs on the platelet aggregation induced by arachidonic acid was evaluated. It was found that the liposomal drug containing lipoic acid (1.5 mM) and carnosine (2.1 mM) inhibited platelet aggregation by 50–55% relative to the control (platelets and arachidonic acid), while liposomes without antioxidants and water-soluble forms of carnosine and lipoic acid had almost no effect on platelet aggregation caused by arachidonic acid.



中文翻译:

含有肌肽和硫辛酸的脂质体药物:制备、抗氧化和抗血小板特性

确定了生产含有硫辛酸和肌肽的磷脂酰胆碱脂质体的条件。获得的脂质体是 180-250-nm 的球形颗粒,硫辛酸的包含效率为 50-70%(对于肌肽,17-33%)。基于过氧化氢氧化磷脂酰胆碱的模型,证明了肌肽、硫辛酸或硫辛酸与肌肽共同作用的抗氧化作用;它包括抑制脂质过氧化过程,这表现为与硫代巴比妥酸反应的脂质过氧化产物的形成减少。已确定脂质体中的硫辛酸 (5 mM) 和肌肽 (0.1-10 mM) 具有抗氧化作用。同时,结果表明,含有抗氧化剂(硫辛酸 + 肌肽)的脂质体中适当脂质过氧化产物的含量比对照脂质体(不含抗氧化剂)低 15 倍。评价所得脂质体药物对花生四烯酸诱导的血小板聚集的影响。发现含有硫辛酸 (1.5 mM) 和肌肽 (2.1 mM) 的脂质体药物相对于对照(血小板和花生四烯酸)抑制了 50-55% 的血小板聚集,而不含抗氧化剂和水溶性肌肽的脂质体硫辛酸对花生四烯酸引起的血小板聚集几乎没有影响。评价所得脂质体药物对花生四烯酸诱导的血小板聚集的影响。发现含有硫辛酸 (1.5 mM) 和肌肽 (2.1 mM) 的脂质体药物相对于对照(血小板和花生四烯酸)抑制了 50-55% 的血小板聚集,而不含抗氧化剂和水溶性肌肽的脂质体硫辛酸对花生四烯酸引起的血小板聚集几乎没有影响。评价所得脂质体药物对花生四烯酸诱导的血小板聚集的影响。发现含有硫辛酸 (1.5 mM) 和肌肽 (2.1 mM) 的脂质体药物相对于对照(血小板和花生四烯酸)抑制了 50-55% 的血小板聚集,而不含抗氧化剂和水溶性肌肽的脂质体硫辛酸对花生四烯酸引起的血小板聚集几乎没有影响。

更新日期:2021-07-02
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