有机酸对人中性粒细胞髓过氧化物酶过氧化、氯化和硝化活性的抑制作用

B. Sarkarati
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引用次数: 0

摘要

多形核白细胞髓过氧化物酶是一种重要的氧化代谢酶,在氧化应激和炎症条件下的组织损伤中起关键作用。因此,其抑制剂成为近年来新药开发的研究热点。本研究的目的是确定有机酸对髓过氧化物酶的过氧化、氯化和硝化活性的抑制作用。方法对植物中富含的7种天然有机酸进行测定。测定了不同有机酸对骨髓过氧化物酶活性的影响,并测定了不同有机酸对骨髓过氧化物酶的抑制率和动力学参数。结果所有有机酸均对脊髓过氧化物酶的不同活性有抑制作用。过氧化、氯化和硝化活性的IC50值比较表明,草酸是髓过氧化物酶活性最强的抑制剂,而柠檬酸和琥珀酸是最弱的抑制剂。结论所检测的有机酸均为髓过氧化物酶抑制剂。特别是草酸和富马酸是药物开发研究的热门候选物质。需要更多的研究来确定有机酸在体内的作用及其在疾病治疗中的作用。
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Inhibitory effect of organic acids on human neutrophil Myeloperoxidase’s peroxidation, chlorination, and nitration activities
Abstract Objectives Myeloperoxidase from polymorphonuclear leukocytes is an important enzyme in oxidative metabolism and has a key role in tissue injuries in oxidative stress and inflammatory conditions. Therefore, its inhibitors have become the focus of studies on new drug development in recent years. The aim of the study was to determine the inhibitory effect of organic acids on the peroxidation, chlorination, and nitration activities of myeloperoxidase. Methods Seven organic acids naturally abundant in plants were tested. Different activities of myeloperoxidase were measured in the presence of various amounts of organic acids, and inhibition rates and kinetic parameters were determined for each organic acid separately. Results All the organic acids examined had inhibitory effects on the different activities of myeloperoxidase. Comparison of the IC50 values obtained for peroxidation, chlorination, and nitration activities showed that oxalic acid was the strongest inhibitor of myeloperoxidase activity, while citric acid and succinic acid were the weakest. Conclusions The results suggested that all the organic acids examined are inhibitors of myeloperoxidase. In particular, oxalic acid and fumaric acid are popular candidates for drug development research. More studies are needed to determine the in vivo effects of organic acids and their effects in the treatment of disease.
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