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报告:钯与谷胱甘肽、N-乙酰半胱氨酸、D-青霉胺的共轭化学。

Report: Palladium glutathione, N-acetylcysteine, D-penicillamine conjugation chemistry.

作者信息

Mukhtiar Muhammad, Jan Syed Umer, Khan Muhammad Farid, Ullah Naseem, Hussain Abid, Rehman Saifur, Qureshi Muhammad Murtaza

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gomal University, DI Khan, Pakistan.

Faculty of Pharmacy, University of Balochistan, Quetta, Pakistan.

出版信息

Pak J Pharm Sci. 2018 Jan;31(1):213-219.

Abstract

The metalloelement Palladium has a number of potential Pharmaco-clinical advantages. Palladium compounds have antiviral, antibacterial, neuroprotective and antitumor properties. However studies have also indicated some mild to serious toxic effects of Palladium metalloelements. Biothiols are important antioxidants that provide protection against metals toxicity. The interaction of metalloelements with biothiols can provide valuable information about the level of toxicity of the metalloelements and about the protective role of biothiols thereof. In this piece of work the effect of salt and complexes of Palladium on the status of different thiols (GSH, NAC, and D-Pen) in aqueous medium, were examined, The thiol quantification was carried out using Elman's method through UV-visible spectrophotometry and H- NMR. Results of the study performed in aqueous medium showed that level of different thiols depleted after the addition of the inorganic salts and organic complexes of Palladium. The mechanism of interaction of Palladium with thiols was examined using H-NMR. The results indicate that the depletion in the level of thiols may be due to 1:1 or 1:2 conjugation of Palladium with thiols. These conjugation reactions further suggest that the Palladium have xenobiotic nature causing oxidative stress and thiols play their role in detoxification and biotransformation of these metalloelements.

摘要

金属元素钯具有许多潜在的药物临床优势。钯化合物具有抗病毒、抗菌、神经保护和抗肿瘤特性。然而,研究也表明钯金属元素存在一些轻度至重度的毒性作用。生物硫醇是重要的抗氧化剂,可提供针对金属毒性的保护作用。金属元素与生物硫醇的相互作用能够提供有关金属元素毒性水平以及生物硫醇在此过程中保护作用的宝贵信息。在这项工作中,研究了钯的盐和配合物对水介质中不同硫醇(谷胱甘肽、N-乙酰半胱氨酸和D-青霉胺)状态的影响,采用埃尔曼法通过紫外可见分光光度法和核磁共振氢谱对硫醇进行定量分析。在水介质中进行的研究结果表明,添加钯的无机盐和有机配合物后,不同硫醇的水平降低。利用核磁共振氢谱研究了钯与硫醇的相互作用机制。结果表明,硫醇水平的降低可能是由于钯与硫醇以1:1或1:2的比例结合。这些结合反应进一步表明,钯具有外源性性质,会引起氧化应激,而硫醇在这些金属元素的解毒和生物转化中发挥作用。

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