Department of Biochemistry and Biophysics, Second University of Naples, Italy.
Neurosci Lett. 2010 Jan 14;468(3):287-91. doi: 10.1016/j.neulet.2009.11.014. Epub 2009 Nov 10.
Hyperhomocysteinaemia was reported in patients with Parkinson's disease (PD) treated with l-Dopa. The increase in plasma concentration of this sulfur compound arises from the massive methylation of the drug operated by the enzyme catechol-O-methyltransferase (COMT), which acts as a powerful sink of methyl groups. The contemporary occurrence of C677T polymorphism in homozygosity, leading to a temperature-labile variant of the MTHFR enzyme, induces an even more marked increase in tHcy. Here we show that l-Dopa administration in hyperhomocysteinemic PD patients is able to lower intracellular concentration of S-Adenosylmethionine (AdoMet) in erythrocytes (RBC), while the occurrence of hyperhomocysteinaemia causes a significant increase in S-Adenosylhomocysteine (AdoHcy) level. In patients with PD treated with l-Dopa and hyperhomocysteinemic, the remarkable decrease in AdoMet and the concurrent increase in AdoHcy concentration both contribute to significantly lower the transmethylation potential ([AdoMet]/[AdoHcy]), a useful index of the effectiveness of methyl group transfer by methyltransferases. This decrease could indeed contribute to partly attenuate, through a self-limiting kinetic mechanism, the tendency of developing drug resistance, partly mediated in these patients by COMT upregulation. Our results also support the conclusion that COMT inhibitors (entacapone or tolcapone), when administered in PD patients treated with l-Dopa, may potentiate the endogenous AdoHcy-dependent COMT inhibition mechanism already operative in a variable fashion.
高同型半胱氨酸血症在接受左旋多巴治疗的帕金森病 (PD) 患者中已有报道。这种含硫化合物在血浆中的浓度增加是由于药物的大量甲基化,这种甲基化由儿茶酚-O-甲基转移酶 (COMT) 酶操作,该酶作为甲基供体的强大汇。当代同型半胱氨酸血症患者中 C677T 多态性的纯合性,导致 MTHFR 酶的温度不稳定变体,导致同型半胱氨酸 (tHcy) 水平显著增加。在这里,我们表明,左旋多巴在高同型半胱氨酸血症 PD 患者中的给药能够降低红细胞 (RBC) 中 S-腺苷甲硫氨酸 (AdoMet) 的细胞内浓度,而高同型半胱氨酸血症的发生导致 S-腺苷同型半胱氨酸 (AdoHcy) 水平显著增加。在接受左旋多巴和高同型半胱氨酸血症治疗的 PD 患者中,AdoMet 的显著降低和 AdoHcy 浓度的同时增加都有助于显著降低转甲基化潜力 ([AdoMet]/[AdoHcy]),这是甲基转移酶转移甲基的有效性的有用指标。这种减少确实可以通过自限性动力学机制部分减弱产生药物抵抗的趋势,在这些患者中部分由 COMT 上调介导。我们的结果还支持这样的结论,即当在接受左旋多巴治疗的 PD 患者中给予 COMT 抑制剂(恩他卡朋或托卡朋)时,可能会增强已经以可变方式起作用的内源性 AdoHcy 依赖性 COMT 抑制机制。