Choi Yujin, Huh Eugene, Lee Seungmin, Kim Jin Hee, Park Myoung Gyu, Seo Seung-Yong, Kim Sun Yeou, Oh Myung Sook
Department of Biomedical and Pharmaceutical Sciences, Graduate School, Kyung Hee University, Seoul 02447, Republic of Korea.
Department of Oriental Pharmaceutical Science, College of Pharmacy, Kyung Hee University, Seoul 02447, Republic of Korea.
Biomol Ther (Seoul). 2023 Jul 1;31(4):402-410. doi: 10.4062/biomolther.2022.141. Epub 2023 Mar 15.
Long-term administration of levodopa (L-DOPA) to patients with Parkinson's disease (PD) commonly results in involuntary dyskinetic movements, as is known for L-DOPA-induced dyskinesia (LID). 5-Hydroxytryptophan (5-HTP) has recently been shown to alleviate LID; however, no biochemical alterations to aberrant excitatory conditions have been revealed yet. In the present study, we aimed to confirm its anti-dyskinetic effect and to discover the unknown molecular mechanisms of action of 5-HTP in LID. We made an LID-induced mouse model through chronic L-DOPA treatment to 6-hydroxydopamine-induced hemi-parkinsonian mice and then administered 5-HTP 60 mg/kg for 15 days orally to LID-induced mice. In addition, we performed behavioral tests and analyzed the histological alterations in the lesioned part of the striatum (ST). Our results showed that 5-HTP significantly suppressed all types of dyskinetic movements (axial, limb, orolingual and locomotive) and its effects were similar to those of amantadine, the only approved drug by Food and Drug Administration. Moreover, 5-HTP did not affect the efficacy of L-DOPA on PD motor manifestations. From a molecular perspective, 5-HTP treatment significantly decreased phosphorylated CREB and ΔFosB expression, commonly known as downstream factors, increased in LID conditions. Furthermore, we found that the effects of 5-HTP were not mediated by dopamine1 receptor (D1)/DARPP32/ERK signaling, but regulated by AKT/mTOR/S6K signaling, which showed different mechanisms with amantadine in the denervated ST. Taken together, 5-HTP alleviates LID by regulating the hyperactivated striatal AKT/mTOR/S6K and CREB/ΔFosB signaling.
长期给帕金森病(PD)患者服用左旋多巴(L-DOPA)通常会导致不自主运动障碍,即L-DOPA诱导的异动症(LID)。最近研究表明,5-羟色氨酸(5-HTP)可缓解LID;然而,尚未发现其对异常兴奋状态的生化改变。在本研究中,我们旨在证实5-HTP的抗异动症作用,并发现其在LID中未知的分子作用机制。我们通过对6-羟基多巴胺诱导的偏侧帕金森病小鼠进行慢性L-DOPA治疗建立LID诱导小鼠模型,然后对LID诱导小鼠口服给予60 mg/kg的�-HTP,持续15天。此外,我们进行了行为测试,并分析了纹状体(ST)损伤部位的组织学改变。我们的结果表明,5-HTP显著抑制了所有类型的异动症(轴向、肢体、口面部和运动性),其效果与金刚烷胺相似,金刚烷胺是唯一经美国食品药品监督管理局批准的药物。此外,5-HTP不影响L-DOPA对PD运动表现的疗效。从分子角度来看,5-HTP治疗显著降低了磷酸化CREB和ΔFosB的表达,这两种蛋白通常被认为是LID状态下增加的下游因子。此外,我们发现5-HTP的作用不是由多巴胺1受体(D1)/DARPP32/ERK信号介导的,而是由AKT/mTOR/S6K信号调节的,这表明其在去神经支配的ST中与金刚烷胺的作用机制不同。综上所述,5-HTP通过调节纹状体过度激活的AKT/mTOR/S6K和CREB/ΔFosB信号来缓解LID。