用于治疗帕金森病的左旋多巴硬脂酸肼共轭物的设计、合成和体外评估--治疗帕金森病的新型共轭物。

IF 1.7 Q3 PHARMACOLOGY & PHARMACY Drug Research Pub Date : 2024-02-01 Epub Date: 2024-01-29 DOI:10.1055/a-2234-9859
Vasanthi Chinraj, Ramakkamma Aishwarya Reddy, Jubie Selvaraj, Raman Sureshkumar
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引用次数: 0

摘要

帕金森病是继阿尔茨海默病之后老年人发病率最高的神经退行性疾病。帕金森病的病理特征是大脑黑质区多巴胺能神经元的缺失,进而导致多巴胺缺乏,影响人体正常的生理和神经功能紊乱。这种治疗方法的重要缺陷在于,左旋多巴只能补充大脑中耗竭的多巴胺,并不能影响神经变性。尽管左旋多巴能控制病情,但仍需要另一种治疗策略来阻止或预防神经元的进一步退化。具有神经保护活性的化合物符合这一要求。其中,硬脂酸在通过磷酸肌酸 3- 激酶依赖机制保护神经元免受氧化应激方面发挥着重要作用。因此,本研究旨在设计、合成和表征左旋多巴硬脂酸酰肼共轭物。此外,还要评估合成化合物在 SHSY5Y 细胞系中的细胞毒性。简而言之,左旋多巴与硬脂酸成功共轭,并通过傅立叶变换红外光谱、核磁共振和质谱进行了确认。在 SHSY5Y 细胞系中进行的体外细胞存活率研究表明,0.134 µm 浓度的共轭物和 0.563 µm 浓度的左旋多巴都能提高细胞存活率。这表明合成的化合物可为帕金森病提供一种更好的治疗策略。
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Design, Synthesis and In Vitro Evaluation of Levodopa Stearic Acid Hydrazide Conjugate for the Management of Parkinson's DiseaseNovel Conjugate for Parkinson's Disease.

Parkinson's disease is the highest prevalent neurodegenerative disease in elderly individuals after Alzheimer's disease. The pathological identification for Parkinson's disease is loss of dopaminergic neurons in substantia nigra region of the brain that in turn leads to dopamine deficiency that affects the body's normal physiological and neurological disorder. The important drawback in the modality of treatment is levodopa is only supplying depleted dopamine in the brain, it does not affect neurodegeneration. Even though levodopa manages the disease, an alternative treatment strategy is required to stop or prevent further degeneration of neuron. The compound with neuroprotector activity suits the requirement. Of them, stearic acid plays a vital role in protecting neurons against oxidative stress through a Phosphoinositide 3-kinase-dependent mechanism. Hence, our present study aimed to design, synthesize, and characterize the levodopa stearic acid hydrazide conjugate. Additionally, evaluate the cytotoxicity of synthesized compound in SHSY5Y: cell lines. In brief, levodopa was conjugated to the stearic acid successfully and was confirmed with Fourier-transform infrared spectroscopy, Nuclear magnetic resonance, and Mass Spectroscopy. In vitro cell viability study in SHSY5Y: cell lines showed elevated cell viability in 0.134 µm concentration of Conjugate, and 0.563 µm concentration of levodopa. Showing that the synthesized compound could offer an improved treatment strategy for Parkinson's disease.

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来源期刊
Drug Research
Drug Research PHARMACOLOGY & PHARMACY-
CiteScore
3.50
自引率
0.00%
发文量
67
期刊介绍: Drug Research (formerly Arzneimittelforschung) is an international peer-reviewed journal with expedited processing times presenting the very latest research results related to novel and established drug molecules and the evaluation of new drug development. A key focus of the publication is translational medicine and the application of biological discoveries in the development of drugs for use in the clinical environment. Articles and experimental data from across the field of drug research address not only the issue of drug discovery, but also the mathematical and statistical methods for evaluating results from industrial investigations and clinical trials. Publishing twelve times a year, Drug Research includes original research articles as well as reviews, commentaries and short communications in the following areas: analytics applied to clinical trials chemistry and biochemistry clinical and experimental pharmacology drug interactions efficacy testing pharmacodynamics pharmacokinetics teratology toxicology.
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