• 생약학회지
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• 제47권3호
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• pp.287-294
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• 2016

Acetylcholinesterase (AChE) activation and amyloid-${\beta}$ ($A{\beta}$) aggregation are major biological markers of Alzheimer's disease. In the present study, we evaluated the inhibitory effects of 50 kinds of herbal formulas on AChE activity and $A{\beta}$ aggregation. Among them, Hwanglyeonhaedok-tang, Cheonwangbosim-dan, Makmundong-tang, and Gamisoyo-san had a potent effects on the inhbition of AChE activity. Sosiho-tang, Samsoeum, Cheonsimyeunjaeum, and Bunsimgieum exerted to have the inhibitory activity on $A{\beta}$ aggregation. In addition, these 8 herbal formulas showed the 3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity, indicating their antioxidant activities.

• Archives of Pharmacal Research
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• 제26권12호
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• pp.985-989
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• 2003

An efficient synthesis of 5-chloro-3-[4-(3-diethylaminopropoxy)benzoyl]-2-(4-methoxyphenyl)benzofuran (8), a potent $\beta$-amyloid aggregation inhibitor, is described. 5-Chloro-2-(4-methoxyphenyl)benzofuran (3) was obtained by the one-pot synthesis of 4-chlorophenol with $\omega$(methylsulfinyl)-p-methoxyacetophenone (1) under Pummerer reaction conditions, and it was followed by the desulfurization of the resultant 5-chloro-3-methylthio-2-(4-methoxyphenyl)benzofuran (2e). Acylation of benzofuran 3 with 4-(3-bromopropoxy)benzoyl chloride (6) gave the ketone 7, which was converted into compound 8 by the treatment of diethylamine.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2002년도 Molecular and Cellular Response to Toxic Substances
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• pp.191-191
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• 2002

Inflammatory as well as oxidative tissue damage has been associated with pathophysiology of Alzheimer's disease (AD), and nonsteroidal anti-inflammatory drugs have been shown to retard the progress of AD. In this study, we have investigated the molecular mechanisms underlying oxidative and inflammatory cell death induced by beta-amyloid (Abeta), a neurotoxic peptide associated with senile plaques formed in the brains of patients with AD, in cultured PC12 cells.(omitted)

• Journal of Yeungnam Medical Science
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• 제35권1호
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• pp.1-6
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• 2018

Alzheimer's disease (AD) is a neurodegenerative disorder associated with extracellular plaques, composed of amyloid-beta ($A{\beta}$), in the brain. Although the precise mechanism underlying the neurotoxicity of $A{\beta}$ has not been established, $A{\beta}$ accumulation is the primary event in a cascade of events that lead to neurofibrillary degeneration and dementia. In particular, the $A{\beta}$ burden, as assessed by neuroimaging, has proved to be an excellent predictive biomarker. Positron emission tomography, using ligands such as $^{11}C$-labeled Pittsburgh Compound B or $^{18}F$-labeled tracers, such as $^{18}F$-florbetaben, $^{18}F$-florbetapir, and $^{18}F$-flutemetamol, which bind to $A{\beta}$ deposits in the brain, has been a valuable technique for visualizing and quantifying the deposition of $A{\beta}$ throughout the brain in living subjects. $A{\beta}$ imaging has very high sensitivity for detecting AD pathology. In addition, it can predict the progression from mild cognitive impairment to AD, and contribute to the development of disease-specific therapies.

• Archives of Pharmacal Research
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• 제27권1호
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• pp.19-24
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• 2004

The facile synthesis of a series of 2-(4-hydroxyphenyl)benzofurans (4a-e) is described. The one-pot reaction of 4-substituted phenols with the chloride 1 in the presence of zinc chloride afforded 3-methylthio-2-(4-acetoxyphenyl)benzofurans (2a-e). The compounds 4a-e were obtained from the hydrolysis of 2a-e followed by the desulfurization of the resulting 3-methylthio-2-(4-hydroxyphenyl)benzofurans (3a-e). 5-Methyl-3-p-toluoyl-2 -[4-(3-diethylaminopropoxy)phenyl]benzofuran (7), a $\beta$-amyloid aggregation inhibitor, was synthesized by three steps starting from 4a.

• 공업화학
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• 제30권3호
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• pp.379-383
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• 2019

The capability of detecting amyloid beta 42 ($A{\beta}42$), a biomarker of Alzheimer's disease, using a thiolated protein A-functionalized bimetallic surface plasmon resonance (SPR) chip was investigated. An optimized configuration of a bimetallic chip containing gold and silver was obtained through calculations in the intensity measurement mode. The surface of the SPR bimetallic chip was functionalized with thiolated protein A for the immobilization of $A{\beta}42$ antibody. The response of the thiolated protein A-functionalized bimetallic chip to $A{\beta}42$ in the concentration range of 50 to 1,000 pg/mL was linear. Compared to protein A without thiolation, the thiolated protein A resulted in greater sensitivity. Therefore, the thiolated protein A-functionalized bimetallic SPR chip can be used to detect very low concentrations of the biomarker for Alzheimer's disease.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.204.1-204.1
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• 2003

Azheimer's Disease (AD) known as senile dementia accounts for 50％ of all dementia cases and is in growing status as population goes up. Generally. AD is a progressive neurodegenerative disease and includes much of senile plaque in cerebral hippocampus and cortex in patient's brain. For decades. AD theory is explained by amyloid cascade hypothesis. In process of the hypothesis, amyloid hypothesis forms fibrillar form beta-amyloid peptide (A${\beta}$ peptide) and extraordinarily accumulates in brain tissue, and lastly senile plaque is formed, which pathologically affect the brain. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.136.1-136.1
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• 2003

$\beta$-amyloid (A$\beta$) peptide produced from amyloid precursor protein (APP) is a major cause of Alzheimer's disease (AD). Therefore, in early phase of AD, imbalance of the production and the clearance of $A\beta$ is regarded as an important factor to progressive AD presenting senile plaque, a hallmark of AD. In the present study, we wanted to verify whether Rg3 can playa role in helping microglia engulfing $A\beta$ peptides. Validations for the study was conducted by using DiI-Ac-LDL, which attached only on type A macrophage scavenger receptor (MSR-A) and ligands for he receptor, fucoidan. (omitted)

• 한국자기공명학회논문지
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• 제26권2호
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• pp.21-23
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• 2022

High-pressure (HP) NMR is a powerful method to elucidate various structural features of amyloidogenic proteins. Following the previous mini-review recapitulating the HP-NMR application for amyloid-β peptides of the last issue [J. H. Kim, J. Kor. Mag. Reson. Soc. 26, 17 (2022)], the recent advancements in the HP NMR application for α-synuclein (α-Syn) are briefly summarized and discussed here. Although α-Syn is a well-known intrinsically disordered protein (IDP), several studies have shown that it can also exhibit heterogeneous yet partially folded conformations, which may correlate with its amyloid-forming propensity. HP NMR has been a valuable tool for investigating the dynamic and transient structural features of α-Syn and has provided unique insights to appreciate its aggregation-prone characters.

• Journal of Yeungnam Medical Science
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• 제39권4호
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• pp.269-277
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• 2022

The amyloid hypothesis has been considered a major explanation of the pathogenesis of Alzheimer disease. However, failure of phase III clinical trials with anti-amyloid-beta monoclonal antibodies reveals the need for other therapeutic approaches to treat Alzheimer disease. Compared to its relatively short history, optogenetics has developed considerably. The expression of microbial opsins in cells using genetic engineering allows specific control of cell signals or molecules. The application of optogenetics to Alzheimer disease research or clinical approaches is increasing. When applied with gamma entrainment, optogenetic neuromodulation can improve Alzheimer disease symptoms. Although safety problems exist with optogenetics such as the use of viral vectors, this technique has great potential for use in Alzheimer disease. In this paper, we review the historical applications of optogenetic neuromodulation with gamma entrainment to investigate the mechanisms involved in Alzheimer disease and potential therapeutic strategies.