The aged population in the world clearly is increasing. With the continuing increase of the elderly population, the prevalence of Alzheimer's disease (AD) is likely to increase. AD is said to be the leading cause of dementia in elderly individuals. AD patients exhibit marked decline in cognitive abi...
The aged population in the world clearly is increasing. With the continuing increase of the elderly population, the prevalence of Alzheimer's disease (AD) is likely to increase. AD is said to be the leading cause of dementia in elderly individuals. AD patients exhibit marked decline in cognitive ability and severe behavioral abnormalities such as irritability, anxiety, depression, disorientation and restlessness. AD is characterized by the presence of excessive amounts of neuritic plaques, containing amyloid β protein and loss of cholinergic markers in the brain. According to the cholinergic hypothesis of the pathogenesis of AD, memory impairments in AD patients result from a deficit of cholinergic functions in the brain. The enzyme acetylcholinesterase (AChE) has long been an attractive target for the rational drug design and discovery of mechanism-based inhibitors because of its role in the hydrolysis of the neurotransmitter acetylcholine. The inhibition of this enzyme is considered as a promising approach for the treatment of AD. True nature or cause of the disease is still unknown, making the development of treatment drugs a complex endeavor. Currently, the loss of cholinergic function is the only evidentiary finding responsible for cognitive decline. Therefore, therapeutic development has focused on this theory. In the course of searching for AChE inhibitors from natural resources, a methanolic extract of the aerial parts of Sophora flauescens (Leguminsae) was found to show inhibitory effects on AChE. Subsequent activity-guided fractionation of the methanolic extracts led to the isolation of a noble compound, 7,9,2',4'-tetrahydroxy-8-isopentenyl-5-methoxychalcone (5), and seven known compounds, leachianone A (1), sophoraflavanone G (2), kuraridin (3), matrine (4), kurarinone (6), trifolirhizin (7) and, oxymatrine (8), from Sophora flauescens. These compounds inhibited AChE activity in a dose-dependent manner, and the IC_(50) values of compounds 3, 4, 6 and 8 were 81.3, 32.8, 60.1 and 68.4 μg/ml, respectively.
The aged population in the world clearly is increasing. With the continuing increase of the elderly population, the prevalence of Alzheimer's disease (AD) is likely to increase. AD is said to be the leading cause of dementia in elderly individuals. AD patients exhibit marked decline in cognitive ability and severe behavioral abnormalities such as irritability, anxiety, depression, disorientation and restlessness. AD is characterized by the presence of excessive amounts of neuritic plaques, containing amyloid β protein and loss of cholinergic markers in the brain. According to the cholinergic hypothesis of the pathogenesis of AD, memory impairments in AD patients result from a deficit of cholinergic functions in the brain. The enzyme acetylcholinesterase (AChE) has long been an attractive target for the rational drug design and discovery of mechanism-based inhibitors because of its role in the hydrolysis of the neurotransmitter acetylcholine. The inhibition of this enzyme is considered as a promising approach for the treatment of AD. True nature or cause of the disease is still unknown, making the development of treatment drugs a complex endeavor. Currently, the loss of cholinergic function is the only evidentiary finding responsible for cognitive decline. Therefore, therapeutic development has focused on this theory. In the course of searching for AChE inhibitors from natural resources, a methanolic extract of the aerial parts of Sophora flauescens (Leguminsae) was found to show inhibitory effects on AChE. Subsequent activity-guided fractionation of the methanolic extracts led to the isolation of a noble compound, 7,9,2',4'-tetrahydroxy-8-isopentenyl-5-methoxychalcone (5), and seven known compounds, leachianone A (1), sophoraflavanone G (2), kuraridin (3), matrine (4), kurarinone (6), trifolirhizin (7) and, oxymatrine (8), from Sophora flauescens. These compounds inhibited AChE activity in a dose-dependent manner, and the IC_(50) values of compounds 3, 4, 6 and 8 were 81.3, 32.8, 60.1 and 68.4 μg/ml, respectively.
Keyword
#고삼 Acetylcholinesterase 활성 억제 성분
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