<i>In vitro</i>BACE-1 Inhibitory Phenolic Components from the Seeds of<i>Psoralea corylifolia</i>

Choi, Young-Hyun; Yon, Gyu Hwan; Hong, Kyung Sik; Yoo, Dae Seok; Choi, Chun Whan; Park, Woo‐Kyu; Kong, Jae Yang; Kim, Young Sup; Ryu, Shi Yong

doi:10.1055/s-2008-1081301

Cited by 73 publications

(44 citation statements)

References 13 publications

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“…Isoflavones including neocorylin, bakuchiol, bavachromene, isobavachromene, bavachalcone, 7,8-dihydro-8-(4-hydrophenyl)-2,2-dimethyl-2-H,6-H-[1,2-B:5,4-B'] dipyran-6-one, isolated from Psoralea corylifolia L. (Fabaceae) were also strong inhibitors of β-secretase activity (Choi et al, 2008b). In addition, luteolin and rosmarinic acid was identified as the active principles of β-secretase inhibition from Perilla frutescens var.…”

Section: β-Secretase Inhibitorsmentioning

confidence: 98%

Potential therapeutic agents against Alzheimer’s disease from natural sources

Park

2010

Arch. Pharm. Res.

106

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The average human life span in developed countries has increased to more than 80 years following rapid breakthrough and developments in modern medicine and science, resulting in prolonged life expectancy and increase in the population counts of the geriatric age group. This translates into a dramatic increase in disease burden of elderly patients suffering from senile disorders including neurodegenerative diseases, particularly Alzheimer's disease (AD). AD is characterized by the death of nerve cells in the cerebral cortex and is the most common subtype of dementia that affected 25 million people worldwide in 2000 and is expected to increase to 114 million by 2050. Despite the exponential growth in the number of AD patients, only acetylcholinesterase (AChE) inhibitors are being currently used to treat AD. It is well known that AChE inhibitors can alleviate the symptoms of AD but not halt the disease progression. Consequently, therapeutic agents against AD acting at various pathologic levels are needed. In the recent decade, natural products with anti-AD properties have attracted much attention. But very few natural products have been investigated in a scientifically justifiable method for these biological activities. Following a detailed research process, it is certain that natural products have a strong potential to develop biologically active compounds with new chemical structures. Many studies have been carried out to identify the naturally occurring anti-AD agents. This review article describes the molecular targets aiming at developing the anti-AD agents including the inhibition of AChE, inhibition of Aβ production by enhancing α-secretase (non-amyloidogenic pathway) or inhibiting β- and γ-secretases (amyloidogenic pathway), alleviating Aβ-induced neurotoxicity or reducing Aβ-induced neuroinflammation. In addition, this paper summarizes the potential of some of the natural products that might inhibit specific molecular targets and slow the progression of this disease.

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Section: β-Secretase Inhibitorsmentioning

confidence: 98%

Potential therapeutic agents against Alzheimer’s disease from natural sources

Park

2010

Arch. Pharm. Res.

106

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“…As a therapeutic plant, PCS is used empirically to prevent brain aging and to treat dementia [1,2] and, more recently, has been proven to possess antidepressant action [3 -5]. Two anecdotal clinical reports showed that this Chinese folklore herb, combined with other herbs when prescribing herb cocktail recipes, can significantly improve parkinsonism [6,7].…”

Section: Introductionmentioning

confidence: 99%

In vitro dopaminergic neuroprotective and in vivo antiparkinsonian-like effects of Δ3,2-hydroxybakuchiol isolated from Psoralea corylifolia (L.)

Zhao

Zheng²,

Qin

et al. 2009

Cell. Mol. Life Sci.

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Cocktail recipes containing Psoralea corylifolia seeds (PCS) are used to empirically treat Parkinson disease. A PCS isolate Delta(3),2-hydroxybakuchiol (BU) can inhibit dopamine uptake in dopamine transporter (DAT) transfected Chinese hamster ovary (CHO) cells, and dopamine reuptake blockade may provide an alternative approach for ameliorating parkinsonism. Here, we assessed the potential dopaminergic neuroprotective, and antiparkinsonian-like activity of BU. BU sample size was increased by using a scale-up extraction paradigm. Pharmacologically, BU significantly protected SK-N-SH cells from 1-methyl-4-phenylpyridinium (MPP(+)) insult, produced striking inhibitory actions on dopamine/norepinephrine uptake and WIN35,428 binding in synaptosomes on in vivo administration, and significantly preventing poor performance on rotarod and dopaminergic loss in substantia nigra in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mice. BU acts by protecting dopaminergic neurons from MPP(+) injury and preventing against MPTP-induced behavioral and histological lesions in the Parkinson's disease (PD) model, possibly by inhibiting monoamine transporters. These findings suggest that BU could be meaningful in PD treatment.

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“…Compound 33d, which displayed the highest BACE 1 activity among the two series, was chosen to study the protein binding pattern and the result showed that it was in close contact with two essential catalytic aspartates (Asp32 and Asp228) of the BACE 1 [Huang et al 2008]. Other compounds with a potential BACE1 inhibitory effect include neocorylin [Choi et al 2008], epigallocatechin-3-gallate and curcumin [Shimmyo et al 2008] and N (4)-substituted piperazine naphthamide derivatives [Laras et al 2009]. …”

Section: Colostrinin Inhibits Abmentioning

confidence: 99%

Disease-modifying treatments for Alzheimer’s disease

Galimberti

Scarpini

2011

Ther Adv Neurol Disord

120

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The first drugs developed for Alzheimer's disease (AD), acetylcholinesterase inhibitors (AChEI), increase acetylcholine levels, previously demonstrated to be reduced in AD. To date, four AChEI are approved for the treatment of mild-to-moderate AD. A further therapeutic option available for moderate-to-severe AD is memantine. These treatments are symptomatic, whereas drugs under development are intended to modify the pathological steps leading to AD, thus acting on the evolution of the disease. For this reason they are have been termed 'disease-modifying' drugs. To block the progression of the disease they have to interfere with the pathogenic steps responsible for the clinical symptoms, including the deposition of extracellular amyloid beta (Ab) plaques and of intracellular neurofibrillary tangles, inflammation, oxidative damage, iron deregulation and cholesterol metabolism. In this review, new perspectives will be discussed. In particular, several approaches will be described, including interference with Ab deposition by anti-Ab aggregation agents, vaccination, g-secretase inhibitors or selective Ab-lowering agents; interference with tau deposition by methylthioninium chloride; and reduction of inflammation and oxidative damage.

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In vitroBACE-1 Inhibitory Phenolic Components from the Seeds ofPsoralea corylifolia

Cited by 73 publications

References 13 publications

Potential therapeutic agents against Alzheimer’s disease from natural sources

Potential therapeutic agents against Alzheimer’s disease from natural sources

In vitro dopaminergic neuroprotective and in vivo antiparkinsonian-like effects of Δ3,2-hydroxybakuchiol isolated from Psoralea corylifolia (L.)

Disease-modifying treatments for Alzheimer’s disease

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