β-secretase (BACE1) inhibitors from Perilla frutescens var. acuta

Choi, Sie−Young; Hur, Jong-Moon; Yang, Eun‐Ju; Jun, Mira; Park, Hyojun; Lee, Kyung‐Bok; Moon, Eunho; Song, Kyung‐Sik

doi:10.1007/s12272-001-1139-9

Cited by 51 publications

(21 citation statements)

References 32 publications

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“…In addition, luteolin and rosmarinic acid was identified as the active principles of β-secretase inhibition from Perilla frutescens var. acuta (Laminaceae) (Choi et al, 2008a).…”

Section: β-Secretase Inhibitorsmentioning

confidence: 99%

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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“…In addition, luteolin and rosmarinic acid was identified as the active principles of β-secretase inhibition from Perilla frutescens var. acuta (Laminaceae) (Choi et al, 2008a).…”

Section: β-Secretase Inhibitorsmentioning

confidence: 99%

Potential therapeutic agents against Alzheimer’s disease from natural sources

Park

2010

Arch. Pharm. Res.

106

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“…3). So far, 13 of the components found within MLC601 have been found to have the ability to reverse and prevent events associated with Aβ-induced toxicity [19,20,21,22,23,24,25,26,27,28,29,30,31,32,33,34,35,36,37,38,39,40,41,42,43,44,45]. Specifically, radix salviae miltiorrhizae, radix paeoniae rubrae, radix angelicae sinensis, radix astragali, rhizoma chuanxiong and Carthamus tinctorius have all been shown to ameliorate critical toxic events within the amyloid cascade hypothesis (fig.…”

Section: Introductionmentioning

confidence: 99%

NeuroAiD® (MLC601) and Amyloid Precursor Protein Processing

et al. 2013

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Background: Amyloid precursor protein (APP) undergoes cleavage under physiological conditions, predominantly by α- and γ-secretases, to form the nonpathogenic sAPPα and p3 fragments. By contrast, amyloid-beta (Aβ) is produced via proteolytic cleavage by β- and γ-secretases. In Alzheimer's disease (AD), APP is preferentially processed via the amyloidogenic pathway, producing large amounts of Aβ that form the major constituent of senile plaques and tau-containing neurofibrillary tangles. Similarly, stroke patients have a higher level of Aβ around the area of infarct, suggesting that Aβ may mediate at least some of the secondary neurotoxicity observed in stroke patients. Methods: To investigate the effects of MLC601 (NeuroAiD^®) on regulation of APP processing, the human neuroblastoma cell line SH-SY5Y was used for all experiments. Stocks of MLC601 were prepared at a final concentration of 50 mg/ml. Cells were treated with different concentrations of MLC601 before assessing changes in the levels of released lactate dehydrogenase (LDH), full-length APP and secreted sAPPα. Results: Concentrations of MLC601 between 1 and 1,000 µg/ml significantly lowered the levels of LDH released into the media when compared to control cells. In contrast, MLC601 concentrations at 5,000 and 10,000 µg/ml resulted in a significant increase in the LDH release. Treatment with 100, 500 and 1,000 μg/ml of MLC601 significantly increases the levels of sAPPα secreted by SH-SY5Y into the media. Treatment with 1,000 μg/ml of MLC601 significantly decreased the levels of full-length APP. Conclusion: MLC601 is a possible modulator of APP processing and has implications as a putative therapeutic strategy for the treatment of poststroke dementia and AD.

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“…Although P. frutescens (L.) Britton var. acuta Kudo is known to contain various components, such as phenylpropanoids and terpenes (Fujita et al ., 1994; Liu et al ., 2000) and to possess various pharmacological actions including antidepressant-like effects (Nakazawa et al ., 2003) and β-secretase inhibiting activity (Choi et al ., 2008), the present study has clearly shown the importance of phenylpropanoids in expressing inhibitory activity against lung inflammation.…”

Section: Discussionmentioning

confidence: 99%

Inhibition of Proinflammatory Cytokine Generation in Lung Inflammation by the Leaves of Perilla frutescens and Its Constituents

Lim

Woo

Lee

et al. 2014

Biomolecules & Therapeutics

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This study was designed to find some potential natural products and/or constituents inhibiting proinflammatory cytokine generation in lung inflammation, since cytokines such as tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) are pivotal for provoking airway inflammation. In our preliminary screening procedure, the 70% ethanol extract of the leaves of Perilla frutescens (PFE) was found to clearly inhibit TNF-α production in the lung at 100 mg/kg, after intranasal lipopolysaccharide treatment of mice. Based on this result, ten constituents including phenylpropanoids (allyltetramethoxybenzene, caffeic acid, dillapiole, elemicin, myristicin, nothoapiole, rosmarinic acid methyl ester, rosmarinic acid) and monoterpenes (perilla aldehyde and perilla ketone) were successfully isolated from the extract. Among them, elemicin and myristicin were found for the first time to concentration-dependently inhibit IL-1β-treated IL-6 production from lung alveolar epithelial cells (A549) at concentrations of 10-100 μM. These findings suggest that the phenylpropanoids including elemicin and myristicin have the potential to be new inhibitory agents against lung inflammation and they may contribute, at least in part, to the inhibitory activity of PFE on the lung inflammatory response.

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β-secretase (BACE1) inhibitors from Perilla frutescens var. acuta

Cited by 51 publications

References 32 publications

Potential therapeutic agents against Alzheimer’s disease from natural sources

Potential therapeutic agents against Alzheimer’s disease from natural sources

NeuroAiD® (MLC601) and Amyloid Precursor Protein Processing

Inhibition of Proinflammatory Cytokine Generation in Lung Inflammation by the Leaves of Perilla frutescens and Its Constituents

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