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Article

Anti-Amyloidogenic Effects of Asarone Derivatives From Perilla frutescens Leaves Against Beta-Amyloid Aggregation and Nitric Oxide Production

1
College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan-si, Chungnam 31116, Korea
2
College of Pharmacy, Chung-Ang University, 84 Heukseok-ro, Dongjak-gu, Seoul 06974, Korea
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Present address: National Agrobiodiversity Center, Rural Development Administration, Jeonbuk 54874, Korea.
Academic Editor: Peter Koulen
Molecules 2019, 24(23), 4297; https://doi.org/10.3390/molecules24234297
Received: 14 October 2019 / Revised: 19 November 2019 / Accepted: 21 November 2019 / Published: 25 November 2019
Alzheimer’s disease (AD) is a progressive, neurodegenerative brain disorder associated with loss of memory and cognitive function. Beta-amyloid (Aβ) aggregates, in particular, are known to be highly neurotoxic and lead to neurodegeneration. Therefore, blockade or reduction of Aβ aggregation is a promising therapeutic approach in AD. We have previously reported an inhibitory effect of the methanol extract of Perilla frutescens (L.) Britton (Lamiaceae) and its hexane fraction on Aβ aggregation. Here, the hexane fraction of P. frutescens was subjected to diverse column chromatography based on activity-guided isolation methodology. This approach identified five asarone derivatives including 2,3-dimethoxy-5-(1E)-1-propen-1-yl-phenol (1), β-asarone (2), 3-(2,4,5-trimethoxyphenyl)-(2E)-2-propen-1-ol (3), asaronealdehyde (4), and α-asarone (5). All five asarone derivatives efficiently reduced the aggregation of Aβ and disaggregated preformed Aβ aggregates in a dose-dependent manner as determined by a Thioflavin T (ThT) fluorescence assay. Furthermore, asarone derivatives protected PC12 cells from Aβ aggregate-induced toxicity by reducing the aggregation of Aβ, and significantly reduced NO production from LPS-stimulated BV2 microglial cells. Taken together, these results suggest that asarone derivatives derived from P. frutescens are neuroprotective and have the prophylactic and therapeutic potential in AD. View Full-Text
Keywords: Perilla frutescens; asarone derivative; Alzheimer’s disease; beta-amyloid aggregation; beta-amyloid disaggregation; nitric oxide Perilla frutescens; asarone derivative; Alzheimer’s disease; beta-amyloid aggregation; beta-amyloid disaggregation; nitric oxide
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MDPI and ACS Style

Lee, J.E.; Kim, N.; Yeo, J.Y.; Seo, D.-G.; Kim, S.; Lee, J.-S.; Hwang, K.W.; Park, S.-Y. Anti-Amyloidogenic Effects of Asarone Derivatives From Perilla frutescens Leaves Against Beta-Amyloid Aggregation and Nitric Oxide Production. Molecules 2019, 24, 4297. https://doi.org/10.3390/molecules24234297

AMA Style

Lee JE, Kim N, Yeo JY, Seo D-G, Kim S, Lee J-S, Hwang KW, Park S-Y. Anti-Amyloidogenic Effects of Asarone Derivatives From Perilla frutescens Leaves Against Beta-Amyloid Aggregation and Nitric Oxide Production. Molecules. 2019; 24(23):4297. https://doi.org/10.3390/molecules24234297

Chicago/Turabian Style

Lee, Jae E.; Kim, Nayeon; Yeo, Ji Y.; Seo, Dae-Gun; Kim, Sunggun; Lee, Jae-Sun; Hwang, Kwang W.; Park, So-Young. 2019. "Anti-Amyloidogenic Effects of Asarone Derivatives From Perilla frutescens Leaves Against Beta-Amyloid Aggregation and Nitric Oxide Production" Molecules 24, no. 23: 4297. https://doi.org/10.3390/molecules24234297

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