香菇对三苯基化合物对β淀粉样蛋白聚集和BACE1的抑制作用及对SH-SY5Y细胞的保护作用

IF 2.5 4区 医学 Q3 CHEMISTRY, MEDICINAL
Shuntaro Hirabayashi, Koji Fujihara, Takehito Saito, Hiroaki Sasaki, Shin Koike, Yuki Ogasawara, Kiyotaka Koyama, Kaoru Kinoshita
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引用次数: 0

摘要

随着人口的老龄化,阿尔茨海默病(AD)患者的数量预计会增加。淀粉样蛋白级联假说被认为是AD的发病机制。本文报道了从金象菌(theelephora aurantiotincta Corner)子实体中分离并鉴定了3个新的对terphenyl化合物:象素P(1)、象素Q(2)和象素R(3),以及4个已知化合物(4-7)。我们评估了这些分离化合物的Aβ聚集和BACE1抑制活性以及神经保护活性。化合物1被证明是AD的多重抑制剂。化合物1的IC50 = 12.9 μM (Aβ), 6.3 μM (BACE1), EC50 = 8.0 μM (neuroprotection)。因此,这些化合物是潜在的阿尔茨海默病治疗剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Inhibition of amyloid β aggregation and BACE1, and protective effect on SH-SY5Y cells, by p-terphenyl compounds from mushroom Thelephora aurantiotincta

Inhibition of amyloid β aggregation and BACE1, and protective effect on SH-SY5Y cells, by p-terphenyl compounds from mushroom Thelephora aurantiotincta

The number of patients with Alzheimer’s disease (AD) is expected to increase as the population ages. The amyloid cascade hypothesis is proposed as the pathogenic mechanism of AD. We report the isolation and structural determination of three new p-terphenyl compounds, thelephantin P (1), thelephantin Q (2), and thelephantin R (3), with four known compounds (47), from the fruiting bodies of Thelephora aurantiotincta Corner. We evaluated Aβ aggregation and BACE1 inhibitory activities and neuroprotective activities of these isolated compounds. Compound 1 was shown to be multi-inhibitors for AD. Compound 1 had an IC50 = 12.9 μM (Aβ), 6.3 μM (BACE1), and EC50 = 8.0 μM (neuroprotection), respectively. Therefore, these compounds are potential therapeutic agents for AD.

Graphical Abstract

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来源期刊
CiteScore
6.90
自引率
3.00%
发文量
79
审稿时长
1.7 months
期刊介绍: The Journal of Natural Medicines is an international journal publishing original research in naturally occurring medicines and their related foods and cosmetics. It covers: -chemistry of natural products -biochemistry of medicinal plants -pharmacology of natural products and herbs, including Kampo formulas and traditional herbs -botanical anatomy -cultivation of medicinal plants. The journal accepts Original Papers, Notes, Rapid Communications and Natural Resource Letters. Reviews and Mini-Reviews are generally invited.
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