Suillin: A mixed-type acetylcholinesterase inhibitor from Suillus luteus which is used by Saraguros indigenous, southern Ecuador.

Suillin: A mixed-type acetylcholinesterase inhibitor from Suillus luteus which is used by Saraguros indigenous, southern Ecuador.
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DOI:
10.1371/journal.pone.0268292
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发表时间:
2022
期刊:
影响因子:
3.7
通讯作者:
--
中科院分区:
综合性期刊3区
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--
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黄豆(L.)Roussel是一种可食用的蘑菇,通常被Loja省的土著居民称为“滑杰克”或“Kallampa”。它在传统医学中用于治疗胃肠道疾病和头痛。此外,食用菌已被用于治疗神经退行性疾病;但目前尚无关于其抗胆碱酯酶作用的报道。本研究旨在分离黄豆主要次生代谢产物,并表征其对乙酰胆碱酯酶的抑制作用。用乙醇(EtOH)和乙酸乙酯(EtOAc)提取子实体。从EtOAc中,suillin被报道为主要化合物。采用Ellman’s法测定提取液和主要分离化合物的胆碱酯酶抑制电位,并在405 nm处记录60 min的进展曲线。以盐酸多奈哌齐为阳性对照。将样品溶解在10 mg/mL的甲醇中,再进行两次10倍稀释,得到混合反应时的最终浓度分别为1、0.1和0.01 mg/mL。计算胰岛素的IC50、Km、Vmax和Ki。分离得到苏林(200mg)、亚油酸、过氧化麦角甾醇和麦角甾醇。EtOH和EtOAc提取物具有中等抑制作用(IC50 ~ 200 μg/mL)。此外,苏林还发挥了一种非竞争性混合机制。IC50为31.50 μM, Ki为17.25 μM。据我们所知,这是第一次报道黄柳和苏林的抗胆碱酯酶作用。在这项研究中确定的动力学参数和化合物的中等效力,鼓励我们提出作为一种有前途的化学预防剂,用于治疗神经退行性疾病,如阿尔茨海默病。
Suillus luteus (L.) Roussel is an edible mushroom commonly known as slippery jack or “Kallampa” by indigenous people from Loja province. It is used in traditional medicine to manage gastrointestinal disorders and headaches. In addition, edible mushrooms have been used for neurodegenerative diseases; however, there is no report about the anticholinesterase effect produced by this species. The aim of this work was to isolate the main secondary metabolite of Suillus luteus and characterize its inhibitory potential against acetylcholinesterase. Fruiting bodies were extracted with ethanol (EtOH) and ethyl acetate (EtOAc). From the EtOAc, suillin, is reported as the major compound. The cholinesterase inhibitory potential of extracts and the major isolated compound was assessed by Ellman´s method and progression curves were recorded at 405 nm for 60 min. Donepezil hydroclhoride was used as a positive control. The samples were dissolved in methanol at 10 mg/mL and two more 10× dilutions were included to obtain final concentrations of 1, 0.1 and 0.01 mg/mL at the mix of reaction. IC50, Km, Vmax, and Ki were calculated for suillin. Suillin (200 mg) along with linoleic acid, ergosterol peroxide and ergosterol were isolated. The EtOH and EtOAc extracts exerted a moderate inhibitory effect (IC50 > 200 μg/mL. In adittion, suillin exerted a non-competitive mixed mechanism. against AChE with an IC50 value of 31.50 μM and Ki of 17.25 μM. To the best of our knowledge, this is the first report of the anticholinesterase effect of Suillus luteus and suillin. The kinetic parameters and the moderate potency of the compound determined in this study, encourage us to propose suillin as a promising chemopreventing agent for the treatment of neurodegenerative diseases such as Alzheimer.
DOI: 10.1016/0006-2952(61)90145-9
发表时间: 1961-01-01
影响因子: 5.8
作者:
ELLMAN, GL;COURTNEY, KD;FEATHERSTONE, RM
通讯作者: FEATHERSTONE, RM
DOI: 10.1177/2472555219829898
发表时间: 2019-06-01
期刊: SLAS DISCOVERY
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DOI: 10.1111/jfbc.13074
发表时间: 2019-12-01
影响因子: 4
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DOI: 10.1016/s0031-9422(02)00050-x
发表时间: 2002-04-01
期刊: PHYTOCHEMISTRY
影响因子: 3.8
作者:
Nukata, M;Hashimoto, T;Asakawa, Y
通讯作者: Asakawa, Y
DOI: 10.1016/j.fitote.2019.104180
发表时间: 2019-09-01
期刊: FITOTERAPIA
影响因子: 3.4
作者:
Kruzselyi, Daniel;Vetter, Janos;Moricz, Agnes M.
通讯作者: Moricz, Agnes M.