SENSORS AND ACTUATORS B-CHEMICAL
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2023
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IF 8.4
Yu Wang,Qilin Zhao,Yu Xue,Donghui Wu,Bing Zhang,Jian Sun,Xiurong Yang
Acetylcholinesterase (AChE) activity and its inhibitor assays play a vital role in the early diagnosis and drug screening of certain diseases. In this work, we for the first time found that the protein-inorganic hybrid nanoflowers (HNFs) [BSA-Cu 3 (PO 4 ) 2 ] exhibits an obvious laccase-like catalytic activity . Further, through the regulation of laccase-mimicking activity, we developed a convenient and original colorimetric tactic for sensitive and selective assaying of acetylcholinesterase (AChE) activity and its inhibitors. Most surprisingly, AChE can catalyze acetylthiocholine (ATCh) into thiocholine (TCh), which could significantly enhance the catalytic activity of BSA-Cu 3 (PO 4 ) 2 HNFs. The enhanced laccase-like activity accelerates the chromogenic reaction between 2,4-dichlorophenol (2,4-DP) and 4-aminoantipyrine (4-AP), and the relevant product exhibits a red color which is owing to the reduction of Cu 2+ in the HNFs to Cu + by TCh. According to the facile signal-on response with clear response mechanism, our method has been successfully applied for the highly sensitive detection of AChE activity with a linear range of 0.25–5 mU/mL, and testing AChE inhibitors , especially obtaining satisfactory results in real samples. It is expected that such facile strategy could pave the way for the potential applications of biometric catalysts in disease diagnosis and environmental monitoring.
研究领域:
生物化学
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医学诊断
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环境监测
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产品关联
DOI
高影响因子
Food Bioscience
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2022
·
IF 5.318
Jingru Zheng,Yuanhong Gao,Jie Ding,Na Sun,Songyi Lin
The study aims to investigate the repair effects of Ser-Ser-Asp-Ala-Phe-Phe-Pro-Phe-Arg (SSDAFFPFR) and Ser-Asn-Val-Phe-Asp-Met-Phe (SNVFDMF) peptides on scopolamine-caused memory impairment in mice. Behavioral experiments have revealed that Antarctic krill peptides can ameliorate scopolamine caused memory impairment by changing the behavior of mice. In comparison with the scopolamine group, the two peptides at a dose of 40 mg/kg could improve memory impairment. The serum SOD activity (82.82 ± 0.19 vs 79.47 ± 2.42 U/mg prot) and hippocampal ACh level (101.46 ± 3.23 vs 99.85 ± 7.13 μg/mg prot) of SSDAFFPFR were higher than those of SNVFDMF. Hippocampal AChE activity (0.20 ± 0.03 vs 0.53 ± 0.02 U/mg prot), hippocampal MDA level (1.56 ± 0.01 vs 1.63 ± 0.05 nmol/mg prot) and the serum MDA level (3.38 ± 0.24 vs 3.88 ± 0.21 nmol/mg prot) was lower than that of SNVFDMF. The state of mouse hippocampal cells was further observed by a microscopic imaging system. In addition, western blot analysis showed that SSDAFFPFR could significantly inhibit the expression of Bax, caspase-3, and p53, and promote the expression of BCL-XL, CREB, and BDNF, thus protecting hippocampal neurons in mice. In conclusion, the Antarctic krill peptide can repair scopolamine-induced memory impairment in mice.
研究领域:
神经科学
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药理学
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生物化学
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产品关联
DOI
高影响因子
Scientific Reports
·
2018
·Vol. 8
·期 1
·1-18
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IF 4.122
Zhou Bohang,Zhang Bingyu,Li Xingqiang,Liu Xiuxiu,Li Hui,Li Ding,Cui Zhiming,Geng Huiling,Zhou Le
A series of 2-aryl-9-methyl- β -carbolinium bromides (B) were synthesized and explored for anti-acetylcholinesterase (AChE) activities in vitro , action mechanism and structure-activity relationship. All the compounds B along with their respective 3,4-dihydro intermediates (A) presented anti-AChE activity at 10 μM. Thirteen compounds B showed the excellent activity with IC 50 values of 0.11 – 0.76 μM and high selectivity toward AChE relative to butyrylcholinesterase (BChE), superior to galantamine (IC 50 = 0.79 μM), a selective AChE inhibitor drug. Kinetic analysis showed that the action mechanisms of both compounds B and A are a competitive inhibition model. Structure-activity relationship analyses showed that the C = N + moiety is a determinant for the activity. Substituents at 6, 7 or 4′ site, the indole-N-alkyl and the aromatization of the C-ring can significantly improve the activity. Molecular docking studies showed that the compounds could combine with the active site of AChE by the π-π or cation-π action between the carboline ring and the phenyl rings of the residues, and the β-carboline moiety is embedded in a cavity surrounded by four aromatic residues of Trp86, Tyr337, Trp439 and Tyr449. The present results strongly suggest that the para-position of the D-ring should be a preferred modification site for further structural optimization design. Thus, 2-aryl-9-methyl- β -carboliniums emerged as novel and promising tool compounds for the development of new AChE inhibitor agents.
研究领域:
药理学
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有机化学
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药物化学
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产品关联
DOI
PubMed
高影响因子
Journal of Applied Spectroscopy
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2018
·Vol. 85
·期 3
·437-444
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IF 0.611
Zhao Lingzhi,Zhao Liu,Zhang Chenxiao,Li Yanqi
We demonstrate the utility of 4-chloro-7-nitrobenzofurazan (NBD-Cl), a simple, low-cost probe, for colorimetrically and fluorescently detecting and differentiating similar thiol species, including cysteine, homocysteine, and glutathione, as well as for assaying acetylcholinesterase (AChE) activity. This assay is a potential tool for investigating thiol functions in disease and diagnosis, and for screening AChE inhibitors. We envision that this versatile probe, which is commercially available and inexpensive, will be useful for further elucidating the roles of thiols in biology and also shows applicability for analysis of AChE inhibitors in physiological samples.
研究领域:
分析化学
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生物化学
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分子生物学
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诊断学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）