Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease

Liu, Xin; Liu, Wenjie; Gao, Yaping; Wu, Limeng; Huang, Yaoguang; Chen, Huanhua; Li, Deping; Zhou, Lijun; Wang, Nan; Xu, Zihua; Jiang, Xiaowen; Zhao, Qingchun

doi:10.1016/j.ejmech.2021.114095

Cited by 20 publications

(8 citation statements)

References 55 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The statistical significance of differences for experiments was determined using one-way analysis of variance (ANOVA), with a minimal level of significance at p < 0.05. 28…”

Section: Discussionmentioning

confidence: 99%

Discovery of novel and potent tacrine derivatives as CDK2 inhibitors

Huang¹,

Li²,

Chang³

et al. 2022

New J. Chem.

Self Cite

View full text Add to dashboard Cite

show abstract

“…The statistical significance of differences for experiments was determined using one-way analysis of variance (ANOVA), with a minimal level of significance at p < 0.05. 28…”

Section: Discussionmentioning

confidence: 99%

Discovery of novel and potent tacrine derivatives as CDK2 inhibitors

Huang¹,

Li²,

Chang³

et al. 2022

New J. Chem.

Self Cite

View full text Add to dashboard Cite

show abstract

“…Molecular docking data showed that compound 67 was tightly bound to both the catalytic active site and peripheral anionic site of AChE, and also formed a stable interaction with GSK-3β. It has been demonstrated that 67 can exert anti-AD effects by inhibiting AChE, BChE, and GSK-3β 92 ( Figure 14 , Table 5 ).…”

Section: Alkaloids and Their Derivativesmentioning

confidence: 99%

Research progress of natural products and their derivatives against Alzheimer’s disease

Liu

Guo

Quan

et al. 2023

Journal of Enzyme Inhibition and Medicinal Chemistry

View full text Add to dashboard Cite

Alzheimer’s disease (AD), a persistent neurological dysfunction, has an increasing prevalence with the aging of the world and seriously threatens the health of the elderly. Although there is currently no effective treatment for AD, researchers have not given up, and are committed to exploring the pathogenesis of AD and possible therapeutic drugs. Natural products have attracted considerable attention owing to their unique advantages. One molecule can interact with multiple AD-related targets, thus having the potential to be developed in a multi-target drug. In addition, they are amenable to structural modifications to increase interaction and decrease toxicity. Therefore, natural products and their derivatives that ameliorate pathological changes in AD should be intensively and extensively studied. This review mainly presents research on natural products and their derivatives for the treatment of AD.

show abstract

“…Some β-carboline alkaloids act as AChE and Aβ inhibitors for the treatment of Alzheimer's disease, but the detailed action mechanism is not well interpreted. [36][37][38] Therefore, it will be very meaningful if the two important plant extracts, harmine and harmol, can be applied to prevent the amyloidosis related to T2DM.…”

Section: Introductionmentioning

confidence: 99%

β‐Carboline Alkaloids Resist the Aggregation and Cytotoxicity of Human Islet Amyloid Polypeptide

et al. 2023

View full text Add to dashboard Cite

β‐carboline alkaloids have a variety of pharmacological activities, such as anti‐tumor, antibiosis and anti‐diabetes. Harmine and harmol are two structurally similar β‐carbolines that occur in many medicinal plants. In this work, we chose harmine and harmol to impede the amyloid fibril formation of human islet amyloid polypeptide (hIAPP) associated with type 2 diabetes mellitus (T2DM), by a series of physicochemical and biochemical methods. The results indicate that harmine and harmol effectively prevent peptide fibrillation and alleviate toxic oligomer species. In addition, both small molecules exhibit strong binding affinities with hIAPP mainly through hydrophobic and hydrogen bonding interactions, reducing the cytotoxicity induced by hIAPP. Their distinct binding pattern with hIAPP is closely linked to the molecular configuration of two small molecules, affecting their ability to impede peptide aggregation. The study is of great significance for the application and development of β‐carboline alkaloids against T2DM.

show abstract

Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease

Cited by 20 publications

References 55 publications

Discovery of novel and potent tacrine derivatives as CDK2 inhibitors

Discovery of novel and potent tacrine derivatives as CDK2 inhibitors

Research progress of natural products and their derivatives against Alzheimer’s disease

β‐Carboline Alkaloids Resist the Aggregation and Cytotoxicity of Human Islet Amyloid Polypeptide

Contact Info

Product

Resources

About