Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors

Shi, Anding; Huang, Ling; Lu, Chuan‐Jun; He, Feng; Li, Xingshu

doi:10.1016/j.bmc.2011.02.025

Cited by 54 publications

(34 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…In previous studies, we demonstrated that BER improved impaired spatial memory and increased both the activation of microglia and the expression of insulin degrading enzyme (IDE) in the rat model of AD [36-38]. Other researchers have demonstrated other pharmacological effects of BER in HEK293 cells, e.g., inhibiting Aβ 42 aggregation and attenuating the Tau hyperphosphorylation induced by calyculin A [39,40]. Together, we consider BER to be a very promising drug for use in AD patients.…”

Section: Resultsmentioning

confidence: 99%

Decrease in the production of beta-amyloid by berberine inhibition of the expression of beta-secretase in HEK293 cells

Zhu

et al. 2011

BMC Neurosci

View full text Add to dashboard Cite

BackgroundBerberine (BER), the major alkaloidal component of Rhizoma coptidis, has multiple pharmacological effects including inhibition of acetylcholinesterase, reduction of cholesterol and glucose levels, anti-inflammatory, neuroprotective and neurotrophic effects. It has also been demonstrated that BER can reduce the production of beta-amyloid40/42, which plays a critical and primary role in the pathogenesis of Alzheimer's disease. However, the mechanism by which it accomplishes this remains unclear.ResultsHere, we report that BER could not only significantly decrease the production of beta-amyloid40/42 and the expression of beta-secretase (BACE), but was also able to activate the extracellular signal-regulated kinase1/2 (ERK1/2) pathway in a dose- and time-dependent manner in HEK293 cells stably transfected with APP695 containing the Swedish mutation. We also find that U0126, an antagonist of the ERK1/2 pathway, could abolish (1) the activation activity of BER on the ERK1/2 pathway and (2) the inhibition activity of BER on the production of beta-amyloid40/42 and the expression of BACE.ConclusionOur data indicate that BER decreases the production of beta-amyloid40/42 by inhibiting the expression of BACE via activation of the ERK1/2 pathway.

show abstract

Section: Resultsmentioning

confidence: 99%

Decrease in the production of beta-amyloid by berberine inhibition of the expression of beta-secretase in HEK293 cells

Zhu

et al. 2011

BMC Neurosci

View full text Add to dashboard Cite

show abstract

“…Berberine, likes many synthetic antidepressant drugs, also binds to sigma receptors (Kulkarni and Dhir, 2008). Berberine may has a potentiality for inhibition and prevention of the occurrence of Alzheimer's disease, by the inhibition of cholinesterase and b-amyloids pathways Shi et al, 2011).…”

Section: Discussionmentioning

confidence: 99%

Three Chinese herbal medicines promote neuroproliferation in vitro, and reverse the effects of chronic mild stress on behavior, the HPA axis, and proliferation of hippocampal precursor cell in vivo

Pao

Sun

et al. 2012

Journal of Ethnopharmacology

View full text Add to dashboard Cite

“…Jatrorrhizine has multiple bioactivities, such as hypoglycemic [7], antimicrobial [8], and antioxidant activities [9]. In recent years, berberine derivatives with various heterocyclic rings, such as thiophene, pyrrole, piperidine, and carbazole, were demonstrated as both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors [10][11][12]. However, no literature reported that jatrorrhizine and its derivatives could be used as inhibitors of both AChE and BuChE.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase

Jiang

Zhang

Xiong

et al. 2017

Journal of Chemistry

View full text Add to dashboard Cite

Jatrorrhizine was considered as one of the active constituents of Coptis chinensis Franch. Herein, jatrorrhizine derivatives with substituted amino groups linked at the 3-position were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Jatrorrhizine derivatives inhibited the activity of acetylcholinesterase (AChE) to a greater extent than the lead compound jatrorrhizine. All these jatrorrhizine derivatives were proved to be potent inhibitors of acetylcholinesterase (AChE) with submicromolar IC 50 values, but less sensitive to butyrylcholinesterase (BuChE), which suggests that these jatrorrhizine derivatives are selective for AChE/BuChE. Compound g gave the most potent inhibitor activity for AChE (IC 50 = 0.301 M), which is greater than the lead compound jatrorrhizine. All these results demonstrated that these jatrorrhizine derivatives are potential inhibitors for AChE.

show abstract

Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors

Cited by 54 publications

References 23 publications

Decrease in the production of beta-amyloid by berberine inhibition of the expression of beta-secretase in HEK293 cells

Decrease in the production of beta-amyloid by berberine inhibition of the expression of beta-secretase in HEK293 cells

Three Chinese herbal medicines promote neuroproliferation in vitro, and reverse the effects of chronic mild stress on behavior, the HPA axis, and proliferation of hippocampal precursor cell in vivo

Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase

Contact Info

Product

Resources

About