Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
11033441 | Neuroscience Letters | 2018 | 31 Pages |
Abstract
An acetylcholinesterase inhibitory compound was isolated from Tephrosia purpurea (L.) Pers. by zebrafish brain based bioassay guided isolation and predicted as trans-tephrostachin.Enzyme kinetics studies (Line weaver-Burk plots and Michaelis Menten equation) favored the reversible / mixed type, with the inhibition constant (Ki) of 53.0â±â7.4âμM in zebrafish brain (IC50 value of 39.0â±â1.4 μM). However, the inhibition constant (Ki) was found to be 36.0â±â0.4âμM with IC50 value of 20.0â±â1.0 μM, whereas donepezil showed 3.2â±â0.3âμM with the IC50 value of 0.12â±â0.04âμM for human acetylcholinesterase. Further, the molecular docking, dynamics and simulation for trans-tephrostachin obtained better binding affinity and efficacy than commercial drugs donepezil and galanthamine. Hence, the isolated compound trans - tephrostachin from T. purpurea shall be further considered for the development of potential drug for the counteraction of Alzheimer's disease progression.
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Authors
Pitchai Arjun, Nagarajan Nagasundaram, Vincent Samuel Gnana Prakash, Rajaretinam Rajesh Kannan,