Synthesis, biological evaluation and molecular docking of novel nereistoxin derivatives containing phosphonates as insecticidal/AChE inhibitory agents

Yan, Qiaoli; Lu, Xiaogang; Wang, Jin; Zhang, Zixuan; Gao, Runli; Pei, Chengxin; Wang, Hongmei

doi:10.1039/d3ra08004h

RSC Adv.

2024

DOI: 10.1039/d3ra08004h

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Synthesis, biological evaluation and molecular docking of novel nereistoxin derivatives containing phosphonates as insecticidal/AChE inhibitory agents

Qiaoli Yan,

Xiaogang Lu,

Jin Wang

et al.

Abstract: In continuation of our program aimed at the discovery and development of natural product-based insecticidal agents, a series of novel nereistoxin derivatives containing phosphonate were synthesized and characterized by 31P, 1H, 13C NMR and HRMS.

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Cited by 2 publications

References 27 publications

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Quaternity method for integrated screening, separation, extraction optimization, and bioactivity evaluation of acetylcholinesterase inhibitors from Sophora flavescens Aiton

Zhang,

et al. 2024

Phytochemical Analysis

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IntroductionSophora flavescens Aiton (Fabaceae), a ubiquitous plant species in Asia, contains a wide range of pharmacologically active compounds, such as flavonoids, with potential anti‐Alzheimer's disease (anti‐AD) effects.ObjectivesThe objective of the study is to develop a quaternity method for the screening, isolation, extraction optimization, and activity evaluation of acetylcholinesterase (AChE)‐inhibiting compounds from S. flavescens to realize high‐throughput screening of active substances in traditional Chinese medicine and to provide experimental data for the development of anti‐AD drugs.MethodsWith AChE as the target molecule, affinity ultrafiltration and liquid chromatography‐mass spectrometry were applied to screen for potential inhibitors of the enzyme in S. flavescens. Orthogonal array experiments combined with the multi‐objective Non‐Dominated Sorting Genetic Algorithm III was used for the first time to optimize the process for extracting the active substances. Enzyme inhibition kinetics and molecular docking studies were performed to verify the potential anti‐AD effects of the active compounds.ResultsFive AChE‐inhibiting compounds were identified: kushenol I, kurarinone, sophoraflavanone G, isokurarinone, and kushenol E. These were successfully separated at purities of 72.88%, 98.55%, 96.86%, 96.74%, and 95.84%, respectively, using the n‐hexane/ethyl acetate/methanol/water (4.0/5.0/4.0/5.0, v/v/v/v), n‐hexane/ethyl acetate/methanol/water (5.0/5.0/6.0/4.0, v/v/v/v), and n‐hexane/ethyl acetate/methanol/water (4.9/5.1/5.7/4.3, v/v/v/v) mobile phase systems. Enzyme inhibition kinetics revealed that kushenol E had the best inhibitory effect.ConclusionThis study elucidates the mechanism of action of five active AChE inhibitors in S. flavescens and provides a theoretical basis for the screening and development of anti‐AD and other therapeutic drugs.

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Quaternity method for integrated screening, separation, extraction optimization, and bioactivity evaluation of acetylcholinesterase inhibitors from Sophora flavescens Aiton

Zhang,

et al. 2024

Phytochemical Analysis

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Coumarin modified Silatrane: A potent probe for Hg(II) ion Detection, biological evaluation and Acetylcholinesterase inhibition

Singh,

Malik,

Heena

et al. 2025

Inorganic Chemistry Communications

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Synthesis, biological evaluation and molecular docking of novel nereistoxin derivatives containing phosphonates as insecticidal/AChE inhibitory agents

Abstract: In continuation of our program aimed at the discovery and development of natural product-based insecticidal agents, a series of novel nereistoxin derivatives containing phosphonate were synthesized and characterized by 31P, 1H, 13C NMR and HRMS.

Cited by 2 publications

References 27 publications

Quaternity method for integrated screening, separation, extraction optimization, and bioactivity evaluation of acetylcholinesterase inhibitors from Sophora flavescens Aiton

Quaternity method for integrated screening, separation, extraction optimization, and bioactivity evaluation of acetylcholinesterase inhibitors from Sophora flavescens Aiton

Coumarin modified Silatrane: A potent probe for Hg(II) ion Detection, biological evaluation and Acetylcholinesterase inhibition

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