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Record W7116695949 · doi:10.1002/ardp.70174

Multi‐Angle Bioactivity Cartography for Computational Screening and Mechanistic Analysis of AChE Inhibitors From Yellow <i>Gastrodia elata</i>

2025· article· en· W7116695949 on OpenAlex
Ruijun Sun, Yuchi Zhang, Jingying Xu, Ming Chen, C. Liu, Xuanlin Liu, Yang Zhou, Rong Tsao, Y. Ito, Li Sainan

Why this work is in the frame

A frame that forgets how it found something cannot be audited. These are the routes that admitted this work.

affAt least one author lists a Canadian institution in the pinned OpenAlex snapshot.

Bibliographic record

VenueArchiv der Pharmazie · 2025
Typearticle
Languageen
FieldMedicine
TopicBiological and pharmacological studies of plants
Canadian institutionsAgriculture and Agri-Food Canada
FundersChangchun Normal UniversityPeople's Government of Jilin ProvinceNatural Science Foundation of Jilin Province
KeywordsAcetylcholinesteraseDocking (animal)PrioritizationEnzymeDrug discoveryIn silicoEnzyme inhibitionEnzyme inhibitor

Abstract

fetched live from OpenAlex

ABSTRACT Acetylcholinesterase (AChE) inhibitors are crucial for the symptomatic management of Alzheimer's disease (AD), with natural products—particularly botanical sources like Yellow Gastrodia elata (YGE)—serving as promising reservoirs of such inhibitors. Nevertheless, comprehensive screening and mechanistic characterization of their inhibitory potential remain limited. This study sought to identify potent AChE inhibitors from YGE, investigate their mechanisms of action, and assess their therapeutic prospects for AD. Methodologically, an integrated approach was employed, combining ultrafiltration‐liquid chromatography (UF‐LC) for rapid inhibitor screening, molecular docking and dynamics simulations for mechanistic insight, two‐stage high‐speed countercurrent chromatography for compound isolation, enzyme kinetics to delineate inhibition modalities, and network pharmacology to uncover relevant AD‐related targets. The findings identified seven active constituents with notable AChE inhibition, among which parishins A and G were obtained at high purity (98.26% and 97.26%, respectively) and exhibited mixed‐type inhibition with low IC 50 values (0.0145 and 0.0148 mM). Molecular dynamics and network pharmacology analyses further revealed critical interactions between these compounds and key AD‐related targets, including ACHE, BCHE, BACE1, and PTGS2. In summary, this work underscores the potential of YGE‐sourced compounds, especially parishins A and G, as effective AChE inhibitors. The established integrative computational platform facilitates multi‐dimensional bioactivity evaluation and enables hierarchical prioritization of candidate compounds, thereby offering a valuable framework for advancing natural product‐derived therapeutics for AD.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Observational · Consensus signal: Observational
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.206
Threshold uncertainty score0.444

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.043
GPT teacher head0.333
Teacher spread0.291 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it