Evidence map›Paper›PMID 40493282›Full record

ArticleJournal of computer-aided molecular design2025

A systematic insight into glycycoumarin as potential IL-8/topo I inhibitor from natural products collected in Taibai mountain based on the combination of in silico and bioassay.

Na-Na Tan, Jia Lu, Zhuang-Hong Li, Shi-Ping Zhang, Huan Wang, Jing-Bo Hu, Tian Wang, Jian Xiao, Xiao-Ling Wang, Le Wang

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Article in Journal of computer-aided molecular design, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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1 · What the graph read from it

What it found

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2 · The registry

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3 · Its place in the literature

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4 · The record

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5 · Who and what money

Authors and funding

10 authors.

Na-Na Tan *Shaanxi Key Laboratory of Phytochemistry, College of Chemistry and Chemical Engineering, Baoji University of Arts and Sciences, High-tech Avenue 1#, Baoji, Baoji, 721013, China.
Jia Lu *Shaanxi Key Laboratory of Phytochemistry, College of Chemistry and Chemical Engineering, Baoji University of Arts and Sciences, High-tech Avenue 1#, Baoji, Baoji, 721013, China.
Zhuang-Hong LiShaanxi Key Laboratory of Phytochemistry, College of Chemistry and Chemical Engineering, Baoji University of Arts and Sciences, High-tech Avenue 1#, Baoji, Baoji, 721013, China.
Shi-Ping ZhangShaanxi Key Laboratory of Phytochemistry, College of Chemistry and Chemical Engineering, Baoji University of Arts and Sciences, High-tech Avenue 1#, Baoji, Baoji, 721013, China.
Huan WangCollege of Computer Science and Technology, Baoji University of Arts and Sciences, Baoji, 721013, China.
Jing-Bo HuCollege of Electronic and Electrical Engineering, Baoji University of Arts and Sciences, Baoji, 721013, China.
Tian WangShaanxi Key Laboratory of Phytochemistry, College of Chemistry and Chemical Engineering, Baoji University of Arts and Sciences, High-tech Avenue 1#, Baoji, Baoji, 721013, China.
Jian XiaoShaanxi Key Laboratory of Phytochemistry, College of Chemistry and Chemical Engineering, Baoji University of Arts and Sciences, High-tech Avenue 1#, Baoji, Baoji, 721013, China.
Xiao-Ling WangShaanxi Key Laboratory of Phytochemistry, College of Chemistry and Chemical Engineering, Baoji University of Arts and Sciences, High-tech Avenue 1#, Baoji, Baoji, 721013, China.
Le WangShaanxi Key Laboratory of Phytochemistry, College of Chemistry and Chemical Engineering, Baoji University of Arts and Sciences, High-tech Avenue 1#, Baoji, Baoji, 721013, China. leolynne@gmail.com.

Funding

Innovation Capability Support Program of Shaanxi 2022TD-63National Natural Science Foundation of China 82104682
6 · The paper itself

Abstract

This study aimed to screen IL-8/topo I inhibitors from natural products collected in Taibai mountain and explore the underlying mechanisms. A natural product library of Taibai mountain (NPTM) was first constructed containing 186 compounds. Then, 15 and 6 potential inhibitors were screened using pharmacophore modeling for IL-8 and topo I, respectively. Molecular docking indicated that glycycoumarin was IL-8/topo I inhibitor. A 200 ns molecular dynamics simulation reflected high binding stability and favorable hydrogen bond interaction within glycycoumarin-IL-8/topo I complexes. MM/GBSA calculation showed that the binding free energy was - 12.81 kcal/mol and - 31.20 kcal/mol, and Pro 32 and DT 10 contributed most to glycycoumarin and IL-8, topo I, respectively. SMD simulation demonstrated a stable binding under physiological conditions with energy demands to dissociate from IL-8/topo I. Glycycoumarin decreased IL-8 production in the inflammatory cells, and exhibited obvious topo I inhibition, as well as strong cytotoxicity to three cancer cells. A PPI network revealed that glycycoumarin might work through proteoglycans in cancer (hsa05205) and IL-17 signaling pathway (hsa04657). These results improved current understanding of natural IL-8/topo I inhibitors from Taibai mountain. The combination of in silico and bioassay could provide a new strategy for exploring natural lead compounds against inflammation and cancer.

Indexed as

Biological ProductsDNA Topoisomerases, Type IInterleukin-8Topoisomerase I InhibitorsBiological AssayCoumarinsHumansMolecular Docking SimulationMolecular Dynamics SimulationBiological ProductsCoumarinsDNA Topoisomerases, Type IInterleukin-8Topoisomerase I InhibitorsInterleukin-8Natural productTaibai mountainTopoisomerase I

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.