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Ursolic Acid Derivatives Bearing 1,2,3-triazole Moieties as Potential PTP1B Inhibitors

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Chemistry of Natural Compounds Aims and scope

Here, a series of ursolic acid (UA) derivatives were identified as potential PTP1B enzyme inhibitors. All of the tested compounds showed potent PTP1B inhibitory activity (87.79–96.80%) at a concentration of 20 μg/mL and dose-dependently inhibited PTP1B enzyme with IC50 values ranging from 4.15 ± 0.01 to 14.10 ± 0.45 μM. Compound 11e showed the best PTP1B inhibitory potency, with IC50 values of 4.15 ± 0.01 μM, which was slightly lower than that of the positive control. Molecular docking simulation and analysis suggested that compound 11e has a good binding interaction with the active pocket.

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Acknowledgment

This work was supported by the Natural Science Foundation of Jilin Province (No. YDZJ202201ZYTS277); The Department of Education of Jilin Province (No. JJKH20210495KJ) and the Health Department of Jilin Province (2020Z005). In addition, Zhe Liu and Xueqian Bai contributed equally to this work.

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Authors and Affiliations

  1. Jilin Medical University, 132013, Jilin, P. R. China

    Zhe Liu, Xueqian Bai & Tianyi Zhang

  2. National Center for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Science, Chinese Academy of Sciences, 201203, Shanghai, P. R. China

    Li Sheng & Jia Li

  3. Yanbian University, 133000, Yanji, P. R. China

    Liangpeng Sun & Tianyi Zhang

Authors
  1. Zhe Liu
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  2. Xueqian Bai
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  3. Li Sheng
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  4. Liangpeng Sun
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  5. Jia Li
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  6. Tianyi Zhang
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Corresponding authors

Correspondence to Jia Li or Tianyi Zhang.

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Published in Khimiya Prirodnykh Soedinenii, No. 3, May–June, 2023, pp. 431–433.

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Liu, Z., Bai, X., Sheng, L. et al. Ursolic Acid Derivatives Bearing 1,2,3-triazole Moieties as Potential PTP1B Inhibitors. Chem Nat Compd 59, 508–511 (2023). https://doi.org/10.1007/s10600-023-04037-0

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  • DOI: https://doi.org/10.1007/s10600-023-04037-0

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