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Engelheptanoxides behave as liver X receptor α agonists

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Abstract

Engelheptanoxide A and C are the active ingredients isolated from Engelhardia roxburghiana, a novel traditional herbal medicine exerting pharmacological effects including the antitubercular effect. Liver X receptor (LXR) acts as a ligand-activated transcription factor that can exert multi-pharmacological functions. In this study, the activity of engelheptanoxide A and C against LXRα was evaluated by the transient transfection reporter and mammalian one-hybrid assays. The results showed that engelheptanoxide A and C respectively transactivated CYP7A1, ABCA1, and Gal4 promoters in the dose-dependent manner. Furthermore, the docking study demonstrated that engelheptanoxide A and C can contact with the LXRα ligand binding pocket in the similar manner as 22(R)-hydroxycholesterol, an endogenous LXRα agonist, to agonize LXRα. These results indicated that Engelhardia roxburghiana might be able to exert pharmacological effects through LXRα pathway.

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Acknowledgements

I thank Dr. Chiang J.Y., at College of Medicine, Northeastern Ohio Universities for kindly offering the CYP7A1 reporter plasmid and Dr. Fielding C.J., at University of California at San Francisco for kindly offering the ABCA1 reporter plasmid.

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Authors and Affiliations

  1. Institute of Clinical Medicine, National Yang Ming Chiao Tung University, Taipei, 112304, Taiwan, ROC

    Yu-Hsuan Liang

  2. Institute of Traditional Medicine, National Yang Ming Chiao Tung University, Taipei, 112304, Taiwan, ROC

    Yu-Han Luo

  3. School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, No. 100, Shih-Chuan 1st Road, Kaohsiung, 80708, Taiwan, ROC

    Ih-Sheng Chen

  4. Department of Chemistry, College of Science, National Kaohsiung Normal University, No. 62, Shenjhong Rd., Yanchao District, Kaohsiung, 82446, Taiwan, ROC

    Hsiang-Ru Lin

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  1. Yu-Hsuan Liang
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Liang, YH., Luo, YH., Chen, IS. et al. Engelheptanoxides behave as liver X receptor α agonists. Med Chem Res 32, 434–441 (2023). https://doi.org/10.1007/s00044-023-03016-y

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  • DOI: https://doi.org/10.1007/s00044-023-03016-y

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