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Review

Therapeutic Potential of Bioactive Compounds from Traditional Chinese Medicine in Modulating Macrophage Cholesterol Metabolism for Atherosclerosis Treatment

1
Guangxi Key Laboratory of Efficacy Study on Chinese Materia Medica, Guangxi University of Chinese Medicine, Nanning 530000, China
2
University Engineering Research Center of Reutilization of Traditional Chinese Medicine Resources, Guangxi University of Chinese Medicine, Nanning 530000, China
3
Guangxi Key Laboratory of TCM Formulas Theory and Transformation for Damp Diseases, Guangxi University of Chinese Medicine, Nanning 530000, China
*
Authors to whom correspondence should be addressed.
Pharmaceuticals 2025, 18(8), 1113; https://doi.org/10.3390/ph18081113
Submission received: 10 June 2025 / Revised: 11 July 2025 / Accepted: 24 July 2025 / Published: 25 July 2025

Abstract

Atherosclerosis (AS) is a complex pathological process characterized by the pivotal involvement of foam cells in its pathogenesis. As the primary cellular components of arterial plaques, foam cells critically determine plaque stability. Foam cells derive mainly from macrophages, and their formation is driven by dysregulated lipid metabolism within these immune cells. Macrophage cholesterol metabolism is a highly regulated process comprising four key phases: uptake, esterification, hydrolysis, and efflux. Under physiological conditions, these four phases maintain a delicate balance. However, disruption of cholesterol homeostasis results in the excessive accumulation of intracellular lipid, promoting the formation of foam cell and inflammasome activation, thereby accelerating the atherosclerotic progression. Therefore, targeting macrophage cholesterol metabolism has emerged as a promising therapeutic approach for AS. This review summarizes the mechanisms underlying macrophage cholesterol metabolism and highlights recent progress in identifying bioactive components of traditional Chinese medicines (TCMs) that mitigate AS through the modulation of macrophage cholesterol homeostasis. These findings may offer novel insights into the development of clinically effective therapies for the prevention of AS.
Keywords: atherosclerosis; macrophage cholesterol metabolism; traditional Chinese medicine; anti-atherosclerosis compounds; mechanism of action atherosclerosis; macrophage cholesterol metabolism; traditional Chinese medicine; anti-atherosclerosis compounds; mechanism of action

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MDPI and ACS Style

Yan, L.; Guo, J.; Huang, D.; Zhang, F.; Du, Z.; Hou, X.; Deng, J.; Xie, Y.; Hao, E. Therapeutic Potential of Bioactive Compounds from Traditional Chinese Medicine in Modulating Macrophage Cholesterol Metabolism for Atherosclerosis Treatment. Pharmaceuticals 2025, 18, 1113. https://doi.org/10.3390/ph18081113

AMA Style

Yan L, Guo J, Huang D, Zhang F, Du Z, Hou X, Deng J, Xie Y, Hao E. Therapeutic Potential of Bioactive Compounds from Traditional Chinese Medicine in Modulating Macrophage Cholesterol Metabolism for Atherosclerosis Treatment. Pharmaceuticals. 2025; 18(8):1113. https://doi.org/10.3390/ph18081113

Chicago/Turabian Style

Yan, Lijiao, Jiageng Guo, Dan Huang, Fan Zhang, Zhengcai Du, Xiaotao Hou, Jiagang Deng, Yan Xie, and Erwei Hao. 2025. "Therapeutic Potential of Bioactive Compounds from Traditional Chinese Medicine in Modulating Macrophage Cholesterol Metabolism for Atherosclerosis Treatment" Pharmaceuticals 18, no. 8: 1113. https://doi.org/10.3390/ph18081113

APA Style

Yan, L., Guo, J., Huang, D., Zhang, F., Du, Z., Hou, X., Deng, J., Xie, Y., & Hao, E. (2025). Therapeutic Potential of Bioactive Compounds from Traditional Chinese Medicine in Modulating Macrophage Cholesterol Metabolism for Atherosclerosis Treatment. Pharmaceuticals, 18(8), 1113. https://doi.org/10.3390/ph18081113

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