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Volume 17
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10.3390/ph17121665
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Review

Rhein: An Updated Review Concerning Its Biological Activity, Pharmacokinetics, Structure Optimization, and Future Pharmaceutical Applications

by
Yuqi Fu
1,
Le Yang
2,
Lei Liu
1,
Ling Kong
1,
Hui Sun
1,*,
Ye Sun
2,
Fengting Yin
1,
Guangli Yan
1 and
Xijun Wang
1,2,*
1
State Key Laboratory of Integration and Innovation of Classic Formula and Modern Chinese Medicine, National Chinmedomics Research Center, National TCM Key Laboratory of Serum Pharmacochemistry, Metabolomics Laboratory, Department of Pharmaceutical Analysis, Heilongjiang University of Chinese Medicine, Heping Road 24, Harbin 150040, China
2
State Key Laboratory of Dampness Syndrome, The Second Affiliated Hospital Guangzhou University of Chinese Medicine, Dade Road 111, Guangzhou 510006, China
*
Authors to whom correspondence should be addressed.
Pharmaceuticals 2024, 17(12), 1665; https://doi.org/10.3390/ph17121665
Submission received: 20 November 2024 / Revised: 8 December 2024 / Accepted: 9 December 2024 / Published: 10 December 2024
(This article belongs to the Section Natural Products)
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Abstract

Rhein is a natural active ingredient in traditional Chinese medicine that has attracted much attention due to its wide range of pharmacological activities. However, its clinical application is limited by low water solubility, poor oral absorption, and potential toxicity to the liver and kidneys. Recently, advanced extraction and synthesis techniques have made it possible to develop derivatives of rhein, which have better pharmacological properties and lower toxicity. This article comprehensively summarizes the biological activity and action mechanism of rhein. Notably, we found that TGF-β1 is the target of rhein improving tissue fibrosis, while NF-κB is the main target of its anti-inflammatory effect. Additionally, we reviewed the current research status of the pharmacokinetics, toxicology, structural optimization, and potential drug applications of rhein and found that the coupling and combination therapy of rhein and other active ingredients exhibit a synergistic effect, significantly enhancing therapeutic efficacy. Finally, we emphasize the necessity of further studying rhein’s pharmacological mechanisms, toxicology, and development of analogs, aiming to lay the foundation for its widespread clinical application as a natural product and elucidate its prospects in modern medicine.
Keywords: rhein; TGF-β1; NF-κB; pharmacokinetics; twin drug; derivatives; combination therapy rhein; TGF-β1; NF-κB; pharmacokinetics; twin drug; derivatives; combination therapy
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MDPI and ACS Style

Fu, Y.; Yang, L.; Liu, L.; Kong, L.; Sun, H.; Sun, Y.; Yin, F.; Yan, G.; Wang, X. Rhein: An Updated Review Concerning Its Biological Activity, Pharmacokinetics, Structure Optimization, and Future Pharmaceutical Applications. Pharmaceuticals 2024, 17, 1665. https://doi.org/10.3390/ph17121665

AMA Style

Fu Y, Yang L, Liu L, Kong L, Sun H, Sun Y, Yin F, Yan G, Wang X. Rhein: An Updated Review Concerning Its Biological Activity, Pharmacokinetics, Structure Optimization, and Future Pharmaceutical Applications. Pharmaceuticals. 2024; 17(12):1665. https://doi.org/10.3390/ph17121665

Chicago/Turabian Style

Fu, Yuqi, Le Yang, Lei Liu, Ling Kong, Hui Sun, Ye Sun, Fengting Yin, Guangli Yan, and Xijun Wang. 2024. "Rhein: An Updated Review Concerning Its Biological Activity, Pharmacokinetics, Structure Optimization, and Future Pharmaceutical Applications" Pharmaceuticals 17, no. 12: 1665. https://doi.org/10.3390/ph17121665

APA Style

Fu, Y., Yang, L., Liu, L., Kong, L., Sun, H., Sun, Y., Yin, F., Yan, G., & Wang, X. (2024). Rhein: An Updated Review Concerning Its Biological Activity, Pharmacokinetics, Structure Optimization, and Future Pharmaceutical Applications. Pharmaceuticals, 17(12), 1665. https://doi.org/10.3390/ph17121665

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