Updated pharmaceutical progress on plant antibiotic rhein and its analogs: Bioactivities, structure–activity relationships and future perspectives

Zhang, Yindi; Jiang, Yueping; Shang, Kaiqi; Ge, Chengyu; Fang, Jing; Liu, Shao

doi:10.1016/j.bmc.2024.117895

Bioorganic & Medicinal Chemistry

2024

DOI: 10.1016/j.bmc.2024.117895

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Updated pharmaceutical progress on plant antibiotic rhein and its analogs: Bioactivities, structure–activity relationships and future perspectives

Yindi Zhang,

Yueping Jiang,

Kaiqi Shang

et al.

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

Fu,

Yang,

Liu

et al. 2024

Pharmaceuticals

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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.

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

Fu,

Yang,

Liu

et al. 2024

Pharmaceuticals

View full text Add to dashboard Cite

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

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Updated pharmaceutical progress on plant antibiotic rhein and its analogs: Bioactivities, structure–activity relationships and future perspectives

Cited by 1 publication

References 64 publications

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

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

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