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Abstract <p>Betulinic acid (BA) is a naturally occurring pentacyclic triterpenoid widely distributed in a variety of medicinal plants and has attracted considerable attention as an active constituent of several traditional herbal medicines. In recent years, research on BA has increasingly focused on cancer and inflammation owing to its broad-spectrum pharmacological activities against tumours and inflammation-related diseases. This review summarizes recent advances in the study of BA and its derivatives, with particular emphasis on their antitumour and anti-inflammatory properties, underlying molecular mechanisms, and strategies to improve therapeutic efficacy. Accumulating evidence indicates that BA exerts its antitumour and anti-inflammatory effects through multiple pathways and molecular targets. In addition, representative structural modification approaches and nano-enabled drug delivery strategies developed to overcome the intrinsic limitations of BA, such as poor aqueous solubility and low bioavailability, are systematically discussed. Finally, key challenges associated with the clinical translation of BA are highlighted from a translational perspective, with the aim of providing references for further experimental investigations and clinical development. Overall, BA represents a promising bioactive monomer with dual anti-tumour and anti-inflammatory potential, particularly in the context of inflammation-associated cancers.</p> Conclusions <p>The research and development prospects of BA and its derivatives as active monomeric compounds in traditional Chinese medicine are promising, yet several challenges remain. In terms of research directions, further structural optimization of these derivatives is needed to enhance their biological activity, selectivity, and pharmacokinetic properties. In addition, exploring new targets and mechanisms of action represents another important avenue, which may provide a more solid theoretical and experimental foundation for the development of BA as a new anti-tumour and anti-inflammatory drug.</p> Graphical abstract <p></p>

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Research advances in the application of betulinic acid for anti-inflammatory and anti-tumour therapy

  • 期刊论文

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  • 发表日期：

    2026年5月26日

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  • Zewen Chu,
  • Shuaiyu Jiang,
  • Yuting Li,
  • Xiang Li,
  • Wan Xin Koh,
  • Pottakorn Aruncharoenphonchai,
  • Yue Ding,
  • Yanwei Xiang

摘要

Abstract

Betulinic acid (BA) is a naturally occurring pentacyclic triterpenoid widely distributed in a variety of medicinal plants and has attracted considerable attention as an active constituent of several traditional herbal medicines. In recent years, research on BA has increasingly focused on cancer and inflammation owing to its broad-spectrum pharmacological activities against tumours and inflammation-related diseases. This review summarizes recent advances in the study of BA and its derivatives, with particular emphasis on their antitumour and anti-inflammatory properties, underlying molecular mechanisms, and strategies to improve therapeutic efficacy. Accumulating evidence indicates that BA exerts its antitumour and anti-inflammatory effects through multiple pathways and molecular targets. In addition, representative structural modification approaches and nano-enabled drug delivery strategies developed to overcome the intrinsic limitations of BA, such as poor aqueous solubility and low bioavailability, are systematically discussed. Finally, key challenges associated with the clinical translation of BA are highlighted from a translational perspective, with the aim of providing references for further experimental investigations and clinical development. Overall, BA represents a promising bioactive monomer with dual anti-tumour and anti-inflammatory potential, particularly in the context of inflammation-associated cancers.

Conclusions

The research and development prospects of BA and its derivatives as active monomeric compounds in traditional Chinese medicine are promising, yet several challenges remain. In terms of research directions, further structural optimization of these derivatives is needed to enhance their biological activity, selectivity, and pharmacokinetic properties. In addition, exploring new targets and mechanisms of action represents another important avenue, which may provide a more solid theoretical and experimental foundation for the development of BA as a new anti-tumour and anti-inflammatory drug.

Graphical abstract