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Volume 31
Issue 2
10.3390/molecules31020246
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This is an early access version, the complete PDF, HTML, and XML versions will be available soon.
Review

Anticancer Potential of Atractylenolides I-III: Efficacy, Mechanisms, Pharmacokinetics, and Safety

by
Lujia Zhang
1,
Jinjian Lu
2,
Mengning Zhang
1,
Yingying Dong
1,
Yutao Luo
1,
Tiantian Lei
1,
Zhujun Bian
1,
Xiaofeng Yuan
3,* and
Hong Zhao
1,*
1
The First School of Clinical Medicine, Zhejiang Chinese Medical University, Hangzhou 310053, China
2
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao 999078, China
3
School of Life Sciences, Zhejiang Chinese Medical University, Hangzhou 310053, China
*
Authors to whom correspondence should be addressed.
Molecules 2026, 31(2), 246; https://doi.org/10.3390/molecules31020246 (registering DOI)
Submission received: 21 November 2025 / Revised: 24 December 2025 / Accepted: 5 January 2026 / Published: 11 January 2026
Versions Notes

Abstract

Atractylenolides (ATs; mainly AT-I, II, and III), as one of the primary active components of the traditional Chinese medicine Atractylodes macrocephala, have demonstrated significant antitumorigenic effects against various cancer cells in both in vitro and in vivo studies. This review aims to systematically review the antitumorigenic effects, mechanisms, pharmacokinetics, and safety profile of ATs, aiming to contribute to clinical research and applications. To achieve this, a systematic literature search was conducted across multiple databases, and findings were synthesized narratively to provide a comprehensive overview of the current evidence. This review comprehensively discusses the antitumorigenic effects and mechanisms of ATs, including arresting tumor cell cycle progression, inducing programmed cell death (apoptosis, autophagy, and ferroptosis), inhibiting tumor angiogenesis, suppressing tumor migration and invasion, modulating the tumor immune microenvironment, and enhancing the efficacy of combination therapies. Additionally, their pharmacokinetic properties and safety profile are summarized, with a focus on their research and application prospects. ATs appear to be safe and reliable candidate anticancer agents in preclinical models, exhibiting potent antitumor efficacy both as monotherapy and in combination regimens. Preliminary clinical data from a small pilot study also indicated no signs of toxicity, but more extensive trials are needed to confirm their safety profile in humans. Further studies on their mechanisms are warranted to facilitate their development into clinically effective antitumor agents.
Keywords: atractylenolides (I, II, and III); cancer; efficacy; mechanism; pharmacokinetics; safety atractylenolides (I, II, and III); cancer; efficacy; mechanism; pharmacokinetics; safety

Share and Cite

MDPI and ACS Style

Zhang, L.; Lu, J.; Zhang, M.; Dong, Y.; Luo, Y.; Lei, T.; Bian, Z.; Yuan, X.; Zhao, H. Anticancer Potential of Atractylenolides I-III: Efficacy, Mechanisms, Pharmacokinetics, and Safety. Molecules 2026, 31, 246. https://doi.org/10.3390/molecules31020246

AMA Style

Zhang L, Lu J, Zhang M, Dong Y, Luo Y, Lei T, Bian Z, Yuan X, Zhao H. Anticancer Potential of Atractylenolides I-III: Efficacy, Mechanisms, Pharmacokinetics, and Safety. Molecules. 2026; 31(2):246. https://doi.org/10.3390/molecules31020246

Chicago/Turabian Style

Zhang, Lujia, Jinjian Lu, Mengning Zhang, Yingying Dong, Yutao Luo, Tiantian Lei, Zhujun Bian, Xiaofeng Yuan, and Hong Zhao. 2026. "Anticancer Potential of Atractylenolides I-III: Efficacy, Mechanisms, Pharmacokinetics, and Safety" Molecules 31, no. 2: 246. https://doi.org/10.3390/molecules31020246

APA Style

Zhang, L., Lu, J., Zhang, M., Dong, Y., Luo, Y., Lei, T., Bian, Z., Yuan, X., & Zhao, H. (2026). Anticancer Potential of Atractylenolides I-III: Efficacy, Mechanisms, Pharmacokinetics, and Safety. Molecules, 31(2), 246. https://doi.org/10.3390/molecules31020246

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