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Review
. 2023 Jan 19;16(2):150.
doi: 10.3390/ph16020150.

Current Progress and Outlook for Agrimonolide: A Promising Bioactive Compound from Agrimonia pilosa Ledeb

Ting Huang  1 , Chun-Cao Zhao  1 , Man Xue  1 , Yun-Feng Cao  1 , Liang-Kang Chen  1 , Jian-Xing Chen  1 , Yi-Jie Sun  2 , Jia Zeng  1
Affiliations
Review

Current Progress and Outlook for Agrimonolide: A Promising Bioactive Compound from Agrimonia pilosa Ledeb

Ting Huang et al. Pharmaceuticals (Basel). .

Abstract

Agrimonolide (AM), which is a derivative of isocoumarins, is found mainly in the herb Agrimonia pilosa Ledeb. This compound is highly lipophilic and readily crosses the blood-brain barrier. In recent years, interest has grown in the use of AM as a multitarget natural treatment for various diseases, such as cancer, inflammation, hepatic injury, myocardial damage, and diabetes mellitus. The potential mechanisms of these pharmacological effects have been clarified at cellular and molecular levels. AM shows no cytotoxicity over a range of concentrations in different types of cells, providing evidence for its good safety profile in vitro. These findings indicate that AM is a promising medicinal agent. However, most studies on AM's pharmacological activities, mechanisms of action, and safety lack substantial animal or human data. Additionally, the pharmacokinetics, metabolism, and disposition of this compound have received little attention. This review highlights the status of current information regarding the sources, properties, pharmacological effects, and safety of AM. Furthermore, potential strategies to resolve problematic issues identified in previous studies are fully discussed. This summary and analysis of the research progress of AM may inspire deeper investigations and more extensive applications of AM in the future.

Keywords: Agrimonia pilosa Ledeb.; agrimonolide; pharmacological effect; safety.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chemical structure of AM.
Figure 2
Figure 2
Chemical synthesis routes of AM [24,25,26].
Figure 3
Figure 3
Mechanism of AM for its antitumor effects. (A) Anti-gastric cancer; and (B) anti-ovarian cancer.
Figure 4
Figure 4
Mechanism of AM for its antioxidative and hepatoprotective effects.
Figure 5
Figure 5
Mechanism of AM for its anti-diabetic effects. (A) Inhibition of α-glucosidase; (B) constraint of gluconeogenesis; and (C) promotion of pancreatic duodenal homeobox-1 expression.
Figure 6
Figure 6
Mechanism of AM for its anti-inflammatory effects.
Figure 7
Figure 7
Mechanism of AM for its myocardial protective effects.
See this image and copyright information in PMC

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