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

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.

Exserolide J ameliorates lipid accumulation in vitro by regulating liver X receptor alpha and peroxisome proliferator-activated receptor alpha proteins

“…However, there are some limitations in the present study. It is estimated that approximately 50 % of drug research and development failures are originated from the in vivo pharmacokinetic properties, particularly hepatic metabolism, of the interested compound [ 49 ]. Cytochrome P450 (CYP) enzymes and other enzymes, such as UDP-glucuronosyltransferases, play vital roles in the metabolism of xenobiotics.…”

“…Cytochrome P450 (CYP) enzymes and other enzymes, such as UDP-glucuronosyltransferases, play vital roles in the metabolism of xenobiotics. Several literatures have demonstrated that isocoumarins may interact with CYP family members, such as CYP2D6 [ 49 , 50 ]. Based on these available literatures, exserolides, a minor existing form of isocoumarin, are predicted be metabolized into their hydroxy and/or ester forms as well as conjugated derivatives with glutathione, sulfate, and glucuronic acid groups.…”