Drug intelligence / Profile preview

paeonol

Development stage
Phase 2
Modality
Small Molecules
Administration
Oral
01

Overview

Paeonol is a naturally occurring phenolic compound primarily extracted from the root bark of Paeonia suffruticosa (moutan cortex) and found in other plants such as Arisaema erubescens and Dioscorea japonica. It is widely used in traditional Chinese medicine. Paeonol exhibits a broad range of pharmacological activities, including anti-inflammatory, analgesic, antimutagenic, immunomodulatory, neuroprotective, cardioprotective, and antitumor effects[1][4][5][6][8]. Mechanistically, it acts as a weak inhibitor of monoamine oxidase A (MAO-A) and B (MAO-B), modulates multiple signaling pathways such as PI3K/Akt and NF-κB to suppress inflammation and tumor progression[1][5][6][8], inhibits the release of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α), regulates macrophage polarization toward an anti-inflammatory phenotype[6], reduces oxidative stress by decreasing reactive oxygen species generation[6], reverses drug resistance by targeting ABC transporter proteins including p-glycoprotein[5], inhibits adhesion molecules like VCAM-1/ICAM-1 via ERK/p38/NF-κB pathways to protect vascular endothelium[4], induces apoptosis in cancer cells through cell cycle arrest and autophagy modulation[8], and mitigates allergic reactions by regulating histamine levels. While extensively studied preclinically for cardiovascular disease, cancer adjunct therapy/resistance reversal, neuroprotection (including Alzheimer's models), allergy/asthma management,[1][4][5][6] there are no approved pharmaceutical indications or major clinical trials confirming its efficacy for specific diseases.

Other names
peonol2'-hydroxy-4'-methoxyacetophenone
02

Targets

MAOA (Monoamine oxidase A)MAOB (Monoamine oxidase B)NF-κB

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