Drug intelligence / Profile preview

puerarin

Development stage
Phase 2
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Puerarin (Chinese name: 葛根素) is an isoflavone compound isolated from the root of the traditional Chinese medicinal plant Pueraria lobata (Kudzu). Chemically known as daidzein-8-C-glucoside (C21H20O9), it appears as a white to off-white crystalline powder and is slightly soluble in water but more soluble in organic solvents. Clinically used mainly in China as an injectable formulation for cardiovascular diseases such as coronary heart disease and angina pectoris[5][7][8], puerarin also finds use in treating hypertension, arrhythmia, myocardial infarction, ischemic cerebrovascular disease (stroke), retinal vascular obstruction, sudden deafness due to vascular causes[7][8], and complications of diabetes. Additional research suggests neuroprotective effects and potential benefits for liver injury and neurodegenerative diseases like Alzheimer's disease[5]. Mechanistically, puerarin acts primarily as a 5-HT2C receptor antagonist[1][3], modulates TGF-beta/Smad signaling pathways[1], exhibits antioxidant activity by upregulating related genes involved in cholesterol metabolism[5], improves microcirculation by dilating coronary and cerebral arteries[2], reduces myocardial oxygen consumption,[2] inhibits platelet aggregation,[2] and may have anti-inflammatory properties. Adverse reactions include fever (most common), allergic dermatitis or shock, laryngeal edema,[8] increased transaminase levels,[8] gastrointestinal bleeding,[8] hemolysis phenomenon,[8] or kidney damage; these typically resolve after discontinuation.

Brand names
PetongxinPeitongxinPuerxin
Other names
葛根素daidzein-8-C-glucosidedaidzein8-C-glucosidedaidzein 8-C-glucosidePuerarinePSYCHOSINEPUERARIN EXTRACTPuerainPUERARINPuerqarinDaidzeine
02

Targets

IL-6 (Interleukin 6)TNFA (Tumor necrosis factor alpha (soluble))ER (Estrogen receptor)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)

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