Drug intelligence / Profile preview

linarin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Linarin is a naturally occurring glycosylated flavonoid, specifically the 7-O-rutinoside of acacetin, found in various medicinal plants such as *Chrysanthemum indicum*, *Buddleja officinalis*, and *Mentha arvensis*. It is recognized for its diverse biological activities, including anti-inflammatory, anti-allergic, and antioxidant properties. Mechanistically, linarin suppresses the activation of the NF-κB and MAPK (including ERK, JNK, and p38) signaling pathways. This inhibition leads to a reduction in the secretion of proinflammatory cytokines such as IL-6, IL-8, and MCP-1. In the context of respiratory health, linarin has demonstrated the ability to reverse histamine-induced upregulation of Mucin 5AC (MUC5AC) and downregulation of Aquaporin 5 (AQP5) in human nasal and bronchial epithelial cells, suggesting its potential as a therapeutic agent for allergic rhinitis and asthma.

Other names
acacetin-7-O-rutinosideacacetin7-O-rutinosideacacetin 7-O-rutinosidebuddleoside
02

Targets

JNK (Mitogen-activated protein kinase kinase kinase family)MAPK3 (Mitogen-activated protein kinase 1)ETS2MsbA (ATP-dependent lipid A-core flippase)SUR1 (Sulfonylurea receptor 1)p38-MAPK (p38 mitogen-activated protein kinase)LptD

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