Drug intelligence / Profile preview

cirsimaritin

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Cirsimaritin is a naturally occurring dimethoxy flavone, specifically a 4',5-dihydroxy-6,7-dimethoxyflavone, found in various plants including Artemisia judaica, Cirsium japonicum, Lithocarpus dealbatus, and others. It has shown a range of pharmacological activities such as antidiabetic, antioxidant, anti-inflammatory, antiproliferative, antimicrobial, antispasmodic, and anticancer effects. In preclinical studies, cirsimaritin reduced blood glucose and insulin levels, improved insulin resistance, modulated AMPK-GLUT4/GLUT2 pathways, and lowered oxidative stress and pro-inflammatory markers[1][4]. Mechanistically, it can inhibit the activity or expression of several signaling pathways, including NF-κB, and interfere with enzymes such as dipeptidyl peptidase-4 (DPP-4). It also exhibits weak binding to the benzodiazepine site of GABAA receptors, displaying some anxiolytic and antidepressant activities[11]. Its anticancer activity is linked to inducing apoptosis mainly via intrinsic caspase pathways, mitochondrial membrane potential changes, and suppression of signaling such as Akt and mTOR[4]. Cirsimaritin remains an experimental compound and is not approved for clinical pharmaceutical use; it is of interest for further development as a drug lead or dietary supplement candidate.

Other names
skrofuleinscrophuleincircimaritin6-methoxygenkwanin4',5-dihydroxy-6,7-dimethoxyflavone5-hydroxy-2-(4-hydroxyphenyl)-6,7-dimethoxy-4H-1-benzopyran-4-one7-o-methylated flavonoid
02

Targets

PRKAA1 (AMP-activated protein kinase alpha catalytic subunit isoform alpha-1)DPP-4 (Dipeptidyl Peptidase-IV)α-MSH (Alpha-melanocyte-stimulating hormone)SLC2A4 (Solute carrier family 2 facilitated glucose transporter member 4)

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