Drug intelligence / Profile preview

isorhamnetin

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Isorhamnetin is a naturally occurring flavonol aglycone and a methylated metabolite of quercetin. It is found in various plants such as Hippophae rhamnoides (sea buckthorn) and Ginkgo biloba. Isorhamnetin exhibits multiple pharmacological activities including antioxidant, anti-inflammatory, anti-tumor, anti-viral, and organ-protective effects. Its mechanisms of action involve modulation of several signaling pathways such as Phosphatidylinositol 3-kinase/Protein kinase B (Akt)/mammalian target of rapamycin (mTOR), Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), Mitogen-activated protein kinase/extracellular signal-regulated kinase (MAPK/ERK1/2), and Nuclear factor erythroid-derived 2-like 2 (Nrf2)/Heme oxygenase-1 (HO-1). Isorhamnetin has been shown to inhibit cell proliferation and induce apoptosis in various cancer cell lines by targeting these pathways. It also demonstrates protective effects against cardiovascular diseases by reducing oxidative stress and inflammation[3][4][6][8]. The compound inhibits the expression of CYP1B1 enzyme and can modulate endothelial function through its antioxidant properties[4][5]. While widely studied for its therapeutic potential in preclinical models for conditions like cancer (colon cancer, gastric cancer), cardiovascular disease (atherosclerosis), diabetes-related complications, neurodegenerative injury protection, obesity prevention and more[3][6], it has not been approved as a pharmaceutical drug.

Other names
3'-methoxy-3,4',5,7-tetrahydroxyflavoneisorhamnetine
02

Targets

CYP1B1 (Cytochrome P450 1B1)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)NF-κBAKT (RAC-alpha serine/threonine-protein kinase)ATM (Ataxia telangiectasia mutated protein)VEGFR (VEGFR family)

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