Drug intelligence / Profile preview

tangeretin

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

Overview

Tangeretin is a naturally occurring O-polymethoxylated flavone found primarily in the peels of citrus fruits such as tangerines and oranges. It is characterized by five methoxyl groups on its flavonoid backbone and is known for its hydrophobic properties and low water solubility[1][2][5]. Tangeretin exhibits a range of biological activities including antioxidant[7], anti-inflammatory[4], cholesterol-lowering (hypolipidemic)[2], neuroprotective[2], antiproliferative[3][7], antimetastatic[7], and anticancer effects across various cancer cell lines such as leukemia and colorectal cancer cells. Mechanistically it induces apoptosis via mitochondrial caspase-dependent pathways as well as ER-stress-mediated mechanisms; it also downregulates anti-apoptotic proteins like Mcl-1 and Bcl-xL in some models[3]. In animal studies it has shown to improve renal function and cognitive impairment through anti-inflammatory actions involving downregulation of NF-κB/TNF-α/iNOS signaling pathways[4]. Due to these properties tangeretin is used in research settings for its potential therapeutic applications in cancer prevention/treatment and neuroprotection. It is commercially available as a dietary supplement but not approved as a pharmaceutical drug.

Other names
tangeritinponkanetin4',5,6,7,8-pentamethoxyflavone5,6,7,8,4’-pentamethoxyflavone (VIII)Tangeritine
02

Targets

MMP9 (Matrix metalloproteinase-9)KEAP1 (Kelch-like ECH-associated protein 1)CHUK (IKKα)PIK3CA (Phosphoinositide 3-kinase alpha)

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