Drug intelligence / Profile preview

nobiletin

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Nobiletin is a polymethoxylated flavonoid naturally found in the peel of citrus fruits, notably tangerines and sweet oranges. Structurally, it is a hexamethoxyflavone (C21H22O8). Nobiletin exhibits a broad range of biological activities in vitro and in vivo, including antioxidant, anti-inflammatory, antitumor, antidiabetic, neuroprotective, and cardioprotective effects. Its main mechanisms of action involve modulation of multiple molecular signaling pathways such as nuclear factor erythroid 2-related factor 2 (Nrf2), nuclear factor kappa B (NF-κB), AMP-activated protein kinase (AMPK), peroxisome proliferator-activated receptor alpha (PPAR-α), extracellular signal-regulated kinase (ERK), protein kinase B (AKT), toll-like receptor 4 (TLR4), and transcription factor EB (TFEB)[1][3][4][9][7]. Preclinical studies suggest roles in improving liver function, insulin resistance, glucose uptake, reducing inflammation and oxidative stress, remodeling gut microflora, and supporting neuronal survival. Nobiletin is being investigated mainly as a dietary supplement ingredient, although combination clinical studies (e.g., with tangeretin) have been conducted for conditions such as nocturia[6]. High-quality clinical trial evidence is lacking for any therapeutic indication[4].

Other names
hexamethoxyflavone5,6,7,8,3′,4′-hexamethoxyflavonebiletinChuanpi glycosidesNobiletin, 98%Chuanchenpi SuNobiletin (6CI)Nobiletin, >=98%2-(3,4-dimethoxyphenyl)-5,6,7,8-tetramethoxychromen-4-one3′,4′,5,6,7,8-hexamethoxyflavone2-(3,4-dimethoxyphenyl)-5,6,7,8-tetramethoxy-4H-chromen-4-one478-01-3[2][5][8]
02

Targets

ABCB1 (P-glycoprotein)RORA (Retinoic acid-related orphan receptor alpha)RORC (Retinoic acid receptor-related orphan receptor gamma)AMPK (Adenosine monophosphate–activated protein kinase)BACE1 (Beta-site APP-cleaving enzyme 1)MAPK3 (Mitogen-activated protein kinase 1)CHUK (IKKα)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)NF-κBPPARA (Peroxisome proliferator-activated receptor alpha)AKT (RAC-alpha serine/threonine-protein kinase)TLR4 (Toll-like receptor 4)TFEB (Transcription factor EB)CREB (Cyclic AMP response element-binding protein)

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