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dihydromyricetin

Development stage
Phase 2
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Dihydromyricetin, also known as ampelopsin or DHM, is a naturally occurring flavanonol (a type of flavonoid) found in several plant species, most notably Hovenia dulcis and various Ampelopsis species. It has been used in traditional Japanese, Chinese, and Korean medicine for the treatment of fever, parasitic infections, liver diseases, and as a hangover remedy[1][5]. Dihydromyricetin exhibits multiple pharmacological effects including anti-inflammatory, antioxidant, antiviral, anti-tumor activities and metabolic regulation[7]. Mechanistically, it acts on several molecular pathways: - It modulates Gamma-aminobutyric acid receptor subunit alpha (GABA-A receptor) at the benzodiazepine site to counteract alcohol intoxication and dependence[3]. - It activates the Nuclear factor erythroid 2-related factor 2 (Nrf2) signaling pathway to upregulate antioxidant enzymes such as HO-1 and NQO1[7]. - It inhibits inflammatory pathways including TLR4/NF-κB and NOD-like receptor family pyrin domain containing 3 inflammasome (NLRP3 inflammasome)[7]. - In cancer models (notably hepatocellular carcinoma), it induces apoptosis via Protein kinase B/Akt pathway down-regulation and cell cycle arrest through Chk2-mediated mechanisms[6]. Dihydromyricetin is under clinical investigation for its effects on glycemic control in type 2 diabetes mellitus (NCT03606694)[2], has shown promise in animal models for treating alcohol use disorder by reducing intoxication symptoms and withdrawal signs[3], improves glucose/lipid metabolism in nonalcoholic fatty liver disease patients[5], protects against drug-induced liver injury by enhancing antioxidant defenses while suppressing inflammation/apoptosis pathways[7][8], and may have potential applications against hepatocellular carcinoma growth/metastasis through multiple pro-apoptotic mechanisms[6].

Brand names
SMARTO ONE
Other names
ampelopsin
02

Targets

GABRR (GABA-A receptor subunit rho)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)

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