129$/KG
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Product Detailed Description
liposomal Dihydromyricetin 70% is a premium-grade dietary supplement ingredient delivering dihydromyricetin in an advanced liposomal delivery system. Dihydromyricetin (DHM), also known as ampelopsin, is a naturally occurring flavanonol belonging to the flavonoid subclass of polyphenols. It is chemically characterized by the molecular formula C₁₅H₁₂O₈ and a molecular weight of 320.25 g/mol. DHM is the most abundant bioactive component in vine tea (Ampelopsis grossedentata), a characteristic industrial cash crop in southern China that has been consumed for more than 600 years. Its content in Ampelopsis grossedentata is as high as 35%.
DHM exhibits diverse biological activities, including antioxidant and anti-inflammatory properties, alongside therapeutic potential for neurological and metabolic disorders. Particularly noteworthy are DHM's significant anti-alcohol properties. Research demonstrates that DHM functions as a negative allosteric modulator of GABA_A receptors, effectively reducing alcohol-induced loss of righting reflex, and accelerates alcohol metabolism by enhancing the activities of alcohol metabolic enzymes (ADH and ALDH) while mitigating liver steatosis and injury through activation of AMPK.
Conventional DHM presents fundamental bioavailability challenges. DHM has a remarkably low absolute bioavailability of only 4.02% in rats, primarily due to its poor water solubility, low intestinal permeability, and strong bitter taste. The compound is susceptible to degradation by gastric acid, and its use in medical practice is limited by physicochemical properties and pharmacokinetic characteristics.
Liposomal encapsulation provides three critical advantages:
1. Gastric Protection and Stability Enhancement — The phospholipid bilayer shields DHM from gastric acid degradation and enzymatic metabolism during digestive transit. In the DHM-Lipo-Rg3 formulation, metabolite profiling suggested that liposomal encapsulation protected against enzymatic degradation while enhancing dehydroxylation pathways. The liposomal system significantly enhanced DHM stability and effectively repaired liver damage, maintaining normal liver metabolic functions.
2. Enhanced Cellular Uptake and Superior Bioavailability — In situ single-pass intestinal perfusion demonstrated approximately two-fold enhancement in absorption parameters for DHM-Lipo-Rg3 versus free DHM. Pharmacokinetic studies revealed DHM-Lipo-Rg3 significantly improved bioavailability by 3.1-fold in males and 5.4-fold in females compared to conventional cholesterol-containing liposomes. A separate chitosan-modified DHM liposome (CDL) demonstrated 3.23-fold and 1.92-fold increases in the drug concentration–time curve compared to free DHM and unmodified liposomes, respectively, with 1.49-fold and 1.31-fold increases in Cmax.
3. Targeted Hepatic Delivery and Sustained Release — NIR fluorescence imaging confirmed that DHM liposomes target hepatic macrophages and polarize macrophages into an anti-inflammatory phenotype. The liposomal formulation demonstrated sustained releasing and hepatic targeting, effectively alleviating liver inflammation. Combined with the long-lasting sustained-release characteristic of liposomes, the formulation takes effect continuously for 8–12 hours, helping to quickly restore mental state without the after-effects of hangover or drowsiness.
High Purity — Standardized to ≥70% dihydromyricetin by HPLC, ensuring consistent active content.
Liposomal Enhancement — Phospholipid bilayer encapsulation achieves >95% encapsulation efficiency with particle size <90 nm, dramatically improving DHM bioavailability.
Superior Bioavailability — Liposomal delivery significantly improved bioavailability by 3.1-fold in males and 5.4-fold in females compared to conventional liposomal formulations in pharmacokinetic studies.
Targeted Liver Protection — Liposomes precisely deliver DHM to liver cells, accelerating alcohol metabolism, reducing acetaldehyde accumulation, and quickly alleviating discomfort such as headache, nausea, and fatigue after drinking.
Powerful Antioxidant Capacity — The antioxidant capacity of DHM exceeds that of vitamins C and E. Liposomal DHM eliminates free radicals and inhibits lipid peroxidation, effectively repairing fatty liver and drug-induced liver damage.
Alcohol Metabolism Support — DHM normalizes hepatic alcohol-metabolizing enzymes (ADH and ALDH), significantly increasing alcohol tolerance time and decreasing sober-up time in animal models.
Gastrointestinal-Liver Axis Synergy — Liposomal DHM moderately regulates intestinal microecology, inhibits harmful bacteria, nourishes beneficial bacteria, and reduces the damage of intestinal toxins to the liver through the “gastrointestinal-liver axis”.
Water-Dispersible and Taste-Masked — Liposomal encapsulation masks the natural bitterness of DHM, improving palatability for functional food and beverage applications.
Batch Traceability — Complete COA, HPLC chromatogram, and identity data provided for each batch.
Clinical studies and commercial products commonly recommend 300–900 mg of dihydromyricetin per day. A Phase I, dose-escalation study (NCT05623501) evaluated DHM in healthy volunteers using a purified form from a cGMP-compliant source, with cohort 1 receiving DHM in two doses of 300 mg as liquid suspension, and dose escalation planned to 900 mg. For general liver protection and antioxidant support, 300–600 mg daily is commonly used. For alcohol metabolism support, 300–600 mg taken before or after alcohol consumption is recommended. Liposomal formulations may allow for more efficient utilization of lower doses due to enhanced bioavailability. The continuous sustained-release characteristic of liposomes provides 8–12 hours of action, supporting rapid recovery without hangover after-effects.
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Bulk / Custom Orders: 2–3 weeks, depending on quantity and customization requirements.
Shipping Methods: International Express (FedEx, DHL, UPS), air freight, and sea freight.
Coverage: Worldwide shipping, including remote areas.
Dihydromyricetin Encyclopedia — Scientific Background
Dihydromyricetin (DHM), also known as ampelopsin, is a naturally occurring flavanonol belonging to the flavonoid subclass of polyphenols. It is chemically characterized by the molecular formula C₁₅H₁₂O₈ and a molecular weight of 320.25 g/mol. DHM is the most abundant bioactive component in vine tea (Ampelopsis grossedentata), a characteristic industrial cash crop in southern China. Its content in Ampelopsis grossedentata is as high as 35%, significantly higher than other bioactive substances in the plant.
| Property | Value |
|---|---|
| CAS No. | 27200-12-0 |
| Molecular Formula | C₁₅H₁₂O₈ |
| Molecular Weight | 320.25 g/mol |
| Synonyms | Ampelopsin, Ampeloptin, Dihydromyricetin |
| Appearance | Off-white to pale yellow crystalline powder |
| Solubility | Poorly soluble in water; soluble in ethanol and hot water |
| Source | Ampelopsis grossedentata (vine tea) tender stems and leaves |
Dihydromyricetin is extracted from vine tea (Ampelopsis grossedentata Hand.-Mazz.), a popular folk tea in southern China that has been consumed for more than 600 years. Vine tea is found in the cloud-covered, humid mountain shrubs and woods of southern China, including provinces such as Hunan, Hubei, Sichuan, and Yunnan. The tender stems and leaves of the plant are used for extraction, with an optimized extraction process achieving a DMY content of 22.09% in the extract.
DHM functions as a negative allosteric modulator of GABA_A receptors, effectively reducing alcohol-induced loss of righting reflex. Additionally, DHM accelerates alcohol metabolism by enhancing the activities of alcohol metabolic enzymes (ADH and ALDH) and mitigates liver steatosis and injury through activation of AMPK. In an acute alcohol intoxication mouse model, DHM-Lipo-Rg3 demonstrated superior therapeutic efficacy, significantly increasing alcohol tolerance time, decreasing sober-up time, and normalizing hepatic alcohol-metabolizing enzymes (ADH and ALDH).
The antioxidant activity and cellular metabolic protective effects of DHM may act via the AMP kinase (AMPK) and nicotinamide adenine dinucleotide (NAD+)-dependent Sirtuin (Sirt)-1 energy regulating pathway. DHM may represent a novel approach to counteract alcohol-induced liver damage and promote alcohol metabolism via changes in hepatocellular bioenergetics and mitochondrial biogenesis driven by the AMPK/Sirt-1/PGC-1α axis. liposomal DHM has been shown to alleviate liver inflammation through sustained releasing and hepatic targeting.
Network pharmacology and machine learning have confirmed that DHM is the core functional component of vine tea with anti-inflammatory activity. Molecular docking and in vitro cell experiments confirmed that DMY could inhibit the expression of Interleukin-1β (IL-1β), Tumor necrosis factor-α (TNF-α), etc. by regulating Mitogen-activated protein kinase (MAPK) and Nuclear factor kappa-B (NF-κB) pathways. Western blotting suggested that chitosan-modified DHM liposomes could alleviate liver injury by modulating inflammatory factors and the transforming growth factor-β1/Smad2/Smad3 signaling pathway.
The antioxidant capacity of DHM exceeds that of vitamins C and E. Liposomal DHM eliminates free radicals and inhibits lipid peroxidation, enhancing stability and effectively repairing fatty liver and drug-induced liver damage, maintaining normal liver metabolic functions. The CDL formulation exhibited superior antioxidant capacity and stability.
DHM liposomes target hepatic macrophages and polarize macrophages into an anti-inflammatory phenotype. The SIRT3/HIF-1α signaling pathway could be the major mechanism of DHM-motivated macrophage polarization, providing new insights into the regional immune effect of DHM against inflammation.
Despite its broad pharmacological potential, DHM presents significant formulation challenges. The compound has a remarkably low absolute bioavailability of only 4.02% in rats. The primary reasons include poor water solubility, low intestinal permeability, and strong bitter taste. Additionally, DHM is susceptible to degradation by gastric acid, further limiting its clinical utility.
Previous approaches to improve DHM bioavailability through solid dispersions, nanocapsules, microemulsions, co-crystallization, cyclodextrin complexes, and phospholipid complexes have improved some drawbacks but still face challenges such as poor stability, recrystallization, and inhomogeneous release.
Liposomal encapsulation of DHM provides a fundamentally different delivery mechanism from conventional forms. The phospholipid bilayer surrounds the DHM molecule, forming a shield that protects it from gastric acid degradation and enzymatic metabolism. This delivery system:
Protects DHM from gastric acid degradation and enzymatic breakdown
Enhances intestinal absorption through lipid-mediated pathways
Provides sustained release with prolonged circulation time
Enables targeted hepatic delivery and hepatic macrophage targeting
The DHM-Lipo-Rg3 formulation incorporating 20(S)-ginsenoside Rg3 as a cholesterol substitute exhibited superior physicochemical characteristics including smaller particle size (<90 nm), lower polydispersity index (∼0.13), and higher encapsulation efficiency (>95%) compared to conventional cholesterol-containing liposomes. In situ single-pass intestinal perfusion demonstrated approximately two-fold enhancement in absorption parameters versus free DHM.
A first-in-human Phase I open-label, dose-escalation study (NCT05623501) is designed to assess the safety, pharmacokinetics, and maximum tolerated dose of DHM among healthy volunteers using a purified form from a cGMP-compliant source. Cohort 1 consists of three healthy volunteers who will receive DHM in two doses of 300 mg as liquid suspension, with dose escalation to 900 mg planned. The study is based on preclinical data suggesting the potential of DHM as a novel therapeutic agent in alcohol-related diseases.
In an acute alcohol intoxication mouse model, DHM-Lipo-Rg3 demonstrated superior therapeutic efficacy, significantly increasing alcohol tolerance time, decreasing sober-up time, and normalizing hepatic alcohol-metabolizing enzymes (ADH and ALDH). Additionally, DHM-Lipo-Rg3 effectively counteracted alcohol-induced oxidative stress by enhancing SOD activity and reducing MDA levels, while significantly lowering plasma liver enzymes (ALT, AST).
A study published in Frontiers in Pharmacology (2022) investigated DHM-encapsulated liposomes for their therapeutic potential in a hepatic inflammatory injury model induced by exhaustive exercise. Liposome encapsulation enhanced DHM bioavailability, and DHM liposome could alleviate liver inflammation more effectively. Moreover, DHM liposome targeted hepatic macrophages and polarized macrophages into an anti-inflammatory phenotype through the SIRT3/HIF-1α signaling pathway.
A study published in International Journal of Biological Macromolecules investigated chitosan-modified DHM liposomes (CDL) for liver injury in mice suffering from diabetes mellitus. Pharmacokinetic analyses revealed a 3.23- and 1.92-fold increase in the drug concentration–time curve (953.60 ± 122.55 ng/mL/h) in the CDL-treated group as opposed to the DHM-treated group (295.15 ± 25.53 ng/mL/h) and DL-treated group (495.31 ± 65.21 ng/mL/h). The maximum drug concentration in blood (Cmax) showed a 1.49- and 1.31-fold increase in the CDL group compared with DHM and DL groups.
Dihydromyricetin is a bioactive flavonoid from an edible plant (Ampelopsis grossedentata) that has been consumed as a folk tea in China for more than 600 years. DHM is marketed as a dietary supplement in the United States and is not regulated by the Food and Drug Administration (FDA) as a drug. The Phase I dose-escalation study is designed to establish the safety and maximum tolerated dose in humans. Preclinical studies have demonstrated that DHM exhibits hepatoprotective effects without serious adverse effects reported. Testing protocols must adhere to international standards including USP, European Pharmacopoeia, and FAO/WHO Codex Alimentarius. Formulators should verify local regulatory requirements prior to market entry.
This product is intended for research, nutraceutical, and functional food applications. Not intended to diagnose, treat, cure, or prevent any disease.
129$/KG
109$/KG
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