Ampelopsis

Other Names

Ampelopsis arborea (L.) KoehneAmpelopsis bipinnata Michx.Ampelopsis brevipedunculata (Maxim.) Trautv.Ampelopsis brevipedunculata var. maximowiczii (Regel) RehderAmpelopsis cantoniensis (Hook. & Arn.) K.KochAmpelopsis citrulloides LebasAmpelopsis cordata Michx.Ampelopsis glandulosa (Wall.) Momiy.Ampelopsis glandulosa f. citrulloides (Lebas) Momiy.Ampelopsis glandulosa f. elegans (K.Koch) Momiy.Ampelopsis glandulosa var. brevipedunculata (Maxim.) Momiy.Ampelopsis glandulosa var. heterophylla (Thunb.) Momiy.Ampelopsis glandulosa var. kulingensis (Rehder) Momiy.Ampelopsis grossedentata (Hand.-Mazz.) W.T.WangAmpelopsis heterophylla (Thunb.) Siebold & Zucc.Ampelopsis heterophylla subvar. sieboldii Planch.Ampelopsis heterophylla var. amurensis Planch.Ampelopsis heterophylla var. brevipedunculata C.L. LiAmpelopsis heterophylla var. integra Siebold & Zucc.Ampelopsis heterophylla var. lavalleei Planch.Ampelopsis japonica (Thunb.) MakinoAmpelopsis japonica C.K.Schneid.Ampelopsis leeoides (Maxim.) Planch.Ampelopsis maximowiczii (Regel) BarkalovAmpelopsis Michx.Ampelopsis mirabilis Diels & GilgAmpelopsis napiformis CarrièreAmpelopsis regeliana DippelAmpelopsis serjaniifolia BungeAmpelopsis tuberosa CarrièreAmur peppervineBai LianBuckvineCissus brevipedunculata Maxim.Cissus bryoniifolia RegelCissus serjaniaefolia WalpersCow ItchCreeperDuan Wu ChaFalse grapeHeart-leaf peppervineHeartleaf peppervineJapanese ampelopsisMao Yan MeiMei ChaMoyeamNekemias arborea (L.) J.Wen & BogganNekemias cantoniensis (Hook. & Arn.) J.Wen & Z.L.NieNekemias grossedentata (Hand.-Mazz.) J.Wen & Z.L.NieNekemias Raf.Paullinia japonica Thunb.PeppervinePorcelain AmpelopsisPorcelain berryPorcelain vinePorcelainberryRaccoon-grapeRadix AmpelopsisRattan teaTeng ChaTochaVine teaVitis brevipedunculata (Maxim.) DippelVitis heterophylla Thunb.Vitis leeoides Maxim.Vitis serjaniifolia (Reg.) Maxim.Wild grape

Synopsis

Ampelopsis: A Comprehensive Reference

1. Identity and Botanical Classification

Genus and Species

Ampelopsis is a genus of deciduous climbing vines in the family Vitaceae (the grape family). The genus Ampelopsis A.Rich. ex Michx. comprises perennial woody vines with a global distribution of over 30 species. Approximately 17 species and varieties are distributed in China, most of which are endemic to China and mainly distributed in hillside shrubs and forests in the southwest, south, and northeast of the country.

Of the many species in the genus, research attention has concentrated on three in particular:

Ampelopsis grossedentata (Hand.-Mazz.) W.T.Wang — by far the most extensively studied species in the modern scientific literature; commonly known as vine tea, Teng Cha, Meicha, or Tocha in Chinese.
Ampelopsis japonica (Thunb.) Makino — a species with a long official pharmacopeial history in China, primarily valued for its roots.
Ampelopsis brevipedunculata (Maxim.) Trautv. — sometimes called porcelain berry, used in folk medicine across East Asia.

Geographic Distribution

Ampelopsis grossedentata is mainly distributed in Chinese provinces and areas south of the Yangtze River Basin, mostly concentrated or scattered in mountainous bushes or woods with high humidity. A. grossedentata, native to southern China, is renowned for its therapeutic and nutritional benefits, often called the "king of flavonoids" due to its high dihydromyricetin content.

Plant Morphology

The cymes arise from leaf axils or branch apices opposite the leaves. The calyx is discoid and 2.2 mm in diameter. The plants have five oblong-shaped petals and five stamens, and the flower disc is shallowly cup-shaped. The fruit is a berry, which is nearly spherical and purple-black when mature, with a diameter of 3–6 mm. The flowering period is from June to September, and the fruiting period is from July to November.

Common Preparations and Forms

The dried stems, leaves, and shoot tips — known as "vine tea" — are consumed as a health beverage and traditional remedy. Scientific investigations have isolated compounds from the dried stems and leaves of A. grossedentata. Modern commercial forms include standardized extracts (standardized to dihydromyricetin content), encapsulated powders, and ready-to-brew vine tea products. Common products on the market include various A. grossedentata drinks and boxed products refined from the tender stems and leaves.

Ampelopsis japonica is used primarily as a root preparation. It has been officially included in the Chinese Pharmacopoeia since 1985, with its inclusion continuing through the latest 2020 edition.

2. Traditional and Historical Use

Ampelopsis grossedentata — Vine Tea

A. grossedentata has a long history of use in China as an ancient medicinal and food homologous plant. Chinese folk use of vine tea dates back approximately 600 years, with the Zhuang and Yao nationalities being the first to utilize it, after which it was extensively used by the Tujia, Lahu, Dong, Jino, and Hakka nationalities.

The plant was first recorded in the Classic of Tea, noted for its functions of clearing heat and detoxifying, relieving cough and phlegm, promoting blood circulation, protecting the liver, and dispelling rheumatism. Ancient texts such as Ying Shan Zheng Yao and Cao Mu Bian Fang subsequently recorded it and its effects.

The usage of A. grossedentata was recorded in the Chinese Materia Medica, mostly for internal use, using 15–30 g of the plant in decoction or tea making.

Traditionally, A. grossedentata is used as tea among the Yao people of China to treat pyretic fever and cough, pain in the pharynx and larynx, and jaundice hepatitis. It is also used for nephritis, hepatitis, halitosis, and in a preventive capacity for various conditions. As a medicinal plant, A. grossedentata has been used for centuries for various therapeutic purposes, including to prevent and treat symptoms such as colds, fevers, sore throats, and toothaches.

A. grossedentata has been used as a herbal medicine for thousands of years in China. It was regarded as having the effects of "regulating Zhong, replenishing Qi and circulating blood and Qi" in the Compendium of Materia Medica.

Ampelopsis japonica

Ampelopsis japonica has a long history of medicinal use, with its therapeutic applications documented in numerous ancient texts, including the Shen Nong Ben Cao Jing (神农本草经), one of the earliest pharmacopeias of traditional Chinese medicine, dating to the Eastern Han Dynasty, where it was recorded for its detoxifying, heat-clearing, and analgesic properties. The efficacy and application were further supplemented and elaborated in classic works such as Ben Cao Gang Mu. Ampelopsis japonica (Thunb.) Makino has traditionally been utilized in the treatment of various kidney diseases.

Ampelopsis brevipedunculata

Ampelopsis brevipedunculata has been used as an herbal folk medicine to treat liver diseases and inflammation in Asia.

3. Key Chemical Constituents and Active Compounds

Overview of Phytochemistry

Approximately 57 chemical components of A. grossedentata have been identified, including flavonoids, phenols, steroids and terpenoids, volatile components, and other chemical compounds. Current research has identified the primary phytochemical constituents of A. grossedentata as flavonoids, terpenoids, and polyphenolic compounds.

Dihydromyricetin (DHM) / Ampelopsin

The single most important and most studied constituent of A. grossedentata is dihydromyricetin (DHM), also known as ampelopsin. Dihydromyricetin (chemically defined as 3,5,7,3′,4′,5′-hexahydroxy-2,3-dihydroflavonol), also known as ampelopsin, is the primary active compound found in Ampelopsis grossedentata (Hand.-Mazz.) W.T.Wang (family Vitaceae).

DHM is a flavonoid extracted from the young stems and leaves of Ampelopsis grossedentata. It is a polyphenolic hydroxy dihydroflavanol with a molecular weight of 320.25 g/mol and a molecular formula of C₁₅H₁₂O₈.

DHM is a major bioactive flavonoid isolated from the traditional Chinese medicinal plant Ampelopsis grossedentata, and is also found in various plant-based foods such as grapes and red bayberry. DMY was first isolated from Ampelopsis meliaefolia by Kotake and Kubota in 1940, and was later reported as a major bioactive component in A. grossedentata.

The content of DHM can be as high as 30–40% (w/w) in A. grossedentata. This exceptional concentration makes it one of the richest known natural sources of this compound.

Other Flavonoids and Polyphenols in A. grossedentata

High levels of flavonoids, especially dihydromyricetin, myricetin, and myricitrin, are present in vine tea. In addition, the plant contains taxifolin (dihydroquercetin), epigallocatechin, quercetin, and astilbin. Astilbin has shown neuroprotective properties by enhancing central nervous system cell function through multiple mechanisms.

Constituents of Ampelopsis japonica

Modern pharmacological research indicates that components such as physcion, chrysophanol, fumaric acid, and gallic acid found in Ampelopsis japonica exhibit antibacterial and anti-inflammatory effects. Additionally, the polysaccharide components demonstrate significant immune-enhancing effects, while the polyphenolic components show notable antioxidant properties.

Three glycosylated stilbenes, two anthraquinones, one lignan, five tannins, two amino acids, and one auronol have been isolated from the root of Ampelopsis japonica.

Stilbene Oligomers in Ampelopsis brevipedunculata

The methanol extract of the roots of Ampelopsis brevipedunculata var. hancei exhibited marked protective activity against carbon tetrachloride and d-galactosamine-induced liver damage in primary cultured rat hepatocytes. The extract yielded four novel oxidative oligostilbenes — ampelopsins D, E, H, and cis-ampelopsin E — in addition to known compounds including (−)-epicatechin, pallidol, miyabenol C, piceid, cis-piceid, and resveratroloside. Among them, ampelopsin E and cis-ampelopsin E showed antihepatotoxic activity.

The cytotoxicities and anti-inflammatory activities of five resveratrol derivatives — vitisinol A, (+)-ε-viniferin, (+)-vitisin A, (−)-vitisin B, and (+)-hopeaphenol — have been isolated from Ampelopsis brevipedunculata var. hancei.

4. Mechanisms of Action

Anti-Inflammatory Mechanisms

Ampelopsis grossedentata extract reduced LPS/IFNγ-induced M1-like macrophage polarization, resulting in a significant decrease in the expression of the pro-inflammatory cytokines TNF-α and IL-6, along with a decrease in the percentage of M1 macrophages. Simultaneously, a significant decrease in NF-κB p65 phosphorylation and in the expression of inflammasome genes (NLRP3, IL-1β, and Caspase 1) was observed.

Water extract of A. grossedentata effectively alleviates oxidative stress in animal models by reducing the levels of pro-inflammatory cytokines and increasing the antioxidant enzyme activity in the liver, as well as by activating the Nrf2 signaling pathway in the duodenum.

Antioxidant and Nrf2/Keap1 Pathway

The water extract of A. grossedentata can regulate gut microbiota, promoting the growth of beneficial bacteria and inhibiting harmful microbes. These findings suggest it may serve as a valuable dietary supplement for addressing oxidative stress and inflammation via the Nrf2/Keap1 pathway.

Metabolic and Glucose-Regulatory Mechanisms

The positive results seen in studies on dihydromyricetin consumption and supplementation may be attributed to mechanisms such as the inhibition of carbohydrate digestion, the inhibition of glucose transport, and its action as a GLP-1 receptor agonist.

Total flavonoids of A. grossedentata decreased the concentration of T-β-MCA and T-α-MCA via increasing bile salt hydrolase (BSH)-active bacteria, thereby promoting the enterohepatic FXR-FGF15 axis, which depresses excessive bile acid synthesis. This supplement activated the ileum FXR-FGF15 axis, thereby inhibiting liver gluconeogenesis by downregulating the CREB-PGC-1α pathway.

AMPK Activation and Lipid Metabolism

The underlying mechanism of DHM's anti-adiposity effects involved the activation of adenosine 5′-monophosphate-activated protein kinase (AMPK) and its downstream targets, including CPT1A, as well as acetyl CoA carboxylase (ACC). These findings suggest that A. grossedentata is a valuable plant for adjusting lipid metabolism.

Hepatoprotective Mechanisms

Ampelopsis grossedentata extract was shown to possess hepatoprotective properties against ethanol-induced liver damage involving antioxidative, anti-inflammatory, and anti-necroptosis effects. The TLR4/NF-κB/MLKL pathway has been specifically identified as a target in alcoholic liver disease.

Anti-Fibrotic Mechanisms

Dihydromyricetin, a principal bioactive flavonoid derived from Ampelopsis grossedentata, exhibits diverse pharmacological activities including anti-inflammatory, antioxidant, and autophagy-modulating effects, which contribute to anti-fibrotic activity across various organ systems.

Antioxidant Properties in Gut Microbiota

Administration of total flavonoids from Ampelopsis grossedentata to NAFLD model mice significantly reduced serum levels of IL-6 and TNF-α, ameliorated hepatic steatosis, decreased the Firmicutes/Bacteroidetes ratio (associated with obesity and metabolic disorders), and increased the abundance of probiotics, indicating that their beneficial effects on NAFLD are mediated through modulation of the gut microbiota and the "gut-liver axis."

Alpha-Glucosidase Inhibition

All isolates from A. grossedentata stems and leaves were assessed for α-glucosidase inhibitory activity. One new flavonoid compound exhibited effective inhibitory activity against α-glucosidase, with an IC₅₀ value of 0.21 μM.

Uric Acid–Lowering Mechanisms

Ampelopsis japonica (Thunb.) Makino has traditionally been utilized in the treatment of various kidney diseases; its specific anti-hyperuricemic effects involve downregulation of the renal uric acid transporters URAT1 and GLUT9, and alleviation of inflammation through the TLR4/NF-κB pathway.

ACE Inhibition

Among resveratrol-type stilbene compounds isolated from A. brevipedunculata, (+)-hopeaphenol and (+)-vitisin A showed the lowest IC₅₀ values (~1.5 μM) toward angiotensin-converting enzyme (ACE), suggesting the antihypertension effect of the bark extract may be mainly contributed by these two compounds.

5. Scientific Evidence by Area of Use

5.1 Glycemic Control and Type 2 Diabetes

Human/Clinical Evidence (Moderate):

The strongest clinical evidence for Ampelopsis grossedentata concerns glycemic control. Eighty participants with type 2 diabetes mellitus (T2DM) were randomly assigned in a double-blind, randomized clinical trial to the APL group (n=40, 10 g of A. grossedentata daily, containing 970 mg of dihydromyricetin) or to a placebo group (n=40, 10 g of APL daily with dihydromyricetin deleted) for 1 month. Seventy subjects completed the trial. Compared with the placebo group, the levels of fasting plasma glucose, glycated albumin, cystatin C, and retinol binding protein-4 significantly decreased (all p < 0.05).

One-month supplementation with A. grossedentata (APL) obviously improved glycemic control and parameters of renal function in adults with T2DM, suggesting a potential role for APL in the prevention and treatment of T2DM.

In a double-blind clinical trial, dihydromyricetin — the main active ingredient of Ampelopsis grossedentata — improved glucose and lipid metabolism and showed anti-inflammatory effects in patients with nonalcoholic fatty liver disease (NAFLD).

Limitations: The pivotal T2DM trial lasted only one month, had a modest sample size (n=70 completers), and was conducted at a single center. Long-term efficacy and safety data in humans are lacking. The 2020 Alzheimer's Drug Discovery Foundation cognitive vitality report notes that the therapeutic dose has not been formally established, and clinical trials conducted to date include type 2 diabetes (n=77) and NAFLD (n=60).

5.2 Liver Disease (NAFLD, Alcoholic Liver Disease, Hepatitis)

Preclinical Evidence (Strong); Human Evidence (Limited)

Extracts of A. grossedentata broadly display notable antioxidant, anti-inflammatory, and hypoglycemic properties. Studies have shown that the extract offers significant protection against liver diseases including alcoholic liver disease (ALD), NAFLD, and acute liver injury.

In animal models, supplementation with A. grossedentata extract and its primary compound DHM attenuated the high-fat-induced increase in body weight, liver lipid deposition, serum triglycerides and total cholesterol levels, and normalized endogenous metabolite concentrations.

In a preclinical alcoholic liver disease study, investigators explored the protective effects of A. grossedentata extract (AGE) against chronic alcohol-induced hepatic injury. UPLC-Q/TOF-MS analysis and network pharmacology were used to identify constituents and elucidate potential mechanisms, and C57BL/6 mice were administered AGE (150 and 300 mg/kg/d) and silymarin (200 mg/kg) for 7 weeks.

One randomized controlled trial in NAFLD patients (n=60) examined dihydromyricetin at a dose of 600 mg/d in patients with NAFLD, resulting in significant improvements in glucose and lipid metabolism, along with enhanced insulin sensitivity.

Limitations: The majority of hepatoprotective data derive from animal and cell models. Human clinical trials are few, small, and short in duration. Regulatory bodies have not assessed these claims.

5.3 Lipid Metabolism and Obesity

Preclinical Evidence (Moderate); Human Evidence (Very Limited)

Results showed that A. grossedentata extract and ampelopsin significantly suppressed increases in the weights of body, livers, and abdominal fat, and also up-regulated the expression of carnitine palmitoyltransferase 1A in high-fat-diet-fed mice.

After treatment with total flavonoids extracted from A. grossedentata (AGT) for 6 weeks, the body weight, liver index, fasting blood glucose, OGTT-AUC, and serum lipid levels were reduced, and pathological injuries of the liver improved significantly in Zucker diabetic fatty (ZDF) rats. Total flavonoids could ameliorate glycolipid metabolism disorder effectively in ZDF rats.

Limitations: Evidence for lipid-lowering effects in humans specifically attributable to Ampelopsis preparations remains largely indirect; no dedicated, well-powered human lipid trials were identified.

5.4 Antioxidant and Anti-Inflammatory Activity

In Vitro and Animal Evidence (Strong); Human Evidence (Indirect)

In vitro studies have shown that the flavones of A. grossedentata possess therapeutic properties such as anti-bacterial, anti-inflammatory, anti-oxidant, immunity-enhancing, glucose and lipid metabolism-regulating, hepatoprotective, and anti-tumor activities.

In preclinical animal models, DHM shows a variety of beneficial anti-aging properties by reducing inflammation, oxidative stress, and lipidemia, as well as regulating energy metabolism and promoting autophagy. These effects are primarily derived from its ability to activate sirtuins.

5.5 Neuroprotection

Preclinical Evidence (Preliminary); No Established Human Evidence

DMY showed neuroprotective activity against Alzheimer's disease and Parkinson's disease, as well as beneficial effects on alcohol addiction and depression. These findings are derived from preclinical (animal and cell-based) models and have not been replicated in registered human clinical trials as of the current evidence base.

A. grossedentata and its flavonoids may be therapeutic candidates as neuroprotective agents to attenuate the progression of Alzheimer's disease and other neurodegenerative diseases. Research has verified that extractions of A. grossedentata inhibit apoptosis of PC12 cells induced by Aβ25-35 by blocking the accumulation of reactive oxygen species.

DHM has a wide range of positive effects, including anti-oxidative, anti-inflammatory, and neuroprotective properties, and has been shown to cause motor and memory improvements in preclinical models.

Limitations: All neuroprotection evidence to date is from cell and animal experiments. No human clinical trials have evaluated Ampelopsis or DHM for neurological outcomes.

5.6 Antibacterial Activity

In Vitro Evidence (Moderate); No Human Evidence

DHM exhibits antibacterial activity on five types of food-borne bacteria: Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Salmonella paratyphi, and Pseudomonas aeruginosa. The antibacterial activities of DHM against bacteria are extremely sensitive to pH, thermal processing, and metal ions. The morphology of tested bacteria is changed and damaged more seriously with increased DHM exposure time.

5.7 Oncology (Anticancer)

Preclinical Evidence (Emerging); No Clinical Evidence

DHM has been reviewed for its different mechanisms of action alone or in combination with other drugs against a variety of cancers. It is a natural flavonoid compound extracted from Ampelopsis grossedentata that has been used for centuries in traditional Chinese medicine.

The Chinese herbal ingredient DHM exhibited anti-tumor effects on multiple myeloma by inhibiting cell viability, migration and invasion, epithelial-mesenchymal transition (EMT), and tumor growth, as well as promoting cell apoptosis, in preclinical models.

Limitations: All anticancer data are from in vitro cell studies or animal models. No human oncology trials have been registered or reported for Ampelopsis preparations.

5.8 Hyperuricemia and Gout

Animal Evidence (Preliminary); No Human Evidence

Ampelopsis japonica extract's uric acid–lowering effects and underlying mechanisms have been established in a hyperuricemic animal model using metabolomic analysis and network pharmacology.

5.9 Bone Health

Preclinical Evidence (Preliminary); No Human Evidence

Ampelopsis brevipedunculata extract (ABE) was investigated for anti-osteoclastogenic activity. In this preclinical study, ABE inhibited receptor activator of NF-κB ligand (RANKL)-induced osteoclast differentiation, the formation of filamentous actin rings, and the bone-resorbing activity of mature osteoclasts.

6. Body Systems and Health Areas

Based on the available peer-reviewed literature, Ampelopsis preparations have been investigated in relation to the following body systems and health domains:

Endocrine / Metabolic: Blood glucose regulation, insulin sensitivity, type 2 diabetes, NAFLD, lipid homeostasis, obesity.
Hepatic: Protection against alcoholic liver disease, NAFLD, toxic hepatitis, and drug-induced liver injury; anti-fibrotic effects.
Immune / Inflammatory: Macrophage polarization, cytokine suppression, NF-κB and NLRP3 inflammasome modulation, antioxidant defense via Nrf2/Keap1.
Neurological: Neuroprotection against Alzheimer's and Parkinson's disease-related pathology in preclinical models; anti-addiction (alcohol); motor and cognitive function (preclinical only).
Cardiovascular: Blood pressure regulation via ACE inhibition (stilbene fractions of A. brevipedunculata); cardiac ischemia-reperfusion protection (preclinical).
Renal: Improved renal function parameters in T2DM patients; uric acid reduction in animal models.
Gastrointestinal / Microbiome: Modulation of gut microbiota composition, prebiotic-like effects, lifespan extension in Drosophila models.
Musculoskeletal: Inhibition of osteoclastogenesis (preclinical); skeletal muscle insulin sensitivity.
Antimicrobial: Activity against food-borne pathogens in vitro.
Oncology: Antiproliferative and pro-apoptotic activity in cancer cell lines (in vitro only).

7. Dosage Forms and Reported Dosages

The following dosages are reported as used in specific cited studies; they do not represent established therapeutic recommendations:

Type 2 Diabetes Clinical Trial (Ran et al., 2019, Eur J Clin Nutr): 10 g of A. grossedentata (APL) daily, standardized to contain 970 mg of dihydromyricetin, for 1 month.
NAFLD Clinical Trial (Chen et al., 2015, Pharmacol Res): 600 mg/d of dihydromyricetin.
Traditional Decoction/Tea: 15–30 g of A. grossedentata per day in decoction or tea making, as recorded in the Chinese Materia Medica.
Alcoholic Liver Disease Animal Study (Tang et al., preclinical): AGE was administered at doses of 150 and 300 mg/kg/d for 7 weeks in chronic ethanol-fed mice.
General availability note: As of 2020, DHM is available over-the-counter, and the therapeutic dose has not been formally established.

8. Pharmacokinetics and Bioavailability

The low bioavailability of dihydromyricetin limits its potential applications. Pharmacokinetic properties may differ across patient populations, and there may be drug interactions due to projected CYP inhibition activity.

During the presystemic biotransformation of flavonoids, mainly sulfate and glucuronide derivatives are produced, which are the dominant metabolites in the circulation.

Researchers have explored various formulation strategies to improve DHM's bioavailability, including nanoscale phospholipid complexes.

9. Safety Considerations and Drug Interactions

General Safety Profile

DHM is nearly non-toxic and demonstrates an excellent safety profile. Previous acute toxicity tests have shown that the safe dose of DHM in rats is 10 g/kg.

CYP450 Enzyme Interactions

One of the most important verified safety considerations involves the inhibition of cytochrome P450 drug-metabolizing enzymes. An in vitro study using pooled human liver microsomes found that: DHM could inhibit the activity of CYP3A4, CYP2E1, and CYP2D6, with IC₅₀ values of 14.75, 25.74, and 22.69 μM, respectively, but other CYP isoforms were not affected. Enzyme kinetic studies showed that DHM was not only a non-competitive inhibitor of CYP3A4 but also a competitive inhibitor of CYP2E1 and CYP2D6, with Ki values of 6.06, 9.24, and 10.52 μM, respectively.

CYP3A4, CYP2D6, and CYP2E1 are responsible for metabolizing a large proportion of pharmaceuticals; inhibition of these enzymes in vivo could theoretically alter the metabolism of co-administered drugs, though whether the IC₅₀ values observed in vitro translate to clinically relevant interactions at dietary or supplemental doses in humans has not been established.

Interactions with Transporters

Myricetin (the oxidized form structurally related to DHM) and its glycosides proved to be strong inhibitors of organic anion transporting polypeptides (OATPs) at low micromolar (OATP1B1) and nanomolar (OATP2B1) concentrations. OATPs are important hepatic uptake transporters for a wide range of drugs, including statins. The direct relevance of this finding to DHM/ampelopsin at physiological concentrations requires further study.

Traditional Contraindications

Ampelopsis grossedentata is a "cold-natured" raw material in the category of traditional Chinese medicine, and people with partial cold constitutions should try to control the quantity and frequency of its consumption.

Absence of Established Human Toxicity Data

No serious adverse events have been prominently documented in the small human clinical trials reported to date, but long-term safety data in humans are absent. As noted by the Alzheimer's Drug Discovery Foundation, the therapeutic dose of DHM has not been established, and pharmacokinetic properties may differ across patient populations, with potential drug interactions due to projected CYP inhibition activity.

10. Regulatory and Pharmacopeial Status

Ampelopsis japonica has been officially included in the Chinese Pharmacopoeia since 1985, with its inclusion continuing through the latest 2020 edition. Although Ampelopsis grossedentata can be developed and utilized as health food, ordinary food, food additives, feed additives, cosmetics and cleaning products, Chinese medicinal materials, and special-purpose products, regulatory development of specific health claims continues to evolve.

11. Summary of Evidence Strength

Glycemic control in T2DM: One double-blind RCT (n=70), short-term, single-center. Preliminary positive signal; insufficient to support clinical recommendations.
NAFLD / Liver protection: One small RCT for DHM in NAFLD; robust animal data. Human evidence limited.
Antioxidant / Anti-inflammatory: Strong mechanistic data in vitro and in animal models; no dedicated human RCTs.
Neuroprotection: Preclinical only; no human data.
Anticancer: Cell and animal models only; no human data.
Bone health: Animal/cell data only.
Hyperuricemia: Animal data only.

Results from human immune cell studies suggest that Ampelopsis grossedentata could be a promising option for managing inflammation-related chronic diseases, though further research is needed to optimize dosage and administration methods.

References

Health Conditions

Health conditions that Ampelopsis may help support.

No conditions available.

Body Systems

Body systems that Ampelopsis may help support.

No body systems available.