Ai Di Cha
StarArdisia japonica (Thunb.) Blume
Traditionally used for
- Cough & breathing
- Urinary & fluids
- Menstrual & women's health
- Heart & circulation
- Liver & jaundice
Cautions & contraindications
- Bleeding disorders
- Heart conditions
☯ TCM Properties
Resolves Phlegm and Stops Cough; Calms Wheezing; Clears Damp-Heat; Invigorates Blood and Dispels Stasis; Unblocks the Channels and Alleviates Pain
Traditional Chinese Uses
Ai Di Cha (Japanese ardisia herb) is a folk herb from southern China used primarily to relieve cough and clear phlegm, with particular recognition in the treatment of chronic bronchitis. It also drains Damp-Heat from the body — addressing jaundice, urinary difficulty, and edema — and promotes Blood circulation to relieve pain from injuries and menstrual irregularities. Its combination of Phlegm-clearing and Blood-moving actions makes it useful for complex patterns where both Phlegm and stagnation are present.
Relationships
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Botanical Description
Ardisia japonica, marlberry or Japanese ardisia, is a low, evergreen, rhizomatous subshrub of the family Primulaceae (formerly Myrsinaceae) native to shady, humus-rich forest floors in China, Japan, Korea and Taiwan. It typically reaches only 15-30 cm in height, spreading by slender, creeping underground stems to form loose colonies. The slender, woody, glabrous aerial stems bear several leaves crowded toward the apex, each elliptic to obovate, 4-7 cm long, leathery, dark glossy green above with finely serrate margins. Small, nodding, five-lobed, pink to white, bell- to wheel-shaped flowers 4-6 mm across are borne in few-flowered axillary or sub-terminal cymes in early summer, followed by spherical, bright red, persistent berries 5-7 mm across that often remain on the plant through winter. The whole plant with root is collected in summer or autumn.
Active Constituents
Bergenin
C-glycoside of 4-O-methylgallic acid (isocoumarin C-glucoside)Concentration: the Chinese Pharmacopoeia (2020 edition) requires not less than 0.50% of the dried herb
The Pharmacopoeia assay marker and, with quercitrin, the most abundant constituent of the herb. It is the compound behind the herb's antitussive and expectorant reputation and is used in China as an isolated agent for chronic tracheitis. It is also the constituent that creates the herb's main interaction risk: in human liver microsomes it inhibits CYP3A4, CYP2E1 and CYP2C9.
Norbergenin
C-glycoside of gallic acid (isocoumarin C-glucoside)The demethylated congener of bergenin. In the anti-HIV screen of the aerial parts, bergenin and norbergenin were the only isolates with activity, and that activity was weak; none of the triterpenoid saponins was active.
Quercitrin
Flavonol glycoside (quercetin 3-O-rhamnoside)Co-dominant with bergenin in quantitative HPLC profiling of the herb, and proposed with it as a chemical marker for quality control.
Myricitrin
Flavonol glycoside (myricetin 3-O-rhamnoside)One of the flavonol rhamnosides of the herb. Flavonoids form one of the six main compound classes among the 296 constituents catalogued from this species.
Embelin
Alkyl-1,4-benzoquinoneA benzoquinone characteristic of the Myrsinoideae, reported from Ardisia japonica alongside rapanone, ardisin and the ardisinols. Embelin is pharmacologically potent and has documented antifertility activity in animal studies, which is worth weighing before recommending long courses of the crude herb to someone trying to conceive.
Ardimerin digallate
Dimeric lactone digallateA dimeric lactone isolated from the whole plant that inhibited HIV-1 and HIV-2 ribonuclease H in vitro with IC50 values of 1.5 and 1.1 microM respectively. This is an isolated-compound finding with no clinical follow-up.
Ardisianosides A-K
13,28-Epoxy oleanane-type triterpenoid saponinsA series of triterpenoid saponins from the whole plant. Saponins of this 13,28-epoxy series have been reported to inhibit liver cancer cell proliferation selectively in vitro without affecting normal liver cells.
beta-Eudesmol
Sesquiterpene alcohol (volatile oil)Network pharmacology and molecular docking in the 2026 review flagged beta-eudesmol and 2-methyl-5-isopropylphenol as the constituents most strongly associated with the herb's activity in respiratory disease. This is a computational prediction, not an experimentally validated mechanism.
Gallic acid
Phenolic acidPresent in the herb and measurable in rat plasma after oral dosing of the extract, alongside bergenin, epicatechin, epicatechin gallate, isoquercitrin and quercitrin - the six analytes used to characterise the herb's pharmacokinetics.
⚠ Drug Interactions
CYP3A4 substrates (e.g. midazolam, simvastatin, ciclosporin, vilazodone)
Bergenin, the marker constituent and one of the two most abundant compounds in the herb, inhibits CYP3A4 in human liver microsomes with an IC50 of 14.39 microM. It is a non-competitive inhibitor with a Ki of 7.71 microM and, importantly, a time-dependent inhibitor, with a Kinact/KI of 0.025/3.50 per microM per minute - so the effect can build over repeated dosing rather than washing out between doses. In rats, 80 mg/kg bergenin significantly altered the metabolism of vilazodone, a CYP3A4 substrate, confirming that the microsomal signal translates into a measurable in vivo interaction in at least one species. No human interaction study has been done, and it is not known what plasma bergenin concentrations a conventional decoction dose produces.
Clinical note: Treat this as a real, if unquantified, risk with narrow-therapeutic-index CYP3A4 substrates - ciclosporin, tacrolimus, some statins, several antiarrhythmics and direct oral anticoagulants. Ask about them before prescribing the herb, and if the combination cannot be avoided, monitor the drug rather than assuming the herb is inert.
CYP2C9 substrates (e.g. warfarin, phenytoin, glibenclamide)
Bergenin is a competitive inhibitor of CYP2C9 in human liver microsomes, with an IC50 of 15.11 microM and a Ki of 8.89 microM. Warfarin's more active S-enantiomer is cleared principally by CYP2C9, so inhibition of that isoform is the classic route to an unexpected INR rise. The evidence here is in vitro only; no human data exist.
Clinical note: If the herb is used by a patient on warfarin, check the INR within a week of starting and again after any dose change, and warn the patient about bleeding signs. The same caution applies to phenytoin and to sulfonylureas.
CYP2E1 substrates (e.g. paracetamol/acetaminophen, chlorzoxazone)
Bergenin competitively inhibits CYP2E1 in human liver microsomes with an IC50 of 22.83 microM and a Ki of 11.39 microM - the weakest of the three isoforms it affects. Because CYP2E1 generates the hepatotoxic paracetamol metabolite NAPQI, inhibition might in principle be protective rather than harmful, but this has not been tested and no clinical inference should be drawn either way.
Clinical note: No action needed beyond ordinary care with paracetamol dosing; the point is recorded for completeness rather than because it demands a change in practice.
Dosage
| Form | Amount | Frequency | Duration | Population | Notes |
|---|---|---|---|---|---|
| decoction | 15–30 g | Daily | — | — | 中国药典 2020 【用法与用量】15~30g。 【性味与归经】辛、微苦,平。归肺、肝经。 — Chinese Pharmacopoeia 2020, quoted verbatim; route and cautions preserved. Replaces a cleared category-filler value. |
Evidence Tier
Moderate evidence · 6 studiesRecorded studies by study design, strongest design at the top. This is a study-design tier only, not a GRADE rating: it does not weigh risk of bias, consistency or precision.
Systematic review / meta-analysis
0
Randomized controlled trial
0
Other clinical trial
0
Observational / case report
0
In vitro / animal
6
0 verified · 6 unverified
Show 6 studies
- In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes
- Quantitative investigation of drug-drug interaction between bergenin and vilazodone in rats through UPLC-MS/MS assay
- Qualitative and quantitative analysis of chemical constituents in Ardisiae Japonicae Herba
- Systematic characterization of the effective constituents and molecular mechanisms of Ardisiae Japonicae Herba using UPLC-Orbitrap Fusion MS and network pharmacology
- Metabolomic profiling combined with network analysis of serum pharmacochemistry to reveal the therapeutic mechanism of Ardisiae Japonicae Herba against acute lung injury
- Constituents of Ardisia japonica and Their in Vitro Anti-HIV Activity
Other / unclassified
0
Verified: design read from PubMed for a DOI that resolves to the cited paper Unverified: taken from the study's recorded description
Clinical Studies
In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes
Bergenin at 100 microM was screened against eight human liver CYP isoforms in human liver microsomes. It inhibited CYP3A4, CYP2E1 and CYP2C9, with IC50 values of 14.39, 22.83 and 15.11 microM, and left CYP1A2, 2A6, 2D6, 2C19 and 2C8 unaffected. Kinetics showed non-competitive inhibition of CYP3A4 and competitive inhibition of CYP2E1 and CYP2C9, with Ki values of 7.71, 11.39 and 8.89 microM, and bergenin was a time-dependent inhibitor of CYP3A4.
Quantitative investigation of drug-drug interaction between bergenin and vilazodone in rats through UPLC-MS/MS assay
A validated UPLC-MS/MS assay for vilazodone and its metabolite M10 was used to compare rats given vilazodone alone with rats co-dosed with 80 mg/kg bergenin. Bergenin significantly affected vilazodone metabolism, indicating a genuine pharmacokinetic drug-drug interaction, which the authors attribute to CYP3A4 inhibition. They note that clinical significance is not established and that vilazodone dosing should be watched if the combination is used.
Qualitative and quantitative analysis of chemical constituents in Ardisiae Japonicae Herba
HPLC coupled with quadrupole time-of-flight mass spectrometry identified or tentatively characterised 15 compounds in the herb, including coumarins, flavonoid glycosides and catechins, and a validated HPLC-DAD method was developed for five of them. Bergenin and quercitrin were the most abundant constituents and are proposed as the chemical markers for quality control.
Systematic characterization of the effective constituents and molecular mechanisms of Ardisiae Japonicae Herba using UPLC-Orbitrap Fusion MS and network pharmacology
UPLC-Orbitrap Fusion MS identified 236 compounds in the herb - 33 flavonoids, 21 phenylpropanoids, 46 terpenes, 7 quinones, 27 steroids, 71 carboxylic acids and 31 others - of which 41 were selected as key actives against COPD, acting on 65 predicted targets in inflammation, metabolism and immune pathways. Three of the active compounds reduced IL-6 and MMP9 in TNF-alpha-stimulated A549 cells.
Metabolomic profiling combined with network analysis of serum pharmacochemistry to reveal the therapeutic mechanism of Ardisiae Japonicae Herba against acute lung injury
Serum pharmacochemistry combined with metabolomic profiling and network analysis was used to identify the absorbed constituents of the herb and the metabolic pathways through which it acts in an acute lung injury model, supporting its traditional respiratory indication at a mechanistic level.
Constituents of Ardisia japonica and Their in Vitro Anti-HIV Activity
The methanol extract of the aerial parts showed moderate in vitro anti-HIV activity. On fractionation, several known compounds and a new triterpenoid saponin were isolated. None of the triterpenoid saponins was active; only bergenin and norbergenin showed weak anti-HIV activity.
Historical Texts
Ben Cao Tu Jing
Song dynasty (1061)Ben Cao Gang Mu Shi Yi
Qing dynasty (1765)References
- Pan Gao, Yumin Yang, Yufeng Li, Shanshan Liao, Junyu Liu, Xuhua Qin, Shenrui Jin. Ardisia japonica (Thunb.) Blume: Traditional applications, phytochemistry, pharmacological activities, network pharmacology, and quality control . Journal of Ethnopharmacology (2026) [DOI]
- Nguyen Tien Dat, KiHwan Bae, Antony Wamiru, James B. McMahon, Stuart F. J. Le Grice, Marion Bona, John A. Beutler, Young Ho Kim. A Dimeric Lactone from Ardisia japonica with Inhibitory Activity for HIV-1 and HIV-2 Ribonuclease H . Journal of Natural Products (2007) [DOI]
- Shuding Sun, Xuefang Liu, Di Zhao, Lishi Zheng, Xiaoxiao Han, Yange Tian, Suxiang Feng. Discovery of the Active Compounds of the Ethyl Acetate Extract Site of Ardisia japonica (Thunb.) Blume for the Treatment of Acute Lung Injury . Molecules (2024) [DOI]
This information is for educational purposes only and is not intended to replace professional medical advice. Always consult a qualified healthcare provider before using any herbal remedy, especially if you are pregnant, nursing, or taking medications.
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