Compound Monograph

Coptisine

Alkaloids Isoquinoline Alkaloids Natural (plant-derived)

A bright-yellow protoberberine alkaloid from goldthread and greater celandine — berberine's fully-bridged structural twin, best studied as a potent anti-Helicobacter and anti-inflammatory gut agent, and (unlike berberine) a selective MAO-A inhibitor. Its data are essentially all preclinical.

Sources · 6

Where Does It Come From?

Coptisine is a naturally occurring isoquinoline alkaloid (protoberberine group), found in Chinese goldthread, Greater celandine and 4 other sources. It is well tolerated orally (low toxicity).

Also found in
Corydalis species Monograph coming soon
Other Coptis species Monograph coming soon
Other protoberberine-bearing Ranunculaceae & Papaveraceae Monograph coming soon

Concentration

Content by Source

Reported concentrations across the plants that contain coptisine — the bar marks the typical level, the line shows the reported range.

Typical level Reported range % dry wt
Chinese goldthread (Coptis chinensis) rhizome 1–2.3 [14]

Literature figures for varying plant parts and preparations. Read them as a comparative guide, not exact assays.

Coptisine at a Glance

Coptisine is a bright-yellow protoberberine alkaloid — the characteristic pigment of Coptis (goldthread) rhizome and one of the principal alkaloids of greater celandine. Structurally it is berberine with both of its ring substituents closed into methylenedioxy bridges, which makes it a close chemical relative of the much better-known berberine but not identical to it in behaviour 1,2Reference 1Wu J et al. · 2019ReviewCoptisine from Coptis chinensis exerts diverse beneficial properties: a concise reviewView study →Reference 2Lu Q et al. · 2023ReviewCoptisine, the characteristic constituent from Coptis chinensis, exhibits significant therapeutic potential in treating cancers, metabolic and inflammatory diseases — reviewView study →.

Its evidence base is almost entirely preclinical — in-vitro assays and rodent studies, with no human trials of the isolated molecule. Within that preclinical literature its strongest, most compound-specific signals are in the gut: it is reported the most effective Coptis alkaloid against Helicobacter pylori, and it eases experimental colitis by damping the NLRP3 inflammasome 4,5,3Reference 4Li C et al. · 2018In vitroCoptisine-induced inhibition of Helicobacter pylori: elucidation of specific mechanisms by probing urease active site and its maturation process — in vitroView study →Reference 5Tang Q et al. · 2023In vitroCoptisine inhibits Helicobacter pylori and reduces the expression of CagA to alleviate host inflammation in vitro and in vivoView study →Reference 3Li C et al. · 2024AnimalCoptisine alleviates colitis through modulating gut microbiota and inhibiting TXNIP/NLRP3 inflammasome — DSS-colitis mouse studyView study →. Like berberine it is poorly absorbed orally, so most of what it does happens locally in the gut or through gut-microbial metabolites rather than through high blood levels 10,11Reference 10Su J et al. · 2015AnimalPharmacokinetics and brain distribution and metabolite identification of coptisine, a protoberberine alkaloid with therapeutic potential for CNS disorders, in ratsView study →Reference 11Ai G et al. · 2021Gut microbiota–mediated transformation of coptisine into a novel metabolite 8-oxocoptisine: insight into its superior anti-colitis effectView study →.

One feature sets it apart from berberine pharmacologically: coptisine is a potent, selective inhibitor of monoamine oxidase A — a genuinely different profile from its famous cousin 6Reference 6Ro JS et al. · 2001AnimalInhibition of type A monoamine oxidase by coptisine in mouse brain — reversible competitive MAO-A inhibitor (Ki ≈ 3.3 µM)View study →.

Coptisine vs. Berberine

Coptisine and berberine share the same flat, positively-charged (quaternary) protoberberine skeleton and the same vivid yellow colour, and they occur together in the same roots — so they are often lumped. The difference is in two rings.

Berberine carries a single methylenedioxy bridge on one ring (ring A) and a pair of methoxy groups on the other (ring D). Coptisine replaces that methoxy pair with a second methylenedioxy bridge — hence its chemical nickname, bis(methylenedioxy)protoberberine 1,2Reference 1Wu J et al. · 2019ReviewCoptisine from Coptis chinensis exerts diverse beneficial properties: a concise reviewView study →Reference 2Lu Q et al. · 2023ReviewCoptisine, the characteristic constituent from Coptis chinensis, exhibits significant therapeutic potential in treating cancers, metabolic and inflammatory diseases — reviewView study →. The result is a more rigid, more symmetric molecule with subtly different target selectivity.

That structural difference shows up most clearly at monoamine oxidase. Coptisine is a potent, reversible, competitive inhibitor of MAO-A (Ki ≈ 3.3 µM in mouse brain) and does not inhibit MAO-B 6Reference 6Ro JS et al. · 2001AnimalInhibition of type A monoamine oxidase by coptisine in mouse brain — reversible competitive MAO-A inhibitor (Ki ≈ 3.3 µM)View study → — whereas berberine is only a weak, non-selective MAO inhibitor (IC50 around 126 µM) 1Reference 1Wu J et al. · 2019ReviewCoptisine from Coptis chinensis exerts diverse beneficial properties: a concise reviewView study →. On this axis coptisine is the far stronger compound. (Note: this is MAO-A selectivity, not the MAO-B activity sometimes loosely attributed to the protoberberines.)

The two also diverge in where the evidence sits. Berberine has an unusually large human clinical literature (blood sugar, cholesterol, fatty liver); coptisine has essentially none — its story is preclinical. And their relative abundance flips by plant: berberine dominates goldthread, while coptisine is the most abundant alkaloid measured in some greater-celandine extracts 12Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study →. Where they converge is poor oral bioavailability and a shared reputation for gut-level antimicrobial and anti-inflammatory activity 10,4Reference 10Su J et al. · 2015AnimalPharmacokinetics and brain distribution and metabolite identification of coptisine, a protoberberine alkaloid with therapeutic potential for CNS disorders, in ratsView study →Reference 4Li C et al. · 2018In vitroCoptisine-induced inhibition of Helicobacter pylori: elucidation of specific mechanisms by probing urease active site and its maturation process — in vitroView study →.

What It's Used For

Coptisine’s pharmacology is broad on paper — reviews list anticancer, anti-inflammatory, cardiovascular, antimicrobial, neuroprotective and antidiabetic activity — but nearly all of it is in vitro or in rodents, and much of the “cardiovascular/metabolic” claim actually belongs to Coptis total alkaloids or to berberine rather than to isolated coptisine 1,2Reference 1Wu J et al. · 2019ReviewCoptisine from Coptis chinensis exerts diverse beneficial properties: a concise reviewView study →Reference 2Lu Q et al. · 2023ReviewCoptisine, the characteristic constituent from Coptis chinensis, exhibits significant therapeutic potential in treating cancers, metabolic and inflammatory diseases — reviewView study →.

Best-supported (still preclinical):anti-Helicobacter pylori activity — coptisine is the most effective Coptis alkaloid tested, with a defined urease/CagA mechanism and eradication in infected mice 4,5Reference 4Li C et al. · 2018In vitroCoptisine-induced inhibition of Helicobacter pylori: elucidation of specific mechanisms by probing urease active site and its maturation process — in vitroView study →Reference 5Tang Q et al. · 2023In vitroCoptisine inhibits Helicobacter pylori and reduces the expression of CagA to alleviate host inflammation in vitro and in vivoView study →.
Emerging, mechanistically clean:eases experimental colitis by inhibiting the TXNIP/NLRP3 inflammasome and reshaping the gut microbiota; a gut-microbial metabolite (8-oxocoptisine) is even more active 3,11Reference 3Li C et al. · 2024AnimalCoptisine alleviates colitis through modulating gut microbiota and inhibiting TXNIP/NLRP3 inflammasome — DSS-colitis mouse studyView study →Reference 11Ai G et al. · 2021Gut microbiota–mediated transformation of coptisine into a novel metabolite 8-oxocoptisine: insight into its superior anti-colitis effectView study →.
Compound-unique:a selective, reversible MAO-A inhibitor (Ki ≈ 3.3 µM) and a modest acetylcholinesterase inhibitor — a neuro-enzyme profile berberine lacks 6,7Reference 6Ro JS et al. · 2001AnimalInhibition of type A monoamine oxidase by coptisine in mouse brain — reversible competitive MAO-A inhibitor (Ki ≈ 3.3 µM)View study →Reference 7Kong XP et al. · 2019Synergistic inhibition of acetylcholinesterase by alkaloids derived from Stephaniae Tetrandrae Radix, Coptidis Rhizoma and Phellodendri Chinensis CortexView study →.
The caveat:oral bioavailability is poor (~9% in rats, falling with dose) and no human trials of isolated coptisine exist — read all of this as promising preclinical signal, not established use 10,1Reference 10Su J et al. · 2015AnimalPharmacokinetics and brain distribution and metabolite identification of coptisine, a protoberberine alkaloid with therapeutic potential for CNS disorders, in ratsView study →Reference 1Wu J et al. · 2019ReviewCoptisine from Coptis chinensis exerts diverse beneficial properties: a concise reviewView study →.
Evidence by IndicationStrength of support · Beta

Support is an experimental score I’m building — a composite weighted by study type (human > animal > in vitro > review) and study volume, tempered for isolate-vs-plant match and bioavailability. It’s a beta: a fast way to rank strength of evidence at a glance, not a validated metric. Every row here is capped low because no human trials of isolated coptisine exist — the scores rank preclinical strength. Each application links down to its write-up.

Mechanisms

Target / pathwayEffectRelevant to
H. pylori urease (active-site thiol + Ni metallocentre; UreG maturation)slow-binding inhibition → blocks acid survival
anti-H. pylori
CagA virulence factor↓ expression & translocation → less gastric inflammation
anti-H. pylori / gastric
TXNIP / NLRP3 inflammasomesuppression → ↓ IL-1β, IL-18
colitisanti-inflammatory
NF-κB / MAPK signalling↓ pro-inflammatory transcription
anti-inflammatory
Gut microbiota↑ Akkermansia; converts coptisine → 8-oxocoptisine (more active)
colitis
Monoamine oxidase A (MAO-A)reversible competitive inhibition (Ki ≈ 3.3 µM); MAO-B not inhibited
neuro / catecholamine tone
Acetylcholinesterase (AChE)inhibition (IC50 ≈ 13.5 µM), synergistic with related alkaloids
neuro (cognition)
Caspase-3/7, PI3K/Akt, mitochondrial pathwayspro-apoptotic in tumour cells
anticancer (in vitro)
AMPK / α-glucosidasemetabolic modulation
lipid & glucose

Pharmacokinetics

Coptisine is a quaternary protoberberine, and — like berberine — it is poorly absorbed by mouth: oral bioavailability was ~8.9% in rats with a short plasma half-life (~0.71 h), and bioavailability fell further as the dose rose (saturable, non-linear absorption) 10Reference 10Su J et al. · 2015AnimalPharmacokinetics and brain distribution and metabolite identification of coptisine, a protoberberine alkaloid with therapeutic potential for CNS disorders, in ratsView study →. After intravenous dosing it crosses the blood–brain barrier and distributes broadly, but tissue levels stay low except in the intestine, where concentrations are an order of magnitude higher — consistent with a compound that acts mainly in the gut 10Reference 10Su J et al. · 2015AnimalPharmacokinetics and brain distribution and metabolite identification of coptisine, a protoberberine alkaloid with therapeutic potential for CNS disorders, in ratsView study →. The gut microbiota further transform it into metabolites such as 8-oxocoptisine, which can be more pharmacologically active than the parent 11Reference 11Ai G et al. · 2021Gut microbiota–mediated transformation of coptisine into a novel metabolite 8-oxocoptisine: insight into its superior anti-colitis effectView study →. The practical read is the same as for berberine: plasma exposure is low, formulation (cyclodextrin complexes, nanocarriers) is the main lever discussed for raising it, and much of the observed benefit is plausibly enteric or metabolite-driven rather than systemic 1,10,11Reference 1Wu J et al. · 2019ReviewCoptisine from Coptis chinensis exerts diverse beneficial properties: a concise reviewView study →Reference 10Su J et al. · 2015AnimalPharmacokinetics and brain distribution and metabolite identification of coptisine, a protoberberine alkaloid with therapeutic potential for CNS disorders, in ratsView study →Reference 11Ai G et al. · 2021Gut microbiota–mediated transformation of coptisine into a novel metabolite 8-oxocoptisine: insight into its superior anti-colitis effectView study →.

Clinical Trials

There are no registered clinical trials of isolated coptisine. The human-facing evidence is limited to whole Coptis/goldthread and greater-celandine preparations, where coptisine is only one of several alkaloids; everything specific to the molecule is in vitro or in rodents.

CompletedPlannedTerminatedPreclinical
———Extensive(in vitro + rodent)

Last checked: July 2026.

Isolate vs. Plant Studies

Coptisine sits at the isolate-heavy end for mechanism and the plant-only end for human evidence. The anti-H. pylori, anti-colitis, MAO-A, AChE and anticancer findings above were all generated with purified coptisine (usually the chloride salt), which is a strength — they genuinely describe the molecule, not an extract standing in for it 4,5,6,8Reference 4Li C et al. · 2018In vitroCoptisine-induced inhibition of Helicobacter pylori: elucidation of specific mechanisms by probing urease active site and its maturation process — in vitroView study →Reference 5Tang Q et al. · 2023In vitroCoptisine inhibits Helicobacter pylori and reduces the expression of CagA to alleviate host inflammation in vitro and in vivoView study →Reference 6Ro JS et al. · 2001AnimalInhibition of type A monoamine oxidase by coptisine in mouse brain — reversible competitive MAO-A inhibitor (Ki ≈ 3.3 µM)View study →Reference 8Nakonieczna S et al. · 2022Isoquinoline alkaloids from Coptis chinensis Franch: focus on coptisine as a potential therapeutic candidate against gastric cancer cellsView study →. But there is no human trial of the isolate at all, so any real-world use claim rests on whole-plant preparations — goldthread (Coptidis rhizoma) and greater celandine — in which coptisine co-occurs with berberine, palmatine, jatrorrhizine, epiberberine and (in celandine) the benzophenanthridines sanguinarine, chelerythrine and chelidonine, plus protopine 12,2Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study →Reference 2Lu Q et al. · 2023ReviewCoptisine, the characteristic constituent from Coptis chinensis, exhibits significant therapeutic potential in treating cancers, metabolic and inflammatory diseases — reviewView study →. A whole-root effect therefore cannot be assigned to coptisine alone, and the “metabolic” literature in particular is dominated by berberine. Read the mechanism studies as evidence for the molecule and the traditional record as evidence for the plants.

Its Role in Plants

Coptisine is a benzylisoquinoline (protoberberine) alkaloid, built — like berberine — from two molecules of the amino acid tyrosine by way of (S)-reticuline, the branch-point of this whole alkaloid family. The committed step to the protoberberine skeleton is the formation of (S)-scoulerine by the flavin-dependent berberine bridge enzyme; the pathway then runs on toward (S)-stylopine, which a Coptis flavin oxidase (CcTHBO) oxidises to coptisine 13Reference 13Wu L et al. · 2024A biosynthetic network for protoberberine production in Coptis chinensisView study →. Coptisine’s defining feature — its two methylenedioxy bridges — is installed by CYP719-clan cytochrome-P450 enzymes that close a methylenedioxy ring on ring A and, via specialised CYP719A variants, on ring D, directing biosynthetic flux toward coptisine rather than the methoxylated berberine 13Reference 13Wu L et al. · 2024A biosynthetic network for protoberberine production in Coptis chinensisView study →.

As a quaternary, brightly pigmented alkaloid concentrated in roots and rhizomes, coptisine plays the usual protoberberine ecological role — a chemical defence compound with antimicrobial activity against would-be pathogens — rather than a signalling one. These are plant-biology functions and should not be read as human pharmacology.

Prevalence in Nature

Coptisine is largely restricted to the protoberberine-producing plant families — chiefly Ranunculaceae (Coptis) and Papaveraceae (Chelidonium, Corydalis) — and concentrates in roots, rhizomes and latex rather than leaves 12,2Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study →Reference 2Lu Q et al. · 2023ReviewCoptisine, the characteristic constituent from Coptis chinensis, exhibits significant therapeutic potential in treating cancers, metabolic and inflammatory diseases — reviewView study →. Its richest source is goldthread rhizome (Coptis chinensis), where it is a major protoberberine alongside the dominant berberine; total quaternary protoberberine alkaloids in Coptis rhizome run to roughly 9–20% of dry weight, with coptisine one of the larger individual contributors (on the order of ~1–2% dry weight) 14,15Reference 14Yang Y et al. · 2017Determination of alkaloid contents in various tissues of Coptis chinensis Franch by RP-HPLC and UV spectrophotometryView study →Reference 15Meng FC et al. · 2018ReviewCoptidis rhizoma and its main bioactive components: recent advances in chemical investigation, quality evaluation and pharmacological activity — reviewView study →. In greater celandine (Chelidonium majus) coptisine is reported the most abundant single alkaloid measured in some extracts (~6.4 mg/g of a 25% ethanol extract), though celandine’s total alkaloid content varies several-fold with plant part (root and latex ≫ aerial parts), ecotype and season 12Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study →.

Major Natural Sources

SourceBotanicalPartCoptisine levelNote
Chinese goldthreadCoptis chinensisRhizome~1–2% dry wt (major protoberberine)Richest & best-characterised source 14Reference 14Yang Y et al. · 2017Determination of alkaloid contents in various tissues of Coptis chinensis Franch by RP-HPLC and UV spectrophotometryView study →
Greater celandineChelidonium majusAerial / latexMost abundant alkaloid in some extracts (~6.4 mg/g extract)Extract-based figure; varies with part/season 12Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study →
Other Coptis spp.C. deltoidea, C. teetaRhizomePresent (protoberberine mix)Co-occurs with berberine/palmatine 12Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study →
Corydalis spp.Corydalis spp.TuberMinor protoberberineOne of many alkaloids

Discovery & Synthesis

Coptisine takes its name directly from the genus Coptis (goldthread), of which it is a characteristic alkaloid; it has long been recognised as one of the principal protoberberines of Coptidis rhizoma, though its exact first-isolation date is not well documented in the accessible literature. Chemically it is defined as bis(methylenedioxy)protoberberine — the fully methylenedioxy-bridged congener of berberine 1,2Reference 1Wu J et al. · 2019ReviewCoptisine from Coptis chinensis exerts diverse beneficial properties: a concise reviewView study →Reference 2Lu Q et al. · 2023ReviewCoptisine, the characteristic constituent from Coptis chinensis, exhibits significant therapeutic potential in treating cancers, metabolic and inflammatory diseases — reviewView study →.

Commercially, coptisine is not manufactured by total synthesis; it is isolated from Coptis rhizome (and related protoberberine-rich plants) by solvent extraction and chromatographic separation from the accompanying alkaloids, the same practical logic that makes berberine a plant-extracted rather than synthesised commodity 12Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study →. Most coptisine in circulation is a reference standard / research chemical rather than a bulk supplement ingredient.

Patents: not yet researched (future patent-loop pass).

Toxicity & Safety

Coptisine carries a low flag: it is a protoberberine closely related to well-tolerated berberine, systemic exposure after oral dosing is very low, and no serious toxicity of the isolated compound is established. Two honest caveats keep it from being “clean”: reviews flag possible hepatotoxicity and poor solubility as development hurdles, and coptisine (with the other celandine alkaloids) has measurable cardiac ion-channel (hERG) activity in vitro 2,12Reference 2Lu Q et al. · 2023ReviewCoptisine, the characteristic constituent from Coptis chinensis, exhibits significant therapeutic potential in treating cancers, metabolic and inflammatory diseases — reviewView study →Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study →.

Safety at a Glance
Low / no toxicityDrug interactions
  • No established serious toxicity of the isolate. A protoberberine relative of berberine, poorly absorbed orally, well tolerated in the rodent studies performed to date.
  • Greater celandine — the whole herb — is hepatotoxic. Documented idiosyncratic liver injury is attributed to Chelidonium majus preparations, not specifically to isolated coptisine; don’t read celandine’s liver risk onto the pure molecule (or vice-versa).
  • Cardiac (hERG) signal in vitro. Coptisine and other celandine alkaloids affect hERG potassium channels / cardiac action potential in preclinical safety assays — relevance to real exposures is unknown.
  • No human safety data for the isolate. No trials, no defined interactions or contraindications; absence of data is not evidence of safety.
Full Safety & Interactions Detail

The isolated molecule has a thin but reassuring preclinical safety record — it is a protoberberine cousin of berberine with very low oral bioavailability, and the rodent efficacy studies above did not report serious toxicity 3,5,10Reference 3Li C et al. · 2024AnimalCoptisine alleviates colitis through modulating gut microbiota and inhibiting TXNIP/NLRP3 inflammasome — DSS-colitis mouse studyView study →Reference 5Tang Q et al. · 2023In vitroCoptisine inhibits Helicobacter pylori and reduces the expression of CagA to alleviate host inflammation in vitro and in vivoView study →Reference 10Su J et al. · 2015AnimalPharmacokinetics and brain distribution and metabolite identification of coptisine, a protoberberine alkaloid with therapeutic potential for CNS disorders, in ratsView study →.

The two flags to hold in mind are, first, that mechanistic reviews list possible hepatotoxicity and poor solubility among the barriers to developing coptisine as a drug 2Reference 2Lu Q et al. · 2023ReviewCoptisine, the characteristic constituent from Coptis chinensis, exhibits significant therapeutic potential in treating cancers, metabolic and inflammatory diseases — reviewView study →.

Second, that in a cardiac-safety screen coptisine and the other major Chelidonium alkaloids interacted with hERG potassium channels and the dog cardiac action potential in vitro 12Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study → — a preclinical signal whose significance at realistic (low) systemic exposures is unclear.

Crucially, the well-known hepatotoxicity of greater celandine is a whole-herb phenomenon: cases of idiosyncratic, cholestatic liver injury are attributed to Chelidonium majus preparations as a whole, and cannot be pinned on coptisine specifically — the herb is a complex mixture of benzophenanthridine and protoberberine alkaloids. Equally, coptisine’s own safety cannot be inferred from berberine’s. By class analogy, berberine-type protoberberines can inhibit drug-metabolising CYP enzymes, so a drug-interaction potential is plausible for coptisine but has not been characterised. No isolate reproductive/developmental-toxicity dataset exists; pregnancy and lactation decisions belong to the herb or product page where intake is decided, not to this molecule page.

Dosage

There is no established human dose for coptisine. It has not been tested in human trials as an isolated compound and is not sold as a stand-alone supplement — it circulates mainly as a research chemical and analytical reference standard. The figures below are the doses used in preclinical research, given for context only:

SettingModelDose (studied)Source
H. pylori eradicationInfected mice, oral~150 mg/kg/day5Reference 5Tang Q et al. · 2023In vitroCoptisine inhibits Helicobacter pylori and reduces the expression of CagA to alleviate host inflammation in vitro and in vivoView study →
ColitisDSS mice, oralRodent oral dosing3Reference 3Li C et al. · 2024AnimalCoptisine alleviates colitis through modulating gut microbiota and inhibiting TXNIP/NLRP3 inflammasome — DSS-colitis mouse studyView study →
PharmacokineticsRats50 mg/kg oral / 10 mg/kg IV10Reference 10Su J et al. · 2015AnimalPharmacokinetics and brain distribution and metabolite identification of coptisine, a protoberberine alkaloid with therapeutic potential for CNS disorders, in ratsView study →

Human exposure is entirely indirect — as one of several alkaloids in goldthread (Coptidis rhizoma) and greater-celandine preparations, standardised (if at all) to total alkaloids or to berberine rather than to coptisine 12Reference 12Orvos P et al. · 2015Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approachView study →. These are research doses in animals and are not a personal recommendation.

References

  1. Wu J, Luo Y, Deng D, Su S, Li S, Xiang L, Hu Y, Wang P, Meng X. (2019). Coptisine from Coptis chinensis exerts diverse beneficial properties: a concise review. Journal of Cellular and Molecular Medicine, 23(12), 7946–7960. https://pubmed.ncbi.nlm.nih.gov/31622015/
  2. Lu Q, Tang Y, Luo S, Gong Q, Li C. (2023). Coptisine, the characteristic constituent from Coptis chinensis, exhibits significant therapeutic potential in treating cancers, metabolic and inflammatory diseases — review. The American Journal of Chinese Medicine, 51(8), 2121–2156. https://pubmed.ncbi.nlm.nih.gov/37930333/
  3. Li C, Deng L, Pu M, Ye X, Lu Q. (2024). Coptisine alleviates colitis through modulating gut microbiota and inhibiting TXNIP/NLRP3 inflammasome — DSS-colitis mouse study. Journal of Ethnopharmacology, 335, 118680. https://pubmed.ncbi.nlm.nih.gov/39117021/
  4. Li C, Huang P, Wong K, Xu Y, Tan L, Chen H, Lu Q, Luo C, Tam C, Zhu L, Su Z, Xie J. (2018). Coptisine-induced inhibition of Helicobacter pylori: elucidation of specific mechanisms by probing urease active site and its maturation process — in vitro. Journal of Enzyme Inhibition and Medicinal Chemistry, 33(1), 1362–1375. https://pubmed.ncbi.nlm.nih.gov/30191728/
  5. Tang Q, et al. (2023). Coptisine inhibits Helicobacter pylori and reduces the expression of CagA to alleviate host inflammation in vitro and in vivo. Journal of Ethnopharmacology, 315, 116663. https://pubmed.ncbi.nlm.nih.gov/37164257/
  6. Ro JS, Lee SS, Lee KS, Lee MK. (2001). Inhibition of type A monoamine oxidase by coptisine in mouse brain — reversible competitive MAO-A inhibitor (Ki ≈ 3.3 µM). Life Sciences, 70(6), 639–645. https://pubmed.ncbi.nlm.nih.gov/11833714/
  7. Kong XP, Liu EYL, Chen ZC, Xu ML, Yu AXD, Wu QY, Xia YJ, Duan R, Dong TTX, Tsim KWK. (2019). Synergistic inhibition of acetylcholinesterase by alkaloids derived from Stephaniae Tetrandrae Radix, Coptidis Rhizoma and Phellodendri Chinensis Cortex. Molecules, 24(24), 4567. https://pubmed.ncbi.nlm.nih.gov/31847089/
  8. Nakonieczna S, Grabarska A, Gaweł K, Wróblewska-Łuczka P, Czerwonka A, Stepulak A, Kukula-Koch W. (2022). Isoquinoline alkaloids from Coptis chinensis Franch: focus on coptisine as a potential therapeutic candidate against gastric cancer cells. International Journal of Molecular Sciences, 23(18), 10330. https://pubmed.ncbi.nlm.nih.gov/36142236/
  9. Friedemann T, Schumacher U, Tao Y, Leung AKM, Schröder S. (2015). Neuroprotective activity of coptisine from Coptis chinensis (Franch). Evidence-Based Complementary and Alternative Medicine, 2015, 827308. https://pubmed.ncbi.nlm.nih.gov/26229546/
  10. Su J, Miao Q, Miao P, Zhao Y, Zhang Y, Chen N, Zhang Y, Ma S. (2015). Pharmacokinetics and brain distribution and metabolite identification of coptisine, a protoberberine alkaloid with therapeutic potential for CNS disorders, in rats. Biological & Pharmaceutical Bulletin, 38(10), 1518–1528. https://pubmed.ncbi.nlm.nih.gov/26228628/
  11. Ai G, Huang Z, Cheng J, Xie J, Zeng H, Liu Y, Li Y, Huang X, Chen J, Su Z. (2021). Gut microbiota–mediated transformation of coptisine into a novel metabolite 8-oxocoptisine: insight into its superior anti-colitis effect. Frontiers in Pharmacology, 12, 639020. https://pubmed.ncbi.nlm.nih.gov/33859564/
  12. Orvos P, Virág L, Tálosi L, Hajdú Z, Csupor D, Jedlinszki N, Szél T, Varró A, Hohmann J. (2015). Effects of Chelidonium majus extracts and major alkaloids on hERG potassium channels and on dog cardiac action potential — a safety approach. Fitoterapia, 100, 156–165. https://pubmed.ncbi.nlm.nih.gov/25481375/
  13. Wu L, Zhao B, Deng Z, Wang B, Yu Y. (2024). A biosynthetic network for protoberberine production in Coptis chinensis. Horticulture Research, 11(1), uhad259. https://pubmed.ncbi.nlm.nih.gov/38282690/
  14. Yang Y, Peng J, Li F, Liu X, Deng M, Wu H. (2017). Determination of alkaloid contents in various tissues of Coptis chinensis Franch by RP-HPLC and UV spectrophotometry. Journal of Chromatographic Science, 55(5), 556–563. https://pubmed.ncbi.nlm.nih.gov/28203760/
  15. Meng FC, Wu ZF, Yin ZQ, Lin LG, Wang R, Zhang QW. (2018). Coptidis rhizoma and its main bioactive components: recent advances in chemical investigation, quality evaluation and pharmacological activity — review. Chinese Medicine, 13, 13. https://pubmed.ncbi.nlm.nih.gov/29541156/