Compound Monograph
Lobetyolin
Lobetyolin is the polyacetylene glucoside used as the standardization marker for dang shen (Codonopsis pilosula). It carries a small but distinctive preclinical anticancer signal — it suppresses the glutamine transporter ASCT2 (SLC1A5) to starve tumor cells of glutamine — alongside early anti-inflammatory and gastroprotective data. All of it is in cells and rodents, it is present in the root only at trace levels, and it is very poorly absorbed by mouth.
Sources · 1
Where Does It Come From?
Lobetyolin is a naturally occurring polyacetylene glycoside, found in Dang Shen. It is well tolerated orally (low toxicity).
Concentration
Content by Source
Concentrations not reported. No percent-dry-weight or mg/g figures have been published for this compound in its source plants.
Lobetyolin at a Glance
Lobetyolin is a polyacetylene glucoside and the standardisation marker for dang shen (Codonopsis pilosula), the gentler qi tonic often substituted for ginseng.
Its distinctive preclinical signal is anticancer and mechanistically specific: it suppresses the glutamine transporter ASCT2, cutting off a nutrient many tumour cells depend on — a metabolic-starvation approach rather than direct cytotoxicity, in the same spirit as arctigenin’s antiausterity mechanism.
What It's Used For
Lobetyolin is the polyacetylene glucoside (the mono-glucoside of lobetyol) used as the standardization marker for dang shen (Codonopsis pilosula), the tonic root of traditional Chinese medicine. Two caveats frame the page. First, it is a trace/sub-percent quality marker, not a bulk bioactive — dang shen’s tonic action is attributed to its polysaccharides/fructans, so isolate potency does not transfer to whole-root doses. Second, its oral bioavailability is poor (~4% in rats). Within those limits it has one genuinely distinctive hook: a preclinical anticancer mechanism that starves tumor cells of glutamine by suppressing the transporter ASCT2 (SLC1A5) 2,
There are no human trials of the isolate.
Support is an experimental score — weighted by study type (human > animal > in vitro) and volume. A beta, not a validated metric. No human isolate data and trace abundance, so scores stay low by design.
The distinctive mechanism: lobetyolin downregulates ASCT2 (SLC1A5), the sodium-dependent glutamine transporter tumors depend on, cutting glutamine uptake → ROS accumulation → mitochondria-mediated apoptosis, shown in gastric 2Reference 2Lobetyolin inhibits cell proliferation and induces apoptosis by downregulating ASCT2 in gastric cancerView study → and colon 3Reference 3Lobetyolin induces apoptosis of colon cancer cells by inhibiting glutamine metabolismView study → cancer cells with in-vivo tumor-growth restraint in gastric xenografts 2Reference 2Lobetyolin inhibits cell proliferation and induces apoptosis by downregulating ASCT2 in gastric cancerView study →; a separate hepatocellular-carcinoma study reports a different DUSP1–ERK1/2 axis 4Reference 4Lobetyolin suppresses the proliferation of hepatocellular carcinoma through activating the DUSP1-ERK1/2 signalling pathwayView study →, and a review collates the field 1Reference 1ReviewAnticancer properties of lobetyolin, an essential component of Radix Codonopsis (dang shen) — reviewView study →.
Gap: entirely cell-line/xenograft with no isolate human data, and effective concentrations are far above anything reachable from dietary dang shen given trace abundance and ~4% oral bioavailability 2,
Lobetyolin lowered pro-inflammatory cytokine output from macrophages and protected mice against LPS-induced sepsis 5Reference 5AnimalLobetyolin protects mice against LPS-induced sepsis by downregulating inflammatory-cytokine production in macrophagesView study →.
Gap: a single primary in-vivo study, with the mechanism thin (NF-κB the plausible node but not dissected) and no dose-response translation to humans 5Reference 5AnimalLobetyolin protects mice against LPS-induced sepsis by downregulating inflammatory-cytokine production in macrophagesView study →.
By spectrum-effect analysis of dang shen, lobetyolin (with tangshenoside I) was identified as an active contributor to gastric-ulcer prevention 6Reference 6The effect and mechanism of Codonopsis Radix and its active components tangshenoside I and lobetyolin on preventing gastric ulcer based on a spectrum-effect relationshipView study →.
Gap: the effect is attributed within a whole-herb spectrum-effect model, not a standalone isolate efficacy trial, and it is co-active with other markers 6Reference 6The effect and mechanism of Codonopsis Radix and its active components tangshenoside I and lobetyolin on preventing gastric ulcer based on a spectrum-effect relationshipView study →.
Lobetyolin has been profiled as a dietary “anti-Alzheimer factor” in a metabolism/target-exploration study 7Reference 7Lobetyolin, an anti-Alzheimer factor from a dietary Campanulaceae source: metabolism regulation and target explorationView study →.
Gap: a single mechanistic paper — speculative and not a supported clinical claim 7Reference 7Lobetyolin, an anti-Alzheimer factor from a dietary Campanulaceae source: metabolism regulation and target explorationView study →.
Mechanisms
| Target / pathway | Effect | Relevant to |
|---|---|---|
| ASCT2 / SLC1A5 (glutamine transporter) | downregulated → ↓ glutamine uptake | anticancer (the distinctive hook) |
| Glutamine metabolism → ROS | ↓ glutaminolysis, ROS accumulation → mitochondrial apoptosis | anticancer |
| DUSP1 → ERK1/2 | activated → antiproliferative | hepatocellular carcinoma |
| Macrophage cytokines (NF-κB-type output) | ↓ pro-inflammatory cytokines | anti-inflammatory / sepsis |
| CYP450 (CYP2C19, 1A1, 2C9, 1A2) | substrate; oxidation/glucuronidation/GSH conjugation | pharmacokinetics |
Only mechanisms with a verified supporting study are listed.
Pharmacokinetics
Lobetyolin is a polyacetylene glucoside subject to gut hydrolysis/deglycosylation — the aglycone lobetyol is metabolically stable in liver microsomes, while the glucosides are extensively transformed (dozens of metabolites via oxidation, glucuronidation and glutathione conjugation; CYP2C19/1A1/2C9/1A2 implicated) 8Reference 8In-vitro/in-vivo metabolic pathways of lobetyol, lobetyolin and lobetyolinin, three polyacetylenes from Codonopsis Radix, by UHPLC-Q/TOF-MSView study →. Its oral bioavailability is poor — ~3.9% for pure lobetyolin in rats, rising to ~7.0% when dosed within Codonopsis pilosula extract (a matrix effect), consistent with the whole-root-over-isolate pattern 9Reference 9AnimalComparative pharmacokinetic and bioavailability study of lobetyolin in rats after administration of lobetyolin and Codonopsis pilosula extractView study →. Polyacetylenes as a class can be light/oxygen-labile, and formal lobetyolin degradation kinetics were not located, so isolate stability is uncertain.
Clinical trials
There are no human trials of isolated lobetyolin; all human exposure is indirect, as a trace marker within Codonopsis pilosula (dang shen) preparations, and all efficacy data are cell-line, xenograft or rodent.
| Completed | Planned | Terminated | Preclinical |
|---|---|---|---|
| —(none, isolate) | — | — | Early(anticancer-led) |
Last checked: July 2026.
Toxicity & Safety
No isolate toxicology of concern turned up — but that is absence of data, not a clean bill. The reassurance here is indirect: lobetyolin is a sub-percent trace constituent of a food-grade tonic root with a long dietary history.
- A trace constituent of a food-grade herb. Dang shen has a long dietary and medicinal history, and lobetyolin is present at sub-percent levels.
- Avoid isolated or concentrated use in pregnancy and lactation. No reproductive-safety data.
- No isolate toxicology at all. No genotoxicity, reproductive-toxicity or repeat-dose studies were located for the purified compound.
Full Safety & Interactions Detail
No isolate toxicology of concern was identified. Lobetyolin is a natural trace constituent of dang shen — a food-grade tonic herb with a long dietary and medicinal history, ingested at sub-percent levels in the root — which is a strong if indirect safety signal at dietary exposure, supporting a low flag. No genotoxicity, reproductive-toxicity or repeat-dose isolate studies were located, so this reflects absence of data rather than an affirmative clean bill for concentrated/isolated use.
Dosage
There is no established human dose for isolated lobetyolin — it is a standardization/quality marker, not a dosed supplement. Preclinical figures (in-vitro µM ranges, rodent mg/kg) are experimental exposures, not guidance, and practical human intake occurs only as a trace fraction of Codonopsis pilosula root preparations.
References
- Bailly C (2021). Anticancer properties of lobetyolin, an essential component of Radix Codonopsis (dang shen) — review. Natural Products and Bioprospecting. https://pubmed.ncbi.nlm.nih.gov/33161560/
- Cheng L, Zhai H, Du J, et al. (2023). Lobetyolin inhibits cell proliferation and induces apoptosis by downregulating ASCT2 in gastric cancer. Cytotechnology. https://pubmed.ncbi.nlm.nih.gov/37655270/
- He W, Tao W, Zhang F, et al. (2020). Lobetyolin induces apoptosis of colon cancer cells by inhibiting glutamine metabolism. Journal of Cellular and Molecular Medicine. https://pubmed.ncbi.nlm.nih.gov/31990147/
- Hu J, Wang D, Wang F, et al. (2024). Lobetyolin suppresses the proliferation of hepatocellular carcinoma through activating the DUSP1-ERK1/2 signalling pathway. Biological & Pharmaceutical Bulletin. https://pubmed.ncbi.nlm.nih.gov/39477468/
- Chen Z, Su Y, Ding J, et al. (2024). Lobetyolin protects mice against LPS-induced sepsis by downregulating inflammatory-cytokine production in macrophages. Frontiers in Pharmacology. https://pubmed.ncbi.nlm.nih.gov/38799158/
- Chen Q, Sun Y, Hu X, et al. (2025). The effect and mechanism of Codonopsis Radix and its active components tangshenoside I and lobetyolin on preventing gastric ulcer based on a spectrum-effect relationship. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/40653041/
- Huang W, Liu Y, Jiang H, et al. (2025). Lobetyolin, an anti-Alzheimer factor from a dietary Campanulaceae source: metabolism regulation and target exploration. Natural Products and Bioprospecting. https://pubmed.ncbi.nlm.nih.gov/40938450/
- Xie Q, Wang H, Guan H, et al. (2023). In-vitro/in-vivo metabolic pathways of lobetyol, lobetyolin and lobetyolinin, three polyacetylenes from Codonopsis Radix, by UHPLC-Q/TOF-MS. Journal of Pharmaceutical and Biomedical Analysis. https://pubmed.ncbi.nlm.nih.gov/36356406/
- Dong J, Cheng M, Xue R, et al. (2021). Comparative pharmacokinetic and bioavailability study of lobetyolin in rats after administration of lobetyolin and Codonopsis pilosula extract. Biomedical Chromatography. https://pubmed.ncbi.nlm.nih.gov/33783828/
