Compound Monograph
Albiflorin
Albiflorin is a monoterpene glycoside of peony (Paeonia lactiflora) root and a structural isomer of paeoniflorin, best known for an antidepressant-like and neuroprotective signal in rodent depression models — monoamine modulation, anti-neuroinflammation and HPA/NO normalization — with essentially no standalone human trials of the isolate.
Sources · 5
Where Does It Come From?
Albiflorin is a naturally occurring monoterpene glycoside (pinane-type; a paeoniflorin isomer), found in White peony root, Red peony root and 3 other sources. It is well tolerated orally (low toxicity).
Concentration
Content by Source
Reported concentrations across the plants that contain albiflorin — the bar marks the typical level, the line shows the reported range.
Literature figures for varying plant parts and preparations. Read them as a comparative guide, not exact assays.
Albiflorin at a Glance
Albiflorin is a monoterpene glycoside found in the root of peony (Paeonia lactiflora). It is a structural isomer of paeoniflorin — the two molecules share a formula and a caged pinane skeleton and differ only in the position of the benzoate ester — and they co-occur and are routinely co-quantified in peony root 18,
Its most distinctive research signal is antidepressant-like and neuroprotective activity. In rodent depression models the isolated molecule raises brain monoamines, restores stress-blunted behaviour and normalises stress-axis and nitric-oxide signalling 1,
The honest caveat runs through the whole file: nearly all of the evidence is rodent or in-vitro work on the isolate, human data belong to the whole peony/TGP extract rather than purified albiflorin, and the molecule’s oral bioavailability is very low 14Reference 14Systematic reviewAlbiflorin on neuropsychiatric and neurodegenerative disorders: a systematic reviewView study →.
Albiflorin vs. Paeoniflorin
Albiflorin is almost always discussed next to paeoniflorin, and keeping the two straight is the key to reading its literature.
They are isomers, not the same molecule. Both are pinane-type monoterpene glycosides built on the same paeoniflorin-type skeleton; albiflorin carries its benzoate ester on a different position, which is enough to change its chemistry, its chromatographic behaviour (the two are resolved as a distinct isomer pair by HPLC/UPLC) and — importantly — some of its pharmacology 15,
They are co-quantified but unequally distributed. In Paeonia lactiflora root the two travel together, but albiflorin is consistently more abundant in white peony root than in red peony root, where paeoniflorin dominates 18Reference 18Genetic and chemical characterization of white and red peony root derived from Paeonia lactifloraView study →. Peony pharmacopoeial standards are written around paeoniflorin; albiflorin rides along as the companion glycoside.
Their pharmacology overlaps but is not interchangeable. The clearest demonstration is a PC12-cell study in which the neuroprotective effect belonged to paeoniflorin — “but not the isomer albiflorin” — with paeoniflorin (not albiflorin) suppressing intracellular calcium and CaMKII 11Reference 11Neuroprotective effects of paeoniflorin, but not the isomer albiflorin, are associated with the suppression of intracellular calcium and calcium/calmodulin protein kinase II in PC12 cellsView study →. Yet albiflorin has its own signature the isomer lacks emphasis on: it behaves in rodents as a serotonin/noradrenaline reuptake inhibitor 2Reference 2Antidepressant-like effects of albiflorin: receptor and transporter binding and activity profilesView study →, and much of its antidepressant action is now attributed to a gut-microbial metabolite rather than the parent molecule 6Reference 6Gut-brain axis metabolic pathway regulates antidepressant efficacy of albiflorinView study →. Older peony pharmacology points the same way: the classic neuromuscular-junction blocking studied for peony glycosides was reported for paeoniflorin and its related compounds (albiflorin among them), typically potentiated by co-administered glycyrrhizin from licorice 17Reference 17AnimalBlocking effects of blended paeoniflorin or its related compounds with glycyrrhizin on neuromuscular junctions in frog and mouseView study →. In other words, the two isomers are complementary rather than redundant — a reason the whole TGP fraction, not either molecule alone, is what most human-facing peony products are standardised to.
How Albiflorin’s Antidepressant Effect Works
Albiflorin’s antidepressant-like activity is its best-developed story, and it is unusually multi-route for a single glycoside.
Monoamine modulation. In rats, albiflorin acts as a selective serotonin and noradrenaline reuptake inhibitor — microdialysis showed it raised extracellular 5-HT and noradrenaline in the hypothalamus, with no meaningful affinity at the panel of CNS receptors tested 2Reference 2Antidepressant-like effects of albiflorin: receptor and transporter binding and activity profilesView study →. Behavioural studies echo this: albiflorin raised hippocampal 5-HT, 5-HIAA and noradrenaline and increased hippocampal BDNF while reversing chronic-stress behaviour 1Reference 1Antidepressant-like effects of albiflorin extracted from Radix paeoniae AlbaView study →.
HPA / nitric-oxide normalisation. In chronic-restraint-stress rats, albiflorin restored depressive-like behaviour and hippocampal monoamines by modulating the nitric-oxide-mediated network and the HPA stress cascade 5Reference 5AnimalAntidepressant-like effects of albiflorin involved the NO signaling pathway in rats model of chronic restraint stressView study →, and a companion study tracked its effect on hippocampal BDNF and NO alongside paeoniflorin 4Reference 4AnimalZhang H, et al. (2016). [Investigation of effects of albiflorin and paeoniflorin on hippocampal BDNF and NO in chronic restraint stress rats]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/28933095/View study →.
A gut-brain metabolite route. Strikingly, part of the effect is not the parent molecule at all: gut microbiota hydrolyse albiflorin (via intestinal carboxylesterase) to benzoic acid, which crosses the blood-brain barrier and inhibits D-amino-acid oxidase (DAAO) in the brain — a metabolic gut-brain-axis pathway that helps explain how a poorly-absorbed glycoside produces central effects 6Reference 6Gut-brain axis metabolic pathway regulates antidepressant efficacy of albiflorinView study →.
Metabolic and anti-inflammatory repair. Metabolomic work frames albiflorin as restoring stress-disrupted hippocampal phospholipid and tryptophan metabolism (cPLA2/IDO1 pathways) across several depression models 3Reference 3Targeting hippocampal phospholipid and tryptophan metabolism for antidepressant-like effects of albiflorinView study →, and its anti-neuroinflammatory action (below) reinforces the antidepressant read where inflammation drives mood symptoms 7Reference 7Albiflorin attenuates mood disorders under neuropathic pain state by suppressing the hippocampal NLRP3 inflammasome activation during chronic constriction injuryView study →.
What It's Used For
The evidence base is preclinical and isolate-heavy: rodent behavioural pharmacology plus in-vitro cell work, with the human record belonging to whole peony/TGP rather than purified albiflorin 14Reference 14Systematic reviewAlbiflorin on neuropsychiatric and neurodegenerative disorders: a systematic reviewView study →.
Support is an experimental score — weighted by study type (human > animal > in vitro) and volume. A beta, not a validated metric. There are no standalone human trials of isolated albiflorin, so every score is capped at the preclinical tier by design.
Albiflorin’s flagship application, and the only one with a converging, mechanism-backed rodent literature. The isolated molecule is antidepressant-like across forced-swim, tail-suspension, chronic-unpredictable-stress and chronic-restraint-stress paradigms, at roughly 3.5–14 mg/kg 1,
Mechanistically it behaves as a selective serotonin/noradrenaline reuptake inhibitor (microdialysis: raised extracellular 5-HT and NA, negligible direct receptor binding) 2Reference 2Antidepressant-like effects of albiflorin: receptor and transporter binding and activity profilesView study →, raises hippocampal 5-HT/5-HIAA/NA and BDNF 1Reference 1Antidepressant-like effects of albiflorin extracted from Radix paeoniae AlbaView study →, normalises the HPA and nitric-oxide stress network 5Reference 5AnimalAntidepressant-like effects of albiflorin involved the NO signaling pathway in rats model of chronic restraint stressView study →, repairs stress-disrupted phospholipid/tryptophan metabolism 3Reference 3Targeting hippocampal phospholipid and tryptophan metabolism for antidepressant-like effects of albiflorinView study →, and is partly hydrolysed by gut microbiota to benzoic acid, a brain DAAO inhibitor — a gut-brain-axis route that reconciles central efficacy with poor absorption 6Reference 6Gut-brain axis metabolic pathway regulates antidepressant efficacy of albiflorinView study →.
Gap: every study is rodent on the isolate; there is no standalone human antidepressant trial, and the marquee human peony data are for the whole TGP extract, not purified albiflorin 14Reference 14Systematic reviewAlbiflorin on neuropsychiatric and neurodegenerative disorders: a systematic reviewView study →.
A coherent, mechanism-named secondary signal. In LPS-stimulated BV2 microglia and an MPTP mouse model, albiflorin inhibited microglial NF-κB and MAPK signalling and reduced pro-inflammatory mediators, limiting microglia-driven neuronal apoptosis 8Reference 8Albiflorin ameliorates neuroinflammation and exerts neuroprotective effects in Parkinson’s disease modelsView study →. Under chronic-constriction-injury neuropathic pain with comorbid mood disorder, it suppressed hippocampal NLRP3-inflammasome activation and shifted the Nrf2/NF-κB balance 7Reference 7Albiflorin attenuates mood disorders under neuropathic pain state by suppressing the hippocampal NLRP3 inflammasome activation during chronic constriction injuryView study →; a PC12 corticosterone-apoptosis study found albiflorin (synergistic with saikosaponin A) likewise lowered NLRP3 and repaired metabolic disorder 9Reference 9Synergistic neuroprotective effect of saikosaponin A and albiflorin on corticosterone-induced apoptosis in PC12 cells via regulation of metabolic disorders and neuroinflammationView study →.
Gap: in-vitro microglia/PC12 and rodent models only; the anti-inflammatory concentrations and the isolate-vs-extract translation to humans are uncharacterised 7,
Exploratory neuroprotection beyond mood. Albiflorin inhibited β-amyloid aggregation and reduced the toxicity and ROS of monomeric and oligomeric Aβ in primary hippocampal cells 10Reference 10Inhibition of β-amyloid aggregation by albiflorin, aloeemodin and neohesperidin and their neuroprotective effect on primary hippocampal cells against β-amyloid induced toxicityView study →, and — via its anti-neuroinflammatory action — protected dopaminergic neurons and improved motor deficits in the MPTP Parkinson’s model 8Reference 8Albiflorin ameliorates neuroinflammation and exerts neuroprotective effects in Parkinson’s disease modelsView study →.
This is also where the isomer distinction bites: on a directly comparative PC12 assay the neuroprotective effect (calcium/CaMKII suppression) was paeoniflorin’s, explicitly not albiflorin’s 11Reference 11Neuroprotective effects of paeoniflorin, but not the isomer albiflorin, are associated with the suppression of intracellular calcium and calcium/calmodulin protein kinase II in PC12 cellsView study →.
Gap: cell-culture and acute-toxin rodent models; no disease-modification or human neurodegeneration data, and one head-to-head study assigns the protective effect to the isomer, not albiflorin 10,
A smaller, ion-channel-flavoured signal that dovetails with the CNS mechanisms above. In mouse pain models albiflorin was antinociceptive largely through central calcium-channel involvement (with NOS/5-HT/CaMKII contributions) 13Reference 13AnimalCalcium channels contribute to albiflorin-mediated antinociceptive effects in mouse modelView study →, consistent with in-vitro work showing it reduces glutamate release from cortical nerve terminals by depressing P/Q-type calcium channels and PKA 12Reference 12AnimalAlbiflorin decreases glutamate release from rat cerebral cortex nerve terminals (synaptosomes) through depressing P/Q-type calcium channels and protein kinase A activityView study →.
Gap: rodent and synaptosome models only, mechanistic rather than clinical, and overlapping with the mood/neuropathic-pain literature rather than an independent analgesic use 12,
Mechanisms
| Target / pathway | Effect | Relevant to |
|---|---|---|
| Serotonin & noradrenaline transporters | selective reuptake inhibition → ↑ extracellular 5-HT/NA (microdialysis), little direct receptor binding | antidepressant |
| BDNF / hippocampal monoamines | ↑ hippocampal BDNF, 5-HT, 5-HIAA, noradrenaline in stressed rodents | antidepressant |
| HPA axis & nitric-oxide network | normalises stress-axis and NO/cGMP signalling; restores stress-blunted behaviour | antidepressant |
| Gut microbiota → benzoic acid → brain DAAO | hydrolysed to benzoic acid, which crosses the BBB and inhibits D-amino-acid oxidase | antidepressant (gut-brain axis) |
| cPLA2 / IDO1 (phospholipid & tryptophan metabolism) | reverses stress-disrupted hippocampal lipid/tryptophan metabolism | antidepressant / metabolic |
| Microglial NF-κB & MAPK | suppresses microglial activation and pro-inflammatory mediators | anti-neuroinflammation |
| NLRP3 inflammasome / Nrf2 | inhibits NLRP3 activation, favours Nrf2 antioxidant signalling | anti-neuroinflammation |
| β-amyloid aggregation | inhibits Aβ aggregation and Aβ-induced ROS/toxicity | neurodegeneration (in vitro) |
| P/Q-type Ca²⁺ channels / PKA | depresses presynaptic Ca²⁺ entry → ↓ glutamate release | antinociceptive |
The load-bearing point is that albiflorin’s central effects are reached through several parallel routes — monoamine reuptake, HPA/NO normalisation, a gut-microbial benzoic-acid metabolite, and anti-neuroinflammation — rather than one receptor, and that a head-to-head assay put classical neuroprotection on the isomer paeoniflorin instead 11Reference 11Neuroprotective effects of paeoniflorin, but not the isomer albiflorin, are associated with the suppression of intracellular calcium and calcium/calmodulin protein kinase II in PC12 cellsView study →.
Pharmacokinetics
Albiflorin is a polar monoterpene glycoside and, like its isomer, is poorly absorbed orally — rapidly absorbed and rapidly eliminated, with very low oral bioavailability and low brain concentrations after dosing 14Reference 14Systematic reviewAlbiflorin on neuropsychiatric and neurodegenerative disorders: a systematic reviewView study →. This is the file’s central PK paradox: a molecule that barely reaches the brain nonetheless produces central antidepressant effects, which the gut-microbiota → benzoic acid → brain-DAAO pathway helps explain (an active metabolite doing part of the work) 6Reference 6Gut-brain axis metabolic pathway regulates antidepressant efficacy of albiflorinView study →. Because albiflorin and paeoniflorin are isomers, they are co-analysed in peony PK studies — UPLC-MS/MS work on single-herb Radix Paeoniae Alba decoction and on the Total Glucosides of White Paeony capsule reports distinct plasma profiles for the two, with formula context altering albiflorin’s AUC and residence time 15,
Clinical Trials
There are no controlled efficacy trials of isolated albiflorin. The human peony evidence belongs to the whole Total Glucosides of Paeony extract and to peony-containing formulas, within which albiflorin is one co-quantified glycoside — not to the purified molecule 14Reference 14Systematic reviewAlbiflorin on neuropsychiatric and neurodegenerative disorders: a systematic reviewView study →.
| Completed | Planned | Terminated | Preclinical |
|---|---|---|---|
| None for the isolate (human data are the whole TGP extract) | — | — | Extensive: rodent antidepressant + anti-neuroinflammation + neurodegeneration models |
Last checked: July 2026.
Isolate vs. Plant Studies
Albiflorin sits on the isolate-heavy end of the spectrum, which is both a strength and the main caveat. The mechanistic and behavioural work is overwhelmingly the purified molecule in rodents and cells — the reuptake-inhibition microdialysis 2Reference 2Antidepressant-like effects of albiflorin: receptor and transporter binding and activity profilesView study →, the chronic-stress antidepressant series 1,
The human side, by contrast, is a plant extract. Peony’s clinical footprint runs through the standardised TGP fraction and peony-containing formulas, where albiflorin is a minor, co-quantified partner to paeoniflorin — so the whole-extract effects cannot be attributed to albiflorin alone 14,
Prevalence in Nature
Albiflorin is largely restricted to the genus Paeonia, where it is a principal monoterpene glycoside of the root. It co-occurs with its isomer paeoniflorin and with related glycosides such as oxypaeoniflorin and the galloyl ester 6-O-galloylalbiflorin, plus the acetophenone paeonol 18,
Its concentration tracks the white-vs-red processing of peony root. In a chemical characterisation of Paeonia lactiflora-derived material, albiflorin ran from about 1.5–19.7 mg/g in white peony root (roughly 0.15–2% of the dried root) but only 0.5–2.3 mg/g in red peony root, i.e. it is consistently richer in white than in red peony root — the mirror image of paeoniflorin and paeonol, which concentrate in red root 18Reference 18Genetic and chemical characterization of white and red peony root derived from Paeonia lactifloraView study →. This makes albiflorin part of the chemotype fingerprint that distinguishes the peony forms.
Discovery & Synthesis
Albiflorin was isolated from peony root in the mid-twentieth-century phytochemical work that resolved Paeonia lactiflora’s monoterpene-glycoside complex, and it takes its name from the plant’s old botanical synonym Paeonia albiflora (Pallas) — the “white-flowered peony” now folded into P. lactiflora. It was characterised alongside its dominant isomer paeoniflorin, from which it differs only in the position of the benzoate ester, and the two have been studied as an isomer pair ever since 15,
Manufacture today is by extraction from peony root (and from the Total Glucosides of Paeony fraction), not by total synthesis: albiflorin is obtained as a co-eluting partner of paeoniflorin and separated chromatographically. No well-documented total synthesis is established for the molecule; microbial biotransformation of the peony glycosides has been explored as a route to related structures 15Reference 15AnimalPharmacokinetic comparisons by UPLC-MS/MS of isomer paeoniflorin and albiflorin after oral administration decoctions of single-herb Radix Paeoniae Alba and Zengmian Yiliu prescription to ratsView study →.
Patents: not yet researched.
Toxicity & Safety
Albiflorin carries a low flag. It is a monoterpene glycoside of an edible/medicinal root with a long history of use as part of peony preparations, it is studied in rodents at low milligram-per-kilogram doses without reported organ toxicity, and its very poor oral bioavailability limits systemic exposure of the parent molecule 14Reference 14Systematic reviewAlbiflorin on neuropsychiatric and neurodegenerative disorders: a systematic reviewView study →. The important qualifier is not a danger signal but a data gap: dedicated single-molecule safety, genotoxicity and reproductive-toxicity packages for isolated albiflorin are largely absent, and most human exposure is as a minor component of the whole peony/TGP extract rather than the isolate.
- Low apparent toxicity. A peony-root monoterpene glycoside studied in rodents at low mg/kg doses with no reported organ toxicity, and with very low oral bioavailability limiting parent-molecule exposure 14Reference 14Systematic reviewAlbiflorin on neuropsychiatric and neurodegenerative disorders: a systematic reviewView study →.
- Human data are the extract, not the isolate. Safety and efficacy in people rest on whole peony / Total Glucosides of Paeony preparations, where albiflorin is one co-quantified glycoside among many 14,
18Reference 14Systematic reviewAlbiflorin on neuropsychiatric and neurodegenerative disorders: a systematic reviewView study →Reference 18Genetic and chemical characterization of white and red peony root derived from Paeonia lactifloraView study → . - Limited single-molecule safety dataset. No comprehensive isolate genotoxicity/repeat-dose/reproductive package is characterised; absence of findings is not evidence of safety.
- Interactions not formally mapped. Drug-interaction, CYP/transporter and pregnancy questions are decided on the herb or product page where intake happens, not on this molecule page.
Dosage
There is no established or recommended human dose for isolated albiflorin. The figures in the literature are preclinical rodent research doses — the antidepressant studies commonly used 3.5, 7 and 14 mg/kg in mice and rats 1,
In practice, human exposure to albiflorin is indirect: it arrives as a minor constituent of peony root and, most relevantly, of the standardised Total Glucosides of Paeony (TGP) extract, which is dosed and studied as a whole fraction rather than as purified albiflorin 14,
References
- Wang YL, et al. (2016). Antidepressant-like effects of albiflorin extracted from Radix paeoniae Alba. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/26719283/
- Jin ZL, et al. (2016). Antidepressant-like effects of albiflorin: receptor and transporter binding and activity profiles. Scientific Reports. https://pubmed.ncbi.nlm.nih.gov/27646789/
- Wang J, et al. (2021). Targeting hippocampal phospholipid and tryptophan metabolism for antidepressant-like effects of albiflorin. Phytomedicine. https://pubmed.ncbi.nlm.nih.gov/34601221/
- Zhang H, et al. (2016). [Investigation of effects of albiflorin and paeoniflorin on hippocampal BDNF and NO in chronic restraint stress rats]. Zhongguo Zhong Yao Za Zhi. https://pubmed.ncbi.nlm.nih.gov/28933095/
- Zhu YL, Wang LY, Zhao DP, et al. (2020). Antidepressant-like effects of albiflorin involved the NO signaling pathway in rats model of chronic restraint stress. Chinese Journal of Natural Medicines. https://pubmed.ncbi.nlm.nih.gov/33308610/
- Zhao HB, et al. (2018). Gut-brain axis metabolic pathway regulates antidepressant efficacy of albiflorin. Theranostics. https://pubmed.ncbi.nlm.nih.gov/30613273/
- Liu Y, et al. (2021). Albiflorin attenuates mood disorders under neuropathic pain state by suppressing the hippocampal NLRP3 inflammasome activation during chronic constriction injury. International Journal of Neuropsychopharmacology. https://pubmed.ncbi.nlm.nih.gov/33000169/
- Gao Y, et al. (2025). Albiflorin ameliorates neuroinflammation and exerts neuroprotective effects in Parkinson’s disease models. Immunopharmacology and Immunotoxicology. https://pubmed.ncbi.nlm.nih.gov/39924948/
- Li J, et al. (2022). Synergistic neuroprotective effect of saikosaponin A and albiflorin on corticosterone-induced apoptosis in PC12 cells via regulation of metabolic disorders and neuroinflammation. Molecular Biology Reports. https://pubmed.ncbi.nlm.nih.gov/36002654/
- Ho SL, Poon CY, Lin C, et al. (2015). Inhibition of β-amyloid aggregation by albiflorin, aloeemodin and neohesperidin and their neuroprotective effect on primary hippocampal cells against β-amyloid induced toxicity. Current Alzheimer Research. https://pubmed.ncbi.nlm.nih.gov/25938872/
- Wang K, et al. (2013). Neuroprotective effects of paeoniflorin, but not the isomer albiflorin, are associated with the suppression of intracellular calcium and calcium/calmodulin protein kinase II in PC12 cells. Journal of Molecular Neuroscience. https://pubmed.ncbi.nlm.nih.gov/23695964/
- Lin TY, et al. (2024). Albiflorin decreases glutamate release from rat cerebral cortex nerve terminals (synaptosomes) through depressing P/Q-type calcium channels and protein kinase A activity. International Journal of Molecular Sciences. https://pubmed.ncbi.nlm.nih.gov/39201534/
- Zhang XJ, et al. (2016). Calcium channels contribute to albiflorin-mediated antinociceptive effects in mouse model. Neuroscience Letters. https://pubmed.ncbi.nlm.nih.gov/27038516/
- Sun Y, et al. (2025). Albiflorin on neuropsychiatric and neurodegenerative disorders: a systematic review. CNS Neuroscience & Therapeutics. https://pubmed.ncbi.nlm.nih.gov/40708436/
- Gong X, et al. (2015). Pharmacokinetic comparisons by UPLC-MS/MS of isomer paeoniflorin and albiflorin after oral administration decoctions of single-herb Radix Paeoniae Alba and Zengmian Yiliu prescription to rats. Biomedical Chromatography. https://pubmed.ncbi.nlm.nih.gov/25042570/
- Feng C, et al. (2016). Sensitive analysis and pharmacokinetic study of the isomers paeoniflorin and albiflorin after oral administration of Total Glucosides of White Paeony capsule in rats. Journal of Chromatography B. https://pubmed.ncbi.nlm.nih.gov/27070118/
- Kimura M, et al. (1984). Blocking effects of blended paeoniflorin or its related compounds with glycyrrhizin on neuromuscular junctions in frog and mouse. Japanese Journal of Pharmacology. https://pubmed.ncbi.nlm.nih.gov/6521072/
- Shu Z, et al. (2015). Genetic and chemical characterization of white and red peony root derived from Paeonia lactiflora. Journal of Natural Medicines. https://pubmed.ncbi.nlm.nih.gov/25151277/
- Washida K, et al. (2009). Androgen modulators from the roots of Paeonia lactiflora (paeoniae radix) grown and processed in Nara prefecture, Japan. Chemical & Pharmaceutical Bulletin. https://pubmed.ncbi.nlm.nih.gov/19721258/
