Compound Monograph
Asiaticoside
Asiaticoside is the principal ursane-type triterpenoid saponin of gotu kola (Centella asiatica) — the marker behind the herb's wound-healing and scar reputation, acting on fibroblast collagen synthesis via TGF-β/Smad signalling, with anti-inflammatory and preclinical neuro/cognitive data. Poorly absorbed orally, it is hydrolysed to its aglycone asiatic acid, the main circulating form.
Sources · 2
Where Does It Come From?
Asiaticoside is a naturally occurring ursane-type triterpenoid saponin (glycoside), found in Gotu kola and 1 other source. It is well tolerated orally (low toxicity).
Concentration
Content by Source
Reported concentrations across the plants that contain asiaticoside — 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.
Asiaticoside at a Glance
Asiaticoside is the principal ursane-type triterpenoid saponin of gotu kola (Centella asiatica) and the marker compound behind the herb’s centuries-old reputation for wound healing and connective-tissue repair. Its aglycone is asiatic acid, and it co-occurs with the oleanane saponin madecassoside (whose aglycone is madecassic acid) in the standardised “centelloside” fraction used clinically.
The honest evidence posture: the strongest, most real-world signal is topical — asiaticoside drives fibroblast collagen synthesis and appears in the long-marketed Centella extracts (TECA / Madecassol / TTFCA) for wounds and scars. The oral story is complicated by pharmacology — asiaticoside is barely absorbed intact and is hydrolysed to asiatic acid before it reaches the circulation, so much of what “oral asiaticoside” does is really asiatic-acid activity. Almost every positive human result used a standardised extract, not the isolated saponin. Safety is reassuring at culinary/therapeutic levels (low), with one historical topical tumour-promotion finding worth flagging.
Established Uses
Asiaticoside’s one genuinely established, real-world role is topical skin and wound repair. It is a defined active of the Centella asiatica titrated extracts marketed for decades — TECA (titrated extract of Centella asiatica), TTFCA, and the topical Madecassol — used for wounds, burns, and hypertrophic/scar management 7,
Asiaticoside vs. Asiatic Acid — The Prodrug Relationship
The single most important fact for reading asiaticoside’s evidence is that the glycoside and its aglycone are not interchangeable across routes. Asiaticoside is a large, polar trisaccharide saponin: applied topically it acts directly on skin fibroblasts, but taken orally it is poorly absorbed and extensively hydrolysed by gut microbiota to asiatic acid, which is the main triterpene actually measured in plasma 18,
Human pharmacokinetic studies make this stark — after oral standardised Centella extract, the parent glycosides asiaticoside and madecassoside are rarely or not detectable in plasma, while their aglycones asiatic acid and madecassic acid rise dose-dependently 19,
- Topical claims (collagen, scar, wound) can reasonably be attributed to asiaticoside itself acting on fibroblasts 1,
3, .5Reference 1In vitroIn vitro and in vivo wound healing activity of asiaticoside isolated from Centella asiaticaView study →Reference 3Asiaticoside induces human collagen I synthesis through TGFβ receptor I kinase (TβRI kinase)-independent Smad signalingView study →Reference 5Asiaticoside suppresses collagen expression and TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblastsView study → - Oral / systemic claims (cognition, mood, systemic anti-inflammatory) are better read as asiatic-acid effects downstream of asiaticoside, and belong as much to asiatic acid as to this molecule 19Reference 19Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteersView study →.
This is why the page keeps the isolate-vs-plant and route distinctions explicit throughout.
What It's Used For
The evidence divides cleanly by route: a mechanistically solid, clinically-adjacent topical/fibroblast base, and a preclinical (in-vitro / rodent) systemic base whose oral relevance is capped by the poor bioavailability above.
Support is an experimental score — weighted by study type (human > animal > in vitro) and volume. A beta, not a validated metric. Human data is extract-level (not isolate), so scores stay measured by design.
Asiaticoside’s marquee and best-supported activity. The isolated saponin accelerated wound healing in rat and guinea-pig models, increasing collagen content, tensile strength and epithelialisation in both normal and delayed (diabetic) wounds 1Reference 1In vitroIn vitro and in vivo wound healing activity of asiaticoside isolated from Centella asiaticaView study →, and raised wound-tissue antioxidant enzymes (SOD, catalase, glutathione peroxidase) while lowering lipid peroxides in early healing 2Reference 2Asiaticoside-induced elevation of antioxidant levels in healing woundsView study →.
Mechanistically, asiaticoside induces human type I collagen synthesis via a TGF-β-receptor-kinase-independent Smad pathway in fibroblasts 3Reference 3Asiaticoside induces human collagen I synthesis through TGFβ receptor I kinase (TβRI kinase)-independent Smad signalingView study →, and drives collagen/fibronectin production in periodontal-ligament cells 4Reference 4Asiaticoside induces type I collagen synthesis and osteogenic differentiation in human periodontal ligament cellsView study →.
It is a defined active of the marketed Centella topicals (TECA/Madecassol) used for wounds and burns 7,
Gap: the controlled efficacy data are rodent/in-vitro or use the whole standardised extract; there is no modern RCT of isolated asiaticoside on human wounds.
A biphasic, context-dependent effect that is the interesting part of the collagen story. In normal fibroblasts asiaticoside promotes collagen (pro-healing), but in keloid fibroblasts it suppresses collagen and TGF-β/Smad signalling — inducing the inhibitory Smad7 and down-regulating TGF-β receptors I and II 5Reference 5Asiaticoside suppresses collagen expression and TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblastsView study →.
This dual behaviour underpins its candidacy in keloid/hypertrophic-scar management 6Reference 6Molecular signalings in keloid disease and current therapeutic approaches from natural based compoundsView study → and its appearance in anti-scarring formulations.
Gap: keloid-fibroblast data are in-vitro; the clinical scar evidence rests on the extract (Madecassol/TECA), not the pure saponin, so the isolate’s stand-alone anti-scar efficacy in humans is unproven 5,
A consistent preclinical signal. Asiaticoside was antipyretic and anti-inflammatory in LPS-challenged rats, dose-dependently lowering fever and inflammatory markers, partly via heme oxygenase-1 (HO-1) induction 10Reference 10AnimalAntipyretic and anti-inflammatory effects of asiaticoside in lipopolysaccharide-treated rat through up-regulation of heme oxygenase-1View study →. A Centella extract standardised to asiaticoside reduced inflammatory cytokines in a DNCB-induced atopic-dermatitis model 11Reference 11AnimalInhibitory effect of Centella asiatica extract on DNCB-induced atopic dermatitis in HaCaT cells and BALB/c miceView study →, and mechanistic reviews attribute broad NF-κB-linked anti-inflammatory activity to the centellosides 16,
Gap: rodent/in-vitro; the effective tissue concentrations are unlikely to be reached from oral saponin given its poor absorption, and the systemic effect is plausibly asiatic-acid-mediated 10,
The systemic-neuro signal that motivates gotu kola’s “brain tonic” reputation — but note the prodrug caveat throughout. Asiaticoside ameliorated β-amyloid-induced learning and memory deficits in rats, reducing mitochondrial apoptosis and neuroinflammation 12Reference 12AnimalAsiaticoside ameliorates β-amyloid-induced learning and memory deficits in rats by inhibiting mitochondrial apoptosis and reducing inflammatory factorsView study →, protected neurons against glutamate excitotoxicity by limiting calcium influx 13Reference 13Neuroprotective effects of asiaticosideView study →, and promoted neurite outgrowth via sustained ERK signalling in Neuro-2a cells 14Reference 14Differences in neuritogenic activity and signaling activation of madecassoside, asiaticoside, and their aglycones in Neuro-2a cellsView study →.
It sits within a broader Centella neuroprotection/cognitive-enhancement literature 16Reference 16Centella asiatica — phytochemistry and mechanisms of neuroprotection and cognitive enhancementView study →.
Gap: entirely preclinical (rodent/in-vitro); since oral asiaticoside is barely absorbed and converts to asiatic acid, the systemic neuro effects belong as much to the aglycone as to this saponin 16,
The thinnest of the ranked signals. Asiaticoside produced an antidepressant-like effect in a chronic-unpredictable-mild-stress mouse model, associated with PKA/pCREB/BDNF signalling and reduced neuroinflammation 15Reference 15AnimalAsiaticoside produces an antidepressant-like effect in a chronic unpredictable mild stress model of depression in mice, involving reversion of inflammation and the PKA/pCREB/BDNF signaling pathwayView study →.
Gap: a single rodent model, single molecule, no human data, and the oral-bioavailability caveat applies in full 15,
Mechanisms
| Target / pathway | Effect | Relevant to |
|---|---|---|
| Type I collagen synthesis (TGF-β-receptor-kinase-independent Smad) | induced in normal fibroblasts | wound healing / collagen |
| Fibroblast / periodontal-ligament-cell proliferation | increased collagen + fibronectin | wound healing |
| Wound-tissue antioxidant enzymes (SOD, catalase, GPx) | up-regulated; lipid peroxides down | wound healing |
| TGF-β/Smad in keloid fibroblasts (Smad7 ↑, TβRI/TβRII ↓) | collagen suppressed | scar / keloid modulation |
| Heme oxygenase-1 (HO-1) | induced → antipyretic/anti-inflammatory | anti-inflammatory |
| Inflammatory cytokines / NF-κB axis | lowered | anti-inflammatory |
| Mitochondrial apoptosis; neuroinflammation (β-amyloid model) | reduced | cognition / neuroprotection |
| Glutamate/NMDA-linked Ca²⁺ influx | limited → neuroprotection | neuroprotection |
| ERK signalling → neurite outgrowth | activated | neuroprotection |
| PKA / pCREB / BDNF | up-regulated | antidepressant-like |
Pharmacokinetics
Asiaticoside behaves like a classic saponin glycoside: large, polar, poorly membrane-permeant, and a poor oral-bioavailability drug. After oral standardised Centella extract in humans, the parent glycosides asiaticoside and madecassoside are rarely or not detected in plasma, while their aglycones — asiatic acid and madecassic acid — appear and rise dose-dependently 19,
Clinical Trials
There are no clinical trials of isolated asiaticoside. Human data come from standardised Centella asiatica extracts (ECa 233 oral capsules; TECA/TTFCA/Madecassol topicals), whose effects cannot be attributed to this single saponin — especially given that it barely reaches the circulation intact 18,
| Completed | Planned | Terminated | Preclinical |
|---|---|---|---|
| —(none, isolate); extract-level PK/safety only 18Reference 18Safety and pharmacokinetics of standardized extract of Centella asiatica (ECa 233) capsules in healthy Thai volunteersView study → | — | — | Substantial(wound/collagen-, anti-inflammatory-, neuro-led) |
Last checked: July 2026.
Isolate vs. Plant Studies
The split is sharp. Mechanistic and topical work uses the isolated saponin — the collagen-induction, keloid-suppression, antipyretic and neurite studies are all pure-compound experiments 1,
Prevalence in Nature
Asiaticoside is essentially a Centella asiatica compound — one of the four “centelloside” markers (with madecassoside, asiatic acid and madecassic acid) 16,
Discovery & Synthesis
Asiaticoside was isolated from Centella asiatica in the 1940s (attributed to Bontems), and the titrated topical extract Madecassol was pharmacologically characterised through the 1950s–70s — early work studied its action on granulation tissue and cultured fibroblasts, with clinical application to systemic scleroderma 7Reference 7Studies on the mechanism of action of asiaticoside (Madecassol) on experimental granulation tissue and cultured fibroblasts and its clinical application in systemic sclerodermaView study →. Structurally it is the ursane-type aglycone asiatic acid bearing a trisaccharide (glucose-glucose-rhamnose) at C-28, closely related to the pentacyclic triterpene acids ursolic acid and oleanolic acid; the plant sterol β-sitosterol is a common co-occurring lipid.
A practical total synthesis is not well documented — asiaticoside is obtained by extraction from C. asiatica (the economically dominant route, since the plant accumulates it and the standardised fractions are the commercial products), not by synthesis. Semi-synthetic access to the aglycone/derivatives exists for research, but manufacture today is extractive.
Patents: not yet researched (future patent-loop pass).
Toxicity & Safety
Asiaticoside carries a low flag, consistent with gotu kola’s long culinary and medicinal use and the good tolerability of standardised extracts in human PK/safety studies 18Reference 18Safety and pharmacokinetics of standardized extract of Centella asiatica (ECa 233) capsules in healthy Thai volunteersView study →. Poor oral absorption further limits systemic exposure. The centellosides are broadly antioxidant rather than pro-oxidant 24Reference 24Comparison of the antioxidant potency of four triterpenes of Centella asiatica against oxidative stressView study →, and a Centella triterpene fraction was protective (not toxic) against cyclophosphamide-induced immune/hepatic dysfunction in rats 25Reference 25AnimalProtective effect of centella triterpene saponins against cyclophosphamide-induced immune and hepatic system dysfunction in ratsView study →.
Two honest caveats keep this from being a blank cheque. First, a historical topical finding: repeated skin application of asiaticoside (with cantharidin) produced epidermal tumours and reticuloses in hairless mice, seeding a long-running debate about high-dose topical genotoxicity/tumour-promotion 23Reference 23AnimalReticuloses and epidermal tumors in hairless mice after topical skin applications of cantharidin and asiaticosideView study →. This is an old, high-dose animal model and has not been borne out in the decades of clinical topical use, but it is why the genotoxicity question is still raised for concentrated topicals. Second, interactions are not comprehensively characterised for the isolate; the reassuring signal is that a Centella water extract showed low CYP450-interaction potential in vitro 21Reference 21Centella asiatica water extract shows low potential for cytochrome P450-mediated drug interactionsView study →. Any reproductive-safety decision belongs on the gotu-kola herb and supplement pages, not here.
- Low toxicity at culinary/therapeutic levels. Long food/medicinal use; standardised extracts well tolerated in human PK/safety studies 18Reference 18Safety and pharmacokinetics of standardized extract of Centella asiatica (ECa 233) capsules in healthy Thai volunteersView study →.
- Poor oral absorption limits systemic exposure, and a Centella extract showed low CYP450-interaction potential in vitro 19,
21Reference 19Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteersView study →Reference 21Centella asiatica water extract shows low potential for cytochrome P450-mediated drug interactionsView study → . - Historical topical tumour-promotion finding. Epidermal tumours in hairless mice after repeated high-dose topical asiaticoside — the basis of the genotoxicity debate for concentrated topicals 23Reference 23AnimalReticuloses and epidermal tumors in hairless mice after topical skin applications of cantharidin and asiaticosideView study →.
- Interactions not fully characterised for the isolate, and pregnancy/lactation is a herb/supplement-level decision, not settled here.
Dosage
There is no established dose for isolated asiaticoside — it has not been dosed as a pure compound in humans, and its poor oral absorption means intact-saponin dosing would be pharmacologically inefficient. Real-world exposure is via standardised Centella asiatica extracts:
| Application | Form | Exposure |
|---|---|---|
| Cognitive / systemic (research) | Oral standardised extract (e.g. ECa 233 capsules) | Studied in healthy-volunteer PK/safety trials; asiaticoside itself barely enters plasma 18, |
| Wound / scar (topical) | TECA / TTFCA / Madecassol cream/ointment | Standardised to defined asiaticoside + madecassoside content 7, |
These are exposures studied in research and are not a personal recommendation.
References
- Shukla A, et al. (1999). In vitro and in vivo wound healing activity of asiaticoside isolated from Centella asiatica. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/10350364/
- Shukla A, et al. (1999). Asiaticoside-induced elevation of antioxidant levels in healing wounds. Phytotherapy Research. https://pubmed.ncbi.nlm.nih.gov/10189951/
- Lee J, et al. (2006). Asiaticoside induces human collagen I synthesis through TGFβ receptor I kinase (TβRI kinase)-independent Smad signaling. Planta Medica. https://pubmed.ncbi.nlm.nih.gov/16557473/
- Nowwarote N, et al. (2013). Asiaticoside induces type I collagen synthesis and osteogenic differentiation in human periodontal ligament cells. Phytotherapy Research. https://pubmed.ncbi.nlm.nih.gov/22628285/
- Tang B, et al. (2011). Asiaticoside suppresses collagen expression and TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts. Archives of Dermatological Research. https://pubmed.ncbi.nlm.nih.gov/21240513/
- Unahabhokha T, et al. (2015). Molecular signalings in keloid disease and current therapeutic approaches from natural based compounds. Pharmaceutical Biology. https://pubmed.ncbi.nlm.nih.gov/25331681/
- Sasaki S, et al. (1972). Studies on the mechanism of action of asiaticoside (Madecassol) on experimental granulation tissue and cultured fibroblasts and its clinical application in systemic scleroderma. Acta Dermato-Venereologica. https://pubmed.ncbi.nlm.nih.gov/4127803/
- Bylka W, et al. (2013). Centella asiatica in cosmetology. Postępy Dermatologii i Alergologii. https://pubmed.ncbi.nlm.nih.gov/24278045/
- Agra LC, et al. (2015). Triterpenes with healing activity: a systematic review. Journal of Dermatological Treatment. https://pubmed.ncbi.nlm.nih.gov/25893368/
- Wan J, et al. (2013). Antipyretic and anti-inflammatory effects of asiaticoside in lipopolysaccharide-treated rat through up-regulation of heme oxygenase-1. Phytotherapy Research. https://pubmed.ncbi.nlm.nih.gov/22972613/
- Lee JH, et al. (2020). Inhibitory effect of Centella asiatica extract on DNCB-induced atopic dermatitis in HaCaT cells and BALB/c mice. Nutrients. https://pubmed.ncbi.nlm.nih.gov/32033291/
- Zhang Z, et al. (2017). Asiaticoside ameliorates β-amyloid-induced learning and memory deficits in rats by inhibiting mitochondrial apoptosis and reducing inflammatory factors. Experimental and Therapeutic Medicine. https://pubmed.ncbi.nlm.nih.gov/28352309/
- Qi FY, et al. (2014). Neuroprotective effects of asiaticoside. Neural Regeneration Research. https://pubmed.ncbi.nlm.nih.gov/25221579/
- Nalinratana N, et al. (2018). Differences in neuritogenic activity and signaling activation of madecassoside, asiaticoside, and their aglycones in Neuro-2a cells. Planta Medica. https://pubmed.ncbi.nlm.nih.gov/29719882/
- Wang L, et al. (2020). Asiaticoside produces an antidepressant-like effect in a chronic unpredictable mild stress model of depression in mice, involving reversion of inflammation and the PKA/pCREB/BDNF signaling pathway. Molecular Medicine Reports. https://pubmed.ncbi.nlm.nih.gov/32705202/
- Gray NE, et al. (2018). Centella asiatica — phytochemistry and mechanisms of neuroprotection and cognitive enhancement. Phytochemistry Reviews. https://pubmed.ncbi.nlm.nih.gov/31736679/
- Bandopadhyay S, et al. (2023). Therapeutic properties and pharmacological activities of asiaticoside and madecassoside: a review. Journal of Cellular and Molecular Medicine. https://pubmed.ncbi.nlm.nih.gov/36756687/
- Songvut P, et al. (2019). Safety and pharmacokinetics of standardized extract of Centella asiatica (ECa 233) capsules in healthy Thai volunteers. Planta Medica. https://pubmed.ncbi.nlm.nih.gov/30699457/
- Songvut P, et al. (2021). Pharmacokinetics and metabolomics investigation of an orally modified formula of standardized Centella asiatica extract in healthy volunteers. Scientific Reports. https://pubmed.ncbi.nlm.nih.gov/33767223/
- Wright KM, et al. (2023). Bioanalytical method validation and application to a phase 1, double-blind, randomized pharmacokinetic trial of a standardized Centella asiatica (L.) Urban water extract product in healthy older adults. Frontiers in Pharmacology. https://pubmed.ncbi.nlm.nih.gov/37680716/
- Wright KM, et al. (2020). Centella asiatica water extract shows low potential for cytochrome P450-mediated drug interactions. Drug Metabolism and Disposition. https://pubmed.ncbi.nlm.nih.gov/32581050/
- Boonyarattanasoonthorn T, et al. (2022). Increase water solubility of Centella asiatica extract by indigenous bioenhancers could improve oral bioavailability and disposition kinetics of triterpenoid glycosides in beagle dogs. Scientific Reports. https://pubmed.ncbi.nlm.nih.gov/35190633/
- Laerum OD, Iversen OH (1972). Reticuloses and epidermal tumors in hairless mice after topical skin applications of cantharidin and asiaticoside. Cancer Research. https://pubmed.ncbi.nlm.nih.gov/4113114/
- Lim W, et al. (2024). Comparison of the antioxidant potency of four triterpenes of Centella asiatica against oxidative stress. Antioxidants. https://pubmed.ncbi.nlm.nih.gov/38671930/
- Duggina P, et al. (2015). Protective effect of centella triterpene saponins against cyclophosphamide-induced immune and hepatic system dysfunction in rats. Journal of Physiology and Biochemistry. https://pubmed.ncbi.nlm.nih.gov/26168711/
