a seco-iridoid glycoside abundant in Gentiana species. Beyond its well-known oral pharmacology, several recent studies show that GPS can be delivered topically to support skin health thanks to a cluster of anti-inflammatory, antioxidant, anti-glycation and pro-healing activities.
Gentiopicroside (GPS, sometimes called gentiopicrin) is a seco-iridoid glycoside abundant in Gentiana species. Beyond its well-known oral pharmacology, several recent studies show that GPS can be delivered topically to support skin health thanks to a cluster of anti-inflammatory, antioxidant, anti-glycation and pro-healing activities. pmc.ncbi.nlm.nih.gov
1. Anti-inflammatory & Antioxidant Shield
- Cellular studies – GPS lowers ROS and suppresses NF-κB / MAPK signalling in TNF-α- or IFN-γ-stimulated keratinocytes, partly by releasing Nrf2 from Keap1, thereby reducing IL-6, IL-23A and other cytokines. mdpi.com pubmed.ncbi.nlm.nih.gov
- Inflammation-driven skin models – In mouse models of atopic-like dermatitis, topical or intradermal GPS markedly cut epidermal thickness and inflammatory cell infiltration, again via Nrf2 up-regulation. pubmed.ncbi.nlm.nih.gov
Formulation takeaway: These pathways are triggered at low micromolar GPS, making 0.05 – 0.5 % w/w a pragmatic starting range for soothing gels or serums.
2. Anti-psoriatic Activity
- GPS-loaded chitosan nanoparticles (≈ 100 nm) inhibited HaCaT keratinocyte hyper-proliferation, down-regulated K17/VEGF-A expression, and visibly improved erythema and scaling in imiquimod-induced psoriatic mice. pmc.ncbi.nlm.nih.gov researchgate.net
- Free GPS likewise relieved psoriasiform lesions through Keap1–Nrf2 signalling; the effect was lost in Nrf2-knock-out mice, confirming a direct antioxidative-anti-inflammatory mechanism. pubmed.ncbi.nlm.nih.gov
3. Wound & Ulcer Healing
- Pressure-injury model (rats): local GPS injections accelerated re-epithelialisation and cut inflammatory cell counts compared with saline. pmc.ncbi.nlm.nih.gov
- Diabetic ulcers (mice): topical GPS re-activated the AKT1 → HIF-1α → VEGF pathway, boosting angiogenesis, collagen deposition and granulation-tissue formation, which closed wounds faster than control dressings. pmc.ncbi.nlm.nih.gov
The pro-healing profile makes GPS a candidate for hydrogels, hydrocolloid dressings or spray-on emulsions aimed at chronic wounds.
4. Anti-glycation & “Inflamm-aging” Defence
Dermal fibroblasts exposed to glyoxal-derived AGEs showed restored viability, reduced MMP-1 and better ECM homeostasis when pre-treated with GPS, supporting its use as an AGE-breaker to delay wrinkle formation and stiffness in photo-exposed skin. nature.com
5. UV-related Skin Injury (Emerging Patent Evidence)
A recent Chinese patent describes a GPS–eriocitrin complex for cosmetics that “effectively treats and relieves skin injury caused by ultraviolet induction,” pointing toward future photoprotective or after-sun applications. patents.google.com
6. Physicochemical & Formulation Notes
| Property |
Practical implication |
| Water solubility ≈ 20 mg mL⁻¹ (room T) |
GPS can be dissolved directly into aqueous or hydroalcoholic phases; no harsh solvents needed. chemicalbook.com |
| Slight solubility in ethanol, DMSO |
Use ≤ 15 % ethanol for clear solutions; pair with humectants to prevent crystallisation. |
| pH stability 4 – 7 |
Compatible with most leave-on and rinse-off formats. |
| Suggested use level |
0.05 – 2 % w/w (higher for masks or patches). |
| Synergistic carriers |
Chitosan, hyaluronic acid, phospholipid liposomes, or low-viscosity hydro-gels enhance residence time and penetration. |
7. Formulation Guidance at a Glance
- Dissolve GPS in the aqueous phase (40 – 50 °C) or create a concentrated 5 – 10 % stock in water + 10 % propanediol for easy dosing.
- Combine with calming humectants (panthenol, β-glucan) if targeting irritated skin.
- Avoid strong oxidants or metal ions that might degrade iridoid glycosides.
- Package in light-protected containers; store < 25 °C to limit hydrolysis.
Key Take-Home Messages
- GPS is a multi-functional botanical active offering anti-inflammatory, anti-oxidant, anti-glycation, anti-psoriatic and pro-healing effects when applied topically.
- Efficacy is backed by recent in vitro keratinocyte data, rodent wound studies and psoriasis models.
- Its water solubility and safety profile allow straightforward incorporation into modern “clean-label” gels, serums, sprays and hydrogel patches targeting sensitive, aged or lesion-prone skin.
Usage: Can be used in any cosmetics product due to its benefits.
How to mix: Mix in the formula in water part.
Usage rate: 0.1-0.2%
Product appearance: Off-white to beige powder
Solubility: Soluble in water
Storage: For long-term storage Store in the refrigerator. Avoid exposure to light or heat. Seal the lid tightly. Shelf life is at least 2 years.
INCI Name : Gentiopicrin
