In vitro assessment of triterpenoids NVX-207 and betulinyl-bis-sulfamate as a topical treatment for equine skin cancer.
Authors: Weber Lisa Annabel, Funtan Anne, Paschke Reinhard, Delarocque Julien, Kalbitz Jutta, Meißner Jessica, Feige Karsten, Kietzmann Manfred, Cavalleri Jessika-Maximiliane V
Journal: PloS one
Summary
Equine sarcoid and malignant melanoma represent significant dermatological challenges in practice, with existing topical therapies proving inadequate for consistent clinical resolution. Researchers evaluated two naturally derived compounds—betulinyl-bis-sulfamate and NVX-207—using in vitro cell culture models of equine sarcoid cells, melanoma cells and healthy dermal fibroblasts, assessing their antiproliferative, cytotoxic and apoptotic properties alongside skin penetration studies using Franz diffusion cells. Both triterpenoids inhibited cell proliferation and metabolism dose- and time-dependently (p<0.001), with NVX-207 demonstrating superior efficacy; crucially, apoptosis rather than necrosis was the mechanism of action, with necrotic cell death remaining below 2% after 48 hours of exposure. Skin penetration analysis revealed that NVX-207 concentrations accumulating across dermal layers substantially exceeded the half-maximal inhibitory concentrations required for tumour cell death, suggesting promising topical bioavailability. Whilst these in vitro findings are encouraging, the authors appropriately emphasise that clinical translation requires in vivo validation before practitioners could consider NVX-207 as a viable topical treatment option for either condition.
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Practical Takeaways
- •NVX-207 shows promise as a potential topical treatment for equine sarcoid and melanoma, but in vivo clinical trials are essential before any practical application
- •The mechanism of action is apoptosis with minimal necrosis, which may reduce inflammation compared to other topical therapies
- •This is early-stage research; expect several years of development before availability to practitioners
Key Findings
- •NVX-207 demonstrated superior antiproliferative and cytotoxic effects compared to betulinyl-bis-sulfamate against equine sarcoid and melanoma cells (p < 0.001)
- •Both compounds induced apoptosis in cancer cells through phosphatidylserine externalization and DNA fragmentation, with necrotic cell death less than 2% after 48 h
- •NVX-207 skin penetration exceeded half-maximal inhibitory concentrations in all skin layers within 24 h using Franz diffusion cells