Stiftung Tierärztliche Hochschule Hannover (TiHo)

Betulinic acid shows anticancer activity against equine melanoma cells and permeates isolated equine skin in vitro

Weber, Lisa A; Meißner, Jessica GND; Delarocque, Julien ORCID; Kalbitz, Jutta; Feige, Karsten GND; Kietzmann, Manfred GND; Michaelis, Anne; Paschke, Reinhard; Michael, Julia; Pratscher, Barbara; Cavalleri, Jessika-M V

BACKGROUND:Equine malignant melanoma (EMM) is a frequently occurring dermoepidermal tumor in grey horses. Currently available therapies are either challenging or inefficient. Betulinic acid (BA), a naturally occurring triterpenoid, is a promising compound for cancer treatment. To evaluate the potential of BA as a topical therapy for EMM, its anticancer effects on primary equine melanoma cells and dermal fibroblasts and its percutaneous permeation through isolated equine skin were assessed in vitro. RESULTS:BA showed antiproliferative and cytotoxic effects on both primary equine melanoma cells and fibroblasts in a time- and dose-dependent manner. The lowest half-maximal inhibitory concentrations were obtained 96 h after the beginning of drug exposure (12.7 μmol/L and 23.6 μmol/L for melanoma cells eRGO1 and MelDuWi, respectively, in cytotoxicity assay). High concentrations of the compound were reached in the required skin layers in vitro. CONCLUSION:BA is a promising substance for topical EMM treatment. Further clinical studies in horses are necessary to assess safety and antitumoral effects in vivo.

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Weber, L.A., Meißner, J., Delarocque, J., Kalbitz, J., Feige, K., Kietzmann, M., Michaelis, A., Paschke, R., Michael, J., Pratscher, B., Cavalleri, J.-M.V., 2020. Betulinic acid shows anticancer activity against equine melanoma cells and permeates isolated equine skin in vitro. BMC veterinary research 16: 44. https://doi.org/10.1186/s12917-020-2262-5
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