Betulinic acid shows anticancer activity against equine melanoma cells and permeates isolated equine skin in vitro.
Animals
Antineoplastic Agents
/ pharmacokinetics
Cell Line, Tumor
Fibroblasts
/ drug effects
Horse Diseases
/ drug therapy
Horses
Melanoma
/ drug therapy
Pentacyclic Triterpenes
Skin
/ drug effects
Skin Neoplasms
/ drug therapy
Triterpenes
/ pharmacokinetics
Betulinic Acid
Melanoma, Cutaneous Malignant
Betulinic acid
Cell culture assay
Equine malignant melanoma (EMM)
Franz-type diffusion cell
Journal
BMC veterinary research
ISSN: 1746-6148
Titre abrégé: BMC Vet Res
Pays: England
ID NLM: 101249759
Informations de publication
Date de publication:
05 Feb 2020
05 Feb 2020
Historique:
received:
02
05
2019
accepted:
24
01
2020
entrez:
7
2
2020
pubmed:
7
2
2020
medline:
30
9
2020
Statut:
epublish
Résumé
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. 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. BA is a promising substance for topical EMM treatment. Further clinical studies in horses are necessary to assess safety and antitumoral effects in vivo.
Sections du résumé
BACKGROUND
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
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
CONCLUSIONS
BA is a promising substance for topical EMM treatment. Further clinical studies in horses are necessary to assess safety and antitumoral effects in vivo.
Identifiants
pubmed: 32024502
doi: 10.1186/s12917-020-2262-5
pii: 10.1186/s12917-020-2262-5
pmc: PMC7003431
doi:
Substances chimiques
Antineoplastic Agents
0
Pentacyclic Triterpenes
0
Triterpenes
0
Betulinic Acid
4G6A18707N
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
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