Anti-angiogenic activity and safety of intraocular application of triterpenes.
Doc Ophthalmol
; 143(3): 259-270, 2021 12.
Article
em En
| MEDLINE
| ID: mdl-34036478
PURPOSE: Assessment of the anti-angiogenic activity and the safety of ophthalmic use of four pentacyclic triterpenes (friedelin, friedelinol, lupenone, and lupeol). METHODS: Triterpenes cytotoxicity (5-640 µmol L-1) was examined in ARPE-19 cells by sulforhodamine B colorimetric method, and the anti-angiogenic activity (50-1000 µmol L-1) was evaluated in the chorioallantoic membrane model. Full-field electroretinography and histological analysis were performed to evaluate intraocular effects of these four triterpenes (at 100 or 500 µmol L-1) in eyes of Wistar rats, for 15 days. RESULTS: In the cytotoxicity assay, friedelin and friedelinol were not able to drastically reduce cell growth. A dose-dependent response was observed in groups exposed to lupeol or lupenone. During the chorioallantoic membrane assay, friedelinol at 500 µmol L-1 reduced the vascularity in 26%; lupeol and lupenone showed promising anti-angiogenic activity, reducing three parameters: vascularized area (> 30%), number of junctions (> 20%), and vessel length (> 15%). According to the electroretinographic and histologic findings, triterpenes at 100 µmol L-1 or lupenone at 500 µmol L-1 did not induce any transient or permanent disturbance in retinal structure or functioning. CONCLUSIONS: Triterpenes at 100 µmol L-1 or lupenone at 500 µmol L-1 were considered safe for potential ophthalmic use.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Triterpenos
/
Eletrorretinografia
Tipo de estudo:
Prognostic_studies
Limite:
Animals
Idioma:
En
Revista:
Doc Ophthalmol
Ano de publicação:
2021
Tipo de documento:
Article
País de afiliação:
Brasil
País de publicação:
Holanda