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- Title
Inclusion complex of O-allyl-lawsone with 2-hydroxypropyl-β-cyclodextrin: Preparation, physical characterization, antiparasitic and antifungal activity.
- Authors
Nicoletti, Caroline Deckmann; dos Santos Galvão, Raíssa Maria; de Sá Haddad Queiroz, Marcella; Barboclher, Lais; Faria, Ana Flávia Martins; Teixeira, Guilherme Pegas; Souza, André Luis Ameida; de Carvalho da Silva, Fernando; Ferreira, Vitor Francisco; da Silva Lima, Camilo Henrique; Borba-Santos, Luana P.; Rozental, Sonia; Futuro, Débora Omena; Faria, Robson Xavier
- Abstract
The subclass naphthoquinone represents a substance group containing several compounds with important activities against various pathogenic microorganisms. Accordingly, we evaluated O-allyl-lawsone (OAL) antiparasitic and antifungal activity free and encapsulated in 2-hydroxypropyl-β-cyclodextrin (OAL MKN) against Trypanosoma cruzi and Sporothrix spp. OAL and OAL MKN were synthesized and characterized by physicochemical methods. The IC50 values of OAL against T. cruzi were 2.4 µM and 96.8 µM, considering epimastigotes and trypomastigotes, respectively. At the same time, OAL MKN exhibited a lower IC50 value (0.5 µM) for both trypanosome forms and low toxicity for mammalian cells. Additionally, the encapsulation showed a selectivity index approximately 240 times higher than that of benznidazole. Regarding antifungal activity, OAL and OAL MKN inhibited Sporothrix brasiliensis growth at 16 µM, while Sporothrix schenckii was inhibited at 32 µM. OAL MKN also exhibited higher selectivity toward fungus than mammalian cells. In conclusion, we described the encapsulation of O-allyl-lawsone in 2-hydroxypropyl-β-cyclodextrin, increasing the antiparasitic activity compared with the free form and reducing the cytotoxicity and increasing the selectivity towardSporothrix yeasts and the T. cruzi trypomastigote form. This study highlights the potential development of this inclusion complex as an antiparasitic and antifungal agent to treat neglected diseases.
- Subjects
ANTIFUNGAL agents; TRYPANOSOMA cruzi; ANTIPARASITIC agents; NAPHTHOQUINONE; NEGLECTED diseases; INCLUSION compounds; PATHOGENIC microorganisms
- Publication
Journal of Bioenergetics & Biomembranes, 2023, Vol 55, Issue 3, p233
- ISSN
0145-479X
- Publication type
Article
- DOI
10.1007/s10863-023-09970-x