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Inclusion complex of O-allyl-lawsone with 2-hydroxypropyl-β-cyclodextrin: Preparation, physical characterization, antiparasitic and antifungal activity
by
Borba-Santos, Luana P
, Futuro, Débora Omena
, Faria, Robson Xavier
, da Silva Lima, Camilo Henrique
, Faria, Ana Flávia Martins
, Teixeira, Guilherme Pegas
, Ferreira, Vitor Francisco
, Nicoletti, Caroline Deckmann
, Rozental, Sonia
, de Sá Haddad Queiroz, Marcella
, Barboclher, Lais
, de Carvalho da Silva, Fernando
, dos Santos Galvão, Raíssa Maria
, Souza, André Luis Ameida
in
Antifungal activity
/ Antifungal agents
/ Antiparasitic agents
/ Benznidazole
/ Cyclodextrins
/ Cytotoxicity
/ Encapsulation
/ Epimastigotes
/ Free form
/ Fungicides
/ Inclusion complexes
/ Mammalian cells
/ Mammals
/ Microorganisms
/ Protozoa
/ Toxicity
/ Trypanosome
/ Trypomastigotes
/ Yeast
/ β-Cyclodextrin
2023
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Inclusion complex of O-allyl-lawsone with 2-hydroxypropyl-β-cyclodextrin: Preparation, physical characterization, antiparasitic and antifungal activity
by
Borba-Santos, Luana P
, Futuro, Débora Omena
, Faria, Robson Xavier
, da Silva Lima, Camilo Henrique
, Faria, Ana Flávia Martins
, Teixeira, Guilherme Pegas
, Ferreira, Vitor Francisco
, Nicoletti, Caroline Deckmann
, Rozental, Sonia
, de Sá Haddad Queiroz, Marcella
, Barboclher, Lais
, de Carvalho da Silva, Fernando
, dos Santos Galvão, Raíssa Maria
, Souza, André Luis Ameida
in
Antifungal activity
/ Antifungal agents
/ Antiparasitic agents
/ Benznidazole
/ Cyclodextrins
/ Cytotoxicity
/ Encapsulation
/ Epimastigotes
/ Free form
/ Fungicides
/ Inclusion complexes
/ Mammalian cells
/ Mammals
/ Microorganisms
/ Protozoa
/ Toxicity
/ Trypanosome
/ Trypomastigotes
/ Yeast
/ β-Cyclodextrin
2023
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Inclusion complex of O-allyl-lawsone with 2-hydroxypropyl-β-cyclodextrin: Preparation, physical characterization, antiparasitic and antifungal activity
by
Borba-Santos, Luana P
, Futuro, Débora Omena
, Faria, Robson Xavier
, da Silva Lima, Camilo Henrique
, Faria, Ana Flávia Martins
, Teixeira, Guilherme Pegas
, Ferreira, Vitor Francisco
, Nicoletti, Caroline Deckmann
, Rozental, Sonia
, de Sá Haddad Queiroz, Marcella
, Barboclher, Lais
, de Carvalho da Silva, Fernando
, dos Santos Galvão, Raíssa Maria
, Souza, André Luis Ameida
in
Antifungal activity
/ Antifungal agents
/ Antiparasitic agents
/ Benznidazole
/ Cyclodextrins
/ Cytotoxicity
/ Encapsulation
/ Epimastigotes
/ Free form
/ Fungicides
/ Inclusion complexes
/ Mammalian cells
/ Mammals
/ Microorganisms
/ Protozoa
/ Toxicity
/ Trypanosome
/ Trypomastigotes
/ Yeast
/ β-Cyclodextrin
2023
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Inclusion complex of O-allyl-lawsone with 2-hydroxypropyl-β-cyclodextrin: Preparation, physical characterization, antiparasitic and antifungal activity
Journal Article
Inclusion complex of O-allyl-lawsone with 2-hydroxypropyl-β-cyclodextrin: Preparation, physical characterization, antiparasitic and antifungal activity
2023
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Overview
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.
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