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BIBTEX RIS

β-Cyclodextrin complex improves the bioavailability and antitumor potential of cirsiliol, a flavone isolated from Leonotis nepetifolia (Lamiaceae)

2019; Elsevier BV; Volume: 5; Issue: 10 Linguagem: Inglês

10.1016/j.heliyon.2019.e01692

ISSN

2405-8440

Autores

Ana Paula de Oliveira, Andressa L. N. Silva, Lucas Gustavo Ferreira Cordeiro Viana, Mariana G. Silva, Érica Martins de Lavor, Raimundo Gonçalves de Oliveira Júnior, Edilson Beserra de Alencar Filho, Ricardo Santana de Lima, Rosemairy Luciane Mendes, Larissa Araújo Rolim, Débora Santos Carvalho dos Anjos, Leslie Raphael de Moura Ferraz, Pedró José Rolim Neto, Maria Francilene Souza Silva, Cláudia Pessoa, Jackson Roberto Guedes da Silva Almeida,

Tópico(s)

Essential Oils and Antimicrobial Activity

Resumo

Cirsiliol is a flavone found in many Lamiaceae species with high cytotoxic activity against tumor cell lines. Although cirsiliol is being used in cancer therapy, its pharmacological potential is limited by its low solubility and bioavailability. In this paper, a cirsiliol-β-cyclodextrin inclusion complex was developed in order to increase its solubility and bioavailability. The formation of inclusion complex was proved by scanning electron microscopy, Fourier-transform infrared spectroscopy (FTIR) and nuclear magnetic resonance (NMR) and solubility increment was verified through the ultraviolet-visible (UV-Vis) method. The cytotoxic effect against tumor cells (PC3, HCT-116 and HL-60 human cell lines, and S-180 murine cell line) and the antitumor activity in mice bearing sarcoma S-180 were also investigated. The inclusion complex was obtained with 71.45% of total recovery and solubility 2.1 times higher compared to the compound in its free form. This increment in solubility was responsible by a tumor growth inhibition potentiation (1.5 times greater compared to compound in its free form). In addition, this study showed that cirsiliol and its inclusion complex in β-cyclodextrin have strong antitumor potential at low doses without promoting side effects commonly observed for conventional drugs as doxorubicin.

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