In vitro and in vivo evaluation of enzymatic and antioxidant activity, cytotoxicity and genotoxicity of curcumin-loaded solid dispersions

• Autor(a) principal: Silva, Igor
• Data de Publicação: 2018
• Outros Autores: Peron, Ana Paula, Leimann, Fernanda Vitória, Bressan, Getúlio Nicola, Krum, Bárbara Nunes, Fachinetto, Roselei, Pinela, José, Calhelha, Ricardo C., Barreiro, M.F., Ferreira, Isabel C.F.R., Gonçalves, Odinei Hess, Ineu, Rafael P.
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
• Texto Completo: http://hdl.handle.net/10198/18731
• topic: Allium cepa; Bioactivity; Cholinesterase; Monoamine oxidase; Nanoparticles; Poloxamer 407; Solid dispersion

Curcumin, the main bioactive polyphenolic compound in Curcuma longa L. rhizomes has a wide range of bioactive properties. Curcumin presents low solubility in water and thus limited bioavailability, which decreases its applicability. In this study, cytotoxic effects of curcumin solid dispersions (CurSD) were evaluated against tumor (breast adenocarcinoma and lung, cervical and hepatocellular carcinoma) and non-tumor (PLP2) cells, while cytotoxic and genotoxic effects were evaluated in Allium cepa. The effect of the CurSD on the acetylcholinesterase (AChE), butyrylcholinesterase (BChE), glutathione S-transferase (GST), andmonoamine oxidase (MAO A-B) enzymes was determined, as well as its capacity to inhibit the oxidative hemolysis (OxHLIA) and the formation of thiobarbituric acid reactive substances (TBARS). CurSD are constituted by nanoparticles that are readily dispersible in water, and inhibited 24% and 64% of the AChE and BChE activity at 100μM, respectively. GST activity was inhibited at 30μM while MAO-A and B activity were inhibited at 100μM. CurSD showed cytotoxicity against all the tested tumor cell lines without toxic effects for non-tumor cells. No cytotoxic and genotoxic potential was detected with the Allium cepa test.CurSD maintained the characteristics of free curcumin on the in vitro modulation of important enzymes without appreciable toxicity.