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

被引:53
作者
de Sa, Igor Silva [1 ]
Peron, Ana Paula [2 ]
Leimann, Fernanda Vitoria [1 ,3 ,4 ]
Bressan, Getulio Nicola [5 ]
Krum, Barbara Nunes [6 ]
Fachinetto, Roselei [5 ,6 ]
Pinela, Jose [3 ]
Calhelha, Ricardo Costa [3 ]
Barreiro, Maria Filomena [3 ,4 ]
Ferreira, Isabel C. F. R. [3 ]
Goncalves, Odinei Hess [1 ,3 ,4 ]
Ineu, Rafael Porto [1 ]
机构
[1] Fed Univ Technol Parana UTFPR, Postgrad Program Food Technol PPGTA, Campus Campo Mourao, BR-87301899 Campo Mourao, PR, Brazil
[2] Fed Univ Technol Parana UTFPR, Biodivers & Nat Conservat Dept, Campus Campo Mourao, BR-87301899 Campo Mourao, PR, Brazil
[3] Inst Politecn Braganca, Ctr Invest Montanha CIMO, Campus Santa Apolonia, P-5300253 Braganca, Portugal
[4] Politecn Inst Braganca, LCM, LSRE, Campus Santa Apolonia, P-5300253 Braganca, Portugal
[5] Univ Fed Santa Maria, Postgrad Program Biol Sci Toxicol Biochem, Ave Roraima 1000, BR-97105900 Santa Maria, RS, Brazil
[6] Univ Fed Santa Maria, Postgrad Program Pharmacol, Ave Roraima 1000, BR-97105900 Santa Maria, RS, Brazil
关键词
Bioactivity; Nanoparticles; Solid dispersion; Poloxamer; 407; Cholinesterase; Monoamine oxidase; Allium cepa; GLUTATHIONE S-TRANSFERASES; MONOAMINE-OXIDASE; DROSOPHILA-MELANOGASTER; OXIDATIVE HEMOLYSIS; BUTYRYLCHOLINESTERASE; INHIBITORS; ACETYLCHOLINESTERASE; DISEASE; ACID; BIOAVAILABILITY;
D O I
10.1016/j.fct.2018.12.037
中图分类号
TS2 [食品工业];
学科分类号
0832 ;
摘要
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), and monoamine 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 (TSARS). CurSD are constituted by nanoparticles that are readily dispersible in water, and inhibited 24% and 64% of the AChE and BChE activity at 100 mu M, respectively. GST activity was inhibited at 30 mu M while MAO-A and B activity were inhibited at 100 mu M. 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.
引用
收藏
页码:29 / 37
页数:9
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