Chromatographic profile, in silico and in vivo study of the pharmacokinetic and toxicological properties of major constituent present in kefir, the kefiran
Kefiran is a polysaccharide present in kefir grains that have been widely explored due to its potential health benefits. The objective of this work was to characterize and quantify the components present in the ethanolic extract of milk kefir grains; to study its pharmacokinetic and toxicological pr...
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Published in: | Toxicology research (Cambridge) Vol. 11; no. 3; pp. 520 - 528 |
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Abstract | Kefiran is a polysaccharide present in kefir grains that have been widely explored due to its potential health benefits. The objective of this work was to characterize and quantify the components present in the ethanolic extract of milk kefir grains; to study its pharmacokinetic and toxicological properties in silico and evaluate the acute toxicity of the kefiran in zebrafish. The prediction of pharmacokinetic properties was performed by QikProp software. In silico toxicity assessment was performed using the DEREK (deductive estimate of risk from existing knowledge) software. In the chromatographic, kefiran was identified as the major component. Results showed that the kefiran had low human oral absorption and intestinal absorption its due poor solubility profile; low logP value, indicating its lipophilicity and the low MDCK and Caco-2 cells permability, and unable to cross the blood-brain barrier. Kefiran did not present any structural warning for in silico toxicity. In zebrafish, the dose of 2,000 mg/kg of kefiran produced nonsignificant alterations in the analyzed organs. It can be said then that kefiran has an acceptable degree of safety for use in the development of drugs or functional foods. Further research such as in vivo testing to confirm its pharmacological potential is currently underway. |
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AbstractList | Kefiran is a polysaccharide present in kefir grains that have been widely explored due to its potential health benefits. The objective of this work was to characterize and quantify the components present in the ethanolic extract of milk kefir grains; to study its pharmacokinetic and toxicological properties in silico and evaluate the acute toxicity of the kefiran in zebrafish. The prediction of pharmacokinetic properties was performed by QikProp software. In silico toxicity assessment was performed using the DEREK (deductive estimate of risk from existing knowledge) software. In the chromatographic, kefiran was identified as the major component. Results showed that the kefiran had low human oral absorption and intestinal absorption its due poor solubility profile; low logP value, indicating its lipophilicity and the low MDCK and Caco-2 cells permability, and unable to cross the blood–brain barrier. Kefiran did not present any structural warning for in silico toxicity. In zebrafish, the dose of 2,000 mg/kg of kefiran produced nonsignificant alterations in the analyzed organs. It can be said then that kefiran has an acceptable degree of safety for use in the development of drugs or functional foods. Further research such as in vivo testing to confirm its pharmacological potential is currently underway. |
Author | de Lima, Henrique Barros Carvalho, José Carlos Tavares Brito, Maiara de Fátima de Brito Correia, Lenir Cabral Cruz, Rodrigo Alves Soares da Silva Hage-Melim, Lorane Izabel Silva, Guilherme Martins Barros, Susy Érika de Lima Barcelos, Mariana Pegrucci da Costa, Rafael Garrett Gonçalves, Leandra Karoline Alves da Silva, Carlos Henrique Tomich de Paula |
Author_xml | – sequence: 1 givenname: Susy Érika de Lima orcidid: 0000-0002-9224-8809 surname: Barros fullname: Barros, Susy Érika de Lima organization: Laboratory of Pharmaceutical and Medicinal Chemistry (PharMedChem), Department of Biological and Health Sciences, Federal University of Amapá, 68903-419, Macapá, Amapá, Brazil – sequence: 2 givenname: Henrique Barros orcidid: 0000-0002-8973-4902 surname: de Lima fullname: de Lima, Henrique Barros organization: Laboratory of Pharmaceutical and Medicinal Chemistry (PharMedChem), Department of Biological and Health Sciences, Federal University of Amapá, 68903-419, Macapá, Amapá, Brazil – sequence: 3 givenname: Leandra Karoline Alves surname: Gonçalves fullname: Gonçalves, Leandra Karoline Alves organization: Laboratory of Pharmaceutical and Medicinal Chemistry (PharMedChem), Department of Biological and Health Sciences, Federal University of Amapá, 68903-419, Macapá, Amapá, Brazil – sequence: 4 givenname: Lenir Cabral surname: Correia fullname: Correia, Lenir Cabral organization: Laboratory of Pharmaceutical and Medicinal Chemistry (PharMedChem), Department of Biological and Health Sciences, Federal University of Amapá, 68903-419, Macapá, Amapá, Brazil – sequence: 5 givenname: Maiara de Fátima de Brito surname: Brito fullname: Brito, Maiara de Fátima de Brito organization: Laboratory of Pharmaceutical and Medicinal Chemistry (PharMedChem), Department of Biological and Health Sciences, Federal University of Amapá, 68903-419, Macapá, Amapá, Brazil – sequence: 6 givenname: Mariana Pegrucci surname: Barcelos fullname: Barcelos, Mariana Pegrucci organization: Computational Laboratory of Pharmaceutical Chemistry, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, 14040-90, Ribeirão Preto, São Paulo, Brazil – sequence: 7 givenname: Guilherme Martins surname: Silva fullname: Silva, Guilherme Martins organization: Departamento de Química, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto, Universidade de São Paulo, 14040-903, Ribeirão Preto, São Paulo, Brazil – sequence: 8 givenname: Carlos Henrique Tomich de Paula surname: da Silva fullname: da Silva, Carlos Henrique Tomich de Paula organization: Computational Laboratory of Pharmaceutical Chemistry, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, 14040-90, Ribeirão Preto, São Paulo, Brazil – sequence: 9 givenname: Rafael Garrett surname: da Costa fullname: da Costa, Rafael Garrett organization: Metabolomics Laboratory (LabMeta, LADETEC), Instituto of Chemistry, Federal University of Rio de Janeiro (UFRJ), 21941-598 Rio de Janeiro, Rio de Janeiro, Brazil – sequence: 10 givenname: Rodrigo Alves Soares surname: Cruz fullname: Cruz, Rodrigo Alves Soares organization: Phytopharmaceutical Nanobiotechnology Laboratory (NanoFito), Department of Biological and Health Sciences, Federal University of Amapá, 68903-419, Macapá, Amapá, Brazil – sequence: 11 givenname: José Carlos Tavares surname: Carvalho fullname: Carvalho, José Carlos Tavares organization: Laboratory of Drug Research, Department of Biological and Health Sciences, Federal University of Amapá, 68903-419, Macapá, Amapá, Brazil – sequence: 12 givenname: Lorane Izabel surname: da Silva Hage-Melim fullname: da Silva Hage-Melim, Lorane Izabel organization: Computational Laboratory of Pharmaceutical Chemistry, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, 14040-90, Ribeirão Preto, São Paulo, Brazil |
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Keywords | functional foods kefiran in silico polysaccharide ADME/Tox kefir |
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Snippet | Kefiran is a polysaccharide present in kefir grains that have been widely explored due to its potential health benefits. The objective of this work was to... |
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Title | Chromatographic profile, in silico and in vivo study of the pharmacokinetic and toxicological properties of major constituent present in kefir, the kefiran |
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