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
Main Authors: Barros, Susy Érika de Lima, de Lima, Henrique Barros, Gonçalves, Leandra Karoline Alves, Correia, Lenir Cabral, Brito, Maiara de Fátima de Brito, Barcelos, Mariana Pegrucci, Silva, Guilherme Martins, da Silva, Carlos Henrique Tomich de Paula, da Costa, Rafael Garrett, Cruz, Rodrigo Alves Soares, Carvalho, José Carlos Tavares, da Silva Hage-Melim, Lorane Izabel
Format: Journal Article
Language:English
Published: England Oxford University Press 01-06-2022
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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.
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
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  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
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  givenname: Henrique Barros
  orcidid: 0000-0002-8973-4902
  surname: de Lima
  fullname: de Lima, Henrique Barros
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  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
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  givenname: Maiara de Fátima de Brito
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– 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
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  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
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  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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Issue 3
Keywords functional foods
kefiran
in silico
polysaccharide
ADME/Tox
kefir
Language English
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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
URI https://www.ncbi.nlm.nih.gov/pubmed/35782641
https://pubmed.ncbi.nlm.nih.gov/PMC9244975
Volume 11
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