Structure and activity in assessing antioxidant activity in vitro and in vivo

a critical appraisal illustrated with the flavonoids

Guido R.M.M. Haenen, Mariken J.T.J. Arts, Aalt Bast, Micheal D. Coleman

Research output: Contribution to journalArticle

Abstract

Structure–activity relationships are indispensable to identify the most optimal antioxidants. The advantages of in vitro over in vivo experiments for obtaining these relationships are, that the structure is better defined in vitro, since less metabolism takes place. It is also the case that the concentration, a parameter that is directly linked to activity, is more accurately controlled. Moreover, the reactions that occur in vivo, including feed-back mechanisms, are often too multi-faceted and diverse to be compensated for during the assessment of a single structure–activity relationship. Pitfalls of in vitro antioxidant research include: (i) by definition, antioxidants are not stable and substantial amounts of oxidation products are formed and (ii) during the scavenging of reactive species, reaction products of the antioxidants accumulate. Another problem is that the maintenance of a defined concentration of antioxidants is subject to processes such as oxidation and the formation of reaction products during the actual antioxidant reaction, as well as the compartmentalization of the antioxidant and the reactive species in the in vitro test system. So determinations of in vitro structure-activity relationships are subject to many competing variables and they should always be evaluated critically. (c) 2005 Published by Elsevier B.V.
Original languageEnglish
Pages (from-to)191-198
Number of pages8
JournalEnvironmental Toxicology and Pharmacology
Volume21
Issue number2
Early online date15 Aug 2005
DOIs
Publication statusPublished - Feb 2006

Fingerprint

Flavonoids
Antioxidants
Reaction products
Oxidation
Scavenging
Structure-Activity Relationship
In Vitro Techniques
Metabolism
Maintenance
Feedback
Research
Experiments

Keywords

  • activity
  • antioxidant
  • flavonoid
  • stability
  • structure
  • toxicity

Cite this

@article{7f86be65476e4c8c8ccabcaaeafe753f,
title = "Structure and activity in assessing antioxidant activity in vitro and in vivo: a critical appraisal illustrated with the flavonoids",
abstract = "Structure–activity relationships are indispensable to identify the most optimal antioxidants. The advantages of in vitro over in vivo experiments for obtaining these relationships are, that the structure is better defined in vitro, since less metabolism takes place. It is also the case that the concentration, a parameter that is directly linked to activity, is more accurately controlled. Moreover, the reactions that occur in vivo, including feed-back mechanisms, are often too multi-faceted and diverse to be compensated for during the assessment of a single structure–activity relationship. Pitfalls of in vitro antioxidant research include: (i) by definition, antioxidants are not stable and substantial amounts of oxidation products are formed and (ii) during the scavenging of reactive species, reaction products of the antioxidants accumulate. Another problem is that the maintenance of a defined concentration of antioxidants is subject to processes such as oxidation and the formation of reaction products during the actual antioxidant reaction, as well as the compartmentalization of the antioxidant and the reactive species in the in vitro test system. So determinations of in vitro structure-activity relationships are subject to many competing variables and they should always be evaluated critically. (c) 2005 Published by Elsevier B.V.",
keywords = "activity, antioxidant, flavonoid, stability, structure, toxicity",
author = "Haenen, {Guido R.M.M.} and Arts, {Mariken J.T.J.} and Aalt Bast and Coleman, {Micheal D.}",
year = "2006",
month = "2",
doi = "10.1016/j.etap.2005.07.010",
language = "English",
volume = "21",
pages = "191--198",
journal = "Environmental Toxicology and Pharmacology",
issn = "1382-6689",
publisher = "Elsevier",
number = "2",

}

Structure and activity in assessing antioxidant activity in vitro and in vivo : a critical appraisal illustrated with the flavonoids. / Haenen, Guido R.M.M.; Arts, Mariken J.T.J.; Bast, Aalt; Coleman, Micheal D.

In: Environmental Toxicology and Pharmacology, Vol. 21, No. 2, 02.2006, p. 191-198.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Structure and activity in assessing antioxidant activity in vitro and in vivo

T2 - a critical appraisal illustrated with the flavonoids

AU - Haenen, Guido R.M.M.

AU - Arts, Mariken J.T.J.

AU - Bast, Aalt

AU - Coleman, Micheal D.

PY - 2006/2

Y1 - 2006/2

N2 - Structure–activity relationships are indispensable to identify the most optimal antioxidants. The advantages of in vitro over in vivo experiments for obtaining these relationships are, that the structure is better defined in vitro, since less metabolism takes place. It is also the case that the concentration, a parameter that is directly linked to activity, is more accurately controlled. Moreover, the reactions that occur in vivo, including feed-back mechanisms, are often too multi-faceted and diverse to be compensated for during the assessment of a single structure–activity relationship. Pitfalls of in vitro antioxidant research include: (i) by definition, antioxidants are not stable and substantial amounts of oxidation products are formed and (ii) during the scavenging of reactive species, reaction products of the antioxidants accumulate. Another problem is that the maintenance of a defined concentration of antioxidants is subject to processes such as oxidation and the formation of reaction products during the actual antioxidant reaction, as well as the compartmentalization of the antioxidant and the reactive species in the in vitro test system. So determinations of in vitro structure-activity relationships are subject to many competing variables and they should always be evaluated critically. (c) 2005 Published by Elsevier B.V.

AB - Structure–activity relationships are indispensable to identify the most optimal antioxidants. The advantages of in vitro over in vivo experiments for obtaining these relationships are, that the structure is better defined in vitro, since less metabolism takes place. It is also the case that the concentration, a parameter that is directly linked to activity, is more accurately controlled. Moreover, the reactions that occur in vivo, including feed-back mechanisms, are often too multi-faceted and diverse to be compensated for during the assessment of a single structure–activity relationship. Pitfalls of in vitro antioxidant research include: (i) by definition, antioxidants are not stable and substantial amounts of oxidation products are formed and (ii) during the scavenging of reactive species, reaction products of the antioxidants accumulate. Another problem is that the maintenance of a defined concentration of antioxidants is subject to processes such as oxidation and the formation of reaction products during the actual antioxidant reaction, as well as the compartmentalization of the antioxidant and the reactive species in the in vitro test system. So determinations of in vitro structure-activity relationships are subject to many competing variables and they should always be evaluated critically. (c) 2005 Published by Elsevier B.V.

KW - activity

KW - antioxidant

KW - flavonoid

KW - stability

KW - structure

KW - toxicity

UR - http://www.scopus.com/inward/record.url?scp=31544477682&partnerID=8YFLogxK

U2 - 10.1016/j.etap.2005.07.010

DO - 10.1016/j.etap.2005.07.010

M3 - Article

VL - 21

SP - 191

EP - 198

JO - Environmental Toxicology and Pharmacology

JF - Environmental Toxicology and Pharmacology

SN - 1382-6689

IS - 2

ER -