Antioxidant, Anti-Inflammatory, and Multidrug Resistance Modulation Activity of Silychristin Derivatives.
ABC superfamily
Adriamycin
BCRP
P-glycoprotein
expression profile
immunomodulation
silychristin
silymarin
Journal
Antioxidants (Basel, Switzerland)
ISSN: 2076-3921
Titre abrégé: Antioxidants (Basel)
Pays: Switzerland
ID NLM: 101668981
Informations de publication
Date de publication:
14 Aug 2019
14 Aug 2019
Historique:
received:
27
06
2019
revised:
08
08
2019
accepted:
12
08
2019
entrez:
17
8
2019
pubmed:
17
8
2019
medline:
17
8
2019
Statut:
epublish
Résumé
Silychristin A is the second most abundant compound of silymarin. Silymarin complex was previously described as an antioxidant with multidrug resistance modulation activity. Here, the results of a classical biochemical antioxidant assay (ORAC) were compared with a cellular assay evaluating the antioxidant capacity of pure silychristin A and its derivatives (anhydrosilychristin, isosilychristin and 2,3-dehydrosilychristin A). All the tested compounds acted as antioxidants within the cells, but 2,3-dehydro- and anhydro derivatives were almost twice as potent as the other tested compounds. Similar results were obtained in LPS-stimulated macrophages, where 2,3-dehydro- and anhydrosilychristin inhibited NO production nearly twice as efficiently as silychristin A. The inhibition of P-glycoprotein (P-gp) was determined in vitro, and the respective sensitization of doxorubicin-resistant ovarian carcinoma overproducing P-gp was detected. Despite the fact that the inhibition of P-gp was demonstrated in a concentration-dependent manner for each tested compound, the sensitization of the resistant cell line was observed predominantly for silychristin A and 2,3-dehydrosilychristin A. However, anhydrosilychristin and isosilychristin affected the expression of both the P-gp (
Identifiants
pubmed: 31416138
pii: antiox8080303
doi: 10.3390/antiox8080303
pmc: PMC6720199
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Ministerstvo Školství, Mládeže a Tělovýchovy
ID : INTER-COST LTC19007 and LTC19020
Organisme : Grantová agentura České Republiky
ID : 18-00150S
Organisme : Operational Program Prague-Competitiveness
ID : CZ.2.16/3.1.00/21537 and CZ.2.16/3.1.00/24503
Organisme : Czech National Program of Sustainability
ID : NPU I (LO) (MSMT-43760/2015)
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