Antioxidant, anti-inflammatory, and multidrug resistance modulation activity of silychristin derivatives

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F75010330%3A_____%2F19%3A00012658" target="_blank" >RIV/75010330:_____/19:00012658 - isvavai.cz</a>

Alternative codes found

RIV/61388971:_____/19:00510067 RIV/60461373:22330/19:43918918 RIV/00216208:11140/19:10396195

Result on the web

<a href="https://www.mdpi.com/2076-3921/8/8/303" target="_blank" >https://www.mdpi.com/2076-3921/8/8/303</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/antiox8080303" target="_blank" >10.3390/antiox8080303</a>

Result language

angličtina

Original language name

Antioxidant, anti-inflammatory, and multidrug resistance modulation activity of silychristin derivatives

Original language description

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 (ABCB1) and ABCG2 genes. This is the first report showing that silychristin A and its 2,3-dehydro-derivative modulate multidrug resistance by the direct inhibition of P-gp, in contrast to anhydrosilychristin and isosilychristin modulating multidrug resistance by downregulating the expression of the dominant transmembrane efflux pumps.

Czech name

—

Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

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OECD FORD branch

10609 - Biochemical research methods

Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2019

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Antioxidants

ISSN

2076-3921

e-ISSN

—

Volume of the periodical

8

Issue of the periodical within the volume

8

Country of publishing house

CH - SWITZERLAND

Number of pages

19

Pages from-to

303

UT code for WoS article

000482958900065

EID of the result in the Scopus database

2-s2.0-85073269518