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Evaluation of firefly and Renilla luciferase inhibition in reporter-gene assays : a case of isoflavonoids
ID
Kenda, Maša
(
Author
),
ID
Vegelj, Jan
(
Author
),
ID
Herlah, Barbara
(
Author
),
ID
Perdih, Andrej
(
Author
),
ID
Mladěnka, Přemysl
(
Author
),
ID
Sollner Dolenc, Marija
(
Author
)
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https://www.mdpi.com/1422-0067/22/13/6927
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Abstract
Firefly luciferase is susceptible to inhibition and stabilization by compounds under investigation for biological activity and toxicity. This can lead to false-positive results in in vitro cell-based assays. However, firefly luciferase remains one of the most commonly used reporter genes. Here, we evaluated isoflavonoids for inhibition of firefly luciferase. These natural compounds are often studied using luciferase reporter-gene assays. We used a quantitative structure–activity relationship (QSAR) model to compare the results of in silico predictions with a newly developed in vitro assay that enables concomitant detection of inhibition of firefly and Renilla luciferases. The QSAR model predicted a moderate to high likelihood of firefly luciferase inhibition for all of the 11 isoflavonoids investigated, and the in vitro assays confirmed this for seven of them: daidzein, genistein, glycitein, prunetin, biochanin A, calycosin, and formononetin. In contrast, none of the 11 isoflavonoids inhibited Renilla luciferase. Molecular docking calculations indicated that isoflavonoids interact favorably with the D-luciferin binding pocket of firefly luciferase. These data demonstrate the importance of reporter-enzyme inhibition when studying the effects of such compounds and suggest that this in vitro assay can be used to exclude false-positives due to firefly or Renilla luciferase inhibition, and to thus define the most appropriate reporter gene.
Language:
English
Keywords:
isoflavonoids
,
firefly luciferase
,
Renilla luciferase
,
inhibition
,
quantitative structure–activity relationships
,
molecular docking
,
reporter-gene assay
,
OECD test guidelines
,
alternative methods
Work type:
Article
Typology:
1.01 - Original Scientific Article
Organization:
FFA - Faculty of Pharmacy
Publication status:
Published
Publication version:
Version of Record
Year:
2021
Number of pages:
14 str.
Numbering:
Vol. 22, iss. 13, art. 6927
PID:
20.500.12556/RUL-135754
UDC:
547.972:615.4.:54
ISSN on article:
1422-0067
DOI:
10.3390/ijms22136927
COBISS.SI-ID:
72671747
Publication date in RUL:
30.03.2022
Views:
1246
Downloads:
130
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Record is a part of a journal
Title:
International journal of molecular sciences
Shortened title:
Int. j. mol. sci.
Publisher:
MDPI
ISSN:
1422-0067
COBISS.SI-ID:
2779162
Licences
License:
CC BY 4.0, Creative Commons Attribution 4.0 International
Link:
http://creativecommons.org/licenses/by/4.0/
Description:
This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.
Secondary language
Language:
Slovenian
Keywords:
izoflavonoidi
,
zaviralci
,
alternativne metode
,
molekularno mapiranje
,
farmacevtska kemija
,
flavonoidi
Projects
Funder:
ARRS - Slovenian Research Agency
Funding programme:
Young researchers
Funder:
ARRS - Slovenian Research Agency
Project number:
P1-0208
Name:
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin
Funder:
ARRS - Slovenian Research Agency
Project number:
P1-0012
Name:
Molekulske simulacije, bioinformatika in načrtovanje zdravilnih učinkovin
Funder:
EC - European Commission
Funding programme:
ERDF
Project number:
CZ.02.1.01/0.0/0.0/16_019/0000841
Acronym:
EFSA-CDN
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