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Evaluation of firefly and renilla luciferase inhibition in reporter-gene assays [Elektronski vir] : a case of IsoflavonoidsKenda, Maša, farmacevtka ...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.Source: International journal of molecular sciences [Elektronski vir]. - ISSN 1422-0067 (Vol. 22, no. 13, 2021, str. 1-14)Type of material - e-articlePublish date - 2021Language - englishCOBISS.SI-ID - 72671747
Author
Kenda, Maša, farmacevtka |
Vegelj, Jan |
Herlah, Barbara, farmacevtka |
Perdih, Andrej, farmacevt |
Mladěnka, Přemysl |
Sollner Dolenc, Marija
Topics
Farmacevtska kemija |
Flavonoidi |
izoflavonoidi |
zaviralci |
alternativne metode |
molekularno mapiranje |
isoflavonoids |
firefly luciferase |
Renilla luciferase |
inhibition |
quantitative structure-activity relationships |
molecular docking |
reporter-gene assay |
OECD test guidelines |
alternative methods
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Author | Kenda, Maša, farmacevtka ... |
Title | Evaluation of firefly and renilla luciferase inhibition in reporter-gene assays [Elektronski vir] : a case of Isoflavonoids |
Publication date | 2021-06-28 |
COBISS.SI-ID | 72671747 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
---|---|---|---|
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Molekulske simulacije, bioinformatika in načrtovanje zdravilnih učinkovin | P1-0012-2019 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Kenda, Maša, farmacevtka | 39201 |
Vegelj, Jan | ![]() |
Herlah, Barbara, farmacevtka | 54668 |
Perdih, Andrej, farmacevt | 25493 |
Mladěnka, Přemysl | ![]() |
Sollner Dolenc, Marija | 08519 |
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