التفاصيل البيبلوغرافية
| العنوان: |
Exploration of the Fluorescent Properties and the Modulated Activities against Sirtuin Fluorogenic Assays of Chromenone-Derived Natural Products |
| المؤلفون: |
Hui Wen, Nina Xue, Feng Wu, Yujun He, Gang Zhang, Zebin Hu, Huaqing Cui |
| المصدر: |
Molecules, Vol 23, Iss 5, p 1063 (2018) |
| بيانات النشر: |
MDPI AG, 2018. |
| سنة النشر: |
2018 |
| المجموعة: |
LCC:Organic chemistry |
| مصطلحات موضوعية: |
chromenone, isoflavone, osthole, AMC, fluorescence, fluorogenic assay, sirtuin, SIRT1 activator, Organic chemistry, QD241-441 |
| الوصف: |
Chromenone-derived natural products include chromones (flavone, isoflavone) and coumarins. Chromenone compounds not only exhibit impressive biological activities, but also are an important resource of experimentally used fluorophores, such as, 7-amino-4-methylcoumarin (AMC). Various chromenone compounds have reported to have weak fluorescence, and this has the potential to interfere with the measurements during AMC fluorogenic assays and result in non-robust assay readouts. Several flavones and isoflavones were found as SIRT1 activators, while fluorogenic sirtuin assays utilized AMC labelled peptides as the substrates. In this study we investigated whether the fluorescent properties of chromenone-derived natural products interrupt the measurement of SIRT1/2 modulated activities. We found that the reported SIRT1 activators: flavones were detected with the SIRT1 activation activity, but isoflavones were not detected with SIRT1 activation activity, and instead that they were found to be fluorogenic compounds. Another chromenone compound, osthole, exhibited a moderate SIRT2 inhibitory activity with an IC50 of 10 μM. In conclusion, the fluorescent properties of these chromenone compounds do affect the measurement of the sirtuin activities of both inhibitors and activators. However, if the possible fluorescence properties are mitigated in the assay readout, these fluorogenic assays enable the screening of activity modulators. |
| نوع الوثيقة: |
article |
| وصف الملف: |
electronic resource |
| اللغة: |
English |
| تدمد: |
1420-3049 |
| Relation: |
http://www.mdpi.com/1420-3049/23/5/1063; https://doaj.org/toc/1420-3049 |
| DOI: |
10.3390/molecules23051063 |
| URL الوصول: |
https://doaj.org/article/9bf9472371284979bac2f35cb1d40c3d |
| رقم الانضمام: |
edsdoj.9bf9472371284979bac2f35cb1d40c3d |
| قاعدة البيانات: |
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