دورية أكاديمية
Inhibitions of monoamine oxidases by ferulic acid hydrazide derivatives: synthesis, biochemistry, and computational evaluation
| العنوان: | Inhibitions of monoamine oxidases by ferulic acid hydrazide derivatives: synthesis, biochemistry, and computational evaluation |
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| المؤلفون: | Arshida Thottile Peedikayil, Jiseong Lee, Mohamed A. Abdelgawad, Mohammed M. Ghoneim, Mohamed E. Shaker, Samy Selim, Sunil Kumar, Sanal Dev, Hoon Kim, Bijo Mathew |
| المصدر: | Applied Biological Chemistry, Vol 66, Iss 1, Pp 1-9 (2023) |
| بيانات النشر: | SpringerOpen, 2023. |
| سنة النشر: | 2023 |
| المجموعة: | LCC:Agriculture (General) LCC:Chemistry |
| مصطلحات موضوعية: | Ferulic acid, Monoamine oxidase, Kinetics, Reversibility, Molecular docking, Molecular dynamics, Agriculture (General), S1-972, Chemistry, QD1-999 |
| الوصف: | Abstract Monoamine oxidases (MAOs) regulate neurotransmitters, and changes in their regulation lead to neurogenerative diseases (NDs). Therefore, MAO inhibitors are used to treat NDs. Ferulic acid, a phenolic compound found in various plant species, has been demonstrated to have a variety of biological functions, including anti-inflammatory, anticancer, and neuroprotective effects. In this study, ten ferulic acid hydrazide derivatives (FA1–FA10) were synthesized, and their ability to inhibit monoamine oxidase (MAO) enzymes was tested. Six candidates demonstrated a more pronounced pattern of inhibitory action against MAO-B than against MAO-A. FA3 had the highest inhibitory efficacy in MAO-B inhibition (IC50 value of 1.88 μM), followed by FA9 (2.08 μM). FA3 has a Ki of 1.92 ± 0.73 μM. A reversibility experiment of MAO-B inhibition by FA3 was conducted using dialysis, and the recovery pattern showed FA3 was a reversible MAO-B inhibitor with a similar recovery to safinamide, a reversible reference inhibitor. These results indicate that FA3 is an effective reversible MAO-B inhibitor. In molecular dynamics and docking, FA3 paired with pi-pi stacking helped stabilize the protein ligand in the active site of MAO-B. According to this study, lead compounds can be used as therapeutic agents to treat neurological conditions, such as Parkinson's disease (PD). |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 2468-0842 |
| العلاقة: | https://doaj.org/toc/2468-0842Test |
| DOI: | 10.1186/s13765-023-00823-0 |
| الوصول الحر: | https://doaj.org/article/4f81b228609b431d89c59789a7225902Test |
| رقم الانضمام: | edsdoj.4f81b228609b431d89c59789a7225902 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 24680842 |
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| DOI: | 10.1186/s13765-023-00823-0 |