Pharmacological appraisal of ligustrazine based cyclohexanone analogs as inhibitors of inflammatory markers
Copyright © 2020 Elsevier B.V. All rights reserved..
The targeting of pro-inflammatory enzymes becomes a therapeutic intervention when acute inflammation is proliferating in pathological conditions. This research is intended to carry out an evaluation of inhibiting and inducing enzymes with inflammatory associations with 28 cyclohexanone analogs based on the ligustrazine. Tests were undertaken with inhibitor screening assay kits using a range of synthetic compounds to investigate how they could inhibit the activity of cyclooxygenase (COX) enzymes, secretory phospholipase A2 (sPLA2), and lipoxygenase (LOX) enzyme. Significant and similar inhibitory activities against sPLA2 with were noted with synthetic compounds which included 1f and 1g (IC50 = 2.2 μM). The optimal inhibitory activity regarding LOX enzyme was shown with compounds 1d (IC50 = 8.1 μM) and 1e (IC50 = 7.5 μM). Additionally, the compounds 1b, 1d, 1e, 2n, and 2o were shown to be significant inhibitors of COX-1 activity with IC50 values 0.09 to 0.7 μM. The outcomes of assays for COX inhibition demonstrated that the same compounds had a further strong inhibitive influence on the COX-2 enzyme, and certain compounds such as 1d, 1e, and 2n demonstrated enhanced potency compared with positive controls.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:147 |
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| Enthalten in: |
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences - 147(2020) vom: 30. Apr., Seite 105299 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Alotaibi, Nasser Hadal [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 05.02.2021 Date Revised 05.02.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejps.2020.105299 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM307534596 |
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| 520 | |a Copyright © 2020 Elsevier B.V. All rights reserved. | ||
| 520 | |a The targeting of pro-inflammatory enzymes becomes a therapeutic intervention when acute inflammation is proliferating in pathological conditions. This research is intended to carry out an evaluation of inhibiting and inducing enzymes with inflammatory associations with 28 cyclohexanone analogs based on the ligustrazine. Tests were undertaken with inhibitor screening assay kits using a range of synthetic compounds to investigate how they could inhibit the activity of cyclooxygenase (COX) enzymes, secretory phospholipase A2 (sPLA2), and lipoxygenase (LOX) enzyme. Significant and similar inhibitory activities against sPLA2 with were noted with synthetic compounds which included 1f and 1g (IC50 = 2.2 μM). The optimal inhibitory activity regarding LOX enzyme was shown with compounds 1d (IC50 = 8.1 μM) and 1e (IC50 = 7.5 μM). Additionally, the compounds 1b, 1d, 1e, 2n, and 2o were shown to be significant inhibitors of COX-1 activity with IC50 values 0.09 to 0.7 μM. The outcomes of assays for COX inhibition demonstrated that the same compounds had a further strong inhibitive influence on the COX-2 enzyme, and certain compounds such as 1d, 1e, and 2n demonstrated enhanced potency compared with positive controls | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Anti-inflammatory activity | |
| 650 | 4 | |a Cyclooxygenase | |
| 650 | 4 | |a Enzyme | |
| 650 | 4 | |a Lipoxygenase | |
| 650 | 4 | |a Unsaturated ketones | |
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| 650 | 7 | |a Cyclohexanones |2 NLM | |
| 650 | 7 | |a Cyclooxygenase 2 Inhibitors |2 NLM | |
| 650 | 7 | |a Cyclooxygenase Inhibitors |2 NLM | |
| 650 | 7 | |a Lipoxygenase Inhibitors |2 NLM | |
| 650 | 7 | |a Pyrazines |2 NLM | |
| 650 | 7 | |a cyclohexanone |2 NLM | |
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| 650 | 7 | |a tetramethylpyrazine |2 NLM | |
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| 700 | 1 | |a Alharbi, Khalid Saad |e verfasserin |4 aut | |
| 700 | 1 | |a Alzarea, Abduaziz Ibrahim |e verfasserin |4 aut | |
| 700 | 1 | |a Alruwaili, Nabil K |e verfasserin |4 aut | |
| 700 | 1 | |a Alotaibi, Moureq Rashed |e verfasserin |4 aut | |
| 700 | 1 | |a Alotaibi, Nawaf M |e verfasserin |4 aut | |
| 700 | 1 | |a Alotaibi, Badriyah S |e verfasserin |4 aut | |
| 700 | 1 | |a Bukhari, Syed Nasir Abbas |e verfasserin |4 aut | |
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