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Pharmacological appraisal of ligustrazine based cyclohexanone analogs as inhibitors of inflammatory markers.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-03-09 , DOI: 10.1016/j.ejps.2020.105299 Nasser Hadal Alotaibi 1 , Khalid Saad Alharbi 1 , Abduaziz Ibrahim Alzarea 1 , Nabil K Alruwaili 1 , Moureq Rashed Alotaibi 2 , Nawaf M Alotaibi 3 , Badriyah S Alotaibi 4 , Syed Nasir Abbas Bukhari 1
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-03-09 , DOI: 10.1016/j.ejps.2020.105299 Nasser Hadal Alotaibi 1 , Khalid Saad Alharbi 1 , Abduaziz Ibrahim Alzarea 1 , Nabil K Alruwaili 1 , Moureq Rashed Alotaibi 2 , Nawaf M Alotaibi 3 , Badriyah S Alotaibi 4 , Syed Nasir Abbas Bukhari 1
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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.
中文翻译：
川gust嗪类环己酮类似物作为炎性标记抑制剂的药理鉴定。
当急性炎症在病理状态中扩散时，促炎酶的靶向成为治疗干预。这项研究旨在评估与基于川azine嗪的28种环己酮类似物具有炎症相关性的抑制和诱导酶。使用抑制剂筛选测定试剂盒进行了测试，使用了一系列合成化合物来研究它们如何抑制环氧合酶（COX），分泌性磷脂酶A2（sPLA2）和脂氧合酶（LOX）的活性。对于包括1f和1g（IC50 = 2.2μM）的合成化合物，发现对sPLA2具有明显和相似的抑制活性。化合物1d（IC50 = 8.1μM）和1e（IC50 = 7.5μM）对LOX酶具有最佳抑制活性。另外，化合物1b，1d，1e，2n和2o被证明是COX-1活性的重要抑制剂，IC50值为0.09至0.7μM。抑制COX的测定结果表明，相同的化合物对COX-2酶具有更强的抑制作用，与阳性对照相比，某些化合物（如1d，1e和2n）具有增强的效力。
更新日期：2020-03-09
中文翻译：
川gust嗪类环己酮类似物作为炎性标记抑制剂的药理鉴定。
当急性炎症在病理状态中扩散时，促炎酶的靶向成为治疗干预。这项研究旨在评估与基于川azine嗪的28种环己酮类似物具有炎症相关性的抑制和诱导酶。使用抑制剂筛选测定试剂盒进行了测试，使用了一系列合成化合物来研究它们如何抑制环氧合酶（COX），分泌性磷脂酶A2（sPLA2）和脂氧合酶（LOX）的活性。对于包括1f和1g（IC50 = 2.2μM）的合成化合物，发现对sPLA2具有明显和相似的抑制活性。化合物1d（IC50 = 8.1μM）和1e（IC50 = 7.5μM）对LOX酶具有最佳抑制活性。另外，化合物1b，1d，1e，2n和2o被证明是COX-1活性的重要抑制剂，IC50值为0.09至0.7μM。抑制COX的测定结果表明，相同的化合物对COX-2酶具有更强的抑制作用，与阳性对照相比，某些化合物（如1d，1e和2n）具有增强的效力。
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