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Exploration of collagenase, cyclooxigenases, angiogenesis and free radical processes as the putative pharmacological targets of Arum maculatum L.
Biotechnology & Biotechnological Equipment ( IF 1.5 ) Pub Date : 2020-01-01 , DOI: 10.1080/13102818.2020.1722239
Vladimir Kochmarov 1, 2 , Lyubomir Marinov 1 , Ekaterina Kozuharova 3 , Nadya Hristova-Avakumova 4 , Vera Hadjimitova 4 , Trayko Traykov 4 , Sefedin Biljali 5 , Nexhibe Nuhiu 6 , Niko Benbassat 3 , Georgi Momekov 1
Affiliation  

Abstract In line with the well-established ethnobotanical use of Arum maculatum for the treatment of hemorrhoidal disease, we sought to determine the activities of 30% or 70% ethanol extracts of the plant tubers in an array of pharmacological and biochemical models of some crucial events implicated in the pathogenesis of this disorder, namely angiogenesis, collagenase activity remodeling, cyclooxygenase activity, IL-2 secretion and oxidative stress. The tested hydro-alcoholic extracts from A. maculatum tubers inhibited the proliferation of EA.hy926 vascular endothelial cells, but even at the highest administered concentrations no decrease in viability was observed. The extracts induced a concentration-dependent decrease in collagenase activity, whereby the effects were more pronounced at the lower concentration of ethanol in the extragent. Moreover the tested extracts induced concentration-dependent suppression of cyclooxygenase activity (COX-1 and 2), albeit at very high and presumably supraphysiological concentrations. The extracts augmented the PHA/PMA-induced secretion of IL-2 from Jurkat E.6 (human T-cells), which was more pronounced following exposure to the 30% ethanol-derived product. The 30% EtOH extract demonstrated anti-radical properties against both stable free radicals (ABTS and DPPH) and biologically relevant reactive oxygen species (ROS), which could be considered as important mediators of inflammation and signaling molecules. Our findings give us reason to conclude that the hydroalcoholic extracts of A. maculatum tubers possess anti-inflammatory, antiangiogenic and antioxidant effects which in concert could contribute to its efficacy for the management of hemorrhoidal disease.

中文翻译:

胶原酶、环氧酶、血管生成和自由基过程作为黄斑魔芋推定药理靶点的探索。

摘要 与黄斑魔芋治疗痔病的民族植物学应用相一致,我们试图在一些关键事件的药理和生化模型中确定植物块茎的 30% 或 70% 乙醇提取物的活性。参与该疾病的发病机制,即血管生成、胶原酶活性重塑、环氧合酶活性、IL-2 分泌和氧化应激。来自 A. maculatum 块茎的测试水醇提取物抑制了 EA.hy926 血管内皮细胞的增殖,但即使在最高给药浓度下,也未观察到活力降低。提取物诱导胶原酶活性的浓度依赖性降低,由此在提取剂中较低浓度的乙醇下效果更显着。此外,测试的提取物诱导浓度依赖性抑制环氧合酶活性(COX-1 和 2),尽管浓度非常高并且可能是超生理浓度。提取物增强了 PHA/PMA 诱导的 Jurkat E.6(人 T 细胞)分泌 IL-2,在暴露于 30% 乙醇衍生产品后,这种分泌更为明显。30% 乙醇提取物显示出对稳定自由基(ABTS 和 DPPH)和生物相关活性氧 (ROS) 的抗自由基特性,可将其视为炎症和信号分子的重要介质。我们的发现使我们有理由得出结论,A. maculatum 块茎的水醇提取物具有抗炎作用,
更新日期:2020-01-01
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