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Inhibition of carbonic anhydrase isozymes I and II with natural products extracted from plants, mushrooms and honey

机译:从植物,蘑菇和蜂蜜中提取的天然产物对碳酸酐酶同工酶I和II的抑制作用

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Different natural products and secondary metabolites from mushrooms, teas, honeys, mosses, plants and seaweeds were investigated for their in vitro inhibitory effects on human carbonic anhydrase (hCA, E.C.4.2.1.1) isoforms I and II. Inhibition data were correlated with the total phenol content in the extract and investigated with the pure compounds believed to be responsible for this activity. Methanolic extracts were prepared for 17 such pure chemicals present in the natural products and for 41 diverse natural products. The IC50 values were in the range of 0.11–66.50 μg/mL against hCA I and of 0.09–54.54 μg/mL against hCA II, respectively. The total phenol content was in the range of 0.02–1318.96 (as milligrams of gallic acid equivalents) per gram of sample. These data offer new insights on possible novel classes of CA inhibitors based on natural products, possessing a range of chemical structures not present in the classical inhibitors with pharmacological applications, such as the sulfonamides and sulfamates.
机译:研究了来自蘑菇,茶,蜂蜜,苔藓,植物和海藻的不同天然产物和次生代谢产物对人碳酸酐酶(hCA,E.C.4.2.1.1)亚型I和II的体外抑制作用。抑制数据与提取物中的总酚含量相关,并用据信对此活性负责的纯化合物进行了研究。制备了针对天然产物中存在的17种此类纯化学品和41种天然产物的甲醇提取物。针对hCA I的IC 50 值分别在0.11–66.50μg/ mL和针对hCA II的0.09–54.54μg/ mL范围内。每克样品中总苯酚含量在0.02–1318.96(以没食子酸当量毫克计)的范围内。这些数据为基于天然产物的可能的新型CA抑制剂提供了新的见解,具有一系列具有药理学应用的经典抑制剂(如磺酰胺和氨基磺酸盐)中不存在的化学结构。

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