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Anti-Helicobacter pylori activities of selected N-substituted cinnamamide derivatives evaluated on reference and clinical bacterial strains.
The Journal of Antibiotics ( IF 3.3 ) Pub Date : 2018-May-01 , DOI: 10.1038/s41429-018-0027-1
Karolina Klesiewicz , Elżbieta Karczewska , Paweł Nowak , Iwona Skiba-Kurek , Edward Sito , Katarzyna Pańczyk , Paulina Koczurkiewicz , Dorota Żelaszczyk , Elżbieta Pękala , Anna M. Waszkielewicz , Alicja Budak , Henryk Marona , Agnieszka Gunia-Krzyżak

In this study, thirty-five N-substituted derivatives of cinnamic acid amide (cinnamamide) were evaluated for anti-Helicobacter pylori activity using an agar disc-diffusion method. Qualitative screening was performed on a reference H. pylori strain (ATCC 43504), resulting in the identification of the three most active compounds, 8 (R,S-(2E)-3-(4-chlorophenyl)-N-(2-hydroxypropyl)prop-2-enamide, minimal inhibitory concentration, MIC = 7.5 µg/mL), 23 ((2E)-3-(4-chlorophenyl)-N-(2-hydroxycyclohexyl)prop-2-enamide, MIC = 10 µg/mL), and 28 ((2E)-3-(4-chlorophenyl)-N-(4-oxocyclohexyl)prop-2-enamide, MIC = 10 µg/mL). These compounds were further tested on twelve well-characterized clinical strains, yielding MIC values that ranged from 10 to 1000 µg/mL. Preliminary safety assessments of the compounds were made using the MTT viability test for cytotoxicity and Ames test for mutagenicity, which showed them to be generally safe, although compounds 8 and 28 showed mutagenic activity at some of the tested concentrations. The results of this study showed the anti-H. pylori potential of cinnamamide derivatives.

中文翻译:

在参考菌株和临床细菌菌株上评估了选定的N-取代肉桂酰胺衍生物的抗幽门螺杆菌活性。

在这项研究中,使用琼脂圆盘扩散法评估了35种N-取代的肉桂酸酰胺(肉桂酰胺)衍生物的抗幽门螺杆菌活性。对参考幽门螺杆菌菌株(ATCC 43504)进行了定性筛选,从而鉴定出三种活性最高的化合物8(R,S-(2E)-3-(4-氯苯基)-N-(2-羟丙基)丙-2-烯酰胺,最小抑菌浓度,MIC = 7.5 µg / mL),23(((2E)-3-(4-氯苯基)-N-(2-羟基环己基)丙-2-烯酰胺,MIC = 10 µg / mL)和28((2E)-3-(4-氯苯基)-N-(4-氧代环己基)丙-2-烯酰胺,MIC = 10 µg / mL)。这些化合物在十二种特征明确的临床菌株上进行了进一步测试,得出的MIC值为10至1000 µg / mL。化合物的初步安全性评估是使用MTT细胞毒性的存活力测试和诱变的Ames测试进行的,这表明它们总体上是安全的,尽管化合物8和28在某些测试浓度下具有诱变活性。这项研究的结果显示了抗H。肉桂酰胺衍生物的幽门螺杆菌潜能。
更新日期:2018-02-13
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