Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, Kraków, Poland.
Falck Medycyna Outpatient Clinic of Gastroenterology, Mazowiecka 4-6, Kraków, Poland.
J Antibiot (Tokyo). 2018 May;71(5):543-548. doi: 10.1038/s41429-018-0027-1. Epub 2018 Feb 13.
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.
在这项研究中,使用琼脂扩散法评估了 35 种 N-取代肉桂酰胺(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,鉴定出了三种最活性的化合物,8(R,S-(2E)-3-(4-氯苯基)-N-(2-羟基丙基)丙烯酰胺,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)丙烯酰胺,MIC = 10 µg/mL)和 28((2E)-3-(4-氯苯基)-N-(4-氧代环己基)丙烯酰胺,MIC = 10 µg/mL)。这些化合物进一步在 12 种经过充分表征的临床菌株上进行了测试,MIC 值范围为 10 至 1000 µg/mL。使用 MTT 活力试验进行细胞毒性和 Ames 试验进行致突变性的初步安全性评估表明,这些化合物通常是安全的,尽管化合物 8 和 28 在某些测试浓度下表现出致突变活性。这项研究的结果表明了肉桂酰胺衍生物的抗幽门螺杆菌潜力。