幽门螺杆菌(H.幽门螺杆菌)近年来有所增加,促使新药研发的趋势。在我们的研究中,以6-姜酚为主要成分合成了三种衍生物(JF-1,JF-2和JF-3),而JF-4以6-姜酚和6-姜酚为主要成分,是从干姜中提取的。最小抑制浓度(MIC),使用比例稀释法确定,JF-1为80μg/mL,JF-2为40μg/mL,JF-3为30μg/mL,JF-4为40μg/mL,6-姜辣素标准品(SS)为60μg/mL,阿莫西林(AMX)为0.03μg/mL。治疗幽门螺杆菌感染的小鼠后,胃粘膜的炎症被抑制。Hp根除率为16.7%的JF-3低剂量治疗(LDT),25.0%的JF-3大剂量治疗(HDT),JF-4LDT的16.7%,JF-4HDT的16.7%,30%的SSLDT,50%的SSHDT,阳性对照组(PCG)的36.4%。胃泌素的水平,生长抑素(SST),IFN-γ,IL-4和IL-8在JF-3和JF-4给药组中显著恢复,但高剂量组的效果更强。这些结果表明,6-姜辣素及其衍生物具有显著的抗幽门螺杆菌作用,并且是幽门螺杆菌感染的有希望的潜在治疗方法。
The resistance of Helicobacter pylori (H. pylori) has increased in recent years, prompting a trend in the research and development of new drugs. In our study, three derivatives (JF-1, JF-2, and JF-3) were synthesized using 6-gingerol as the main component, while JF-4, containing both 6-gingerol and 6-shogaol as the main components, was extracted from dried ginger. The minimum inhibitory concentrations (MICs), determined using the ratio dilution method, were 80 μg/mL for JF-1, 40 μg/mL for JF-2, 30 μg/mL for JF-3, 40 μg/mL for JF-4, 60 μg/mL for 6-gingerol standard (SS), and 0.03 μg/mL for amoxicillin (AMX). After treating H. pylori-infected mice, the inflammation of the gastric mucosa was suppressed. The eradication rate of H. pylori was 16.7% of JF-3 low-dose treatment (LDT), 25.0% of JF-3 high-dose treatment (HDT), 16.7% of JF-4 LDT, 16.7% of JF-4 HDT, 30% of SS LDT, 50% of SS HDT, and 36.4% of the positive control group (PCG). The levels of gastrin,
somatostatin (SST), IFN-γ, IL-4, and IL-8 were significantly recovered in the JF-3 and JF-4 administration groups, but the effect was stronger in the high-dose group. These results demonstrate that 6-gingerol and its derivatives have significant anti-Helicobacter pylori effects and are promising potential treatments for H. pylori infection.