Aroonrerk Nuntana, Niyomtham Nattisa, Yingyoungnarongkul Boon-Ek
Department of Stomatology, Faculty of Dentistry, Srinakharinwirot University, Bangkok, Thailand.
Med Princ Pract. 2016;25(2):130-6. doi: 10.1159/000442164. Epub 2015 Nov 4.
To evaluate the effect of N-benzyl-4-bromobenzamide (NBBA) on lipopolysaccharide (LPS)-induced IL-6 and prostaglandin E2 (PGE2) production in human gingival fibroblasts (HGFs).
The benzamide compound was synthesized. The condition for IL-6 production of HGFs after induction with LPS was optimized. The HGFs were incubated with NBBA (10 µg/ml) for 30 min before LPS (1 μg/ml) was added. After 24 h of incubation time, the culture media were harvested and their IL-6 and PGE2 contents were determined using an enzyme-linked immunosorbent assay. Prednisolone (PDS) and NS-398 were used as positive controls. Statistical analysis of the IL-6 and PGE2 contents was performed using the ANOVA test followed by the Tukey multiple-comparisons test to compare replicate means. p < 0.001 was considered statistically significant.
The maximum IL-6 production was achieved when HGFs were exposed to 1 μg/ml of LPS for 24 h, which was inhibited by the IL-6 immunosuppressant PDS. The benzamide compound, NBBA, exhibited a potent anti-IL-6 activity with inhibition of 35.6 ± 0.5%, significantly different from in the LPS-induced HGFs (p < 0.001). In addition, it inhibited 75.6 ± 0.52% PGE2 production. Cell viability was not significantly affected by treatment with NBBA at a concentration <10 µg/ml (p < 0.001).
NBBA exhibited an inhibitory effect on the production of IL-6 and PGE2 in LPS-induced HGFs. It could serve as a compound with inhibiting inflammatory activity in periodontal disease.
评估N-苄基-4-溴苯甲酰胺(NBBA)对脂多糖(LPS)诱导的人牙龈成纤维细胞(HGFs)产生白细胞介素-6(IL-6)和前列腺素E2(PGE2)的影响。
合成苯甲酰胺化合物。优化LPS诱导后HGFs产生IL-6的条件。在加入LPS(1μg/ml)之前,将HGFs与NBBA(10μg/ml)孵育30分钟。孵育24小时后,收集培养基,使用酶联免疫吸附测定法测定其IL-6和PGE2含量。泼尼松龙(PDS)和NS-398用作阳性对照。使用方差分析(ANOVA)检验对IL-6和PGE2含量进行统计分析,随后进行Tukey多重比较检验以比较重复均值。p<0.001被认为具有统计学意义。
当HGFs暴露于1μg/ml LPS 24小时时,可实现最大IL-6产生,这被IL-6免疫抑制剂PDS所抑制。苯甲酰胺化合物NBBA表现出强大的抗IL-6活性,抑制率为35.6±0.5%,与LPS诱导的HGFs中的情况有显著差异(p<0.001)。此外,它抑制了75.6±0.52%的PGE2产生。浓度<10μg/ml的NBBA处理对细胞活力没有显著影响(p<0.001)。
NBBA对LPS诱导的HGFs中IL-6和PGE2的产生具有抑制作用。它可作为一种在牙周疾病中具有抑制炎症活性的化合物。