人牙周膜成纤维细胞对甲硝唑摄取机制的研究

Study on the Uptake Mechanisms of metronidazole by human periodontal ligament fibroblasts

目的:研究人牙周膜成纤维细胞对甲硝唑的摄取,探讨摄取的机制及为通过牙根管给药途径提供实验依据。方法:采用高效液相色谱法研究人牙周膜成纤维细胞与甲硝唑孵育后不同时间细胞内药物的浓度,细胞内药物浓度与细胞外药物浓度的关系,以及温度、pH和转运抑制剂丙磺舒和腺嘌呤对细胞摄取甲硝唑的影响。结果:(1)孵育3min后人牙周膜成纤维细胞胞内甲硝唑浓度即可达到细胞外水平,之后胞内甲硝唑浓度出现逐渐降低,并在15min后达到平稳;(2)细胞内甲硝唑浓度随着细胞外甲硝唑浓度的增加而呈线性增加;(3)温度、pH和转运抑制剂对人牙周膜成纤维细胞摄取甲硝唑无明显影响。结论:人牙周膜成纤维细胞可快速摄取甲硝唑;甲硝唑通过简单扩散方式进入细胞内。

Objective： To investigate the uptake mechanisms of metronidazole by human periodontal ligament fibroblasts （HPDLF）, and explore the feasibility of drug delivery through the root canal. Methods： Using high performance liquid chromatography, the influences of extracellular metronidazole concentrations, temperature, pH and inhibitors of transporters on the uptake of metronidazole by cultured HPDLF were tested. Results： （1）The intracellular metronidazole concentrations reached the extracellular levels in 3 minutes after incubation, thereafter cell-associated agent progressively declined until it reached a stable plateau in 15 minutes. （2）The intracellular metronidazole concentrations increased linearly with the extracellular levels. （3） Temperature, pH and transport inhibitors had no significant effect on the uptake of agent by HPDLF. Conclusion： HPDLF can takeup metronidazole rapidly. Metronidazole enters into HPDLF in simple diffusion manner.