无抗菌活性的红霉素衍生物对体外培养T淋巴细胞增殖的影响

Effects of erythromycin derivatives without antibacterial activity on T lymphocyte proliferation in vitro

目的:观察无抗菌活性的红霉素衍生物对体外培养T淋巴细胞增殖的影响,探讨其抗炎活性的机制。方法:利用MTT方法比较9种红霉素衍生物对体外培养T淋巴细胞增殖影响的不同。结果:红霉素、克拉霉素、N-去甲基红霉素衍生物、9(S-)羟基红霉素和十二元环红霉素衍生物抑制T淋巴细胞增殖的活性较明显,其IC50值分别是(606.28±35.43)(、431.62±25.60)、(367.31±32.60)(、425.62±32.08)和(176.38±10.42)μmol/L,其中十二元环红霉素衍生物的IC50值明显低于红霉素和克拉霉素。结论:红霉素及其衍生物具有抑制T淋巴细胞增殖的活性,此活性可能与其抗炎活性有一定关联。

Objective： To study the effect of erythromyein derivatives without antibacterial activity on the proliferation of T lymphocytes in vitro and to evaluate their anti-inflammatory mechanism. Melhods： T lymphocytes were treated with erythromycin and 9 erythromycin derivatives within the dose range of 3 to 100 μg/mL for 24 hours. The inhibitory effects of erythromycin and 9 erythromycin derivatives on the proliferation of T lymphocytes cultured in vitro were determined by MTT assay. Results： The proliferation of T lymphocytes was inhibited by erythromycin, clarithromycin, N-demethyl erythromycin,9（S）-hydroxyl erythromycin, and 12-membered-ring erythromycin derivative, and 50% inhibitory concentrations （IC50） were 606.28±35.43,431.62±25.60, 367.31±32.60, 425.62±32.08, and 176.38±10.42 μmol/L, respectively. The IC50 of 12-membered-ring erythromycin derivative was significantly lower than that of erythromycin and clarithromycin. Conclusion： Erythromycin and its derivatives could inhibit the proliferation of T lymphocytes, which may be related with the anti-inflammatory activity to some extent.