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新型喹诺酮类抗生素DW-116的免疫调节活性

Immunomodulating activity of DW-116, a new quinolone antibiotic.

作者信息

Moon E Y, Choi C H, Pyo S, Chung Y H, Yoon S J, Lee D K

机构信息

Central Research Laboratories, Dong-Wha Pharm. Ind. Co. Ltd., Anyang City, Kyunggi-do, Korea.

出版信息

Arch Pharm Res. 1998 Oct;21(5):610-4. doi: 10.1007/BF02975383.

Abstract

DW-116, (1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazinyl)-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid hydrochloride), is a new quinolone antibiotic with a broad antibacterial spectrum against G(+) and G(-) bacteria. DW-116 was evaluated for the immunomodulating activities, which is one of the efforts to investigate the mechanism of action related to the good in vivo antibacterial efficacy. The results of in vitro studies revealed there was no statistically significant increase in B and T lymphocyte proliferation. But the results of in vivo studies showed that the number of plaque forming cells (PFC), the amount of polyclonal antibodies and delayed-type hypersensitivity (DTH) were significantly increased after the repeat administration with 12 and 60 mg/kg of DW-116. Taken together, these results proposed that immunostimulating effect of DW-116 could be one of the action mechanisms for demonstrating in vivo antibacterial activities under these experimental conditions.

摘要

DW - 116,即1 -(5 - 氟 - 2 - 吡啶基)- 6 - 氟 - 7 -(4 - 甲基 - 1 - 哌嗪基)- 1,4 - 二氢 - 4 - 氧代喹啉 - 3 - 羧酸盐酸盐,是一种新型喹诺酮类抗生素,对革兰氏阳性菌和革兰氏阴性菌均具有广谱抗菌活性。对DW - 116的免疫调节活性进行了评估,这是研究其体内良好抗菌效果相关作用机制的工作之一。体外研究结果显示,B淋巴细胞和T淋巴细胞增殖无统计学意义的显著增加。但体内研究结果表明,重复给予12毫克/千克和60毫克/千克的DW - 116后,空斑形成细胞(PFC)数量、多克隆抗体量和迟发型超敏反应(DTH)均显著增加。综上所述,这些结果表明,在这些实验条件下,DW - 116的免疫刺激作用可能是其发挥体内抗菌活性的作用机制之一。

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