Department of Pathology and Laboratory Medicine, University of California, Irvine, CA 92697-4800, USA.
J Infect Dis. 2011 Nov;204(9):1313-20. doi: 10.1093/infdis/jir552. Epub 2011 Sep 20.
The salicylidene acylhydrazide INP0341 inhibits growth of Chlamydia in HeLa cells, has negligible cell toxicity, and does not inhibit the growth of lactobacilli. The antichlamydial activity of INP0341 was retained when tested in vaginal and semen simulants. Vaginal tissue from INP0341-treated mice appeared similar to control sham-treated mice. To determine whether INP0341 can protect mice from a vaginal challenge, C3H/HeJ mice were either sham or INP0341 treated intravaginally pre- and postinoculation with 5 × 10(2) inclusion-forming units (IFUs) of Chlamydia trachomatis serovar D. Vaginal cultures taken over a month-long period showed a significant difference in the number of control mice that were culture positive versus the number in the INP0341-treated group, 100% (25/25) and 31% (8/26), respectively (P < .05). The quantity of IFUs shed and antibody titers to Chlamydia were significantly higher for the control group (P < .05). In summary, INP0341 is a promising compound to be considered for formulation as a vaginal microbicide.
水杨酰腙 INP0341 抑制 HeLa 细胞中的衣原体生长，细胞毒性可忽略不计，并且不抑制乳杆菌的生长。在阴道和精液模拟物中进行测试时，INP0341 的抗衣原体活性得以保留。经 INP0341 处理的小鼠阴道组织与对照假处理的小鼠相似。为了确定 INP0341 是否可以保护小鼠免受阴道挑战，C3H/HeJ 小鼠在阴道接种 5×10(2)包涵体形成单位（IFU）沙眼衣原体血清型 D 前后经阴道给予 INP0341 假处理或 INP0341 处理。在一个月的时间内进行的阴道培养显示，对照组中培养阳性的小鼠数量与 INP0341 处理组相比有显著差异，分别为 100%（25/25）和 31%（8/26）（P<.05）。对照组中 IFU 的脱落量和针对衣原体的抗体滴度明显更高（P<.05）。总之，INP0341 是一种很有前途的化合物，可考虑作为阴道杀微生物剂进行制剂开发。
