Screening for anti-anaerobic drug candidates is still challenging although the anaerobic bacteria are important sources for human infections, because the method for anti-anaerobic activity testing is not readily available with low-cost and -expertise. We report a novel method for the determination of the anti-anaerobic activity of drug candidates by automated headspace-gas chromatography (HS-GC). Anaerobic bacteria were inoculated in an anaerobic atmosphere or rapidly using sterile syringe in an air-tight manner, and incubated with and without drugs for 48 h. The metabolic acidities of the cultured media were used as an indicator of cell activities and measured as end-products in place by HS-GC after being completely converted to CO2 with sodium bicarbonate. The present method is precise (relative standard deviation is below 5%) and validated by excellent agreements with a reference method on the determinations of the inhibition rates (root-mean-square error = 10%, n = 48) and half maximal inhibitory concentrations (R2 = 0.996, n = 8) of both pure drug compounds and plant extracts. Advantageously, the present method is sensitive in response to cell activity, safe with regard to cross contamination, and suitable for routine screening of diversified drug candidates for anti-anaerobic activity.

中文翻译：

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基于培养基中代谢酸度变化的相变顶空技术，用于确定候选药物的抗厌氧活性。

尽管厌氧细菌是人类感染的重要来源，但筛选抗厌氧药物的候选药物仍具有挑战性，因为低成本，专业性的抗厌氧活性测试方法不易获得。我们报告了一种通过自动顶空气相色谱法（HS-GC）确定候选药物的抗厌氧活性的新方法。将厌氧细菌在无氧环境中或使用无菌注射器以气密方式快速接种，并在有毒和无毒条件下孵育48小时。培养基的代谢酸度用作细胞活性的指标，并在用碳酸氢钠完全转化为二氧化碳后，通过HS-GC作为最终产物进行测量。本方法精确（相对标准偏差低于5％），并且与参考方法在抑制率（均方根误差= 10％，n = 48）和最大抑制浓度的一半的测定上具有很好的一致性，从而得到了验证。纯药物化合物和植物提取物的（R2 = 0.996，n = 8）。有利地，本发明方法对细胞活性敏感，对于交叉污染是安全的，并且适合常规筛选多种候选药物的抗厌氧活性。