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首页> 外文期刊>International journal of antimicrobial agents >SILA 421, an inhibitor of efflux pumps of cancer cells, enhances the killing of intracellular extensively drug-resistant tuberculosis (XDR-TB)
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SILA 421, an inhibitor of efflux pumps of cancer cells, enhances the killing of intracellular extensively drug-resistant tuberculosis (XDR-TB)

机译：SILA 421是癌细胞外排泵的抑制剂，可增强细胞内广泛耐药结核（XDR-TB）的杀伤力

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Multidrug-resistant and extensively drug-resistant tuberculosis (MDR/XDR-TB) are problematic to manage, especially in patients with acquired immune deficiency syndrome (AIDS). There is therefore a dire need for effective anti-MDR/XDR-TB agents. We have previously shown that agents that inhibit the efflux pumps of MDR bacteria and cancer cells also enhance killing of intracellular mycobacteria, possibly by increasing the availability of K~+ and Ca~(2+) needed for the activation of lysosomal enzymes of the phagolyso_somal unit. In this study, the newly synthesised and recently patented SILA 409 and 421 were tested for in vitro and ex vivo activity against XDR-TB. The minimum inhibitory concentration (MIC) of SILA compounds was determined by the BACTEC 460 TB system. The effect of each compound on the killing activity of human macrophages infected with XDR-TB was determined by exposing the macrophage that had phagocytosed the bacterium to the compounds and assessing the killing activity by colony-forming unit counting. Amongst the two compounds tested, SILA 421 was shown to have in vitro activity against XDR-TB (MIC <3.5 mg/L) and to transform non-killing macrophages into effective killers of phagocytosed bacteria, without any cytotoxic activity. Because SILA 421 revealed good in vitro and ex vivo activities and is devoid of any cytotoxic activity, it is a potential candidate as an anti-MDR/XDR-TB drug.
机译：多重耐药和广泛耐药结核病（MDR / XDR-TB）的管理存在问题，特别是在获得性免疫缺陷综合症（AIDS）患者中。因此，迫切需要有效的抗MDR / XDR-TB药物。先前我们已经表明，抑制MDR细菌和癌细胞外排泵的药物还可以增强细胞内分枝杆菌的杀伤力，这可能是通过增加激活吞噬酶溶酶体酶所需的K〜+和Ca〜（2+）的可用性来实现的。单元。在这项研究中，测试了新合成且最近获得专利的SILA 409和421对XDR-TB的体外和离体活性。 SILA化合物的最低抑菌浓度（MIC）由BACTEC 460 TB系统确定。通过将吞噬了细菌的巨噬细胞暴露于化合物中并通过菌落形成单位计数评估其杀伤活性，从而确定每种化合物对感染了XDR-TB的人类巨噬细胞的杀伤活性的影响。在测试的两种化合物中，已显示SILA 421具有抗XDR-TB（MIC <3.5 mg / L）的体外活性，并且可以将非杀伤性巨噬细胞转化为吞噬细胞的有效杀伤剂，而没有任何细胞毒活性。因为SILA 421表现出良好的体外和离体活性，并且没有任何细胞毒活性，所以它是抗MDR / XDR-TB药物的潜在候选者。

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