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Carbon Nanotubes Modulate Activity of Cytotoxic Compounds via a Trojan Horse Mechanism.
Chemical Research in Toxicology ( IF 3.7 ) Pub Date : 2020-02-10 , DOI: 10.1021/acs.chemrestox.9b00370 Lokesh Mehta 1 , Shweta Kumari 1 , Raman Preet Singh 1
Chemical Research in Toxicology ( IF 3.7 ) Pub Date : 2020-02-10 , DOI: 10.1021/acs.chemrestox.9b00370 Lokesh Mehta 1 , Shweta Kumari 1 , Raman Preet Singh 1
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Carbon nanotubes (CNTs) are an emerging drug delivery system, but their success is thwarted by potential toxicity concerns. In vitro and in vivo studies imply toxic potential of CNTs, but their potential to influence toxicity of coadministered compounds still remains elusive. Therefore, the present study was conducted to determine the effect of multiwalled CNTs (MWCNTs) on the toxicity of cytotoxic compounds in macrophage (RAW 264.7), lung epithelial (A549), and breast cancer (MCF-7) cell lines. The results suggest that hydrophilicity/lipophilicity of the compounds is a critical parameter. The correlation between log P and enhanced cytotoxic activity followed an inverted U-shaped curve and log P close to 1 exhibited the highest increase in cytotoxicity. Further, the increase in cytotoxicity of drug/MWCNT combinations was proportional to the degree of cellular uptake of MWCNTs. A mathematical model was developed and validated with a test set of compounds. These results suggest that MWCNTs act as a "Trojan horse" for increased intracellular delivery of drugs resulting in enhanced cytotoxic activity.
中文翻译：
碳纳米管通过特洛伊木马机制调节细胞毒性化合物的活性。
碳纳米管（CNTs）是新兴的药物递送系统，但潜在的毒性问题阻碍了它们的成功。体外和体内研究暗示了CNTs的潜在毒性，但其影响共同给药化合物毒性的潜力仍然难以捉摸。因此，进行本研究以确定多壁CNT（MWCNT）对巨噬细胞（RAW 264.7），肺上皮细胞（A549）和乳腺癌（MCF-7）细胞系中细胞毒性化合物毒性的影响。结果表明，化合物的亲水性/亲脂性是关键参数。log P和增强的细胞毒性活性之间的相关性呈倒U形曲线，log P接近1时显示出最高的细胞毒性增加。进一步，药物/ MWCNT组合的细胞毒性增加与MWCNT的细胞摄取程度成正比。建立了数学模型，并通过化合物测试集进行了验证。这些结果表明，MWCNT充当“特洛伊木马”，用于增加药物的细胞内递送，从而导致增强的细胞毒性活性。
更新日期：2020-02-03
中文翻译：
碳纳米管通过特洛伊木马机制调节细胞毒性化合物的活性。
碳纳米管（CNTs）是新兴的药物递送系统，但潜在的毒性问题阻碍了它们的成功。体外和体内研究暗示了CNTs的潜在毒性，但其影响共同给药化合物毒性的潜力仍然难以捉摸。因此，进行本研究以确定多壁CNT（MWCNT）对巨噬细胞（RAW 264.7），肺上皮细胞（A549）和乳腺癌（MCF-7）细胞系中细胞毒性化合物毒性的影响。结果表明，化合物的亲水性/亲脂性是关键参数。log P和增强的细胞毒性活性之间的相关性呈倒U形曲线，log P接近1时显示出最高的细胞毒性增加。进一步，药物/ MWCNT组合的细胞毒性增加与MWCNT的细胞摄取程度成正比。建立了数学模型，并通过化合物测试集进行了验证。这些结果表明，MWCNT充当“特洛伊木马”，用于增加药物的细胞内递送，从而导致增强的细胞毒性活性。
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