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A niclosamide–tobramycin hybrid adjuvant potentiates cefiderocol against P. aeruginosa
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2021-07-27 , DOI: 10.1039/d1md00206f Liam Berry 1 , Marc Brizuela 1 , Gregory Jackson 1 , Frank Schweizer 1, 2
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2021-07-27 , DOI: 10.1039/d1md00206f Liam Berry 1 , Marc Brizuela 1 , Gregory Jackson 1 , Frank Schweizer 1, 2
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There is an urgent need for new therapies to overcome antimicrobial resistance (AMR) especially against Gram-negative bacilli (GNB). Multicomponent therapy combining antibiotics with enhancer molecules known as adjuvants is an emerging strategy to combat AMR. We have previously reported tobramycin-based adjuvants which are able to potentiate various antibiotics. In order to expand the repertoire of tobramycin hybrid adjuvants, a new hybrid containing niclosamide, an FDA approved anthelmintic which has recently demonstrated a variety of interesting biological effects, was synthesized. It was found that this conjugate can potentiate several antibiotics against multidrug-resistant GNB, including the recently approved siderophore cephalosporin cefiderocol. 8 μg ml−1 of the niclosamide–tobramycin hybrid in combination therapy against a pandrug-resistant strain of P. aeruginosa was able to lower the cefiderocol MIC 32-fold, from 8 μg ml−1 to 0.25 μg ml−1 in iron-rich media where siderophore uptake is reduced. These results indicate that a niclosamide–tobramycin hybrid adjuvant can serve to potentiate a newly approved antibiotic.
中文翻译：
氯硝柳胺-妥布霉素混合佐剂可增强头孢地洛对铜绿假单胞菌的抵抗力
迫切需要新的疗法来克服抗菌素耐药性 (AMR)，尤其是针对革兰氏阴性杆菌 (GNB)。将抗生素与被称为佐剂的增强剂分子相结合的多组分疗法是对抗 AMR 的新兴策略。我们之前曾报道过能够增强各种抗生素的基于妥布霉素的佐剂。为了扩大妥布霉素杂合佐剂的库，合成了一种含有氯硝柳胺的新杂合剂，一种 FDA 批准的驱虫剂，最近证明了多种有趣的生物效应。发现这种结合物可以增强几种抗生素对多重耐药 GNB 的作用，包括最近批准的铁载体头孢菌素头孢哌啶醇。8微克毫升-1氯硝柳胺-妥布霉素杂合体联合治疗铜绿假单胞菌的泛耐药菌株能够在铁载体吸收的富铁培养基中将头孢地洛 MIC 从 8 μg ml -1降低到 0.25 μg ml -1 32 倍降低了。这些结果表明，氯硝柳胺-妥布霉素混合佐剂可用于增强新批准的抗生素。
更新日期：2021-08-09
中文翻译：
氯硝柳胺-妥布霉素混合佐剂可增强头孢地洛对铜绿假单胞菌的抵抗力
迫切需要新的疗法来克服抗菌素耐药性 (AMR)，尤其是针对革兰氏阴性杆菌 (GNB)。将抗生素与被称为佐剂的增强剂分子相结合的多组分疗法是对抗 AMR 的新兴策略。我们之前曾报道过能够增强各种抗生素的基于妥布霉素的佐剂。为了扩大妥布霉素杂合佐剂的库，合成了一种含有氯硝柳胺的新杂合剂，一种 FDA 批准的驱虫剂，最近证明了多种有趣的生物效应。发现这种结合物可以增强几种抗生素对多重耐药 GNB 的作用，包括最近批准的铁载体头孢菌素头孢哌啶醇。8微克毫升-1氯硝柳胺-妥布霉素杂合体联合治疗铜绿假单胞菌的泛耐药菌株能够在铁载体吸收的富铁培养基中将头孢地洛 MIC 从 8 μg ml -1降低到 0.25 μg ml -1 32 倍降低了。这些结果表明，氯硝柳胺-妥布霉素混合佐剂可用于增强新批准的抗生素。
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