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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Synergistic enhancement of beta-lactam antibiotics by modified tunicamycin analogs TunR1 and TunR2
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Synergistic enhancement of beta-lactam antibiotics by modified tunicamycin analogs TunR1 and TunR2

机译：通过改性的unicamycin类似物Tunr1和TunR2通过改性β-内酰胺抗生素的协同增强

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摘要

The beta-lactams are the most widely used group of antibiotics in human health and agriculture, but this is under threat due to the persistent rise of pathogenic resistance. Several compounds, including tunicamycin (TUN), can enhance the antibacterial activity of the beta-lactams to the extent of overcoming resistance, but the mammalian toxicity of TUN has precluded its use in this role. Selective hydrogenation of TUN produces modified compounds (TunR1 and TunR2), which retain the enhancement of beta-lactams while having much lower mammalian toxicity. Here we show that TunR1 and TunR2 enhance the antibacterial activity of multiple beta-lactam family members, including penems, cephems, and third-generation penicillins, to a similar extent as does the native TUN. Eleven of the beta-lactams tested were enhanced from 2 to >256-fold against Bacillus subtilis, with comparable results against a penicillin G-resistant strain. The most significant enhancements were obtained with third-generation aminothiazolidyl cephems, including cefotaxime, ceftazidime, and cefquinome. These results support the potential of low toxicity tunicamycin analogs (TunR1 and TunR2) as clinically valid, synergistic enhancers for a broad group of beta-lactam antibiotics.
机译：β-内酰胺是人类健康和农业中使用最广泛的抗生素组，但由于致病性抵抗的持续上升，这受到威胁。几种化合物，包括胞苷（屯），可以增强β-内酰胺的抗菌活性，以克服耐药程度，但猪的哺乳动物毒性排除了其在这种作用中的用途。 TUN的选择性氢化产生改性化合物（TUNR1和TUNR2），其保留β-内酰胺的增强，同时具有更低的哺乳动物毒性。在这里，我们表明TunR1和TunR2增强了多个β-内酰胺家族成员的抗菌活性，包括PEPEMS，Cephems和第三代青霉素，在类似的程度上尽可能多地。测试的β-内酰胺的110％从枯草芽孢杆菌的2〜> 256倍上增强，具有与青霉素G抗性菌株的相当的结果。最显着的增强率是用第三代氨基噻唑烷基Cephems获得的，包括头孢噻肟，头孢他啶和Cefinome。这些结果支持低毒性胞苷类霉素类似物（TUNR1和TUNR2）作为临床有效的β-内酰胺抗生素的协同增强剂。

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