A light-activatable antibiotic with high activation efficiency and uncompromised bactericidal potency in the activated state

Delong Hou , Rui Wang , Zhonghui Wang , Gaofu Yang , Zhou Xu , Qi Zeng , Yi Chen

Collagen and Leather ›› 2021, Vol. 3 ›› Issue (1)

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Collagen and Leather ›› 2021, Vol. 3 ›› Issue (1) DOI: 10.1186/s42825-021-00051-6
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A light-activatable antibiotic with high activation efficiency and uncompromised bactericidal potency in the activated state

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Abstract

Abstract

Achieving activatable antibiotics represents one promising solution to tackle the occurrence of side effects, one major issue now plaguing antibiotic usage in collagen-based biomaterials. Despite considerable effort, however, rationale design of activatable antibiotics that display high activation efficiency and uncompromised bactericidal potency in the activated state remains difficult. Here, we demonstrate a design principle that helps to address this challenge. This strategy differs from previous attempts by underscoring photolytic removal of a functionality directly conjugated to the pharmacophore of an antibiotic, enabling not only an activation efficiency significantly improved beyond previous light-activatable antibiotics, but also bactericidal activity in the activated state as potent as the parent drug.

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Delong Hou, Rui Wang, Zhonghui Wang, Gaofu Yang, Zhou Xu, Qi Zeng, Yi Chen. A light-activatable antibiotic with high activation efficiency and uncompromised bactericidal potency in the activated state. Collagen and Leather, 2021, 3(1): DOI:10.1186/s42825-021-00051-6

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Funding

National Natural Science Foundation of China(21878196)

Sichuan Science and Technology Program(2020YJ0315)

Science and Technology Program of State Administration for Market Regulation(2020YJ024)

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