journal article·2021-03-17

In Vitro and In Vivo Demonstration of Ultraefficient and Broad-Spectrum Antibacterial Agents for Photodynamic Antibacterial Chemotherapy

Qicai Xiao, Bingjie Mai, Yichu Nie, Chuang Yuan, Menghua Xiang, Zihan Shi, Juan Wu, Wingnang Leung, Chuanshan Xu, Shao Q. Yao, Pan Wang, Liqian Gao

ACS Applied Materials & Interfaces· Volume 13· Issue 10
Publisher page

Abstract

Increasing threats from both pathogenic infections and antibiotic resistance highlight the pressing demand for nonantibiotic agents and alternative therapies. Herein, we report several new phenothiazinium-based derivatives, which could be readily synthesized via fragment-based assembly, which exhibited remarkable bactericidal activities both in vitro and in vivo. Importantly, in contrast to numerous clinically and preclinically used antibacterial photosensitizers, these compounds were able to eliminate various types of microorganisms, including Gram-(+) Staphylococcus aureus (S. aureus), Gram-(−) Escherichia coli, multidrug-resistant S. aureus, and their associated biofilms, at low drug and light dosages (e.g., 0.21 ng/mL in vitro and 1.63 ng/cm2 in vivo to eradicate S. aureus at 30 J/cm2). This study thus unveils the potential of these novel phenothiaziniums as potent antimicrobial agents for highly efficient photodynamic antibacterial chemotherapy.
Source: openalex_inverted_index · Quality: baseline

Research context

OpenAlex topics: Phenothiazines and Benzothiazines Synthesis and Activities · Innovative Microfluidic and Catalytic Techniques Innovation · Antibiotic Resistance in Bacteria

SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.

Affiliations

School of Pharmaceutical Sciences (Shenzhen), Sun Yat-Sen University, Shenzhen 518107, P. R. China

School of Chinese Medicine, The Chinese University of Hong Kong, Hong Kong, China

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore

Key Laboratory of Medicinal Resources and Natural Pharmaceutical Chemistry, Ministry of Education, College of Life Sciences, Shaanxi Normal University, Xi’an 710119, P. R. China

Department of Hematology, Xiangya Hospital, Central South University, Changsha 410000, P. R. China

Department of Critical Care Medicine, The Second People’s Hospital of Shenzhen & First Affiliated Hospital of Shenzhen University, Health Science Center, Shenzhen 518035, P. R. China

The Fifth Affiliated Hospital, Key Laboratory of Molecular Target & Clinical Pharmacology and the State Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou 511436, P. R. China

Funding

National Sun Yat-sen University · Government of Guangdong Province · National Natural Science Foundation of China · Natural Science Foundation of Guangdong Province · Funds of Talents for High-level University in the Construction of Guangzhou Medical University · Innovation and Technology Fund of Shenzhen

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