Abstract
The increasing morbidity and mortality caused by infections with pathogenic bacteria (fungus or bacteria) have highlighted an urgent requirement for developing novel anti-bacterial agents to protect the health and integrity of human life. 18β-glycyrrhetinic acid has a wide range of pharmacological effects including anti-bacterial, anti-inflammatory, and anti-tumor effects. Nevertheless, its relatively low biological activity and high toxicity limit its potential for anti-bacterial and other pharmaceutical applications. To improve the anti-bacterial activity of 18β-glycyrrhetinic acid, we designed and synthesized a total of 21 glycyrrhizic acid derivatives in 40–82% yields, among which 18 novel glycyrrhetinic acid derivatives, and the anti-bacterial and anti-fungal activities of all synthesized derivatives, were evaluated in vitro by measuring the minimum inhibitory concentration (MIC) of the compounds against the strain. The evaluation results showed that most of the compounds showed good inhibitory activity against different strains, among which compound 1 (MIC: 2 μg/mL) and compound 3 (MIC: 2 μg/mL) showed the strongest anti-fungal activity against Cryptococcus; compound 20 (MIC: 4 μg/mL) showed high anti-bacterial activity against Pseudomonas aeruginosa and merits further exploration as a new anti-bacterial and anti-fungal agent.
Supplementary Materials
The poster presentation can be downloaded at: https://www.mdpi.com/article/10.3390/ECMC2022-13193/s1.
Author Contributions
Conceptualization, X.P. and X.Y.; methodology, X.P. and X.Y.; experiment, C.Y.; validation, X.P.; formal analysis, C.Y.; investigation, C.Y.; resources, C.Y.; data curation, C.Y.; writing—original draft preparation, C.Y.; writing—review and editing, X.P.; supervision, X.P. and X.Y. All authors have read and agreed to the published version of the manuscript.
Funding
This study was supported by National Natural Science Foundation of China (82160651); The Open Project of Stake Key Laboratory of Natural and Biomimetic Drugs, Peking University (K202103); The Open Project of Key Laboratory of Xinjiang Phytomedicine Resource and Utilization, Ministry of Education (XPRU202004); Youth Innovative Talent Cultivation Projects of Shihezi University (CXPY202005) and The Open Sharing Fund for the Large-scale Instruments and Equipments of Shihezi University.
Institutional Review Board Statement
Not applicable.
Informed Consent Statement
Not applicable.
Data Availability Statement
The data presented in this study are available in the article.
Conflicts of Interest
The authors declare no conflict of interest.
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