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Design, Synthesis,and Biological Activity of 18β-Glycyrrhetinic Acid Derivatives and Their Metal Complexes
1 , * 1 , * 2
1  Laboratory of Xinjiang Phytomedicine Resource and Utilization, Ministry of Education, School of Pharmaceutical Sciences, Shihezi University, Shihezi, 832002
2  Stake Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing, 100191
Academic Editor: Alfredo Berzal-Herranz


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. 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.

Keywords: Glycyrrhetinic acid; Synthesis; Anti-bacterial activity; Anti-fungal activity
Comments on this paper
Ke Yang
This paper is informative and provides a reference for a wide range of scholars on the study of natural compounds.

Qiaohui Liu
18β-glycyrrhetinic acid (18β-glycyrrhetinic acid) is a monomer with a wide range of pharmacological activities. It is of certain significance to use it as a candidate drug for the synthesis and evaluation of biological activities, which can provide a certain reference for the utilization and development of glycyrrhiza licorice

Guanzhong Chen
This paper provides a new reference for the modification of natural products

Guanzhong Chen
This paper provides a new reference for the modification of natural products

xiaoying sun
The article clear thinking, strong application

The experimental design is reasonable

Caiyun Yang
In this study, the structure of glycyrrhizic acid was modified and screened for in vitro antibacterial activity, and the resulting compound showed better antibacterial activity than the parent compound, providing some new ideas for the development of glycyrrhizic acid.