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Volume 14
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10.3390/ECMC2022-13193
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Abstract

Design, Synthesis, and Biological Activity of 18β-Glycyrrhetinic Acid Derivatives and Their Metal Complexes †

by
Caiyun Yang
1,
Xinhui Pan
1,* and
Xiaoda Yang
2,*
1
Laboratory of Xinjiang Phytomedicine Resource and Utilization, Ministry of Education, School of Pharmaceutical Sciences, Shihezi University, Shihezi 832002, China
2
Stake Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
*
Authors to whom correspondence should be addressed.
†
Presented at the 8th International Electronic Conference on Medicinal Chemistry, 1–30 November 2022; Available online: https://ecmc2022.sciforum.net/.
Med. Sci. Forum 2022, 14(1), 129; https://doi.org/10.3390/ECMC2022-13193
Published: 1 November 2022
(This article belongs to the Proceedings of The 8th International Electronic Conference on Medicinal Chemistry)
Versions Notes

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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Share and Cite

MDPI and ACS Style

Yang, C.; Pan, X.; Yang, X. Design, Synthesis, and Biological Activity of 18β-Glycyrrhetinic Acid Derivatives and Their Metal Complexes. Med. Sci. Forum 2022, 14, 129. https://doi.org/10.3390/ECMC2022-13193

AMA Style

Yang C, Pan X, Yang X. Design, Synthesis, and Biological Activity of 18β-Glycyrrhetinic Acid Derivatives and Their Metal Complexes. Medical Sciences Forum. 2022; 14(1):129. https://doi.org/10.3390/ECMC2022-13193

Chicago/Turabian Style

Yang, Caiyun, Xinhui Pan, and Xiaoda Yang. 2022. "Design, Synthesis, and Biological Activity of 18β-Glycyrrhetinic Acid Derivatives and Their Metal Complexes" Medical Sciences Forum 14, no. 1: 129. https://doi.org/10.3390/ECMC2022-13193

APA Style

Yang, C., Pan, X., & Yang, X. (2022). Design, Synthesis, and Biological Activity of 18β-Glycyrrhetinic Acid Derivatives and Their Metal Complexes. Medical Sciences Forum, 14(1), 129. https://doi.org/10.3390/ECMC2022-13193

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