Application of 18 <i>β</i> -glycyrrhetinic acid Fluorescent probes in cell imaging

Fluorescently labelled small molecule probes (fluorescent probes) play an important role in cell imaging and are often used in combination with light-affinity probes to determine the subcellular localisation of target proteins. To investigate the target proteins of 18<i>β</i>-glycyrrhetinic acid (18<i>β</i>-GA), which regulates the macrophage inflammatory response, we designed and synthesised three types of fluorescent probes. We analysed its structure-activity relationship by evaluating the biological activity and screening for fluorescent probes with high activity. Our results showed that modifying C-3 hydroxyl and C-30 carboxyl groups enhanced the anti-inflammatory activity of 18<i>β</i>-GA, and found that two preferred probes had similar effects on LPS-induced, inflammation-related factor release (IL-1β, TNF-α, IL-6, HDAC8, P-STAT3, and SOCS3) to those of 18<i>β</i>-GA. Fluorescence signals of the preferred probes <b>Ia</b> and <b>IIc</b> were observed in the cytoplasm. The above results indicated that the anti-inflammatory site of 18<i>β</i>-GA may be located in proteins in the cytoplasm, which would provide useful information for research on the anti-inflammatory targets of 18<i>β</i>-GA.

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Publication Details

Journal
Journal of Enzyme Inhibition and Medicinal Chemistry
Published
2026-03-09
DOI
https://doi.org/10.1080/14756366.2026.2631869
Primary Topic
Pharmacological Effects of Natural Compounds
Type
article
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article

Application of 18 β -glycyrrhetinic acid Fluorescent probes in cell imaging

T Wang, Yifan Zhao, Shuai Li, Li Zhang et al.
Journal of Enzyme Inhibition and Medicinal Chemistry
Pharmacological Effects of Natural Compounds
article

Application of 18 β -glycyrrhetinic acid Fluorescent probes in cell imaging

T Wang, Yifan Zhao, Shuai Li, Li Zhang, Yachun Guo, Chengjun Song, Yuxing Wang, Hongxia Sun, Zhiwei Yan, Guangxin Miao
article en

Abstract

Fluorescently labelled small molecule probes (fluorescent probes) play an important role in cell imaging and are often used in combination with light-affinity probes to determine the subcellular localisation of target proteins. To investigate the target proteins of 18<i>β</i>-glycyrrhetinic acid (18<i>β</i>-GA), which regulates the macrophage inflammatory response, we designed and synthesised three types of fluorescent probes. We analysed its structure-activity relationship by evaluating the biological activity and screening for fluorescent probes with high activity. Our results showed that modifying C-3 hydroxyl and C-30 carboxyl groups enhanced the anti-inflammatory activity of 18<i>β</i>-GA, and found that two preferred probes had similar effects on LPS-induced, inflammation-related factor release (IL-1β, TNF-α, IL-6, HDAC8, P-STAT3, and SOCS3) to those of 18<i>β</i>-GA. Fluorescence signals of the preferred probes <b>Ia</b> and <b>IIc</b> were observed in the cytoplasm. The above results indicated that the anti-inflammatory site of 18<i>β</i>-GA may be located in proteins in the cytoplasm, which would provide useful information for research on the anti-inflammatory targets of 18<i>β</i>-GA.

Journal of Enzyme Inhibition and Medicinal ChemistryVol. 41(1)
Chengde Medical University (CN), Hebei University of Chinese Medicine (CN)
Openalex Percentile: Top 27%
Pharmacological Effects of Natural Compounds
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Application of 18 <i>β</i> -glycyrrhetinic acid Fluorescent probes in cell imaging — T Wang, Yifan Zhao, et al. · Journal of Enzyme Inhibition and Medicinal Chemistry (2026) | TGRS Research Map | TGRS