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Screening of Urea Transporters Inhibitors in Celery Seeds by UPLC-TOF-MS
1 , 1 , 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


Urea transporters (UTs) are a kind of transmembrane proteins that specifically permeate urea and play an important role in the mechanism of urine concentration. Selective knockout of UT can concentrate urea without affecting water and electrolytes, resulting in selective diuresis, which is a promising new diuretic target. Most of the currently reported UT inhibitors are obtained from small molecular libraries screened for poor oral activity. We subjected the methanolic extract of celery seed to silica gel column chromatography analysis and screened the column chromatographic fractions of celery seed for UT-B inhibitory activity using the reported erythrocyte lysis model, and the UT-B inhibitory activity was screened for the fractions of celery seed separated by column chromatography using the reported erythrocyte lysis model. The chemical composition of the active site was identified using UPLC-TOF-MS, and the active compounds were screened in combination with molecular docking and ADMET prediction. Screening of the extracted parts of celery seed using an erythrocyte lysis model yielded nine small molecules with good inhibitory activity, namely esters, phenols, and organic acids. This experiment shows that compounds with UT-B inhibitory effects can be found in ethnic medicinal materials, which not only provides new ideas for the discovery of UT-B inhibitors but also contributes to the development of ethnic medicines.

Keywords: Celery Seed; UT-B inhibitor; Erythrocyte lysis model
Comments on this paper
Ke Yang
Urea transporters is rarely studied and links to natural compounds with detailed content. Very interesting.

Qiaohui Liu
It provides a whole research idea of developing new diuretics from ethnic medicine, which is of great reference significance

The experimental design is reasonable

xiaoying sun
The article is rigorous in structure and rich in content,worth learning by researchers.

Caiyun Yang
This paper is informative and provides a reference for a wide range of scholars on the study of natural compounds.

li guo
It is very valuable to develop the ethnic medicines.