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Volume 31
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10.3390/molecules31020309
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This is an early access version, the complete PDF, HTML, and XML versions will be available soon.
Article

Regioselective Glycosylation of Demethylbellidifolin by Glycosyltransferase AbCGT Yields Potent Anti-Renal Fibrosis Compound

by
Limin Zeng
1,2,†,
Shichao Cui
2,†,
Xingyu Ji
2,†,
Yuhong Liu
2,
Guozhang Long
2,3,
Yulan Xia
2,3,
Gang Cheng
4,*,
Jingya Li
1,2,3,5,* and
Youhong Hu
1,2,3,5,*
1
School of Chinese Materia Medica, College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
2
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
3
University of Chinese Academy of Sciences, Beijing 100049, China
4
School of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou 310053, China
5
Key Laboratory of Glyco-Drug Research of Zhejiang Province, School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310024, China
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Molecules 2026, 31(2), 309; https://doi.org/10.3390/molecules31020309
Submission received: 4 December 2025 / Revised: 29 December 2025 / Accepted: 12 January 2026 / Published: 15 January 2026
(This article belongs to the Special Issue Application of Organic Synthesis to Bioactive Compounds, 3rd Edition)
Versions Notes

Abstract

Glycosylation serves as an effective strategy to enhance the solubility, bioavailability, and pharmacological activity of polyhydroxyphenols. In this study, we explored the glycosylation of natural and natural-inspired phenolic compounds using the glycosyltransferase AbCGT and evaluated the anti-renal fibrotic potential of the resulting glycosides. Among them, 1,3,5,8-tetrahydroxyxanthone 5-O-β-D-glucopyranoside (2-1a), synthesized via the regioselective 5-O-glycosylation of demethylbellidifolin, demonstrated significant anti-renal fibrotic activity. In contrast, its homologous glycosyltransferase, UGT73AE1, predominantly glycosylated demethylbellidifolin at the 3-OH position. Molecular docking studies revealed the structural basis for this regioselectivity difference. To enhance the production of 2-1a, we established a UDP-glucose (UDPG) recycling system by coupling AbCGT with Glycine max sucrose synthase (GmSuSy) and subsequently optimized the reaction conditions. Furthermore, targeted mutagenesis of AbCGT informed by molecular docking analysis identified a F138A mutant that enhanced glycosylation yield by 2.3-fold. This work develops a novel glycosyltransferase-based catalytic system and identifies a new compound with potential anti-renal fibrotic activity.
Keywords: glycosyltransferase; regioselectivity; anti-renal fibrosis; biosynthesis; molecular docking glycosyltransferase; regioselectivity; anti-renal fibrosis; biosynthesis; molecular docking

Share and Cite

MDPI and ACS Style

Zeng, L.; Cui, S.; Ji, X.; Liu, Y.; Long, G.; Xia, Y.; Cheng, G.; Li, J.; Hu, Y. Regioselective Glycosylation of Demethylbellidifolin by Glycosyltransferase AbCGT Yields Potent Anti-Renal Fibrosis Compound. Molecules 2026, 31, 309. https://doi.org/10.3390/molecules31020309

AMA Style

Zeng L, Cui S, Ji X, Liu Y, Long G, Xia Y, Cheng G, Li J, Hu Y. Regioselective Glycosylation of Demethylbellidifolin by Glycosyltransferase AbCGT Yields Potent Anti-Renal Fibrosis Compound. Molecules. 2026; 31(2):309. https://doi.org/10.3390/molecules31020309

Chicago/Turabian Style

Zeng, Limin, Shichao Cui, Xingyu Ji, Yuhong Liu, Guozhang Long, Yulan Xia, Gang Cheng, Jingya Li, and Youhong Hu. 2026. "Regioselective Glycosylation of Demethylbellidifolin by Glycosyltransferase AbCGT Yields Potent Anti-Renal Fibrosis Compound" Molecules 31, no. 2: 309. https://doi.org/10.3390/molecules31020309

APA Style

Zeng, L., Cui, S., Ji, X., Liu, Y., Long, G., Xia, Y., Cheng, G., Li, J., & Hu, Y. (2026). Regioselective Glycosylation of Demethylbellidifolin by Glycosyltransferase AbCGT Yields Potent Anti-Renal Fibrosis Compound. Molecules, 31(2), 309. https://doi.org/10.3390/molecules31020309

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