Integrating Serum Pharmacochemistry, Network Pharmacology, and Metabolomics to Explore the Therapeutic Mechanism of Ardisia crenata Sims in Acute Pharyngitis via Regulation of the PI3K/Akt Pathway

Background/Objectives: Ardisia crenata Sims (ACS) is widely used in China for treating sore throat and pharyngeal swelling, but the bioactive constituents and mechanisms underlying its efficacy against acute pharyngitis remain unclear. This study combined UPLC-Q-TOF-MS analysis with integrated network pharmacology, metabolomics, and animal experiments to systematically elucidate the material basis and mechanism of ACS in treating acute pharyngitis. Methods: An integrative strategy combining UPLC-Q-TOF-MS-based serum pharmacochemistry, network pharmacology, metabolomics, and in vivo validation was employed. Acute pharyngitis was induced in rats. Therapeutic effects were evaluated by serum inflammatory cytokine levels and histopathological examination. Chemical constituents and absorbed blood components were identified via UPLC-Q-TOF-MS. Putative targets were predicted through network pharmacology, while metabolomics identified differential metabolites and disturbed pathways. Molecular docking was used to assess binding affinities between core compounds and key targets. Immunohistochemistry was used to assess PI3K-Akt pathway-related protein expression in pharyngeal tissue. Results: A total of 73 chemical constituents were identified from ACS, with 14 prototype compounds confirmed to be absorbed into the bloodstream. ACS significantly regulated serum TNF-α, IL-1β, and IL-6, reduced inflammatory cell infiltration, and alleviated pharyngeal mucosal damage. Integrated analysis revealed 19 differential metabolites and 10 hub genes (AKT1, PIK3CA, EGFR, SRC, etc.), primarily enriched in the PI3K-Akt signaling pathway, purine metabolism, and amino acid metabolism. Molecular docking showed strong binding affinities of quercetin, myricetin, and naringenin with key targets. Immunohistochemistry confirmed that ACS significantly downregulated PI3K, p-PI3K, AKT, and p-AKT expression at the pathway level. Conclusions: ACS exerts anti-pharyngitis effects through its flavonoid-rich bioactive constituents, which show high-affinity binding to the upstream kinases EGFR and SRC, thereby indirectly suppressing the overactivation of the PI3K-Akt signaling pathway and modulating inflammation-related metabolic networks, including endohydrolysis of 1,4-alpha-D-glucosidic linkage, purine metabolism, and glycine, serine, alanine, and threonine metabolism.

Authors

Publication Details

Journal
Pharmaceuticals
Published
2026-11-05
DOI
https://doi.org/10.3390/ph19111753
Primary Topic
Traditional Chinese Medicine Analysis
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
NOV
article

Integrating Serum Pharmacochemistry, Network Pharmacology, and Metabolomics to Explore the Therapeutic Mechanism of Ardisia crenata Sims in Acute Pharyngitis via Regulation of the PI3K/Akt Pathway

Tingting Feng, Zhoujie Yang, Wenya Li, Xing Zhao et al.
1 links
Pharmaceuticals
Traditional Chinese Medicine Analysis
article

Integrating Serum Pharmacochemistry, Network Pharmacology, and Metabolomics to Explore the Therapeutic Mechanism of Ardisia crenata Sims in Acute Pharyngitis via Regulation of the PI3K/Akt Pathway

Tingting Feng, Zhoujie Yang, Wenya Li, Xing Zhao, Hui Shi, Man Dai, Ying Zhou
article en

Abstract

Background/Objectives: Ardisia crenata Sims (ACS) is widely used in China for treating sore throat and pharyngeal swelling, but the bioactive constituents and mechanisms underlying its efficacy against acute pharyngitis remain unclear. This study combined UPLC-Q-TOF-MS analysis with integrated network pharmacology, metabolomics, and animal experiments to systematically elucidate the material basis and mechanism of ACS in treating acute pharyngitis. Methods: An integrative strategy combining UPLC-Q-TOF-MS-based serum pharmacochemistry, network pharmacology, metabolomics, and in vivo validation was employed. Acute pharyngitis was induced in rats. Therapeutic effects were evaluated by serum inflammatory cytokine levels and histopathological examination. Chemical constituents and absorbed blood components were identified via UPLC-Q-TOF-MS. Putative targets were predicted through network pharmacology, while metabolomics identified differential metabolites and disturbed pathways. Molecular docking was used to assess binding affinities between core compounds and key targets. Immunohistochemistry was used to assess PI3K-Akt pathway-related protein expression in pharyngeal tissue. Results: A total of 73 chemical constituents were identified from ACS, with 14 prototype compounds confirmed to be absorbed into the bloodstream. ACS significantly regulated serum TNF-α, IL-1β, and IL-6, reduced inflammatory cell infiltration, and alleviated pharyngeal mucosal damage. Integrated analysis revealed 19 differential metabolites and 10 hub genes (AKT1, PIK3CA, EGFR, SRC, etc.), primarily enriched in the PI3K-Akt signaling pathway, purine metabolism, and amino acid metabolism. Molecular docking showed strong binding affinities of quercetin, myricetin, and naringenin with key targets. Immunohistochemistry confirmed that ACS significantly downregulated PI3K, p-PI3K, AKT, and p-AKT expression at the pathway level. Conclusions: ACS exerts anti-pharyngitis effects through its flavonoid-rich bioactive constituents, which show high-affinity binding to the upstream kinases EGFR and SRC, thereby indirectly suppressing the overactivation of the PI3K-Akt signaling pathway and modulating inflammation-related metabolic networks, including endohydrolysis of 1,4-alpha-D-glucosidic linkage, purine metabolism, and glycine, serine, alanine, and threonine metabolism.

PharmaceuticalsVol. 19(11)
Openalex Percentile: Top 7%
Traditional Chinese Medicine Analysis
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.

Laika access coming soon