Author: Sun, Dongbo ; Zhu, Qinghe ; Guo, Donghua ; Yang, Dan ; Jiang, Limin ; Li, Hansong ; Li, Chunqiu ; Gu, Minghui ; Zhao, Yingying ; Guo, Xingyang ; Shen, Fanbo ; Xiao, Jiawei ; Xing, Xiaoxu

Porcine epidemic diarrhea virus (PEDV) can cause severe diarrhea death in newborn piglets, resulting in significant economic losses for the pig industry. Therefore, the advancement of safe and effective anti-PEDV drugs for the treatment of PEDV is of paramount importance. In this study, molecular docking was used to screen natural drugs that can target PEDV 3C like protease (3CLpro). As well, the anti-PEDV effects of the screened drugs were evaluated in vitro and in vivo. Molecular docking and molecular dynamics (MD) simulation results showed that ethyl caffeate (EC) could efficiently bind to the active cavity of PEDV 3CLpro. Biolayer interferometry (BLI) and fluorescence resonance energy transfer (FRET) analyses demonstrated that EC directly interacts with PEDV 3CLpro (K_D = 1650 μM) and inhibits the activity of 3CLpro (IC₅₀ = 33.87 μM). EC has been shown to significantly inhibit the replication of PEDV in Vero E6 cells. The half maximal inhibitory concentration (CC₅₀) and half-effective concentration (EC₅₀) were determined to be 283.1 μM and 8.641 μM, respectively, yielding a selectivity index as high as 32.7. Furthermore, EC was evaluated using a piglet infection model for PEDV. It demonstrated the ability to inhibit PEDV infection in vivo and improve the survival rate of piglets (3/5, 60%). Compared to the control group, oral administration of EC significantly reduced intestinal pathological damage and viral load. Our study indicated that EC, targeting PEDV 3CLpro, is a safe and effective anti-PEDV drug with promising clinical application prospects.

01 Mar 2025·Fish & Shellfish Immunology

Ethyl caffeate modulates systemic and mucosal immune responses, growth performance, and disease resistance against Vibrio parahaemolyticus in hybrid grouper (Epinephelus fuscoguttatus ♀ × E. lanceolatus ♂)

Article

Author: Chu, Yu-Ting ; Widodo, Ari ; Nan, Fan-Hua ; Dewi, Novi Rosmala ; Huang, Huai-Ting

Hybrid groupers become one of the important aquatic animals, but gastric pathogen infection causes losses due to Vibrio sp. infections. Ethyl caffeate (EC), a naturally occurring antioxidant and antibacterial derived from medicinal plant. This study investigated the effects of EC on the immune response, growth performance, as well as the systemic and mucosal immunity following Vibrio parahaemolyticus challenge. The hybrid groupers were fed diets containing EC at the concentrations of 0, 0.1, 0.25, and 0.5 g/kg (control, EC0.1, EC0.25, and EC0.5 groups, respectively). This feeding trial was conducted in three-part separate experiments consist of non-specific immune response, growth performance and challenge test experiment. The result demonstrated that the EC0.25 group had the highest total leukocyte count, phagocytic activity, and respiratory burst (O₂^-) and the highest upregulation of genes related to antioxidant activity, inflammation, antimicrobial peptides, and stress. Furthermore, higher growth performance was observed in all EC groups than in the control group with the EC0.25 group exhibited optimum growth performance. According to the challenge test results, the EC0.25 group exhibited strong resistance to V. parahaemolyticus, with a survival rate of 96.7 %. This study elucidated a novel self-defense mechanism after EC modulating against V. parahaemolyticus challenge in hybrid groupers. The EC0.25 group had increased leukocyte subpopulation and the highest upregulation of Toll-like receptor 4, Toll-like receptor 21, MyD88, major histocompatibility complex II, immunoglobulin M, interleukin-1β, and tumor necrosis factor-α in both systemic and mucosal related-organs. Overall, dietary EC0.25 increased the hybrid groupers health status, activated multiple signaling pathways, and synergistically increased the host's systemic and mucosal immunity.

01 Nov 2024·Talanta

Matrix-assisted laser desorption ionization mass spectrometry imaging reveals the spatial distribution of compounds that may exacerbate inflammation in garden ginseng and ginseng under forest

Article

Author: Ma, Rui ; Sun, Li-Wei ; Mu, Yan-Hong ; Zhao, Yi-Ming ; Liu, Fang-Bing ; Ji, Chun-Lei ; Li, Ying-Na ; Xu, Rong

Ginseng, a highly esteemed herbal medicine, has been utilized over 5000 years, predominantly in Far Eastern countries. Ginseng is categorized into garden ginseng (GG) and ginseng under forest (FG). However, in contrast to FG, excessive intake of GG may lead to potential adverse effects due to disruption of epithelial cell integrity, and the specific population groups that may be at higher risk. In this work, untargeted metabolomics were used to determine the heterogeneity between GG and FG, the data indicates that the content of Ethyl caffeate, Homoorientin, Citric acid and Quinic acid in GG were higher than in FG. Mass spectrometry imaging showed that ethyl caffeate and Homoorientin were concentrated on the brownish yellow exocarp of the primary root. Our experiments demonstrated that excessive exposure to ethyl caffeate and Homoorientin exacerbated the inflammatory response of HUVECs and reduced the expression of cell junctions. This suggest that the compounds causing adverse effects from excessive intake of GG are mainly concentrated in the yellow exocarp of the primary root of GG. These results suggest that untargeted metabolomics coupled with MALDI-MSI can visualize the spatial distribution of endogenous differential molecules of the same herb in different growth environments or developmental stages.

100 Deals associated with Ethyl caffeate

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Indication	Highest Phase	Country/Location	Organization	Date
Renal fibrosis	Preclinical	China	Guangzhou University of Chinese Medicine	01 Nov 2024
Renal fibrosis	Preclinical	China	Macau University of Science & Technology	01 Nov 2024

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