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Soluble epoxide hydrolase (sEH) is an enzyme that is considered a potential therapeutic target in human cardiovascular disease. Triterpenes (-) and phenylpropanoids (-) were isolated from to obtain sEH inhibitors through various chromatographic purificationtechniques. The isolated compounds were evaluated for their inhibitory activity against sEH, and methyl rosmarinate (), martynoside (), dimethyl lithospermate () and 9″ methyl lithospermate () showed remarkable inhibitory activity, with the IC values ranging from 10.6 ± 3.2 to 35.7 ± 2.1 µM. Kinetic analysis of these compounds revealed that , and were competitive inhibitors bound to the active site, and was the preferred mixed type inhibitor for allosteric sites. Additionally, molecular modeling has identified interacting catalytic residues and bindings between sEH and inhibitors. The results suggest that these compounds are potential candidates that can be used for further development in the prevention and treatment for cardiovascular risk.
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http://dx.doi.org/10.3390/plants10020356 | DOI Listing |
Genetic studies have linked (encoding soluble epoxide hydrolase, sEH) and (encoding cyclooxygenase-2, COX-2) to Alzheimer's disease (AD). Elevated levels of sEH and COX-2 found in AD patients and animals suggest their involvement in neurodegeneration, glial activation, vascular dysfunction, and inflammation. This study evaluated the effects of a new dual sEH/COX-2 inhibitor, PTUPB, on cerebrovascular function and cognition in TgF344-AD rats.
View Article and Find Full Text PDFChem Biol Drug Des
September 2025
Department of Pharmacy, Birla Institute of Technology and Science (BITS) Pilani, Medchal, Telangana, India.
A novel series of triazole-linked indole derivatives was designed, synthesized, and evaluated as soluble epoxide hydrolase inhibitors (sEHIs) for their potential anticancer activity. These compounds exhibit strong binding affinity within the hydrophobic pockets of sEH, with compounds 9a and 9b emerging as the most potent inhibitors, achieving IC₅₀ values of 0.270 ± 0.
View Article and Find Full Text PDFACS Omega
August 2025
Institute of Chemistry, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, RS 91501-970, Brazil.
This review examines the role of ionic liquids (ILs) in the catalytic carbonation of epoxides for the synthesis of cyclic carbonates, focusing on the key factors that influence reaction efficiency. The nucleophilicity and basicity of the anions in IL catalysts are highlighted as critical components for promoting the cycloaddition reaction with CO. The solubility and ionicity of the ILs also significantly affect the reaction, with higher ionicity leading to better solubilization and catalytic performance.
View Article and Find Full Text PDFJ Transl Med
August 2025
School of Stomatology, Dalian Medical University, No. 9 West Section, Lvshun South Road, Dalian, 116044, P.R. China.
Background: Macrophage immunomodulation has emerged as a novel intervention and therapeutic strategy for temporomandibular joint osteoarthritis (TMJOA), potentially serving as a key approach for reducing synovial inflammation and promoting cartilage repair. The soluble epoxide hydrolase inhibitor (sEHi), TPPU, has shown potential therapeutic effects against inflammatory diseases and osteogenesis by elevating endogenous Epoxyeicosatrienoic acids (EETs). However, it remains largely unknown whether TPPU can reduce inflammation and cartilage degradation in the TMJOA.
View Article and Find Full Text PDFACS Med Chem Lett
August 2025
Smith, Gambrell & Russell LLP, 1105 W. Peachtree Street NE, Atlanta, Georgia 30309, United States.
Provided herein are novel spiropiperidine urea-derived compounds as soluble epoxide hydrolase inhibitors, pharmaceutical compositions, use of such compounds in treating diabetic retinopathy, and processes for preparing such compounds.
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