Department of Biology Education, Teachers College and Institute for Phylogenomics and Evolution, Kyungpook National University, Daegu 41566, Republic of Korea.
Published: August 2024
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Article Abstract
Soluble epoxide hydrolase (sEH) is essential for converting epoxy fatty acids, such as epoxyeicosatrienoic acids (EETs), into their dihydroxy forms. EETs play a crucial role in regulating blood pressure, mediating anti-inflammatory responses, and modulating pain, making sEH a key target for therapeutic interventions. Current research is increasingly focused on identifying sEH inhibitors from natural sources, particularly marine environments, which are rich in bioactive compounds due to their unique metabolic adaptations. In this study, the sEH inhibitory activities of ten cembranoid diterpenes (-) isolated from the soft coral were evaluated. Among them, compounds and exhibited considerable sEH inhibition, with IC values of 70.68 μM and 78.83 μM, respectively. Enzyme kinetics analysis revealed that these two active compounds inhibit sEH through a non-competitive mode. Additionally, in silico approaches, including molecular docking and molecular dynamics simulations, confirmed their stability and interactions with sEH, highlighting their potential as natural therapeutic agents for managing cardiovascular and inflammatory diseases.
A new sesquiterpene, 8,11-epoxy-cadi-3,9-diene (), along with nine known compounds (-), were isolated from the heartwood of . Their structures were elucidated based on NMR spectroscopic data, and by comparison with data previously reported in literature. The hexane extract from the heartwood of , the EtOH extract from the heartwood of , the CHCl-soluble fraction of the EtOH extract, the EtOAc-soluble fraction of the EtOH extract and the compounds - have been evaluated as acetylcholinesterase inhibitors, and among these, the extracts and fractions exhibited satisfactory results.
Background: Phytophthora sojae (Kaufmann and Gerdemann), a pathogenic oomycete, causes one of the most destructive soybean diseases, Phytophthora root and stem rot (PRR). Previous studies have shown that benzoxazines (BXs) such as 6-methoxy-benzoxazolin-2-one (MBOA) and benzoxazoline-2-one (BOA) in maize root exudates inhibit the chemotaxis of zoospores, as well as the mycelial growth and pathogenicity of P. sojae.
Cellular senescence is a condition characterized by stable, irreversible cell cycle arrest linked to the aging process. The accumulation of senescent cells in the cardiac muscle can contribute to various cardiovascular diseases (CVD). Telomere shortening, epigenetic modifications, DNA damage, mitochondrial dysfunction, and oxidative stress are known contributors to the onset of cellular senescence in the heart.
Inhibiting microsomal prostaglandin E synthase-1 (mPGES-1), an inducible enzyme involved in prostaglandin E (PGE) biosynthesis and tumor microenvironment (TME) homeostasis, is a valuable strategy for treating inflammation and cancer. In this work, 5-methylcarboxamidepyrrole-based molecules were designed and synthesized as new compounds targeting mPGES-1. Remarkably, compounds 1f, 2b, 2c, and 2d were able to significantly reduce the activity of the isolated enzyme, showing IC values in the low micromolar range.
