Therapeutic effect of demethylated hydroxylated phillygenin derivative on Helicobacter pylori infection

Abstract

Modifying and transforming natural antibacterial products is a novel idea for developing new efficacious compounds. Phillygenin has an inhibitory effect on H. pylori. The aim of the present study was to prepare a phillygenin derivative (PHI-Der) through demethylation and hydroxylation. The minimum inhibitory concentration of 18 strains of H. pylori from different sources was 8–32 μg/mL in vitro, and the activity increased 2–8 times than that of phillygenin. PHI-Der could significantly inhibit the colonization of H. pylori in vivo, reduce the inflammatory response, and promote the repair of inflammatory damage. Further, we used SwissTargetPrediction to predict that its main targets are ALOX5, MCL1, and SLC6A4, and find that it can inhibit bacterial biofilm formation and reduce bacterial infection of cells. It can enhance the intracellular oxidative capacity of H. pylori to inhibit H. pylori growth. Further, it could prevent the oxidation of H. pylori-infected cells and reduce the inflammatory response, which plays a role in protection. In conclusion, compared to phillygenin, PHI-Der had better antibacterial activity and was more effective in treating H. pylori infection. It has characteristics of high safety, specificity, resistance to drug resistance and better antibacterial activity than phillygenin, it’s a good antioxidant for host cells.

Phillygenin Suppresses Glutamate Exocytosis in Rat Cerebrocortical Nerve Terminals (Synaptosomes) through the Inhibition of Cav2.2 Calcium Channels

“…The pharmacokinetics of phillygenin in rats exhibit first-order kinetics, with rapid distribution and elimination, while in mice, also shows high oral bioavailability, peaking within 30 min [ 11 , 12 ]. Previous studies have shown that phillygenin has diverse biological activities, including anti-inflammatory, antioxidant, antitumor, antibacterial, antiviral, analgesic, and hepatoprotective effects [ 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 ]. Since free radical-induced oxidative damage to the brain is recognized as a primary cause of neuronal death in various neurodegenerative disorders, compounds with antioxidative properties, such as phillygenin, may be effective at preventing or delaying these central nervous system (CNS) disorders [ 21 , 22 ].…”

Recent Advances in Diagnosing and Treating Helicobacter pylori through Botanical Extracts and Advanced Technologies

“…H. pylori infection involves the colonization of the stomach by the of antibiotic-resistant strains of H. pylori, which can make treatment more difficult. In addition, long-term use of PPIs has been associated with adverse effects, including increased risk of infection, kidney disease, and bone fractures [4]. Studies have shed light on the pathogenesis of H. pylori infection, including the role of virulence factors such as CagA and VacA, and the interaction between H. pylori and the host immune system [5].…”