Helicobacter pylori is a gastroduodenal pathogen that colonizes the human stomach, thereby inducing inflammation of the gastric mucosa causing gastritis, peptic ulcer and gastric cancer. H. pylori finds multiple ways for its survival in the human host which is performed by various virulence factors, collectively responsible for persistence and colonization. One of the major virulence factors produced by H. pylori is Vacuolating cytotoxin A (VacA) exerting multiple effects on epithelial cells.
Resveratrol is a naturally occuring phytoalexin, found, in particular, in grape and in grapeskin, that inhibits a wide array of bacteria. In particular, its role in effecting the oxidative stress and inflammation in H. pylori-infected mucosa has been described. Although resveratrol possesses antimicrobial benefits, it is noteworthy that its availability from plants is limited, and it has been associated with poor bioavailability. In a recent work, we reported the positive effects of a series of resveratrol analogs against resistant H. pylori clinical strains, evaluating antibacterial (MIC/MBC) and antivirulence effects (biofilm reduction and swarming motility inhibition), alone and combined with levofloxacin.
In this communication we describe the synthesis and antibacterial effect of new resveratrol analogs against H. pylori. New molecules kept unaltered the 4’-hydroxyl group of resveratrol, important for biological activity, while 3,5-hydroxy groups were replaced with a substituent in 4-position. Furthermore, a new substituent was added in 3’-position. We also report a preliminary microbiological evaluation.
- Chauhan, A. Chin Yen Tay, B. J. Marshall, U. Jain. Helicobacter pylori VacA, a distinct toxin exerts diverse functionalities in numerous cells: An overview. Helicobacter 2019, 24, e12544
- Di Fermo, S. Di Lodovico, R. Amoroso, B. De Filippis, S. D'Ercole, E. Di Campli, L. Cellini, M. Di Giulio. Searching for new tools to counteract the Helicobacter pylori resistance: the positive action of resveratrol derivatives. Antibiotics 2020, 12, 891
