Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, Italy.
Department of Physical Sciences, Earth and Environment, University of Siena, Siena, Italy.
J Enzyme Inhib Med Chem. 2023 Dec;38(1):2183810. doi: 10.1080/14756366.2023.2183810.
(HP) is among the most common pathogens causing infection in humans worldwide. Oxidative stress and gastric inflammation are involved in the progression of HP-related gastric diseases, and they can be targeted by integrating conventional antibiotic treatment with polyphenol-enriched natural products. In this work, we characterised three different propolis extracts and evaluated their stability under simulated gastric digestion, compared to their main constituents alone. The extract with the highest stability to digestion (namely, the dark propolis extract, DPE) showed a minimum bactericidal concentration (MBC) lower than 1 mg/mL on HP strains with different virulence factors. Finally, since urease is one of the virulence factors contributing to the establishment of a microenvironment that promotes HP infection, we evaluated the possible inhibition of this enzyme by using molecular docking simulations and colorimetric assay, showing that galangin and pinocembrin may be involved in this activity.
(HP)是全球范围内导致人类感染的最常见病原体之一。氧化应激和胃炎症参与了 HP 相关胃病的进展,通过将传统抗生素治疗与富含多酚的天然产物相结合,可以针对这些因素进行治疗。在这项工作中,我们对三种不同的蜂胶提取物进行了表征,并在模拟胃消化的情况下评估了它们与单独的主要成分相比的稳定性。在消化过程中稳定性最高的提取物(即深色蜂胶提取物,DPE)对具有不同毒力因子的 HP 菌株的最小杀菌浓度(MBC)低于 1mg/mL。最后,由于脲酶是导致促进 HP 感染的微环境建立的毒力因子之一,我们使用分子对接模拟和比色法评估了这种酶的可能抑制作用,表明高良姜素和 pinocembrin 可能参与了这种活性。