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BackgroundHelicobacter pylori (H. pylori) is thought to primarily colonize the human stomach and lead to various gastrointestinal disorders, such as gastritis and gastric cancer. Currently, main eradication treatment is triple or quadruple therapy centered on antibiotics. Due to antibiotic resistance, the eradication rate of H. pylori is decreasing gradually. Therefore, searching for anti-H. pylori drugs from herbal sources has become a strategy for the treatment. Our team proposed a Hezi Qingyou Formula (HZQYF), composed of Chebulae Fructus, Ficus hirta Vahl and Cloves, and studied its anti-H. pylori activity and mechanism.MethodsChemical components of HZQYF were studied using UHPLC–MS/MS and HPLC. Broth microdilution method and agar dilution method were used to evaluate HZQYF’s antibacterial activity. The effects of HZQYF on expression of adhesion genes (alpA, alpB, babA), urease genes (ureE, ureF), and flagellar genes (flaA, flaB) were explored using Reverse Transcription-quantitative Polymerase Chain Reaction (RT-qPCR) technology. Effects on morphology and permeability of the extracellular membrane were studied using scanning electron microscopy (SEM) and N-phenylnaphthalen-1-amine (NPN) uptake. Effect on urease activity was studied using a urease kinetics analysis in vitro. Immunofluorescence staining method was used to examine the effect on adhesion. Western blot was used to examine the effect on cagA protein.ResultsMinimum inhibitory concentration (MIC) values of the formula against H. pylori clinical strains and standard strains were 80–160 μg/mL, and minimum bactericidal concentration (MBC) values were 160–320 μg/mL. The formula could down-regulate the expression of adhesion genes (alpA, alpB, babA), urease genes (ureE, ureF) and flagellar genes (flaA, flaB), change the morphology of H. pylori, increase its extracellular membrane permeability, and decrease its urease activity.ConclusionPresent studies confirmed that HZQYF had promising in vitro anti-H. pylori activities and demonstrated its possible mechanism of action by down-regulating the bacterial adhesion, urease, and flagellar gene expression, which provided scientific bases for further clinical investigations.

The primary treatment method for eradicating Helicobacter pylori (H. pylori) infection involves the use of antibiotic-based therapies. Due to the growing antibiotic resistance of H. pylori, there has been a surge of interest in exploring alternative therapies. Cetylpyridinium chloride (CPC) is a water-soluble and nonvolatile quaternary ammonium compound with exceptional broad-spectrum antibacterial properties. To date, there is no documented or described specific antibacterial action of CPC against H. pylori. Therefore, this study aimed to explore the in vitro activity of CPC against H. pylori and its potential antibacterial mechanism. CPC exhibited significant in vitro activity against H. pylori, with MICs ranging from 0.16 to 0.62 μg/mL and MBCs ranging from 0.31 to 1.24 μg/mL. CPC could result in morphological and physiological modifications in H. pylori, leading to the suppression of virulence and adherence genes expression, including flaA, flaB, babB, alpA, alpB, ureE, and ureF, and inhibition of urease activity. CPC has demonstrated in vitro activity against H. pylori by inhibiting its growth, inducing damage to the bacterial structure, reducing virulence and adherence factors expression, and inhibiting urease activity.

The Malvern Mastersizer 3000 laser particle size analyzer and HydroMV wet sampler were used, and the parameters are set as follows: sample refractive index 1.52, funnel width 2.0mm, dispersion air pressure 4.0 bar, ultrasonic intensity 50%, ultrasonic time 30s, stirring speed 1600rpm, laser obscuration 8% ~ 15%. The mean values of particle size distribution d (0.1), d (0.5), and d (0.9) of 3 batches of tadalafil drug substance were 0.819 µm, 2.79 µm, and 8.44 µm, respectively. The measured results were basically consistent with the microscopic method. The method is simple, accurate and precise, and suitable for the particle size determination of tadalafil drug substance. [ABSTRACT FROM AUTHOR]

The Malvern Mastersizer 3000 laser particle size analyzer and HydroMV wet sampler were used, and the parameters are set as follows: sample refractive index 1.52, funnel width 2.0mm, dispersion air pressure 4.0 bar, ultrasonic intensity 50%, ultrasonic time 30s, stirring speed 1600rpm, laser obscuration 8% - 15%. The mean values of particle size distribution d (0.1), d (0.5), and d (0.9) of 3 batches of tadalafil drug substance were 0.819 μm, 2.79 μm, and 8.44 μm, respectively. The measured results were basically consistent with the microscopic method. The method is simple, accurate and precise, and suitable for the particle size determination of tadalafil drug substance. [ABSTRACT FROM AUTHOR]