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Effect of in vitro simulated digestion on the anti-Helicobacter Pylori activity of different Propolis extracts.

ABSTRACT: Helicobacter pylori (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 in vitro 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 in vitro colorimetric assay, showing that galangin and pinocembrin may be involved in this activity.

SUBMITTER: Governa P

PROVIDER: S-EPMC10026752 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature

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Effect of in vitro simulated digestion on the anti-Helicobacter Pylori activity of different Propolis extracts.

Governa Paolo P Romagnoli Giulia G Albanese Paola P Rossi Federico F Manetti Fabrizio F Biagi Marco M

Journal of enzyme inhibition and medicinal chemistry 20231201 1

Helicobacter pylori (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 in vitro simulated gastric digestion, compared to their main co ...[more]

PMID: 36916299

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Project description:Helicobacter pylori (H. pylori) is considered the most common bacterial pathogen colonizing stomach mucosa of almost half the world's population and is associated with various gastrointestinal diseases (from digestive problems and ulcers to gastric cancer). A lack of new drugs and a growing number of H. pylori antibiotic-resistant strains is a serious therapeutic problem.As a mixture of natural compounds, propolis has antimicrobial activity based on high concentrations of bioactive polyphenols (mainly flavonoids and phenolic acid derivates). The chemical composition of tested Georgian propolis is characterized by the presence of flavonoids aglycones, and phenolic acid monoesters, e.g., pinobanksin-5-methyl ether, pinobanksin, chrysin, pinocembrin, galangin, pinobanksin-3-O-acetate, pinostrobin and pinobanksin-3-O-butanoate, or isobutanoate and methoxycinnamic acid cinnamyl ester. The anti-H. pylori activity of 70% ethanol water extracts of 10 Georgian propolis samples was evaluated in vitro by MIC (minimal inhibitory concentration) against the reference strain (H. pylori ATCC 43504) and 10 clinical strains with different antibiotic-resistance patterns. The strongest anti-Helicobacter activity (MIC and MBC = 31.3 µg/mL) was observed for propolis from Orgora, Ota, and Vardzia and two from Khaheti. Lower levels of activity (MIC = 62.5 µg/mL) were found in propolis obtained from Qvakhreli and Pasanauri, while the lowest effect was observed for Norio and Mestia (MIC = 125.0 µg/mL). However, despite differences in MIC, all evaluated samples exhibited bactericidal activity. We selected the most active propolis samples for assessment of urease inhibition property. Enzyme activity was inhibited by propolis extracts, with IC50 ranging from 4.01 to 1484.8 µg/mL. Principal component analysis (PCA) and hierarchical fuzzy clustering (dendrograms) coupled with matrix correlation analysis exhibited that the strongest anti-Helicobacter activity was connected with black poplar origin and high flavonoid content of propolis. Samples with lower activity contained higher presence of aspen markers and/or dominance of non-flavonoid polyphenols over flavonoids. In summary, Georgian propolis can be regarded as a source bioactive compounds that can be used as adjuvant in therapy of H. pylori infection.

Project description:The most evident challenge to treatment of Helicobacter pylori, a bacterium responsible for gastritis, peptic ulcers and gastric cancer, is the increasing rate of resistance to all currently used therapeutic antibiotics. Thus, the development of novel therapies is urgently required. N-geranyl-N'-(2-adamantyl) ethane-1, 2-diamine (SQ109) is an ethylene diamine-based antitubercular drug that is currently in clinical trials for the treatment of tuberculosis (TB). Previous pharmacokinetic studies of SQ109 revealed that persistently high concentrations of SQ109 remain in the stomach 4 hours post oral administration in rats. This finding, combined with the need for new anti-Helicobacter therapies, prompted us to define the in vitro efficacy of SQ109 against H. pylori. Liquid broth micro-dilution was used for susceptibility studies to determine the antimicrobial activity of SQ109 against a total of 6 laboratory strains and 20 clinical isolates of H. pylori; the clinical isolates included a multi-drug resistant strain. All strains tested were susceptible to SQ109 with MIC and MBC ranges of 6-10 µM and 50-60 µM, respectively. SQ109 killing kinetics were concentration- and time-dependent. SQ109 killed H. pylori in 8-10 h at 140 µM (2MBCs) or 4-6 h at 200 µM (~3MBCs). Importantly, though the kinetics of killing were altered, SQ109 retained potent bactericidal activity against H. pylori at low pH. Additionally, SQ109 demonstrated robust thermal stability and was effective at killing slow growing or static bacteria. In fact, pretreatment of cultures with a bacteriostatic concentration of chloramphenicol (Cm) synergized the effects of typically bacteriostatic concentrations of SQ109 to the level of five-logs of bacterial killing. A molar-to-molar comparison of the efficacy of SQ109 as compared to metronidazole (MTZ), amoxicillin (AMX), rifampicin (RIF) and clarithromycin (CLR), revealed that SQ109 was superior to MTZ, AMX and RIF but not to CLR. Finally, the frequency of resistance to SQ109 was low and electron microscopy studies revealed that SQ109 interacted with bacterial inner membrane and cytoplasmic content(s). Collectively, our in vitro data demonstrate that SQ109 is an effective monotherapy against susceptible and multi-drug resistant strains of H. pylori and may be useful alone or in combination with other antibiotics for development as a new class of anti-Helicobacter drugs.

Project description:The digestive tract can be considered a bioreactor. High levels of reactive oxygen species (ROS) during digestion may predispose for local and/or systemic oxidative stress and inflammation, e.g., inflammatory bowel diseases. Food items rich in antioxidants may prevent such aggravation. This investigation analyzed pro-and antioxidant patterns of food matrices/items following in vitro digestion. Gastrointestinal digestion reflecting typically consumed quantities was performed on nine food items (orange and tomato juice, soda, coffee, white chocolate, sausage, vitamin C and E, and curcumin) and their combinations (n = 24), using the INFOGEST model. Antioxidant potential was measured by FRAP, DPPH, and ABTS, and pro-oxidant aspects by MDA (malondialdehyde) and peroxide formation. An anti-pro-oxidant score was developed, combining the five assays. Liquid food items showed moderately high antioxidant values, except for coffee and orange juice, which exhibited a high antioxidant potential. Solid matrices, e.g., white chocolate and sausage, showed both high pro-oxidant (up to 22 mg/L MDA) and high antioxidant potential (up to 336 mg/L vitamin C equivalents) at the same time. Individual vitamins (C and E) at physiological levels (achievable from food items) showed a moderate antioxidant potential (<220 mg/L vitamin C equivalents). Overall, both antioxidant and pro-oxidant assays correlated well, with correlation coefficients of up to 0.894. The effects of food combinations were generally additive, i.e., non-synergistic, except for combinations with sausage, where strong quenching effects for MDA were observed, e.g., with orange juice. In conclusion, as especially highlighted by complex matrices demonstrating both pro- and antioxidant potential, only measuring one aspect would result in physiological misinterpretations. Therefore, it is imperative to employ a combination of assays to evaluate both pro- and antioxidant properties of food digesta to ensure physiological relevance.

Dataset Information

Effect of in vitro simulated digestion on the anti-Helicobacter Pylori activity of different Propolis extracts.

Publications

Effect of <i>in vitro</i> simulated digestion on the anti-<i>Helicobacter Pylori</i> activity of different Propolis extracts.

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