The gastroprotective potential of silibinin against Helicobacter pylori infection and gastric tumor cells

Bittencourt, Milena Lopes Francisco; Rodrigues, Rossana Lott; Kitagawa, Rodrigo Rezende; Gonçalves, Rita de Cássia Ribeiro

doi:10.1016/j.lfs.2020.117977

Cited by 21 publications

(15 citation statements)

References 47 publications

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“…Another explanation regarding the effect of polyphenols upon morphological changes in H. pylori cell wall underlaid the interaction with penicillin-binding protein subunits (PBP). This mechanism has been recently described for silybin (Bittencourt et al, 2020). However, other mechanisms could not be ruled out.…”

Section: Bioactivity-guided Fractionation Of the Total Extract And Anti-h Pylori Activitymentioning

confidence: 86%

Chilean Rhubarb, Gunnera tinctoria (Molina) Mirb. (Gunneraceae): UHPLC-ESI-Orbitrap-MS Profiling of Aqueous Extract and its Anti-Helicobacter pylori Activity

et al. 2021

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The full UHPLC-MS metabolome fingerprinting and anti-Helicobacter pylori effect of Gunnera tinctoria (Molina) Mirb. (Nalca) total extract (GTE) and fractions prepared from its edible fresh petioles were evaluated. The activity of G. tinctoria against H. pylori strains ATCC 45504 and J99 was assessed in vitro by means of agar diffusion assay, Minimum Inhibition Concentration (MIC), and Minimum Bactericidal Concentration (MBC), while killing curve and transmission electronic microscopy (TEM) were conducted in order to determine the effect of the plant extract on bacterial growth and ultrastructure. Additionally, the inhibitory effect upon urease was evaluated using both the Jack Bean and H. pylori enzymes. To determine which molecules could be responsible for the antibacterial effects, tentative identification was done by ultra-high performance liquid chromatography coupled with high-resolution mass spectrometry (UHPLC-Q-Orbitrap®-HR-MS). Furthermore, the total G. tinctoria extract was fractionated using centrifugal partition chromatography (CPC), giving four active fractions (1–4). It was determined that the crude extract and centrifugal partition chromatography fractions of G. tinctoria have a bactericidal effect being the lowest MIC and MBC = 32 μg/ml. In the killing curves, fraction one acts faster than control amoxicillin. In the urease assay, F3 exhibited the lowest IC50 value of 13.5 μg/ml. Transmission electronic microscopy showed that crude G. tinctoria extract promotes disruption and separation of the cellular wall and outer membrane detachment on H. pylori causing bacterial cell death.

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Section: Bioactivity-guided Fractionation Of the Total Extract And Anti-h Pylori Activitymentioning

confidence: 86%

Chilean Rhubarb, Gunnera tinctoria (Molina) Mirb. (Gunneraceae): UHPLC-ESI-Orbitrap-MS Profiling of Aqueous Extract and its Anti-Helicobacter pylori Activity

et al. 2021

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“…Considering the unavoidable side effects of the synthetic antibiotics, we have been interested in searching for some phytochemicals with anti-inflammatory and antioxidative properties as alternatives for the management H. pylori -induced gastritis and gastric cancer. One of the candidates is silibinin which is a component of silymarin mixture [ 13 , 34 ].…”

Section: Discussionmentioning

confidence: 99%

Protective Effects of Silibinin on Helicobacter pylori-induced Gastritis: NF-κB and STAT3 as Potential Targets

et al. 2021

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More than half of the world's populations are considered to be infected by Helicobacter pylori. It causes a chronic inflammation of the stomach, which is implicated in the pathogenesis of gastric ulcer and cancer. Silibinin, a polyphenolic flavonoid derived from milk thistle, has been known for its hepatoprotective effects, and recent studies have revealed its chemopreventive potential. In the present study, we examined the anti-inflammatory effects of silibinin in human gastric cancer MKN-1 cells and in the stomach of C57BL/6 mice infected by H. pylori. Pretreatment with silibinin attenuated the up-regulation of COX-2 and inducible nitric oxide synthase (iNOS) in H. pylori-infected MKN-1 cells and mouse stomach. In addition, the elevated translocation and DNA binding of NF-kB and STAT3 induced by H. pylori infection were inhibited by silibinin treatment. Moreover, H. pylori infection in combination with high salt diet resulted in dysplasia and hyperplasia in mouse stomach, and these pathological manifestations were substantially mitigated by silibinin administration. Taken together, these findings suggest that silibinin exerts anti-inflammatory effects against H. pylori infection through suppression of NF-kB and STAT3 and subsequently, expression of COX-2 and iNOS.

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“…The efficacy and safety of baicalein/ Lactobacillus -based H. pylori eradication therapy need to be validated in clinical trials. The flavonoid silibinin showed anti- H. pylori activities 180 . Mechanistically, silibinin had the potential to interact with H. pylori Penicillin Binding Protein (PBP), causing its suppression and, thus, promoted significant morphological changes in the bacterial cell wall.…”

Section: Flavonoids Gut Microbiota and Gastric Cancermentioning

confidence: 99%

The Effects and Mechanisms of Flavonoids on Cancer Prevention and Therapy: Focus on Gut Microbiota

Wang¹,

Yu²,

Zhang³

et al. 2022

Int. J. Biol. Sci.

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Flavonoids are a group of polyphenolic compounds which are ubiquitously found in plants and are consumed as part of the human diet in substantial amounts. The verification of flavonoids' cancer chemopreventive benefits has led to a significant interest in this field. Gut microbiota includes a diverse community of microorganisms and has a close relationship with cancer development. Increasing evidence has indicated that flavonoids exert anticarcinogenic effects by reshaping gut microbiota. Gut microbiota can convert flavonoids into bioactive metabolites that possess anticancer activity. Here, we present a brief introduction to gut microbiota and provide an overview of the interplay between gut microbiota and cancer pathogenesis. We also highlight the crucial roles of flavonoids in preventing cancer based on their regulation of gut microbiota. This review would encourage research on the flavonoid-intestinal microbiota interactions and clinical trials to validate the chemotherapeutic potentials of targeting gut microbiota by dietary bioactive compounds.

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The gastroprotective potential of silibinin against Helicobacter pylori infection and gastric tumor cells

Cited by 21 publications

References 47 publications

Chilean Rhubarb, Gunnera tinctoria (Molina) Mirb. (Gunneraceae): UHPLC-ESI-Orbitrap-MS Profiling of Aqueous Extract and its Anti-Helicobacter pylori Activity

Chilean Rhubarb, Gunnera tinctoria (Molina) Mirb. (Gunneraceae): UHPLC-ESI-Orbitrap-MS Profiling of Aqueous Extract and its Anti-Helicobacter pylori Activity

Protective Effects of Silibinin on Helicobacter pylori-induced Gastritis: NF-κB and STAT3 as Potential Targets

The Effects and Mechanisms of Flavonoids on Cancer Prevention and Therapy: Focus on Gut Microbiota

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