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An In Vitro and In Silico Investigation about Monteverdia ilicifolia Activity against Helicobacter pylori.

ABSTRACT: Monteverdia ilicifolia is a Brazilian native plant, traditionally used to treat gastric diseases that are now associated with Helicobacter pylori and are commonly associated with several human diseases. We point out the M. ilicifolia extract as active against H. pylori. The crude extract produced with acetone:water presented the best H. pylori inhibitory activity of all five extracts (MIC 64 µg/mL). The ethyl-acetate fractions from crude extracts produced with ethanol and acetone showed a MIC of 64 µg/mL. Both ethyl-acetate fractions and the crude extract produced with acetone showed an antioxidant capacity of between 14.51 and 19.48 µg/mL in the DPPH assay. In the FRAP assay, two ethyl-acetate fractions (EAF2 and EAF4) presented the antioxidant capacity of 5.40 and 5.15 mM Trolox/g of extract. According to the results obtained from the antioxidant and antibacterial assays, two fractions (EAF2 and nBF5) were analyzed by mass spectrometry and confirmed the presence of monomeric, dimeric, trimeric tannins, and glycosylated flavonoids. Some compounds were tested using bioinformatics to evaluate the best enzyme inhibitors and the molecular interaction between the enzyme and the tested ligands. The presence of these polyphenol compounds could play an important role in antioxidant and inhibitory capacities against H. pylori and can be used to assist in the treatment or prevention of infection by H. pylori.

SUBMITTER: de Paula MN

PROVIDER: S-EPMC9854909 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature

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An In Vitro and In Silico Investigation about Monteverdia ilicifolia Activity against Helicobacter pylori.

de Paula Mariana Nascimento MN Ribeiro Taísa Dalla Valle Rörig TDVR Isolani Raquel R de Medeiros Araújo Daniela Cristina DC Borges Augusto Santos AS Philippsen Gisele Strieder GS de Cássia Ribeiro Gonçalves Rita R Kitagawa Rodrigo Rezende RR Seixas Flavio Augusto Vicente FAV de Mello João Carlos Palazzo JCP

Antibiotics (Basel, Switzerland) 20221228 1

Monteverdia ilicifolia is a Brazilian native plant, traditionally used to treat gastric diseases that are now associated with Helicobacter pylori and are commonly associated with several human diseases. We point out the M. ilicifolia extract as active against H. pylori. The crude extract produced with acetone:water presented the best H. pylori inhibitory activity of all five extracts (MIC 64 µg/mL). The ethyl-acetate fractions from crude extracts produced with ...[more]

PMID: 36671247

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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 fruit of Tetradium ruticarpum, known as Evodiae Fructus, is a traditional herbal medicine used to treat gastric and duodenal ulcers, vomiting, and diarrhea. The traditional usage can be potentially associated with the antibacterial activity of T. ruticarpum fruits against Helicobacter pylori. However, so far, the antibacterial activity of T. ruticarpum fruits and antibacterial components against H. pylori has not been investigated despite the traditional folk use. The current study was conducted to investigate the bioactive chemical components of T. ruticarpum fruits and evaluate their antibacterial activity against H. pylori. Phytochemical investigation of the EtOH extract of T. ruticarpum fruits led to the isolation and identification of nine compounds (1-9), including phellolactone (1), the absolute configuration of which has not yet been determined. The chemical structures of the isolated compounds were elucidated by analyzing the spectroscopic data from one-dimensional (1D) and two-dimensional (2D) NMR and high-resolution electrospray ionization mass spectrometry (HR-ESIMS) experiments. Specifically, the absolute configuration of compound 1 was established by the application of computational methods, including electronic circular dichroism (ECD) calculation and the NOE/ROE-based interproton distance measurement technique via peak amplitude normalization for the improved cross-relaxation (PANIC) method. In the anti-H. pylori activity test, compound 3 showed the most potent antibacterial activity against H. pylori strain 51, with 94.4% inhibition (MIC50 and MIC90 values of 22 and 50 μM, respectively), comparable to that of metronidazole (97.0% inhibition, and MIC50 and MIC90 values of 17 and 46 μM, respectively). Moreover, compound 5 exhibited moderate antibacterial activity against H. pylori strain 51, with 58.6% inhibition (MIC50 value of 99 μM), which was higher than that of quercetin (34.4% inhibition) as a positive control. Based on the bioactivity results, we also analyzed the structure-activity relationship of the anti-H. pylori activity. Conclusion: These findings demonstrated that T. ruticarpum fruits had antibacterial activity against H. pylori and could be used in the treatment of gastric and duodenal ulcers. Meanwhile, the active compound, 1-methyl-2-(8E)-8-tridecenyl-4(1H)-quinolinone (3), identified herein also indicated the potential application in the development of novel antibiotics against H. pylori.

Project description:BackgroundHelicobacter pylori (H. pylori) infection has become an international public health problem, and antibiotic-based triple or quadruple therapy is currently the mainstay of treatment. However, the effectiveness of these therapies decreases due to resistance to multiple commonly used antibiotics. Sanguisorba officinalis L. (S. officinalis), a traditional Chinese medicine clinically used for hemostasis and treatment of diarrhea, has various pharmacological activities. In this study, in vitro antimicrobial activity was used for the preliminary evaluation of S. officinalis against H. pylori. And a pharmacology analysis approach was also utilized to elucidate its underlying mechanisms against H. pylori infection.MethodsMicro-broth dilution method, agar dilution method, checkerboard assay, scanning electron microscopy (SEM), and transmission electron microscopy (TEM) were used for the assessment of anti-bacterial activity. Active ingredients screening, GO analysis, KEGG analysis, construction of PPI network, molecular docking, and RT-qPCR were used to elucidate the underlying pharmacological mechanisms of S. officinalis against H. pylori infection.ResultsThe minimum inhibitory concentration (MIC) values of S. officinalis against multiple H. pylori strains including clinically isolated multi-drug resistant (MDR) strains were ranging from 160 to 320 µg/ml. These results showed that S. officinalis had additive interaction with four commonly used antibiotics and could exert antibacterial effect by changing the morphology of bacteria without developing drug resistance. Through network pharmacology analysis, 8 active ingredients in S. officinalis were screened out for subsequent studies. Among 222 putative targets of S. officinalis, 49 targets were identified as potential targets for treatment of H. pylori infection. And these 49 targets were significantly enriched in GO processes such as protein kinase B signaling, protein kinase activity, protein kinase binding, and KEGG pathways such as Pathways in cancer, MicroRNAs in cancer, and TNF signaling pathway. Protein-protein interaction analysis yielded 5 core targets (AKT1, VEGFA, EGFR, SRC, CCND1), which were validated by molecular docking and RT-qPCR.ConclusionsOverall, this study confirmed the in vitro inhibitory activity of S. officinalis against H. pylori and explored the possible pharmacological mechanisms, laying the foundation for further research and clinical application.

Dataset Information

An In Vitro and In Silico Investigation about Monteverdia ilicifolia Activity against Helicobacter pylori.

Publications

An In Vitro and In Silico Investigation about <i>Monteverdia ilicifolia</i> Activity against <i>Helicobacter pylori</i>.

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