In-silico designing, ADMET Analysis, synthesis and biological evaluation of novel derivatives of diosmin against urease protein and Helicobactor Pylori bacterium.

CONCLUSIONS: Selected candidates from the outcome of in-vitro urease inhibitory were further examined for anti- H. pylori activity by well diffusion method against H. pylori bacterium (DSM 4867). Compound D2a showed good anti-H. Pylori activity with zone of inhibition 10.00 ± 0.00 mm and MIC value 500μg/mL as compared to standard drug acetohydroxamic acid having zone of inhibition 9.00 ± 0.50mm and MIC 1000μg/mL. In- silico studies played an important role in designing the potent ligands against urease protein as well as in explaining the binding pattern of designed and synthesized ligand within active pocket of jack bean urease protein. ADMET studies were also carried out to check the drug similarity of designed compounds by the means of quikprop module of molecular docking software. Hence, the present investigation studies will provide a new vision for the discovery of potent agents against H. pylori and urease associated diseases. PMID: 31724503 [PubMed - as supplied by publisher]
Source: Current Topics in Medicinal Chemistry - Category: Chemistry Authors: Tags: Curr Top Med Chem Source Type: research

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In this study H. pylori CagL gene was cloned in pAMJ2008 vector and transferred to Lactococcus lactis MG1363 as the host for CagL antigen production. This recombinant bacterium was orally subjected to mice, and the immune response to CagL was evaluated by ELISA. Intracellular expression of CagL protein was confirmed by Western blot analysis. Mucosal immunization of mice with the recombinant L. lactis significantly stimulated CagL-Specific antibodies: IgA, IgG, cytokine IL-17 and IN-γ. Moreover, the specific anti-CagL IgA response was detected in the feces of immunized mice. These results indicate that CagL of H. pylo...
Source: Microbial Pathogenesis - Category: Infectious Diseases Source Type: research
Authors: Puderecki M, Wronecki L, Cięszczyk K, Szumiło J Abstract Organic basis of gastrointestinal symptoms is in the scope of many specialists. In this article lymphocytic gastritis, relatively newly described and not widely-known entity is presented. The lesion is characterized by presence of numerous mature lymphocytes in the surface and foveolar epithelium, as well as lymphocytic infiltration of the lamina propria. According to the definition at least 25 lymphocytes per 100 gastric epithelial cells is now required for the diagnosis. Literature found in wide r...
Source: Polish Journal of Pathology - Category: Pathology Tags: Pol J Pathol Source Type: research
This study sought to evaluate the inhibitory properties of EOCs immobilised on silica microparticles againstH. pylori and to elucidate the mechanism of action of the immobilised antimicrobials. After the preparation and characterisation of the antimicrobial supports, the susceptibility ofH. pylori in the presence of the immobilised compounds was assessed by plate count, fluorescent viability staining and direct viable count –fluorescent in situ hybridisation analyses. The antimicrobial supports were found to inhibitH. pylori growth, and to induce morphological and metabolic alterations to theH. pylori membrane, with ...
Source: World Journal of Microbiology and Biotechnology - Category: Microbiology Source Type: research
Alaska Native (AN) people experience higher incidence of, and mortality from, gastric cancer compared to other U.S. populations1, 2. Compared to the general U.S. population, gastric cancer in AN people occurs at a younger age, is diagnosed at later stages, is more evenly distributed between the sexes, and is more frequently signet-ring or diffuse histology3. It is known that the prevalence of Helicobacter pylori (Hp) infection, a risk factor for gastric cancer, is high in AN people4; however, high antimicrobial resistance combined with high reinfection rates in Alaska make treatment at the population level complex5.
Source: Gastroenterology - Category: Gastroenterology Authors: Source Type: research
In the original publication of the article, the figure  3 was published with errors. The corrected figure 3 should appear as in this correction.
Source: Journal of Gastroenterology - Category: Gastroenterology Source Type: research
Chem. Commun., 2020, Advance Article DOI: 10.1039/C9CC07915G, CommunicationGuangzong Tian, Chunjun Qin, Zhonghua Liu, Dacheng Shen, Xiaopeng Zou, Junjie Fu, Jing Hu, Peter H. Seeberger, Jian Yin Unique α-(1 → 2)- and α-(1 → 3)-linked oligoglucosides from theH. pylori serotype O2 O-antigen were synthesized with exclusive α-selectivity using remote participation effects. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
Source: RSC - Chem. Commun. latest articles - Category: Chemistry Authors: Source Type: research
Cochrane China Network working groups had an informal meeting included in the 13th China Health Technology Assessment Forum, hosted by Prof Yingyao Chen (from Fudan University) on 17th November.Eight Cochrane China Network working groups reported their work on Cochrane and some achievements in health technology assessment Cochrane. Prof Jianping Liu (Beijing University of Chinese medicine) gave the opening session, and introduced Cochrane China network and the whole session.Prof Shiyao Chen, from Zhongshan hospital affiliated to Fudan University, talked about “The clinical decision on screening helicobacter pylori fo...
Source: Cochrane News and Events - Category: Information Technology Authors: Source Type: news
Total synthesis of the Helicobacter pylori serotype O2 O-antigen α-(1 → 2)- and α-(1 → 3)-linked oligoglucosides. Chem Commun (Camb). 2019 Dec 06;: Authors: Tian G, Qin C, Liu Z, Shen D, Zou X, Fu J, Hu J, Seeberger PH, Yin J Abstract Exploiting synergistic remote participation effects of acyl groups at the O3 and O6 positions was key to the complete α-selectivity during the total synthesis of the unique (1 → 2)- and (1 → 3)-linked α-oligoglucosides from the Helicobacter pylori O2 O-antigen. Acyl remote participation and solvent effects were found to counter...
Source: Chemical Communications - Category: Chemistry Authors: Tags: Chem Commun (Camb) Source Type: research
Authors: Zhang F, Chen C, Hu J, Su R, Zhang J, Han Z, Chen H, Li Y Abstract Helicobacter pylori (H. pylori) is a gram-negative pathogen that colonizes gastric epithelial cells. The drug resistance rates of H. pylori have dramatically increased, causing persistent infections. Chronic infection by H. pylori is a critical cause of gastritis, peptic ulcers and even gastric cancer. In host cells, autophagy is stimulated to maintain cellular homeostasis following intracellular pathogen recognition by the innate immune defense system. However, H. pylori-induced autophagy is not consistent during acute and chronic infectio...
Source: Oncology Letters - Category: Cancer & Oncology Tags: Oncol Lett Source Type: research
Conclusions: The ages of patients with DGR were significantly higher than in the control group, and advanced age was shown to be a risk factor for primary DGR. It was found that the presence of DGR has no effect on the presence and severity of H.pylori. Given this situation, we consider it is important to eradicate H.pylori infection, especially in the case where H.pylori is present together with DGR. PMID: 31817518 [PubMed - in process]
Source: Medicina (Kaunas) - Category: Universities & Medical Training Authors: Tags: Medicina (Kaunas) Source Type: research
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