Synthesis of Chalcones, Screening and and Evaluation of Helicobacter pylori Adhesion by Molecular Docking.

Aims: We synthetized 10 hydroxylated and methoxylated chalcones and evaluated them targeting MMP-9 inhibition, looking for the rate of adhesion of in gastric cells, and then, reduction of the inflammatory response as alternative therapeutic agents for controlling the infection.

Background: is a Gram-negative bacterium that chronically infects the human stomach, a risk factor for the development of inflammatory gastrointestinal diseases, including cancer, and is classified as a group I carcinogen. It is estimated that it infects around 45% of the global population and that the persistence of the infection is related to the adhesion of the bacteria in the gastric epithelium.

Trichilia catigua against Helicobacter pylori: An in vitro, molecular and in silico approach.

Helicobacter pylori is a bacterium that is present in the stomach of about 50% of the global population and is associated with several gastric disorders, including cancer. Natural products with antimicrobial activity have been tested against H. pylori, among them Trichilia catigua (catuaba), which is widely distributed in Brazil.

Can pharmaceutical care decrease the oxidative stress in type 2 diabetes mellitus?

Type 2 diabetes mellitus (T2D) is a chronic metabolic disorder characterized by an increase in oxidative stress, which is itself related to development of T2D's main chronic complications. Oxidative stress caused by elevated production of reactive species of oxygen and decrease of antioxidant defense system level, leads to activation of lipid peroxidation (LPO) and oxidative lipoprotein modification with increasing atherogenicity. Therefore, the aim of this study was to evaluate whether pharmacotherapeutic follow-up in patients with T2D, users and non-users of insulin, interferes with the levels of oxidative stress, measuring lipid peroxidation and protein oxidation, nitric oxide and superoxide dismutase levels.

Characterization of phenolic compounds in leaves by ESI(-) FT-ICR MS, analysis of cytotoxic activity on gastric adenocarcinoma (AGS cells), and anti- activity.

leaves are a source of flavonoids and ellagitannins, and the Brazilian population uses them to treat various diseases, including gastrointestinal disorders. This study aimed to determine if the ethanol extract and other derivatives are effective cytotoxic agents against gastric adenocarcinoma (AGS cells) and anti- agent, its chemical composition, and mass spectrometry characterization of the more abundant compounds. The results were compared with the literature.

Synthesis, Docking Studies and Evaluation of Chalcones as Anti-Helicobacter pylori and antitumoral Agents.

Helicobacter pylori colonizes the gastric epithelium of 50 % of world population and it is the main etiological agent of human chronic gastritis, peptic ulcer, and gastric cancer. In this study, we synthesized and characterized a series of 14 chalcones and evaluated their anti-H. pylori, NO inhibition (in vitro and in silico), and AGS cells cytotoxic effects.

In Vitro and In Silico Evaluation of Red Algae Anticancer Activity.

Studies estimate that nearly 2 million new cases of gastric cancer will occur worldwide during the next two decades, which will increase mortality associated with cancer and the demand for new treatments. Marine algae of the genus have secondary metabolites known for their cytotoxic action, such as terpenes and acetogenins. The species has demonstrated cytotoxicity against many types of tumors in previous analyses.

An In Vitro and In Silico Investigation about Activity against .

is a Brazilian native plant, traditionally used to treat gastric diseases that are now associated with and are commonly associated with several human diseases. We point out the extract as active against . The crude extract produced with acetone:water presented the best inhibitory activity of all five extracts (MIC 64 µg/mL).

Intermittent exposure to chlorpyrifos results in cardiac hypertrophy and oxidative stress in rats.

Forbidden in some countries due to its proven toxicity to humans, chlorpyrifos (CPF) still stands as an organophosphate pesticide (OP) highly used worldwide. Cardiotoxicity assessment is an unmet need in pesticide regulation and should be deeply studied through different approaches to better inform and generate an appropriate regulatory response to OP use. In the present study, we used our 4-week intermittent OP exposure model in rats to address the CPF effects on cardiac morphology allied with cardiovascular functional and biomolecular evaluation.

Anti-Candida, docking studies, and in vitro metabolism-mediated cytotoxicity evaluation of Eugenol derivatives.

The high morbidity and mortality rates of Candida infections, especially among immunocompromised patients, are related to the increased resistance rate of these species and the limited therapeutic arsenal. In this context, we evaluated the anti-Candida potential and the cytotoxic profile of eugenol derivatives. Anti-Candida activity was evaluated on C.

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

Aims: Silibinin is the major component of flavonolignans complex mixture (Silymarin), which is obtained from Silybum marianum (L.) Gaertn. Despite several reports about silibinin, little is known about its effects on gastric diseases.

Nitro-imidazole-based ruthenium complexes with antioxidant and anti-inflammatory activities.

Inflammation is a physiological process triggered in response to tissue damage, and involves events related to cell recruitment, cytokines release and reactive oxygen species (ROS) production. Failing to control the process duration lead to chronification and may be associated with the development of various pathologies, including autoimmune diseases and cancer. Considering the pharmacological potential of metal-based compounds, two new ruthenium complexes were synthesized: cis-[Ru(NO)(bpy)(5NIM)]PF (1) and cis-[RuCl(bpy)(MTZ)]PF (2), where bpy = 2,2'-bipyridine, 5NIM = 5-nitroimidazole and MTZ = metronidazole.

Search for Potential Inducible Nitric Oxide Synthase Inhibitors with Favorable ADMET Profiles for the Therapy of Helicobacter pylori Infections.

Background: Helicobacter pylori is a gram-negative bacterium related to chronic gastritis, peptic ulcer and gastric carcinoma. During its infection process, promotes excessive inflammatory response, increasing the release of reactive species and inducing the production of pro-inflammatory mediators. Inducible Nitric Oxide Synthase (iNOS) plays a crucial role in the gastric carcinogenesis process and a key mediator of inflammation and host defense systems, which is expressed in macrophages induced by inflammatory stimuli.

Avocado seeds (Persea americana Mill.) prevents indomethacin-induced gastric ulcer in mice.

The long-term use of anti-inflammatory drugs is the most common cause of gastric ulcer disease, one of the major gastrointestinal disorders affecting people worldwide. Persea americana Mill. (avocado) seed is a by-product generally discarded as waste, but can be used to treat gastric disorder due to its anti-inflammatory, antioxidant and antimicrobial activities.

Chemical analysis of the semipurified extract of and evaluation of inhibitory effects against .

Kunth, commonly known as guarana, is a native Brazilian plant species from the Amazon area that presents various biological effects, including antimicrobial action. The aim of this study was to chemically analyse the semipurified aqueous extract (AqF) of the plant and to evaluate the activity of crude (CE), ethyl-acetate (EAF), and AqF extracts against . The chemical profile of AqF was determined based on solid analysis C-NMR, direct infusion mass spectrometry (ESI-MS), and MALDI-TOF.

Antitumour, Immunomodulatory activity and in silico studies of naphthopyranones targeting iNOS, a relevant target for the treatment of Helicobacter pylori infection.

The naphthopyranones paepalantine and 5-methoxy-3,4-dehydroxanthomegnin isolated from Paepalanthus sp, showed in previous studies antioxidant, anti-inflammatory, antitumour and antimicrobial potential, such as anti-Helicobacter pylori activity. H. pylori infection is one of the main causes of gastric cancer, causing an excessive inflammatory response through the neutrophils and macrophages infiltration, increasing the release of reactive species and thus inducing the production of pro-inflammatory mediators.

Effect of biotransformation by liver S9 enzymes on the mutagenicity and cytotoxicity of melanin extracted from Aspergillus nidulans.

Context: A mutant that exhibited increased melanin pigment production was isolated from Aspergillus nidulans fungus. This pigment has aroused biotechnological interest due to its photoprotector and antioxidant properties. In a recent study, we showed that melanin from A.

Inhibition of nitric oxide and tumour necrosis factor-α production in peritoneal macrophages by Aspergillus nidulans melanin.

The naturally occurring pigment, melanin is found in organisms of all phylogenetic kingdoms, including fungi, and exhibits a wide range of biological activities. Our objective was to investigate the effects of melanin extracted from the fungus Aspergillus nidulans on the production of the pro-inflammatory mediators nitric oxide (NO) and tumour necrosis factor-α (TNF-α) in peritoneal macrophages and on the viability of McCoy mouse fibroblasts. The results showed that A.