The benzimidazole nucleus is found in a variety of naturally occurring compounds and is of significant importance in medicinal chemistry. Owing to its conspicuous pharmacological properties, benzimidazoles have become an important pharmacophore and sub-structure in drug design and have been screened for a wide range of biological activities. Areas covered in this paper include a review of the biological effects, mechanisms and synthesis of benzimidazole derivatives in the past 2 years based on patents. The patent databases Scifinder and esp@cenet were used to locate patent applications that were published between 2013 to present. Information from articles published is also included. Benzimidazole derivatives are remarkably effective compounds to many diseases and may have the potential to be the first effective therapy against Ebola virus. Therefore, it is of great importance to develop specific design software and sustainable industrial synthetic routes for the development of effective and clinically relevant benzimidazole compounds.

Introduction: Polyphenol-rich sugarcane extract (PRSE) contains bioactive compounds with potential hypoglycemic properties, but its direct interaction with α-glucosidase has not been explored.Methods: This study investigated the inhibitory mechanism of PRSE on α-glucosidase using enzyme kinetics. Bioactive compounds with α-glucosidase-binding affinity were identified through biolayer interferometry-mass spectrometry (BLI-MS), and the binding mechanisms were further explored via molecular docking analysis.Results and discussion: PRSE was found to inhibit α-glucosidase through a mixed-type mechanism. A total of 29 compounds, including 4 coumarins, 9 phenolic acids, and 16 flavonoids, were identified in the PRSE dissociation solution. Representative compounds included coumarin, kaempferol, apigenin 7-o-neohesperidoside, and vicenin 3. Notably, apigenin 7-o-neohesperidoside and vicenin 3 were identified for the first time as potential α-glucosidase inhibitors.These compounds interacted with key residues of α-glucosidase, such as Asp and Glu, via hydrogen bonding, π-anion interactions, and hydrophobic forces. These findings suggest that PRSE could serve as a promising natural source of α-glucosidase inhibitors. The application of BLI-MS proved effective for screening target bioactive compounds in plant extracts. PRSE may have potential applications in functional foods for postprandial glycemic control and type 2 diabetes prevention.

Maca (Lepidium meyeniiWalp.), originated in the high Andes of Peru, is rich in nutrients and phytochemicals. As a new resource food in China, Maca suffers marketing disorders due to the limitation of basic research. Due to the close relationship of Maca quality and origin of place, it’s of scientific, economic and social importance to set up a rapid, reliable and efficient method to identify Maca origin. In the present study, 303 Maca samples were collected from 101 villages of the main producing area in China. Using electronic nose and BP neutral network algorithm, a Maca odor database was set up to trace the origin. GC-MS was then employed to analyze the characteristic components qualitatively and semi-quantitatively. As a result, very significant differences (p < 0.01) were detected in the volatile components of Maca from different areas. This study not only constructs a network model to forecast the Maca origin, but also reveals the relationship between Maca odor fingerprints and origins.

A series of novel 4′-[(benzimidazol-1-yl)methyl]biphenyl-2-sulphonamides was designed, and their molecular model simulation fitting to a new HipHop 3D pharmacophore model was examined. Several compounds showed significantly high simulation fit values. The designed compounds were synthesised, 22 of which were biologically evaluated in vitro using the dual receptor binding assay. Compound 11 showed potent antagonistic activity against both angiotensin II AT₁ and endothelin ET_A receptors. Obtaining a highly active compound from a candidate set of only 22 compounds illustrates the power and utility of our pharmacophore model.

Objectives: This study investigated the efficacy of wheat peptide supplementation compared to regular proteins in elite cross-country skiers, providing insights into the metabolic and performance effects of these supplements in order to guide athletes in selecting optimal energy sources for training and competition. Methods: Nineteen healthy male cross-country skiers were enrolled and assigned to either the peptide group (PEP, n = 9) or the protein group (PRO, n = 10). A four-week intervention study involving supplementation with wheat peptides/regular proteins was conducted, and pre- and post-intervention assessments were performed to evaluate exercise capacity and metabolic profiles. Results: The study found that the PEP group and the PRO group showed distinct within-group effects on exercise performance. The PEP group demonstrated improved aerobic capacity, including better performance in 10 km roller skating, an increased lactate threshold, and reduced resting blood lactate levels. The PRO group enhanced anaerobic capacity, such as improved sprint time, hexagon test performance, and lactate clearance. Metabolomic analysis revealed specific metabolic pathways affected in each group, with the PEP group showing impacts on the α-linolenic acid pathway and the PRO group on ketone body synthesis and degradation as well as vitamin B6 metabolism. Conclusions: Our findings indicate that wheat oligopeptides and regular proteins have comparable effects on exercise performance. However, the wheat peptides may offer greater advantages in enhancing aerobic capacity. No significant variations were observed in blood metabolite profiles between the two groups, but distinct metabolic pathways exhibited different responses.