Small-molecule arginase inhibitors. Ivanenkov Yan A,Chufarova Nina V Pharmaceutical patent analyst Arginase is an enzyme that metabolizes L-arginine to L-ornithine and urea. In addition to its fundamental role in the hepatic ornithine cycle, it also influences the immune systems in humans and mice. Arginase participates in many inflammatory disorders by decreasing the synthesis of nitric oxide and inducing fibrosis and tissue regeneration. L-arginine deficiency, which is modulated by myeloid cell arginase, suppresses T-cell immune response. This mechanism plays a fundamental role in inflammation-associated immunosuppression. Pathogens can synthesize their own arginase to elude immune reaction. Small-molecule arginase inhibitors are currently described as promising therapeutics for the treatment of several diseases, including allergic asthma, inflammatory bowel disease, ulcerative colitis, cardiovascular diseases (atherosclerosis and hypertension), diseases associated with pathogens (e.g., Helicobacter pylori, Trypanosoma cruzi, Leishmania, Mycobacterium tuberculosis and Salmonella), cancer and induced or spontaneous immune disorders. This article summarizes recent patents in the area of arginase inhibitors and discusses their properties. 10.4155/ppa.13.75

Thin-layer chromatography-bioautographic method for the detection of arginase inhibitors. Attia Rym,Zedet Andy,Bourjot Mélanie,Skhiri Eya,Messaoud Chokri,Girard Corine Journal of separation science Arginase represents a promising therapeutic target for various pathologies including inflammatory, cardiovascular, and parasitic diseases or cancers. In the current work, we report, for the first time, about the development of a thin-layer chromatography-based bioautography which can be used to rapidly detect arginase inhibitors in complex matrices such as plant extracts. The assay is based on the detection of urea produced by arginase using the coloring reagent α-isonitrosopropiophenone, resulting in the formation of a pink background on thin-layer chromatography plates. The assay conditions were optimized in order to provide sufficient contrast between the pink colored thin-layer chromatography plate and the clearer zones generated by the presence of arginase inhibitors. Different parameters were tested, such as incubation time and temperature, atmospheric conditions, as well as substrate and enzyme concentrations. This technique makes it possible to detect 0.1 μg of a known arginase inhibitor, N -hydroxy-nor-Arginine, after it has been spotted, either pure or mixed with a Myrtus communis methanolic fruit extract, and the plate has been developed in an appropriate solvent. The newly developed method was used to reveal the presence of an inhibitor in hempseed cakes (Cannabis sativa L.). 10.1002/jssc.201901210