Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185, Rome, Italy. Electronic address:
Published: August 2018
AI Article Synopsis
Article Abstract
We discovered a series of azole antifungal compounds as effective antiprotozoal agents. They displayed promising inhibitory activities within the micromolar-submicromolar range against P. falciparum, L. donovani, and T. b. rhodesiense. Moreover, most of such compounds showed excellent nanomolar IC against T. cruzi, showing also very low cytotoxicity. Discussion of structure-activity relationships and biological data for these compounds are provided against the different parasites. To assess the mechanism of action against T. cruzi we proved that the most potent compounds (3b, 3j-l) inhibited the T. cruzi CYP51. Moreover, the most active derivative 3j dramatically reduced parasitemia in T. cruzi mouse model without acute toxicity.
Recently, research into the oncogenic driver genes associated with non-small cell lung cancer (NSCLC) has advanced significantly, leading to the development and clinical application of an increasing number of approved therapeutic agents. Among these, small molecule inhibitors that target mesenchymal-epithelial transition (MET) have demonstrated successful application in clinical settings. Currently, three categories of small molecule MET inhibitors, characterized by distinct binding patterns to the MET kinase region, have been developed: types Ia/Ib, II, and III.
Introduction: The Sanxingdui site (Sichuan, China) is the typical representative of the ancient Shu culture, which lasts from the late Neolithic to early Western Zhou. The sacrificial pits are located in the core region of Sanxingdui site, and numerous artifacts are unearthed including ivory, seashells, bronzes, pottery, jade, stone, gold, bone, and horn products. The function of the pits and buried artifacts has always been the focus, but the microbiome around artifacts attracts less attention.
Galactooligosaccharides (GOS) are lactose-derived functional ingredients applied in food products and have great potential in health protection. The conversion of lactose to GOS commonly occurs using β-galactosidases of mould, yeast and bacterial origin. The yield and structure of the resulting GOS depend on the enzyme used and the reaction conditions.
State key laboratory of Integration and Innovation of Classic Formula and Modern Chinese Medicine, National Chinmedomics Research Center, National TCM Key Laboratory of Serum Pharmacochemistry, Metabolomics Laboratory, Department of Pharmaceutical Analysis, Heilongjiang University of Chinese Medicine, Heping Road 24, Harbin 150040, China; State Key Laboratory of Dampness Syndrome, The Second Affiliated Hospital Guangzhou University of Chinese Medicine, Dade Road 111, Guangzhou, China. Electronic address:
ASPN-1, a novel glucan with a molecular weight of 33.31 kDa, was purified from Acanthopanax senticosus stems, characterized in structure, and evaluated for antitumor potential. The analysis of the structure of ASPN-1 revealed that it consisted of a backbone constructed from →4)-α-D-Glcp-(1 → glucosyls, branched at the O-3 position by an α-D-Glcp-(1 → residue and at the O-6 positions with α-D-Glcp-(1 → 6)-α-D-Glcp-(1 → and/or α-D-Glcp-(1 → residues.
This study investigated the relationship between pea protein isolates (PPI) emulsifying properties and their structural, interfacial, and physicochemical characteristics at various pH values (native pH, 7, 5, and 3). Emulsion characteristics including emulsifying activity and stability, droplet size, flocculation index (FI) and coalescence index (CI) were examined. Additionally, physicochemical properties such as solubility, zeta potential, surface hydrophobicity, interfacial protein adsorption and protein conformation were analyzed.
