Selenium-rich tea polysaccharides (Se-TPS) were extracted via high hydrostatic pressure technology with a pressure of 400 MPa (200-500 MPa) for 10 min (3-20 min) at a material-to-solvent ratio of 1:40 (1:20-1:50). Subsequently, Se-TPS1-4 were isolated and purified, with Se-TPS3-4 as the main components. A spectral analysis proved that Se, which has antioxidant activity, existed. An in vitro study found that among Se-TPS, Se-TPS3-4 attenuated the release of β-hexosaminidase, histamine, and interleukin (IL)-4. Furthermore, in vivo experiments revealed that treatment with Se-TPS downregulated IL-4 levels and upregulated TGF-β and interferon-γ levels to improve imbalanced Th1/Th2 immunity in tropomyosin-sensitized mice. Moreover, Se-TPS promoted Lactobacillus and norank_f_Muribaculaceaek growth and upregulated metabolites such as genipin and coniferyl alcohol. Overall, these results showed the strong anti-allergy potential of Se-TPS by regulating mast cell-mediated allergic inflammatory responses and microbiota regulation, highlighting the potential of Se-TPS as a novel therapeutic agent to regulate allergy-associated metabolic disorders.

01 Jul 2011·Bioorganic & Medicinal ChemistryQ3 · MEDICINE

4-Alkoxy-3-arylfuran-2(5H)-ones as inhibitors of tyrosyl-tRNA synthetase: Synthesis, molecular docking and antibacterial evaluation

Q3 · MEDICINE

Article

Author: Hai-Liang Zhu ; Tian-Fang Yi ; Ze-Jun Huang ; Xu-Dong Wang ; Peng-Cheng Lv ; She-Rong Yu ; Hui Ouyang ; Ye-Ling Yang ; Zhu-Ping Xiao

A series of novel 4-alkoxy-3-arylfuran-2(5H)-ones as tyrosyl-tRNA synthetase inhibitors were synthesized. Of these compounds, 3-(4-hydroxyphenyl)-4-(2-morpholinoethoxy)furan-2(5H)-one (27) was the most potent. The binding model and structure-activity relationship indicate that replacement of morpholine-ring in the side chain of 27 with a substituent containing more hydrophilic groups would be more suitable for further modification. Antibacterial assay revealed that the synthetic compounds are effective against growth of Gram-positive organisms, and 27 is the most potent agent against Staphylococcus aureus ATCC 25923 with MIC(50) value of 0.23 μg/mL.

01 Aug 2009·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

LC–NMR and LC–MS identification of an impurity in a novel antifungal drug icofungipen

Q3 · MEDICINE

Article

Author: Predrag Novak ; Igor Bratoš ; Predrag Tepeš ; Miljenko Dumić ; Zdenko Hameršak ; Amir Avdagić ; Marina Ilijaš ; Vesna Gabelica Marković ; Ines Fistrić

Successful use of LC-NMR and LC-MS for rapid identification of an impurity in a novel antifungal drug icofungipen has been demonstrated. Complementary information obtained from the two methods made it possible to determine the structure of A1 prior to its isolation and purification. Stop-flow LC-NMR ((1)H and DQFCOSY), LC-MS and LC-MS/MS spectra have shown that A1 is structurally related to icofungipen. It was later isolated and prepared synthetically and its structure was corroborated by high-resolution NMR spectroscopy.

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Indication	Highest Phase	Country/Location	Organization	Date
Candidiasis	Phase 2	-	Bayer AG	-
Candidiasis	Phase 2	-	Teva Pharmaceutical Industries Ltd.	-
Candidiasis	Phase 2	Germany	-	-
Candidiasis, Vulvovaginal	Phase 2	United States	-	-

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