A novel series of 2-benzyl-1-indanone analogs were investigated as IL-5 inhibitory activity. Among the synthesized compounds, 7-(cyclohexylmethoxy)-2-(4-hydroxybenzyl)-2,3-dihydro-1H-inden-1-one (7s, 100.0% inhibition at 30 μM, IC = 4.0 μM), and 7-(cyclohexylmethoxy)-2-(3-hydroxybenzyl)-2,3-dihydro-1H-inden-1-one (7t, 95.0% inhibition at 30 μM, IC = 6.0 μM) showed the best inhibitory activity against IL-5. The 2-benzyl-1-indanone analogs showed moderate to strong IL-5 inhibitory activity. Especially, hydroxyl (HBD/HBA) substituent at position 3 or 4 on phenyl ring B showed potent IL-5 inhibition. Additionally, the bulky hydrophobic cyclohexylmethoxy group at position 7 of the 1-indanone ring is favorable for the inhibitory activity.
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http://dx.doi.org/10.1016/j.ejmech.2018.04.030 | DOI Listing |
J Nat Prod
January 2025
Department of Chemical and Biological engineering, School of Engineering and Technology, National University of Mongolia, Ulaanbaatar 14201, Mongolia.
A chemical examination of a root extract of led to the isolation and identification of 23 compounds, including oxazole-type alkaloids and isoflavonoid derivatives. Notably, three oxazole-type alkaloids (, , and ) and two isoflavonoid derivatives ( and ) were obtained from a natural source for the first time. In addition, derived 2,5-diphenyloxazoles and their derivatives were synthesized.
View Article and Find Full Text PDFNat Prod Res
January 2025
Department of Applied Science, Faculty of Engineering & Technology, Gurukula Kangri (Deemed to be University), Haridwar, India.
The present study aimed to evaluate the nutrition value, phytochemical content, and diverse pharmacological activities of different solvent extracts of L. fruit. Among all, the hydro-alcoholic extract showed high DPPH and ABTS radical scavenging activities with IC values of 82.
View Article and Find Full Text PDFXenotransplantation
January 2025
Institute of Organ Transplantation, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.
Background: Gene-edited pigs for xenotransplantation usually contain one or more transgenes encoding human complement regulatory proteins (CRPs). Because of species differences, human CRP(s) expressed in gene-edited pigs may have difficulty inhibiting the activation of exogenous rabbit complement added to a complement-dependent cytotoxicity (CDC) assay. The use of human complement instead of rabbit complement in CDC experiments may more accurately reflect the actual regulatory activity of human CRP(s).
View Article and Find Full Text PDFBMC Cancer
January 2025
Department of Surgery, Tokushima University, 3-18-15 Kuramoto-Cho, Tokushima, 770-8503, Japan.
The pro-tumor effects of mast cell (MC) in the tumor microenvironment (TME) are becoming increasingly clear. Recently, MC were shown to contribute to tumor malignancy by supporting the migration of tumor-associated macrophages (TAMs), suggesting a relationship with tumor immunity. In the current study, we aimed to examine the correlation between MC infiltration and neoadjuvant chemoradiotherapy (nCRT) response for locally advanced rectal cancer (LARC).
View Article and Find Full Text PDFBMC Microbiol
January 2025
Chair of Microbiology, Jagiellonian University Medical College in Krakow, 18 Czysta Street, Cracow, 31-121, Poland.
Background: Aerobic vaginitis (AV) is a state of abnormal vaginal microbiota, which is associated with increased numbers of aerobic, enteric bacteria and inflammation of the vaginal epithelium. Anti-microbial treatment combined with anti-inflammatory therapy could be useful in the treatment of this condition. It is known that calcitriol, the active form of vitamin D, plays an important role in modulating the immune response in several inflammatory diseases.
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