Eleven triterpenoids (1-11) from the roots of Taraxacum japonicum (Compositae) were examined for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) induced by the tumor promoter, 12-O-tetrade-canoylphorbol-13-acetate (TPA), in Raji cells as a primary screening test for anti-tumor-promoters (cancer chemopreventive agents). Of these triterpenoids, taraxasterol (1) and taraxerol (7) exhibited significant inhibitory effects on EBV-EA induction, but the inhibitory effects of their acetates 2 and 8 were weaker than those of 1 and 7. Furthermore, 1 and 7 exhibited potent anti-tumor-promoting activity in the two-stage carcinogenesis tests of mouse skin using 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter, and 1 showed a remarkable inhibitory effect on mouse spontaneous mammary tumors using C3H/OuJ mouse. These results strongly suggested that taraxasterol (1) could be a valuable chemopreventive agent.
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http://dx.doi.org/10.1248/bpb.22.606 | DOI Listing |
Eur J Med Chem
January 2025
School of Pharmaceutical Sciences, Guizhou University, Guiyang, 550025, China. Electronic address:
Temozolomide, a widely used alkylating agent for glioblastoma treatment, faces significant challenges due to the development of resistance, which severely impacts patient survival. This underscores the urgent need for novel strategies to overcome this barrier. Focal adhesion kinase (FAK), an intracellular non-receptor tyrosine kinase, is highly expressed in glioblastoma cells and has been identified as a promising therapeutic target for anti-glioblastoma drug development.
View Article and Find Full Text PDFOncotarget
January 2025
Department of Neurology, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.
Recently, combination checkpoint therapy of cancer has been recognized as producing additive as opposed to synergistic benefit due in part to positively correlated effects. The potential for uncorrelated or negatively correlated therapies to produce true synergistic benefits has been noted. Whereas the inhibitory receptors PD-1, CTLA-4, TIM-3, LAG-3, and TIGIT have been collectively characterized as exhaustion receptors, another inhibitory receptor KLRG1 was historically characterized as a senescent receptor and received relatively little attention as a potential checkpoint inhibitor target.
View Article and Find Full Text PDFChem Biodivers
January 2025
Toxicology and Pharmacology Laboratory, Department of Biotechnology, Faculty of Science and Humanities, SRM Institute of Science and Technology, Kattankulatur, India.
Catheter-associated urinary tract infections (CAUTIs), often caused by biofilm-forming Staphylococcus aureus, present significant clinical challenges. Skt35, a dioxopiperidinamide derivative of cinnamic acid, was investigated for its potential antibacterial and antibiofilm activities against S. aureus biofilms.
View Article and Find Full Text PDFJ Infect Dev Ctries
December 2024
Department of Immunology, School of Medicine and Dr. Jose Eleuterio Gonzalez University Hospital, Universidad Autónoma de Nuevo León, Monterrey, Mexico.
Co-inhibitory molecules, such as cytotoxic T-lymphocyte-associated protein 4 (CTLA-4) and programmed cell death protein 1 (PD-1), known as immune checkpoints, regulate the activity of T and myeloid cells during chronic viral infections and are well-established for their roles in cancer therapy. However, their involvement in chronic bacterial infections, particularly those caused by pathogens endemic to developing countries, such as Mycobacterium tuberculosis (Mtb), remains incompletely understood. Cytokine microenvironment determines the expression of co-inhibitory molecules in tuberculosis: Results indicate that the cytokine IL-12, in the presence of Mtb antigens, can enhance the expression of co-inhibitory molecules while preserving the effector and memory phenotypes of CD4+ T cells.
View Article and Find Full Text PDFJ Food Sci
January 2025
College of Pharmacy, Changchun University of Chinese Medicine, Changchun, China.
Ginseng and its processed products are valued as health foods for their nutritional benefits. The traditional forms of processed ginseng include white ginseng, dali ginseng (DLG), red ginseng (RG), and black ginseng (BG). However, the impact of processing on the chemical composition and anti-tumor efficacy of these products is not well understood.
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