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Demethylzeylasteral induces PD-L1 ubiquitin-proteasome degradation and promotes antitumor immunity targeting USP22.
Acta Pharm Sin B
October 2024
Shanghai Frontiers Science Center of TCM Chemical Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Programmed cell death ligand-1 (PD-L1) is a T cell inhibitory immune checkpoint molecule that interacts with programmed cell death-1 (PD-1) to promote immune escape of tumor cells. Compared with antibody therapies, small molecule drugs show better prospects due to their advantages such as higher bioavailability, better tissue penetration, and reduced risk of immunogenicity. Here, we found that the small molecule demethylzeylasteral (Dem) can significantly downregulate the expression of PD-L1 in colorectal cancer cells and enhance the killing effect of T cells on tumor cells.
View Article and Find Full Text PDFDemethylzeylasteral alleviates inflammation and colitis via dual suppression of NF-κB and STAT3/5 by targeting IKKα/β and JAK2.
Int Immunopharmacol
December 2024
Department of Laboratory Medicine, Hospital of Chengdu University of Traditional Chinese Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu 610072, China; College of Medical Technology, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China; TCM Regulating Metabolic Diseases Key Laboratory of Sichuan Province, Hospital of Chengdu University of Traditional Chinese Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu 610072, China. Electronic address:
Article Synopsis
- Ulcerative colitis (UC) is a common inflammatory bowel disease that can lead to colorectal cancer, and this study investigates the potential of demethylzeylasteral (DZT), a compound from Tripterygium wilfordii, to treat UC.
- Various laboratory techniques, such as RT-qPCR and Western blot, were used to analyze the effects of DZT on inflammation in macrophage cells and in mice with DSS-induced colitis, showing that it reduces key inflammatory molecules.
- The mechanism of DZT's action involves inhibiting pro-inflammatory signaling pathways (specifically NF-κB and STAT3/5) by directly binding to specific kinases, leading to a reduction in symptoms and inflammation related to
Demethylzeylasteral protects against renal interstitial fibrosis by attenuating mitochondrial complex I-mediated oxidative stress.
J Ethnopharmacol
June 2024
Department of Nephrology, Zhongnan Hospital, Wuhan University, China. Electronic address:
Ethnopharmacological Relevance: Renal interstitial fibrosis (RIF) is a main pathological process in chronic kidney disease (CKD). Demethylzeylasteral (DML), a major component of Tripterygium wilfordii Hook. f.
View Article and Find Full Text PDFA novel SPE-LC-MRM strategy for serum demethylzeylasteral quantitation developed with an O-labeled internal standard.
Anal Bioanal Chem
January 2024
State Key Laboratory for Fine Exploration and Intelligent Development of Coal Resources, Ding11 Xueyuan Road, Beijing, 100083, China.
Natural bioactive compounds (NBCs) are widely used in clinical treatment. For example, Tripterygium wilfordii Hook f. is commonly known in China as Lei-Gong-Teng which means thunder god vine.
View Article and Find Full Text PDFInhibiting NF-κB-S100A11 signaling and targeting S100A11 for anticancer effects of demethylzeylasteral in human colon cancer.
Biomed Pharmacother
December 2023
Oujiang Laboratory, School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou 325035, PR China. Electronic address:
Colon cancer is a common and deadly malignancy of the gastrointestinal tract. Targeting proteins that inhibit tumor proliferation could lead to innovative treatment strategies for this disease. Demethylzeylasteral, extracted naturally from Tripterygium wilfordii Hook.
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