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Norharmane prevents muscle aging via activation of SKN-1/NRF2 stress response pathways.
Redox Biol
January 2025
Aging and Metabolism Research Group, Korea Food Research Institute, Wanju-gun, South Korea; Department of Food Biotechnology, Korea University of Science and Technology, Daejeon-si, South Korea. Electronic address:
Sarcopenia, the age-related decline in muscle mass and function, is a significant contributor to increased frailty and mortality in the elderly. Currently, no FDA-approved treatment exists for sarcopenia. Here, we identified norharmane (NR), a β-carboline alkaloid, as a potential therapeutic agent for mitigating muscle aging.
View Article and Find Full Text PDFSynthesis of harmaline N-9 derivatives and investigation of in vitro anticancer activity.
Bioorg Med Chem Lett
January 2025
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488 China. Electronic address:
Harmaline as a natural compound possessed a wide range of pharmacological activities. In this study, 22 novel harmaline-based derivatives were synthesized and screened for in vitro anti-proliferation activity against three cancer cell lines, HCT116, MCF7, and MGC803. The modification site was at the position N-9 of harmaline.
View Article and Find Full Text PDFAsymmetric Synthesis, Structure Determination, and Biologic Evaluation of Isomers of TLAM as PFK1 Inhibitors.
ACS Med Chem Lett
January 2025
Department of Life Science and Biotechnology, Faculty of Chemistry, Materials and Bioengineering, Kansai University, 3-3-35 Yamate-cho, Suita, Osaka 564-8680, Japan.
Inhibiting phosphofructokinase-1 (PFK1) is a promising approach for treating lactic acidosis and mitochondrial dysfunction by activating oxidative phosphorylation. Tryptolinamide (TLAM) has been shown as a PFK1 inhibitor, but its complex stereochemistry, with 16 possible isomers complicates further development. We conducted an asymmetric synthesis, determined the absolute configurations, and evaluated the PFK1 inhibitory activity of the TLAM isomers.
View Article and Find Full Text PDFRSL3 induces ferroptosis by activating the NF-κB signalling pathway to enhance the chemosensitivity of triple-negative breast cancer cells to paclitaxel.
Sci Rep
January 2025
Department of Breast Surgery, China-Japan Union Hospital of Jilin University, Changchun, China.
Chemotherapy resistance in triple-negative breast cancer (TNBC) leads to poor therapeutic effects and a poor prognosis. Given that paclitaxel-based chemotherapy is the main treatment method for TNBC, enhancing its chemosensitivity has been a research focus. Induced ferroptosis of tumour cells has been proven to increase chemosensitivity, but its ability to sensitize TNBC cells to paclitaxel (PTX) is unknown.
View Article and Find Full Text PDFRevealing the impact of tadalafil-loaded proniosomal gel against dexamethasone-delayed wound healing via modulating oxido-inflammatory response and TGF-β/Macrophage activation pathway in rabbit model.
PLoS One
January 2025
Department of Nutrition and Clinical Nutrition, Faculty of Veterinary Medicine, Menoufia University, Shibin El-Kom, Egypt.
A serious challenge of the chronic administration of dexamethasone (DEX) is a delay in wound healing. Thus, this study aimed to investigate the potential of Tadalafil (TAD)-loaded proniosomal gel to accelerate the healing process of skin wounds in DEX-challenged rabbits. Skin wounds were induced in 48 rabbits of 4 groups (n = 12 per group) and skin wounds were treated by sterile saline (control), TAD-loaded proniosomal gel topically on skin wound, DEX-injected rabbits, and DEX+TAD-loaded proniosomal gel for 4 weeks.
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