2 research outputs found
DataSheet1_Exploring the pharmacological mechanisms of icaritin against nasopharyngeal carcinoma via network pharmacology and experimental validation.PDF
Background: Icaritin is a natural product with a wide range of anti-tumor effects. However, its anti-tumor mechanism has not been thoroughly studied. This study examined the inhibitory effect of icaritin on nasopharyngeal cancer and its underlying mechanism using network pharmacology along with in vivo and in vitro experiments.Methods: MTT and clone formation assays were used to detect the effects of icaritin on the viability and proliferation of nasopharyngeal carcinoma cells, followed by the construction of a HONE1 xenograft tumor model to evaluate the anti-tumor efficacy of icaritin in vivo. A public database was used to predict prospective targets, built a protein-protein interaction (PPI) network, and analyze gene enrichment and biological processes. Based on network pharmacological data, cell cycle-related proteins were identified using western blotting. Besides, cell cycle distribution, apoptosis, and intracellular reactive oxygen species (ROS) generation were identified using flow cytometry. In addition, SA-β-Gal staining was performed to detect cellular senescence, and western blotting was performed to detect the expression of P53, P21, and other proteins to verify key signaling pathways.Results: Icaritin effectively inhibited the viability and proliferation of nasopharyngeal carcinoma cell lines and showed good anti-tumor activity against HONE1 nasopharyngeal carcinoma cells in vivo. Key protein targets, including AKT1, HSP90AA1, CDK4, CCND1, and EGFR, were screened using PPI network topology analysis. GO and KEGG analysis revealed that the cell cycle, p53 signaling, and cell senescence pathways may be the main regulatory pathways. Flow cytometry and western blot experiments showed that icaritin caused S-phase arrest and promoted an increase in ROS. SA-β-Gal staining showed that icaritin significantly induced cellular senescence, and western blotting showed that the expression of senescence-related proteins p53 and P21 increased significantly. Moreover, inhibition of ROS levels by N-Acetylcysteine (NAC) enhanced cell viability, reversed cellular senescence and reduced cellular senescence-associated protein expression.Conclusion: The results of network pharmacological analysis and in vivo and in vitro experiments showed that icaritin effectively inhibited the growth of nasopharyngeal carcinoma cells, promoted ROS production, induced cellular senescence, and inhibited tumor cells, which are related to the regulation of P53/P21 signal pathway.</p
Maltose-Functionalized Hydrophilic Magnetic Nanoparticles with Polymer Brushes for Highly Selective Enrichment of N‑Linked Glycopeptides
Efficient enrichment glycoproteins/glycopeptides
from complex biological
solutions are very important in the biomedical sciences, in particular
biomarker research. In this work, the high hydrophilic polyethylenimine
conjugated polymaltose polymer brushes functionalized magnetic Fe<sub>3</sub>O<sub>4</sub> nanoparticles (NPs) denoted as Fe<sub>3</sub>O<sub>4</sub>–PEI–pMaltose were designed and synthesized
via a simple two-step modification. The obtained superhydrophilic
Fe<sub>3</sub>O<sub>4</sub>–PEI–pMaltose NPs displayed
outstanding advantages in the enrichment of N-linked glycopeptides,
including high selectivity (1:100, mass ratios of HRP and bovine serum
albumin (BSA) digest), low detection limit (10 fmol), large binding
capacity (200 mg/g), and high enrichment recovery (above 85%). The
above-mentioned excellent performance of novel Fe<sub>3</sub>O<sub>4</sub>–PEI–pMaltose NPs was attributed to graft of
maltose polymer brushes and efficient assembly strategy. Moreover,
Fe<sub>3</sub>O<sub>4</sub>–PEI–pMaltose NPs were further
utilized to selectively enrich glycopeptides from human renal mesangial
cell (HRMC, 200 μg) tryptic digest, and 449 N-linked glycopeptides,
representing 323 different glycoproteins and 476 glycosylation sites,
were identified. It was expected that the as-synthesized Fe<sub>3</sub>O<sub>4</sub>–PEI–pMaltose NPs, possessing excellent
performance (high binding capacity, good selectivity, low detection
limit, high enrichment recovery, and easy magnetic separation) coupled
to a facile preparation procedure, have a huge potential in N-glycosylation
proteome analysis of complex biological samples