Purpose: To determine the effect of tangeritin on cadmium-induced cardiotoxicity in rats. Methods: Cardiotoxicity was induced by intra-gastric administration of 5 mg/kg cadmium chloride to rats, once daily for 4 weeks. The animals were treated with tangeritin at 10 and 20 mg/kg p.o. 60 min before the administration of cadmium, for 4 weeks. Thereafter, the concentrations of cadmium in serum and cardiac tissue were determined, and markers of cardiac function, antioxidant enzyme activities and levels of pro-inflammatory mediators were evaluated in cardiac tissues. Histopathological examination and western blot assay were also performed. Results: Treatment with tangeritin significantly decreased the cadmium levels in the heart tissue and serum of the cadmium-exposed rats, when compared to the negative control group (p < 0.01). There was significant decrease in cardiac function markers in the tangeritin-treated rats, relative to negative control group (p < 0.01). However, antioxidant enzyme activity and levels of pro-inflammatory mediators were attenuated in the cardiac tissues of cadmium-treated rats by tangeritin treatment. Expressions of HO-1 and Nrf-2 were significantly enhanced in the cardiac tissues of tangeritin-treated group, relative to negative control group (p < 0.01). Histopathology revealed that tangeritin attenuated cadmium-induced cardiac injury in cadmium-exposed rats. Conclusion: These results demonstrate the protective effect of tangeritin against cadmium-induced cardiotoxicity via attenuation of oxidative stress and pro-inflammatory mediators. Keywords: Tangeritin, Cadmium, Cardiotoxicity, Oxidative stress, Anti-inflammation

Human testis-specific and bromodomain-containing protein (hBRDT) is essential for chromatin remodeling during spermatogenesis and is therefore an attractive target for the discovery of male contraceptive drugs. In this study, pharmacophore modeling was carried out based on the crystal structure of hBRDT in complex with the inhibitor, JQ1. The established pharmacophore model was used as a 3D search query to identify potent hBRDT inhibitors from an in-house chemical database. A molecular docking analysis was carried out to filter the obtained hit compounds. A total of 125 compounds was finally selected based on the ranking order and visual examination. These compounds were further evaluated by a protein-based in vitro assay. Four compounds with new chemical scaffolds were identified to be hBRDT inhibitors. The most active of these compounds, T480, had a half maximal inhibitory concentration (IC50) of 9.02 µM. The detailed analysis of the binding mode of compound T480 provides important information for the further development of novel BRDT inhibitors.

The detailed glycan structural analysis of glycoprotein is amenable to glycopeptide enrichment. Here, we develop a simple, effective and economical approach to enrich glycopeptides from proteolytically digested peptide mixtures by chromatographic column packed with graphite carbon and activated charcoal (G/A-column). Glycopeptide from ovalbumin was efficiently enriched by homemade G/A-column using liquid chromatography and the structure of glycopeptide was obtained by tandem mass spectrometry using Fourier transform ion cyclotron resonance mass spectrometry. The results in this study demonstrate that G/A-column can be used to enrich N-glycolpeptides and be benefit for online identification of glycopeptide using LC-MS.