Current Issue : July - September Volume : 2020 Issue Number : 3 Articles : 6 Articles
The coronavirus disease 19 (COVID-19) is a highly transmittable and pathogenic viral infection caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which emerged in Wuhan, China and spread around the world. There is no clinically approved antiviral drug or vaccine available to be used against COVID-19. However, few broad-spectrum antiviral drugs have been evaluated against COVID-19 in clinical trials, resulted in clinical recovery. In this review, we have highlighted some antiviral drugs such as chloroquine, hydroxyquinoline, arbidol, favipiravir, fedratinib, tecoplanin and its mechanism with its success rate in curing COVID-19. A number of clinical practice results showed that traditional Chinese medicine (TCM) plays significant role in the treatment of COVID-19, bringing new hope for the prevention and control of COVID-19....
The efforts for therapeutic targeting of the aryl hydrocarbon receptor (AhR) have emerged\nin recent years. We investigated the effects of available antimigraine triptan drugs, having an indole\ncore in their structure, on AhR signaling in human hepatic and intestinal cells. Activation of AhR in\nreporter gene assays was observed for Avitriptan and to a lesser extent for Donitriptan, while other\ntriptans were very weak or no activators of AhR. Using competitive binding assay and by homology\ndocking, we identified Avitriptan as a low-affinity ligand of AhR. Avitriptan triggered nuclear\ntranslocation of AhR and increased binding of AhR in CYP1A1 promotor DNA, as revealed by\nimmune-fluorescence microscopy and chromatin immune-precipitation assay, respectively. Strong\ninduction of CYP1A1 mRNA was achieved by Avitriptan in wild type but not in AhR-knockout,\nimmortalized human hepatocytes, implying that induction of CYP1A1 is AhR-dependent. Increased\nlevels of CYP1A1 mRNA by Avitriptan were observed in human colon carcinoma cells LS180 but\nnot in primary cultures of human hepatocytes. Collectively, we show that Avitriptan is a weak\nligand and activator of human AhR, which induces the expression of CYP1A1 in a cell-type specific\nmanner. Our data warrant the potential off-label therapeutic application of Avitriptan as an\nAhR-agonist drug....
Acute T lymphocytic leukemia (T-ALL) is an aggressive hematologic resulting from the malignant transformation of T-cell\nprogenitors. Drug resistance and relapse are major difficulties in the treatment of T-ALL. Here, we report the antitumor potency of\nNL-101, a compound that combines the nitrogen mustard group of bendamustine with the hydroxamic acid group of vorinostat.\nWe found NL-101 exhibited efficient antiproliferative activity in T-ALL cell lines (IC50 1.59â??1.89..................
Recently, we identified the promising anticancer potential of the synthetic\n4-thiazolidinone-based anticancer lead compound Les-3833 which demonstrated tumor-suppressing\naction in vitro and in vivo. Based on the results of previous studies, the aim of this research was\nto investigate the cytotoxicity in vitro and the biodistribution in laboratory mice to support the\nbiotherapeutic drug development of Les-3833. Les-3833 (2.5 mg/kg) was intravenously injected into\nmale Balb/c mice. Measurements were performed at 5 min, 15 min, 1 h, 4 h, and 24 h time points\nin blood plasma, brain, liver, and kidney using high-performance liquid chromatography/tandem\nmass spectrometry. After the administration of Les-3833, the maximum level of this compound\nwas observed in plasma at 2.08 min. In the brain, the mean maximum concentration of Les-3833\nwas 7.17 ng/mL at 5 min, while after 15 min, it was not found. In the liver, at 5 min, the maximum\nconcentration was 1190 ng/g. At 15 min, concentration of Les-3833 in the liver decreased by 14.3%;\nat 6 h by 22.8%; and after 24 h by 64.7%. Its maximum concentration in kidney was 404 ng/g within\n5â??15 min, at 1 h it decreased by 36.1%, and after 24 h by 49.3%. Thus, Les-3833 was rapidly taken\nup by different organs from the bloodstream, partially metabolized in the liver, and excreted mainly\nthrough the kidneys, while in the brain, a very low concentration could be observed for only a short\nperiod of time....
Ischemia/reperfusion (I/R) injury induces an inflammatory response and production of reactive oxygen species (ROS), which affects the organs remote to the sites of I/R. Renal injury associated with liver disease is a common clinical problem which leads to morbidity and mortality in patients with acute renal failure. This study aimed to assess the hepatic changes during various periods of reperfusion after renal I/R injury. Forty male rats were subjected to either sham operation or to 45-minute ischemia followed by 2, 4 and 24 hours of reperfusion. Liver function (ALT/AST) were found to be significantly increased after 45 min ischemia followed by 2, 4 and 24 hours of reperfusion but, the increase in the 4 and 24 hours groups was much higher than that in the 2h reperfusion group. Hepatic MDA was significantly increased after all three periods of reperfusion. Also, hepatic TAC was significantly decreased, as compared with the sham group; the highest change in hepatic MDA and TAC content was observed at 24 hours reperfusion after 45 min of renal ischemia than other reperfusion groups. Finally, hepatic histopathological examinations have confirmed the biochemical results, the severity of hepatic injury after 24 hours reperfusion was higher than other reperfusion groups. Renal I/R injury was associated with hepatic damage at various reperfusion periods but the severity of liver injury at 24 hours reperfusion was higher as compared with the other reperfusion groups....
The process of fracture healing consists of an inflammatory reaction and cartilage and bone\ntissue reconstruction. The inflammatory cytokine interleukin-1Beta (IL-1beta) signal is an important major\nfactor in fracture healing, whereas its relevance to retinoid receptor (an RAR inverse agonist, which\npromotes endochondral bone formation) remains unclear. Herein, we investigated the expressions of......................
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