Recombinant HIV-2 Tat Protein (EHO)

The novel coronavirus (nCoV) has emerged as a severe public health threat globally in the 21st century. Several therapies were reported towards identifying ligand against coronavirus, including targeting specific functional proteins or enzymes that are crucial to viruses, thereby preventing the synthesis and replication of virus RNA. Our study is mainly focused on targeting the virus's structural proteins, which could further block the binding of the virus to human cell receptors. In our study, we have selected nine Flavonoids for the inhibition of COVID-19 Spike protein, which have already been reported with their antiviral efficacies against other virus-infected diseases. AutoDock and PatchDock were used to study the inhibitory potential of flavonoids against COVID-19. Amongst all the eleven screened compounds, baicalin has depicted the highest binding affinity against 2019-nCoV spike glycoprotein. Additionally, we have also compared its potential with two standard HIV drugs Abacavir and hydroxychloroquine, and the docking results clearly revealed the better inhibitory potential of baicalin in comparison to recently used drug Abacavir and hydroxychloroquine for the treatment of COVID-19. Therefore our experimental findings strongly suggested that baicalin can be used as a potential inhibitor against COVID-19 spike protein, which could inhibit the interaction of the virus with the host cell and thus could provide a potential lead molecule for the development of a drug against COVID-19 disease.

New conjugated derivative of pteridine and benzimidazole, 7-(benzimidazol-2-yl)-6-(2,4-dichlorophenyl)-2-thioxo-2,3-dihydropteridin-4(1H)-one (BP) possessing antitumor activity was obtained and thoroughly characterized; its spectrophotometry control in solution was developed. To improve the solubility of the hydrophobic antitumor agent BP in aqueous solutions, amphiphilic systems (micellar solutions and modified liposomes) were fabricated, with their composition optimized. Stable 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC)-based liposomes modified with cationic surfactants, namely cetyltrimetylammonium bromide and 1-methyl-3-hexadecylimidazolium bromide (IA-16), were obtained. It was shown that the use of cationic surfactants for the formation of hybrid drug carriers and varying of the surfactant/lipid molar ratios can be the key factor for obtaining the optimized particles with high efficiency of encapsulation, favorable loading efficacy and prolonged release of the drug. The most beneficial parameters in terms of stability and loading/release efficacy were obtained for IA-16/DPPC hybrid liposomes with the surfactant/lipid molar ratio of 1:50. Free BP demonstrated cytotoxicity toward M-Hela tumor cells, along with the nearly the same toxic effect toward normal Chang liver cells. Importantly, double effect occurred upon the encapsulation of BP into hybrid cationic liposomes, i.e. a sharp decrease in viability of diseased cells and increase of viability of normal cells. Therefore, liposomal BP formulation can be recommended as therapeutics with improved stability and high selective cytotoxicity toward M-Hela tumor cells at the level of commercial drug doxorubicin, in combination with much less toxicity (by 37 times) toward the normal Chang liver cell line. (C) 2020 Published by Elsevier B.V.