Retraction Note to: Silibinin ameliorates arsenic induced nephrotoxicity by abrogation of oxidative stress,inflammation and apoptosis in rats

Molecular Biology Reports -     

Cellular Uptake and In Vitro Drug Release Studies on Paclitaxel-Loaded Poly(caprolactone)-Grafted Dextran Copolymeric Nanoparticles

Biodegradable and biocompatible polymers play a key role to provide a solution for sustained chemotherapy, when engineered to nanostructure. One such effort has been put forward to engineer self-assembled poly(caprolactone)-grafted dextran (PGD) core–shell micellar vehicle for anticancer drug (paclitaxel) and presented in this study. Paclitaxel-loaded PGD nanoparticles (NPs) were prepared by a modified oil/water emulsion method and characterized by laser light scattering, atomic force microscopy, and zeta potential measurements. The effects of the copolymeric compositions of PGD NPs on drug encapsulation efficiency, in vitro drug release, cellular uptake, and cell viability of NP formulation with paclitaxel were investigated. The drug encapsulation efficiency was determined spectrophotometrically, and in vitro drug release was estimated using dialysis bag. Human gastric cancer cell line (SNU-638) were used to image and measure the cellular uptake of fluorescent PGD NPs. Cancer cell viability of the drug-loaded PGD NPs was measured by crystal violet staining method. From the results obtained on various aspects, we inferred that the above formulated drug-loaded PGD NPs have significant drug encapsulation efficiency, cellular uptake, and the cancer cell mortality.     

Microwave-assisted synthesis,molecular docking and antitubercular activity of 1,2,3,4-tetrahydropyrimidine-5-carbonitrile derivatives

Based on bioisosteric similarities with isoniazid, a series of 1,2,3,4-tetrahydropyrimidine-5-carbonitrile derivatives has been designed. The target compounds have been synthesized by multicomponent reaction which involves one-pot organic reactions using ethylcyanoacetate, urea/thiourea and arylaldehydes in presence of ethanolic K₂CO₃. Two methodologies, conventional and microwave-assisted, have been adopted for the synthesis. The later strategy gave high yields in less than 10 min as compared to long hours using the former approach. Molecular docking of the target compounds into the enzyme Mycobacterium tuberculosis enoyl reductase (InhA) revealed important structural information on the plausible binding interactions. Major binding interactions were found to be of dispersion type (residues Tyr158, Ile215, Met103 and Met199) and a hydrogen bond with Tyr158. Binding poses of the all the compounds were energetically favorable and showed good interactions with the active site residues. Few selected compounds were also evaluated for antitubercular activity in vitro against drug-sensitive M. tuberculosis H37Rv strain and clinically isolated S, H, R and E resistant M. tuberculosis by luciferase reporter phage (LRP) assay method. Some compounds displayed promising antimycobacterial activity comparable or less than the standard drugs isoniazid and rifampicin.