An eco-friendly catalytic system for multicomponent, one-pot synthesis of novel spiro-chromeno indoline-triones and their anti-prostate cancer potentials evaluated via alkaline phosphatase inhibition mechanism.

A green and efficient straightforward tactic for the one-pot regioselective synthesis of novel 10,10-dimethyl-9,10,11,11a-tetrahydro-6H-spiro[chromeno[4,3-b]chromene-7,3'-indoline]-2',6,8 (7aH) -triones (4a-n) in one-pot modus has been established using eco-friendly p-toluenesulphonic acid as catalyst. Among the solvents that were used for synthesis, 4a-n were suitably synthesized with maximum yield (90-98%) in water. We avoided column purification and the formed by-product in the process is environmental-friendly. Hence, this reaction may consider as an astonishing piece work in this study, why because, the reaction mechanism that depends on the nature of the group attached to the isatin ring nitrogen atom. The main advantage of this protocol includes short reaction time, good yield, easy to work-up, practical simplicity, high regioselectivity and reduced pollutant, cost and avoids tedious purification. These pharmaceutically important compounds (4a-n) were recognized for their alkaline phosphatase inhibition and prostate cancer medication capabilities. The selective activity relation between alkaline phosphatase and prostate cancer was unveiled through the interaction of 4a-n to Human alkaline phosphatase (PDB ID: 1EW2).

Nanoparticulated polymeric composites enfolding lithium carbonate as brain drug in persuading depression: an in vivo study.

Lithium carbonate is considered an effective drug against mania and acts as a mood stabilizer. It is found that it enhances antidepressants targeting depression, consequently it is prone to have risk factors that leads to adverse effects. The study is devised in confronting depression under nanoscale by preparing nanocomposites which is a matrix of biopolymer chitosan that encapsulates lithium carbonate by ionic gelation method. This facilitates the drug delivery in a regulated manner targeting the therapeutic action with a limited dosage that lessens the side effects in the course of treatment. The drug polymer interaction was validated by XRD studies, whereas the morphology and size characterization by SEM and zetasizer. The average particle size was determined as 193 ± 0.18 nm with a positive zeta potential of 37.9 mV. The in vitro drug release patterns of nanocomposites were comparatively assayed with the standard lithium carbonate which rendered a controlled release in its profile. The in vivo investigation by animal despair studies bestowed a significant difference in the duration of immobility during force swimming and tail suspension tests. These results were substantiated with histopathological examinations of cerebral cortex region which showed mild cellular edema, degenerative changes and lymphocytic infiltration when compared with the control groups. Consequently, the efficacy of nanocomposites encased with lithium carbonate fortifies targeted drug delivery and restrains adverse effects by endorsing it as a lead compound in brain drug developmental research.

Bioactive M(II) complexes of amino acid-based N3O donor mixed ligand: in vitro and in silico DNA binding studies.

Three novel mixed ligand M(II) complexes, namely [CoL1L2Cl2] (1), [CuL1L2Cl2] (2), and [ZnL1L2Cl2] (3), were synthesized using 1,4-naphthoquinone, L-histidine, and 1,10-phenanthroline as ligands. The ligand framework and the corresponding structural changes on complexation were ascertained based on the results of elemental analysis, conductivity measurements, magnetic behavior, FT-IR, UV-visible, 1H NMR, 13C NMR, ESR spectral studies, and ESI mass spectrometry. The biological action of the ligand (L) and complexes 1-3 such as DNA binding and cleaving ability were studied. Results suggest that the ligand and the complexes could interact with calf thymus-DNA (CT-DNA) via intercalation mode. Additionally, complex 2 displayed potential antioxidant activity in in vitro studies. Docking simulation was performed to position the ligand and the complexes into the active site of BDNA (IBNA) to determine the probable binding mode.

Synthesis and multi-spectroscopic study on DNA-binding, cleavage and biological properties of M(II) complexes based on N2 O2 donor Schiff base ligand.

A novel Schiff base, (S,Z)-4-(methylthio)-2-((3-oxo-2,3-dihydro-1H-inden-1-ylidene)amino)butanoic acid (L) and four M(II) complexes (where M = Co, Cu, Ni and Zn) were synthesized and characterized. The DNA-binding characteristics of the complexes were investigated using various spectroscopic methods and viscosity measurements. Analysis of the results suggests that all the complexes bind to calf thymus DNA via intercalation. Among the four, Cu(II) complex was found to promote the photocleavage of plasmid DNA pBR322 under irradiation at 365 nm. These complexes also exhibit good antioxidant activities against 2,2-diphenyl-1-picrylhydrazyl radical. In vitro antibacterial and antifungal assay indicates that these complexes are good antimicrobial agents.

Novel Bioactive Co(II), Cu(II), Ni(II) and Zn(II) Complexes with Schiff Base Ligand Derived from Histidine and 1,3-Indandione: Synthesis, Structural Elucidation, Biological Investigation and Docking Analysis.

Novel bioactive complexes of Co(II), Cu(II), Ni(II) and Zn(II) metal ions with Schiff base ligand derived from histidine and 1,3-indandione were synthesized and thoroughly characterized by various analytical and spectral techniques. The biological investigations were carried out to examine the efficiency of the binding interaction of all the complexes with calf thymus DNA (CT-DNA). The binding properties were studied and evaluated quantitatively by Kb and Ksq values using UV-visible, fluorescence spectroscopy and voltammetric techniques. The experimental results revealed that the mode of binding of all the complexes with CT-DNA is via intercalation. It is further verified by viscosity measurements and thermal denaturation experiments. From the results of the cleavage study with pUC19 DNA it is inferred that all the complexes possess excellent cleaving ability. The present investigation proved that the binding interaction of all the complexes are significantly strong and the order of binding strength of the complexes is [Ni(L)2] (Kb = 3.11 × 106 M-1) > [Co(L)2] (Kb = 2.89 × 106 M-1) > [Cu(L)2] (Kb = 2.64 × 106 M-1) > [Zn(L)2] (Kb = 2.41 × 105 M-1). The complexes were also screened for antibacterial and anticandidal activity. The in vitro cytotoxicity of the ligand and complexes on the NIH/3 T3 mouse fibroblast cell lines were examined using CellTiter-Blue® (CTB) Cell viability assay, which unveiled that all the complexes exhibit more potent activities against NIH/3 T3 cells. Among all the complexes [Zn(L)2] complex showed the maximum efficiency.

Influence of Amino Acid-Nucleobase Hybrid Ligand in Binding and Biological Activity of Co(II) and Zn(II) Complexes.

Synthesis of new metallic complex of cobalt and zinc with amino acid-nucleobase hybrid ligand have been achieved by simple chemical reaction of metal salt with amino acid L-histidine and nucleobase adenine as ligands. Various physicochemical techniques such as elemental analysis, conductometric measurements, FT-IR, UV-visible, (1)H & (13)C NMR, mass spectroscopy and magnetic measurements were employed to characterize the complexes. The results confirmed the formation of the ligand and the complex. The interaction of the complex with calf thymus DNA (CT-DNA) has been carried out using UV-visible titration, fluorescence spectroscopy, cyclic voltammetry and viscosity measurements. The intrinsic binding constant (Kb) and Stern-Volmer constant (Ksv) of the complexes have been calculated. The cleavage activity of the ligand and the complexes with pBR322 DNA was further confirmed by gel electrophoretic technique. The pharmacological activity of the ligand and the complexes was investigated by antioxidant, antimicrobial and cytotoxic activity, and they show promising pharmacological effect. The results of the molecular docking studies of the ligand and the complexes reinforce all the above facts.