Oxoperoxovanadium Complexes of Hetero Ligands: X-Ray Crystal Structure, Density Functional Theory, and Investigations on DNA/BSA Interactions, Cytotoxic, and Molecular Docking Studies.

Oxoperoxovanadium (V) complexes [VO (O)2 (nf) (bp)] (1) and [VO (O)2 (ox) (bp)] (2) based on 5-nitro-2-furoic acid (nf), oxine (ox) and 2, 2' bipyridine (bp) bidentate ligands have been synthesized and characterized by FT-IR, UV-visible, mass, and NMR spectroscopic techniques. The structure of complex 2 shows distorted pentagonal-bipyramidal geometry, as confirmed by a single-crystal XRD diffraction study. The interactions of complexes with bovine serum albumin (BSA) and calf thymus DNA (CT-DNA) are investigated using UV-visible and fluorescence spectroscopic techniques. It has been observed that CT-DNA interacts with complexes through groove binding mode and the binding constants for complexes 1 and 2 are 8.7 × 103 M-1 and 8.6 × 103 M-1, respectively, and BSA quenching constants for complexes 1 and 2 are 0.0628 × 106 M-1 and 0.0163 × 106 M-1, respectively. The ability of complexes to cleave DNA is investigated using the gel electrophoresis method with pBR322 plasmid DNA. Furthermore, the cytotoxic effect of the complexes is evaluated against the HeLa cell line using an MTT assay. The complexes are subjected to density functional theory calculations to gain insight into their molecular geometries and are in accordance with the results of docking studies. Furthermore, based on molecular docking studies, the intermolecular interactions responsible for the stronger binding affinities between metal complexes and DNA are discussed.

DNA Interaction and Cytotoxic studies on Mono/Di-Oxo and Peroxo- Vanadium (V) complexes - A Review.

Vanadium is considered to be biologically significant and several vanadium IV & V complexes have successfully been studied as chemotherapeutic agents like insulin mimetic, antibacterial, antioxidant, and anticancer activities. The divergent ligand systems also play a pivotal role in designing the metal complex with desired properties. Thus, the combination of both with their synergistic advantages results in a potential drug candidate. Different mechanistic pathways have been proposed to explain the antitumor effects of vanadium complexes, including induction of tyrosine residues phosphorylation, inhibition of key protein tyrosine phosphatases (PTPases), which in turn promote the activation of the extracellular regulated kinase cascading (ERK) pathway. In the current review, we have summarized the work on vanadium (V) complexes based on different ligand systems and their biological significance as an anticancer lead compound.

A Review on Oral Liquid as an Emerging Technology in Controlled Drug Delivery System.

BACKGROUND: The Oral Liquid Drug Delivery System (OLDDS) remains the primary choice of dosage form, though challenging, for the pharmaceutical scientists. In the last two decades, Oral Liquid Controlled Release (OLCR) formulation has gained a lot of attention because of its advantages over the conventional dosage forms. METHOD: The world of nanotechnology has paved multiple ways to administer the drug through oral cavity in liquid dosage form with an additional advantage of control over the release. In the current study, the various approaches towards the same have been discussed comprehensively to understand the different mechanisms of OLCR. CONCLUSION: This review also emphasizes on the existing techniques and the developments that have been made to improve on its efficacy including various formulation related factors. It also provides valuable insights into the role of polymers in the development of OLCR formulation that can be used in the management of Gastroesophageal Reflux Disease (GERD).

Spectroscopic investigations on partial intercalative binding behaviour of terpyridine based copper(II) complexes with DNA.

Copper based metal complexes have been studied extensively towards DNA interaction aspects, the possible interactions being at the major or minor grooves, intercalation between base pairs, etc. The nature of the ligand decides the binding mode of the complexes thereby exerting different biological significance. Based on this, we have synthesized two mixed ligand copper(II) complexes, [Cu(meFtpy)(bpy)](NO3)2.2(H2O) (1) and [Cu(meFtpy)(phen)](NO3)2.(H2O) (2) based on new furfuryl substituted tertiary pyridine ligand (meFtpy) and ancillary ligands (phen, bpy). They are characterized by UV Visible, FT-IR, (1)H &(13)C NMR and mass spectroscopic techniques. The structures of both the complexes are confirmed by single crystal XRD revealing triclinic crystal system showing penta coordination possessing distorted square pyramidal geometry. The binding ability of the complexes has been explored based on the results of DNA binding studies assessed by different spectroscopic techniques like UV absorption titration, fluorescence displacement assay and circular dicroism and found to show partial intercalative behaviour. The binding constant (Kb) values as obtained from UV absorption titration are found to be 1.29×10(4)M(-1) for 1 and 1.46×10(4)M(-1) for 2 and are compared with the values obtained for doxorubicin, a partial intercalator drug. The binding affinities obtained from absorption titration are found in the order as Kb(doxo)>Kb(2)>Kb(1)>Kb(meFtpy).

Development of polymer-bound fast-dissolving metformin buccal film with disintegrants.

Fast-dissolving drug-delivery systems are considered advantageous over the existing conventional oral dosage forms like tablets, capsules, and syrups for being patient friendly. Buccal films are one such system responsible for systemic drug delivery at the desired site of action by avoiding hepatic first-pass metabolism. Metformin hydrochloride (Met), an antidiabetic drug, has poor bioavailability due to its high solubility and low permeability. The purpose of the study reported here was to develop a polymer-bound fast-dissolving buccal film of metformin to exploit these unique properties. In the study, metformin fast-dissolving films were prepared by the solvent-casting method using chitosan, a bioadhesive polymer. Further, starch, sodium starch glycolate, and microcrystalline cellulose were the disintegrants added to different ratios, forming various formulations (F1 to F7). The buccal films were evaluated for various parameters like weight variation, thickness, folding endurance, surface pH, content uniformity, tensile strength, and percentage of elongation. The films were also subjected to in vitro dissolution study, and the disintegration time was found to be less than 30 minutes for all formulations, which was attributed to the effect of disintegrants. Formulation F6 showed 92.2% drug release within 6 minutes due to the combined effect of sodium starch glycolate and microcrystalline cellulose.

Exploration of DNA binding mode, chemical nuclease, cytotoxic and apoptotic potentials of diketone based oxovanadium(IV) complexes.

Two diketone based oxovanadium complexes, viz., bis(4,4,4-trifluoro-1-phenylbutane-1,3-dionato)oxovanadium(IV) (1) and bis(1,1,1-trifluoropentane-2,4-dionato)oxovanadium(IV) (2), have been synthesized and characterized by spectroscopic and analytical techniques. The DNA binding and the cleaving ability of the complexes is assessed by UV-vis spectroscopy, fluorescence spectroscopy, viscometry and gel electrophoretic studies. The DNA binding constant values (Kb) are found to be 1.95 ± 0.16 × 10(3)M(-1) for complex 1 and 1.064 ± 0.17 × 10(3)M(-1) for complex 2, respectively. Based on the results of the spectral and viscosity studies, it is observed that the complexes, interestingly, have preferred minor groove binding with DNA. Further, the concentration-dependent oxidative cleavage pattern of pBR322 in the presence of the activating reagent, hydrogen peroxide, has also been discussed. In addition, the complexes have shown moderate cytotoxic activity by inducing apoptosis against the cervical cancer cell line, HeLa. The results of in silico analysis and logP predictions are found to be in good agreement with the experimental observations. Thus, synthesized oxovanadium complexes have displayed promising DNA binding behavior and DNA cleavage activity with moderately cytotoxic nature.