Synthesis,Spectroscopy, Semi‐empirical and Biological Activities of Organotin(IV) Complexes with o‐Isopropyl Carbonodithioic Acid

New organotin(IV) complexes have been synthesized by treating potassium o‐isopropyl carbonodithioate with R₂SnCl₂/R₃SnCl in 1 : 2/1 : 1 M/L ratio. All complexes have been characterized by IR and NMR (¹H, ¹³C) spectroscopy. IR results shows that ligand acts as bidentate which is also confirmed by semi‐empirical study. NMR data reveals four coordinated geometry in solution. Computed positive heat of formation shows that complex 5 is thermodynamically unstable. UV/visible spectroscopy was used to assess the mode of interaction and binding of the complexes with DNA which shows that complex 5 exhibits higher binding constant as compared to complex 3 . In protein kinase inhibition assay, compound 3 was found most active, while other biological activities shows that triorganotin(IV) complexes are biologically more active as compared to diorganotin(IV) complexes.     

Diorganotin(IV) Complexes with Monohydrate Disodium Salt of Iminodiacetic Acid: Synthesis,Characterization, Crystal Structure and Biological Activities

Diorganotin(IV) derivatives have been synthesized by the reaction of R₂SnL₂ (R=n‐Bu 1 , Ph 2 ) with monohydrate disodium salt of iminodiacetic acid ( Na₂L ) in 1 : 1 M/L ratio under reflux conditions. The compounds have been characterized by FT‐IR, NMR (¹H and ¹³C) spectoscopy, electron ionization mass spectrometry (EIMS), thermogravimetric analyses (TGA) and single crystal XRD. FTIR data indicates a mono‐dentate binding mode of the carboxylic acid group as well as participation of the amino nitrogen and aqua oxygen in coordination with organotin(IV) moieties. NMR data demonstrates a tetra‐coordinated environment around tin(IV) in solution. Mass spectrometric and thermogravimetric analyses verify the close similarities between the molecular structures of both complexes. The thermal stability of diphenyltin(IV) derivative ( 2 ) was found slightly higher than that of the free ligand ( Na₂L ). Single crystal X‐ray analysis of the complex 1 have shown a hexa‐coordinated geometry around Sn(IV) with trans configuration. There are evidences for the existence of intermolecular hydrogen bonding in the structure of the complexes. The products displayed significant antibacterial and antifungal activities in contrast to the biologically inactive ligand precursor. However, the hemolytic cytoxicity of the complexes was comparatively high than the free ligand.     

Polymeric emulsion and crosslink-mediated synthesis of super-stable nanoparticles as sustained-release anti-tuberculosis drug carriers

This study focused on evaluating four emulsion-based processing strategies for polymeric nanoparticle synthesis to explicate the mechanisms of nanoparticle formation and the influence on achieving sustained-release of two anti-tuberculosis drugs, isoniazid and rifampicin. Poly(lactic-co-glycolic acid) (PLGA) nanoparticles were formulated with and without sorbitan mono-oleate as a stabilizer using emulsion-solvent-surfactant-evaporation (ESSE) and emulsion-solvent-evaporation (ESE) approaches. An alginate solution gelled by ionic crosslinking with calcium chloride was employed to prepare alginate hydrogel nanoparticles via reverse-emulsion-cationic-gelification (RECG) and reverse-emulsion-surfactant-cationic-gelification (RESCG) approaches. In vitro drug release analysis was performed. The size, zeta potential and morphology of the nanoparticles were analyzed. Molecular mechanics energy relationships (MMER) were employed to explore the spatial disposition of alginate and PLGA with respect to the emulsifying profile of sorbitan monooleate and to corroborate the experimental findings. Results revealed that particle size of the PLGA nanoparticles was influenced by the stabilizer concentration. Nanoparticles synthesized by the ESSE approach had smaller sizes of 240±8.7 nm and 195.5±5.4 nm for rifampicin- and isoniazid-loaded nanoparticles, respectively. This was a substantial size reduction from nanoparticles generated by the ESE approach (>1000 nm). The RESCG approach produced stable and higher nanoparticle yields with desirable size (277±1.0 nm; 289±1.2 nm), a low polydispersity index (27.1±0.3 mV; 28.5±0.5 mV) and drug entrapment efficiency of 73% and 75% for isoniazid and rifampicin, respectively. Drug release from the ESSE and RESCG synthesized nanoparticles displayed desirable release of the two anti-TB drugs with sustained zero-order kinetics over a period of 8h. MMER supported the mechanisms of nanoparticle formation with a sphericalized interlaced network configuration.     

Hyaluronan: from biomimetic to industrial business strategy

Hyaluronan (hyaluronic acid) is a naturally occurring polysaccharide of a linear repeating disaccharide unit consisting of beta-(1-->4)-linked D-glucopyranuronic acid and beta-(1-->3)-linked 2-acetamido-2-deoxy-D-glucopyranose, which is present in extracellular matrices, the synovial fluid of joints, and scaffolding that comprises cartilage. In its mechanism of synthesis, its size, and its physico-chemical properties, hyaluronan is unique amongst other glycosaminoglycans. The network-forming, viscoelastic and its charge characteristics are important to many biochemical properties of living tissues. It is an important pericellular and cell surface constituent; its interaction with other macromolecules such as proteins, participates in regulating cell behavior during numerous morphogenic, restorative, and pathological processes in the body. The knowledge of HA in diseases such as various forms of cancers, arthritis and osteoporosis has led to new impetus in research and development in the preparation of biomaterials for surgical implants and drug conjugates for targeted delivery. A concise and focused review on hyaluronan is timely. This review will cover the following important aspects of hyaluronan: (i) biological functions and synthesis in nature; (ii) current industrial production and potential biosynthetic processes of hyaluronan; (iii) chemical modifications of hyaluronan leading to products of commercial significance; and (iv) and the global market position and manufacturers of hyaluronan.     

Bacterial Lux-Fluoro test for biological assessment of pollutants in water samples from urban and rural origin

During the 20th century, population growth and urbanization, together with changes in production and consumption, have placed unprecedented demands on the quality of water. The ongoing extraordinary economic growth, industrialization, and urbanization of many developing countries results in widespread water pollution from agricultural, industrial, and domestic sources. In consequence, people consume contaminated drinking water, thereby increasing the risk of exposure not only to infectious and parasitic disease but also to a growing volume of genotoxic and cytotoxic chemicals. In light of these trends, new, rapid and low-cost approaches are urgently needed to assess the quality of water supplies. Because of their simplicity and sensitivity, bacterial tests play an important role in the detection and screening of genotoxins or cytotoxins in water. Thus, the bacterial Lux-Fluoro test, which is a combination of two bioassays that simultaneously measure the genotoxicity (SOS-Lux test) and the cytotoxicity (LAC-Fluoro test), was used to identify polluted water from samples of rural and urban sources, collected from 10 different locations in the Punjab rivers’ basin. We identified at least three samples from rural origin having a high cytotoxic potential. The highest toxicity was found for the sample obtained from a draining canal collecting runoff water from the fields. The two other highly contaminated samples identified were taken from two ponds of different villages. The water samples obtained from the Ravi river and from the water tap in a suburb of the megacity Lahore showed no sign of genotoxicity or cytotoxicity. Seven control samples with differing genotoxic and cytotoxic potency were shown for comparison.     

Crystallographic report: Chlorodimethyltin(IV) piperidine‐1‐carbodithioate

Me₂Sn(S₂CN(CH₂)₅)Cl contains five‐coordinated tin with a bidentate dithiocarbamate ligand spanning equatorial and axial positions in a distorted trigonal bipyramidal geometry. Copyright © 2005 John Wiley & Sons, Ltd.     

A shape preserving area true approximation of histogram by rational splines

For a given histogram, we consider an application of a simple rational spline to a shape preserving area true approximation of the histogram. An algorithm for determination of the spline is as easy as one with a quadratic polynomial spline, while the latter does not always preserve the shape of the histogram. Some numerical examples are given at the end of the paper.     

The synthesis and ultraviolet spectra of some N-aryl-2,3-dihydro-3-oxo-4H-1,4-oxazine derivatives

Two new derivatives of the 1,4-oxazine ring system ( 3a and 3b ) derived from p-aminobenz-amides have been synthesized. The uv absorption spectra of sixteen representative 1,4-oxazines all show two high intensity bands (? ～ 10⁵) between 220-400 ran. The positions and intensities of the absorption maxima have been correlated with the steric and electronic effects of the oxazine ring substituents.     

Lipoxygenase inhibiting constituents from Indigofera hetrantha

A lignan and two acylphloroglucinols have been isolated from the ethyl acetate soluble fraction of the whole plant of Indigofera hetrantha. Their structures have been assigned on the basis of spectral analysis including 1D and 2D NMR techniques. Compounds 1-3 displayed promising inhibitory potential against enzyme lipoxygenase in concentration-dependent manner.