Process and purification for manufacture of a modified insulin intended for oral delivery

Oral delivery of insulin is convenient and physiologically desirable in the treatment of diabetes. However, this route of administration has presented substantial challenges as insulin is degraded enzymatically in the gut, resulting in low bioavailability. We have developed a conjugated insulin product (IN-105) that has high bioavailability and is currently undergoing clinical trials for the treatment of diabetes. A process for the manufacture of IN-105 was developed. Initially, recombinant human insulin was conjugated covalently with a monodisperse, short-chain methoxypolyethylene glycol derivative. The desired product, IN-105, was purified from its closely related species using RP-HPLC and cation exchange chromatography to a purity of 98.5%. The elution pool from cation exchange chromatography was crystallized and lyophilized into the dry active pharmaceutical ingredient.     

A difference-equation formalism for the nodal domains of separable billiards

Recently, the nodal domain counts of planar, integrable billiards with Dirichlet boundary conditions were shown to satisfy certain difference equations in Samajdar and Jain (2014). The exact solutions of these equations give the number of domains explicitly. For complete generality, we demonstrate this novel formulation for three additional separable systems and thus extend the statement to all integrable billiards.     

Guanidine catalyzed aerobic reduction: a selective aerobic hydrogenation of olefins using aqueous hydrazine

An efficient aerobic reduction of olefins, internal as well as terminal, is developed using guanidine as an organocatalyst. A remarkable chemoselectivity in reduction has been demonstrated in the presence of a variety of functional groups and protective groups and a selective reduction of a terminal olefin in the presence of an internal olefin is revealed.     

Microwave-assisted synthesis of water-soluble styrylpyridine dye-capped zinc oxide nanoparticles for antibacterial applications

ZnO nanoparticles were successfully synthesized using a microwave method, whose surface was modified with {4-[(E)-2-(furan-2-yl)ethenyl]pyridin-1-ium-1-yl}acetate as a capping agent (1 and 3%). Their structural properties were investigated using FTIR, XRD, SEM, EDS, and UV–visible spectroscopy. XRD confirmed the Wurtzite structure for all compounds, a size of 30.6 nm for uncapped and 22.9 nm for 3% dye-capped nanoparticles were calculated from Scherer's equation. Hexagonal wurtzite shape of nanoparticles can be clearly seen in the SEM images. The DFT calculations were carried out using quantum espresso. These dye-capped ZnO nanoparticles were proved to be potential antibacterial agents, the minimum concentrations of dye-capped ZnO nanoparticles that inhibit the growth of bacteria are 1.5 mg/mL for Escherichia coli and 0.78 mg/mL for Bacillus subtilis, which are much lower than those of uncapped ZnO. The bioactivity data suggest these organic–inorganic hybrid nanoparticles emerged as a new class of antibacterial agents.     

A convenient and mild one pot synthesis of cyclopentenone derivatives

Developed a convenient and mild one pot synthesis of cyclopentenone derivatives using 1-acetyl-1-cyclohexene and wide range of aldehydes. Aromatic and heterocyclic aldehydes with electron donating and withdrawing groups were conveniently converted to the corresponding cyclopentenone derivatives.     

Novel affinity chromatography method for the efficient purification of recombinant Binder of SPerm homolog proteins

In mammalian species, a family of proteins named the Binder of SPerm proteins, which are expressed in the male reproductive tract, have been shown to play a role in epididymal sperm maturation and sperm capacitation. Recently, one homolog from human and two homologs from mouse were characterized. In order to further investigate the biochemical activity of these proteins, efficient purification procedures are required to isolate the proteins. Since these proteins are produced in very minute quantities, we exploited the high capacity of Escherichia coli to produce larger quantities of recombinant proteins that were subsequently purified using affinity chromatography on a diethylaminoethyl‐Sephadex A‐25 column. Binder of SPerm proteins have been shown to interact with pseudo‐choline groups such as diethylaminoethyl through affinity rather than ionic interactions. The aim of the current study was to develop a novel method for purifying these recombinant proteins, produced in Escherichia coli cells. Diethylaminoethyl is positively charged and is a weak anion exchanger, but binder of sperm proteins interacts with affinity to this resin. This study presents a new, rapid, and cost‐effective purification method that provides with an exceptional purity level, which can be used to study their roles in mammalian fertilization.     

Synthesis of spiro[indolo-1,5-benzodiazepines] from 3-acetyl coumarins for use as possible antianxiety agents

3-Acetyl coumarins (1) when allowed react with isatin (2) gave corresponding 3-(3′-hydroxy-2′-oxo indolo) acetyl coumarins (3), which on dehydration afforded the correspondingα,β-unsaturated ketones (4). Cyclocondensation of (4) with substitutedo-phenylene diamines resulted in novel 3-coumarinyl spiro[indolo-1,5-benzodiazepines] (5). Structures of all the compounds have been established on the basis of their IR, NMR and mass spectral data and have been screened for their antimicrobial activity and antianxiety activity in mice     

Microwave-assisted rapid extracellular synthesis of stable bio-functionalized silver nanoparticles from guava (<Emphasis Type="Italic">Psidium guajava</Emphasis>) leaf extract

Our research interest centers on microwave-assisted rapid extracellular synthesis of bio-functionalized silver nanoparticles of 26 ± 5 nm from guava (Psidium guajava) leaf extract with control over dimension and composition. The reaction occurs very rapidly as the formation of spherical nanoparticles almost completed within 90 s. The probable pathway of the biosynthesis is suggested. Appearance, crystalline nature, size and shape of nanoparticles are understood by UV–vis (UV–vis spectroscopy), FTIR (fourier transform infrared spectroscopy), XRD (X-ray diffraction), FESEM (field emission scanning electron microscopy) and TEM (transmission electron microscopy) techniques. Microwave-assisted route is selected for the synthesis of silver nanoparticles to carry out the reaction fast, suppress the enzymatic action and to keep the process environmentally clean and green.     

Experimental Investigation into the Mechanical Behavior of Textile Composites with Various Fiber Reinforcement Architectures

Mechanics of Composite Materials - The role of fiber reinforcement architecture in adjusting the mechanical properties of glass-fiber-reinforced epoxy composite materials is studied. Fibrous...