Analysis of Protein Target Interactions of Synthetic Mixtures by Affinity-LC/MS.

Analysis of interactions between molecules is of fundamental importance in life science research. In this study, we applied weak affinity chromatography, based on high-performance liquid chromatography and mass spectrometry, as a powerful tool for direct analysis of the components of a chemical reaction mixture for their binding to a target protein. As a demonstration of the potential of this method, we analyzed the binding of the compounds of the reaction mixture to the chaperone heat shock protein 90 (Hsp90). It was possible to analyze quantitatively the binding of the components of the mixture to the target independently from each other without any preceding process such as purification. This feature has wide implications in biological sciences as crude mixtures, either natural or synthetic, can be analyzed directly for their possible binding to a target. This method could lead to savings in costs and labor through shortening chemical research project development time.

Electrosprayed nanoparticles and electrospun nanofibers based on natural materials: applications in tissue regeneration, drug delivery and pharmaceuticals.

Nanotechnology refers to the fabrication, characterization, and application of substances in nanometer scale dimensions for various ends. The influence of nanotechnology on the healthcare industry is substantial, particularly in the areas of disease diagnosis and treatment. Recent investigations in nanotechnology for drug delivery and tissue engineering have delivered high-impact contributions in translational research, with associated pharmaceutical products and applications. Over the past decade, the synthesis of nanofibers or nanoparticles via electrostatic spinning or spraying, respectively, has emerged as an important nanostructuring methodology. This is due to both the versatility of the electrospinning/electrospraying process and the ensuing control of nanofiber/nanoparticle surface parameters. Electrosprayed nanoparticles and electrospun nanofibers are both employed as natural or synthetic carriers for the delivery of entrapped drugs, growth factors, health supplements, vitamins, and so on. The role of nanofiber/nanoparticle carriers is substantiated by the programmed, tailored, or targeted release of their contents in the guise of tissue engineering scaffolds or medical devices for drug delivery. This review focuses on the nanoformulation of natural materials via the electrospraying or electrospinning of nanoparticles or nanofibers for tissue engineering or drug delivery/pharmaceutical purposes. Here, we classify the natural materials with respect to their animal/plant origin and macrocyclic, small molecule or herbal active constituents, and further categorize the materials according to their proteinaceous or saccharide nature.

Curcumin- and natural extract-loaded nanofibres for potential treatment of lung and breast cancer: in vitro efficacy evaluation.

Drug-eluting medical implants are more common, particularly for fighting against cancers. FDA and other drug regulatory bodies have approved many nanoformulated devices eluting active pharmaceutical ingredients and thus there is growing demand for further value- added devices. Nanofibre membranes are known for its versatility of drug incorporation and sustained drug release. We intend to fabricate natural ingredient or extract, and their combination loaded polycaprolactone (PCL) nanofibre for usage as drug-eluting stents or implants for anticancer activity against lung and breast cancers. The fabricated nanofibre membranes were characterised by scanning electron microscope for morphology, FT-IR for chemical nature and tensile testing for mechanical strengths. Release of curcumin was studied with time to find the applicability of the device as drug-eluting implant. The activity of the nanofibre membranes was tested against human breast cancer (MCF7) and lung cancer (A459) cell lines in vitro. In both the cell lines tested, 1% aloe vera and 5% curcumin-loaded PCL nanofibre exhibited 15% more cytotoxicity in comparison with the commercial drug 1% cis-Platin-loaded PCL nanofibre after 24 h incubation.

Cross-linking of protein scaffolds for therapeutic applications: PCL nanofibers delivering riboflavin for protein cross-linking.

Nanofibers play a significant role in tissue engineering and drug delivery because of the ease with which drugs or pharmaceuticals may be incorporated into the nano-formulation. Natural protein nanofibers are cross-linked (CXLed) employing a new protocol to improve their stability for perspective usage as tissue engineering or drug delivery scaffolds. The protocol utilizes a non-toxic, natural material vitamin based CXL protocol that works well for stabilizing protein nanofibers. We have tested the generation of reactive oxygen species (ROS) from UV treated riboflavin-gelatin microfibers, film or solution that helps in gelatin (Gel) CXLing and results in improved mechanical properties. Further natural proteins Gel and fibrinogen (Fib) solutions were also CXLed using vitamin B2 (riboflavin (Rib)) released from Rib-loaded polycaprolactone (PCL) nanofibers followed by UV treatment. The sustained release of Rib from PCL nanofibers is studied with in vitro drug release experiments and in vitro hydrogel formation upon treatment with the natural protein solutions. Rib-loaded nanofibers were characterized with SEM and AFM for morphology, mechanical strength calculation and FT-IR for ensuring drug incorporation. The Rib encapsulation in the nanofiber reservoirs enables the sustained release, and the ROS generating nanofibers could find application as a patch for CXLing any protein fiber or fibrous tissue, such as ocular, skin or cardiac tissue engineering.

Vitamin B12 loaded polycaprolactone nanofibers: a novel transdermal route for the water soluble energy supplement delivery.

Biocompatible PCL polymer nanofiber mediated sustained release of hydrophilic drug and applicability as transdermal delivery system is attempted. This new attempt to investigate water soluble vitamin delivery with hydrophobic polymer nanofiber sustained the release of the vitamin and the method is suited for the transdermal patch applications. The drug loaded fibers were characterized with SEM for morphology, porometer for pore size measurements, mechanical strength calculation and FT-IR for drug load characterization. The contact angle measurement showed surface wettability and controlled release of drug was quantified with UV absorption measurements. To further enhance the release of vitamin, the polymer fiber was plasma treated at different time intervals and made hydrophilic gradually. Since the increased surface area and drug encapsulation in nano-reservoirs can able to release drug in small quantities and in a sustained manner we attempted the release of the energy supplement with nanofibrous delivery mode.

Ammonium Trifluoroacetate-Mediated Synthesis of 3,4-dihydropyrimidin-2(1H)-ones.

A simple and economic synthesis of 3,4-dihydropyrimidin-2(1H)-ones using ammonium trifluoroacetate as catalyst and as solid support is accomplished. Easy workup procedure for the synthesis of title compounds is well arrived at and is well documented.