Trace element transfer from alginate dressings to wounds

ABSTRACT

A method has been developed for impregnating alginate-based wound dressings with trace elements required for wound healing and for quantifying the transfer from these dressing to wound fluid (for which a substitute—blood serum—was used in these experiments). Under ideal conditions, up to 85% can be carried across from the tow to the wound fluid.     

Chemical speciation in wound fluid leading to enhanced bioavailability for healing

ABSTRACT

ECCLES computer modelling is used to speciate Ca²⁺, Zn²⁺, Cu²⁺, Mn²⁺ and Fe³⁺ in wound fluid samples analysed for total metal content using Potentiometric stripping analysis. Bioavailability of metals, related to lipid soluble net-neutral complexes, was assessed and found to be broadly similar to the speciation in blood plasma. These appear to be benefits worthy of clinical investigation of keeping the wound fluid at pH = 6.4 and of raising the total cysteine concentration levels in wound fluid.     

Synthesis and applications of cyclopeptides and depsipeptides

Summary A solid phase protocol has been devised for the synthesis of linear precursors to cyclic depsipeptide analogues of dolastatin D.t-Butyldimethylsilyl groups were used for hydroxy group protection, with deprotection being carried out byt-butyl ammonium fluoride. HATU and PyBrop were successful in coupling highly hindered residues and in depside bond formation. Cyclic peptide analogues, cyclo[Arg-Gly-Asp-d-Phe-Lys(or Tyr)] have been synthesised and modified for use as carrier molecules for the transport of radio isotopes (¹¹¹In and¹²⁵I) into blood platelets as prototypes for medical imaging.     

Discovery and SAR of potent,orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors

We have designed and synthesized a novel series of 2,8-diaryl-quinoxalines as Janus kinase 2 inhibitors. Many of the inhibitors show low nanomolar activity against JAK2 and potently suppress proliferation of SET-2 cells in vitro. In addition, compounds from this series have favorable rat pharmacokinetic properties suitable for in vivo efficacy evaluation.     

Synthesis and applications of cyclopeptides and depsipeptides

A solid phase protocol has been devised for the synthesis of linearprecursors to cyclic depsipeptide analogues of dolastatin D.t-Butyldimethylsilyl groups were used for hydroxy group protection, withdeprotection being carried out by t-butyl ammonium fluoride. HATU and PyBropwere successful in coupling highly hindered residues and in depside bondformation. Cyclic peptide analogues, cyclo[Arg-Gly-Asp-d-Phe-Lys(or Tyr)]have been synthesised and modified for use as carrier molecules for thetransport of radio isotopes (¹¹¹In and ¹²⁵I)into blood platelets as prototypes for medical imaging.     

The Effect of pH and NaCl Levels on the Physicochemical and Emulsifying Properties of a Cruciferin Protein Isolate

The influence of pH (3.0, 5.0, and 7.0) and ionic strength (0, 50, 100 mM NaCl) on the physicochemical and emulsifying properties of a cruciferin-rich protein isolate (CPI) was investigated. Surface charge on the CPI was found to substantially reduced in the presence of NaCl. Surface hydrophobicity was found to be the lowest for CPI at pH 7.0 with 100 mM NaCl, and highest at pH 3.0 without NaCl. Solubility was found to be lowest at pH 5.0 and 7.0 without NaCl (<20 %), however greatly improved for all other pH and NaCl conditions (>80 %). Interfacial tension was found to be lowest at 10–11 mN/m for pH 5.0–0 mM NaCl and pH 7.0–50/100 mM NaCl, whereas under all other conditions interfacial tension was higher (15+ mN/m). Overall, NaCl has no effect on EAI at pH 3.0 where it ranged between 18.8 and 19.4 m²/g. At pH 5.0, EAI decreased from 21.1 to 12.8 m²/g as NaCl levels increased from 0 to 100 mM. At pH 7.0, EAI values were found to decrease from 14.9 to 5.2 m²/g as NaCl levels were raised from 0 to 100 mM. Overall, ESI was reduced with the addition of NaCl from ~15.7 min at 0 mM NaCl to ~11.6 min and ~12.0 min for the 50 and 100 mM NaCl levels, respectively.