Synthesis of flavonoids and flavonoid-based designed multiple ligands for hypertension

The flavonoids, a family of compounds found in nature, possess a wealth of established health benefits. In this research, a library of novel flavonoid compounds was synthesised for therapeutic evaluation. A particular focus was the attachment of 3ʹ,4ʹ-dihydroxyflavonol, an antioxidant and antihypertensive flavonoid, to other known antihypertensives, to provide dual action compounds for the treatment of hypertension.

Bridging the gap : from simulation to clinical practice

There has been a shift from the initial learning of skills on patients in the clinical setting to initial learning in a simulated environment, using part-task models, with the risk of a task focus to the learning. We contend that quality learning in both the simulated and the clinical environment is crucial to enhance the transferability of skills to the clinical setting.

Bridging the copyright and licensing knowledge gap

Objectives: The purpose of this project was to examine the copyright and licensing knowledge gap of academic staff to identify their current understanding of, and attitudes towards, copyright, licensing and the open access movement in relation to the content they use, create, and share in their teaching and research practice. The motivation behind this study was to gather information to assist the Library in creating and providing effective information resources and training for academic staff.

Methods: An anonymous online survey was distributed to Faculty of Health academic staff at Deakin University. Seventy individuals in the Faculty of Health completed the survey.

Results: The results suggested that most of the academics have used content created by others in their teaching materials, but they are not confident about complying with copyright or licensing conditions whilst doing so. Most had not posted any of their own content online, but would generally be willing for it to be used by others, with attribution. Around half had never posted their published articles in an institutional or discipline repository, but again, would be willing for them to be used for educational purposes. Most academics have never shared their research data online, and some were very unwilling to do so - despite current pushes to broaden access to research data sets. Finally, most had never applied a Creative Commons licence to a piece of work, and over half were unaware of what rights they had retained under publishing agreements for their work. It was strongly indicated that an informational website would be very helpful in providing guidance around topics of copyright, licensing and sharing.

Conclusions: Results were largely consistent with other similar studies conducted around these topics. There is a clear role for librarians to continue providing such training and resources as the push for Open Access resources, publishing, and data only gains momentum.

Cyclopalladated complexes containing 2-C 6 R 4 PPh 2 ligands (R = H, F): one-electron electrochemical reduction leading to metal–carbon σ-bond cleavage via palladium( i )

Three new ortho -metallated palladium complexes, [Pd(O,O’-hfacac)(κ2-2-C6F4PPh2)] (11), [Pd2(O,O’hfacac)2(μ-2-C6F4PPh2)2](12) and [Pd(O,O’-hfacac)(κC-2-C6F4PPh2)(PPh3)] (13) (hfacac = hexafluoroace-tylacetonate), have been prepared and fully characterised. The electrochemical reductions of complexes 11–13, together with those of other cyclopalladated complexes containing 2C6R4PPh2 ligands (R = H, F) were studied by cyclic, rotating disk and microelectrode voltammetry. Evidence for the one-electron reduction of [PdI(κ2-2-C6F4PPh2)(PPh2Fc)] (6) was obtained from coulometric analysis, although the product is unstable and undergoes further chemical processes. Preparative electro-reduction of [Pd2(μ-Br)2(κ2-2-C6F4PPh2)2] (7) in CH2Cl2 causes reductive cleavage of its Pd–C σ-bonds and formation of the complex [PdBr2{PPh2(2-C6F4H)}2](14); possible mechanisms are discussed.

Blue electrogenerated chemiluminescence from water-soluble iridium complexes containing sulfonated phenylpyridine or tetraethylene glycol derivatized triazolylpyridine ligands

Incorporating phenylpyridine- and triazolylpyridine-based ligands decorated with methylsulfonate or tetraethylene glycol (TEG) groups, a series of iridium(III) complexes has been created for green and blue electrogenerated chemiluminescence under analytically useful aqueous conditions, with tri-n-propylamine as a coreactant. The relative electrochemiluminescence (ECL) intensities of the complexes were dependent on the sensitivity of the photodetector over the wavelength range and the pulse time of the applied electrochemical potential. In terms of the integrated area of corrected ECL spectra, with a pulse time of 0.5 s, the intensities of the Ir(III) complexes were between 18 and 102 % that of [Ru(bpy)3 ](2+) (bpy=2,2'-bipyridine). However, when the intensities were measured with a typical bialkali photomultiplier tube, the signal of the most effective blue emitter, [Ir(df-ppy)2 (pt-TEG)](+) (df-ppy=2-(2,4-difluorophenyl)pyridine anion, pt-TEG=1-(2-(2-(2-(2-hydroxyethoxy)ethoxy)ethoxy)ethyl)-4-(2-pyridyl)-1,2,3-triazole), was over 1200 % that of the orange-red emitter [Ru(bpy)3 ](2+) . A combined experimental and theoretical investigation of the electrochemical and spectroscopic properties of the Ir(III) complexes indicated that the greater intensity from [Ir(df-ppy)2 (pt-TEG)](+) relative to those of the other Ir(III) complexes resulted from a combination of many factors, rather than being significantly favored in one area.

Modular synthesis of linear Bis- and Tris-monodentate fused [6]Polynorbornane-Based Ligands and their assembly into coordination cages

A modular approach has been developed for the synthesis of rigid linear di- and tritopic ligands based on a fused [6]polynorbornane scaffold. The design provides up to three sites for installing functionality, including both "ends" and a "central" position with the advantage that each region can be independently addressed during synthesis. To illustrate the utility of the approach, both pyridyl and picolyl units were incorporated to provide six new ligands, with centers and ends either matched or mismatched. Indeed, both [M2 L4 ] cages with endohedral functionality and [M3 L4 ] complexes were cleanly produced from these ligands with assembled structures confirmed by using (1) H NMR spectroscopy, HRMS, and molecular modelling.

Can cancer therapy be achieved by bridging apoptosis and autophagy: A method based on microRNA-dependent gene therapy and phytochemical targets

A failure of a cell to self destruct has long been associated with cancer progression and development. The fact that tumour cells may not instigate cell arrest or activate cell death mechanisms upon cancer drug delivery is a major concern. Autophagy is a mechanism whereby cell material can be engulfed and digested while apoptosis is a self-killing mechanism, both capable of hindering multiplication after cell injury. In particular situations, autophagy and apoptosis seem to co-exist simultaneously or interdependently with the aid of mutual proteins. This review covers roles of microRNAs and chemopreventive agents and makes an attempt at outlining possible partnerships in maximizing cancer cell death with minimal normal cell damage.

A comparison of novel organoiridium(III) complexes and their ligands as a potential treatment for prostate cancer

A range of 1,4-substituted 2-pyridyl-N-phenyl triazoles were synthesised and evaluated for their antiproliferative properties against lymph node cancer of the prostate (LNCaP) and bone metastasis of prostate cancer (PC-3) cells. Excellent-to-low IC50 values were determined (5.6-250 μM), and a representative group of 4 ligands were then complexed to iridium(III) giving highly luminescent species. Re-evaluation of these compounds against both cell lines was then undertaken and improved potency (up to 72-fold) was observed, giving IC50 values of 0.36-11 μM for LNCaP and 0.85-5.9 μM for PC-3. Preliminary screens for in vivo toxicity were conducted using a zebrafish model showing a wide range of induced toxicity depending of the compound evaluated. Apoptosis and Caspase-3 levels were also determined and showed no statistical difference between some of the treated specimens and the controls. This study may identify novel therapeutic agents for advanced stage of prostate cancer in humans.

Metal ion ligands in hyperaccumulating plants

Metal-hyperaccumulating plants have the ability to take up extraordinary quantities of certain metal ions without succumbing to toxic effects. Most hyperaccumulators select for particular metals but the mechanisms of selection are not understood at the molecular level. While there are many metal-binding biomolecules, this review focuses only on ligands that have been reported to play a role in sequestering, transporting or storing the accumulated metal. These include citrate, histidine and the phytosiderophores. The metal detoxification role of metallothioneins and phytochelatins in plants is also discussed.