Open Access. Powered by Scholars. Published by Universities.®
Physical Sciences and Mathematics Commons™
Open Access. Powered by Scholars. Published by Universities.®
- Publication
Articles 1 - 6 of 6
Full-Text Articles in Physical Sciences and Mathematics
Anti-Cancer Activity Of An Acid-Labile N-Alkylisatin Conjugate Targeting The Transferrin Receptor, Vineesh Indira Chandran, Lidia Matesic, Julie Locke, Danielle Skropeta, Marie Ranson, Kara Vine
Anti-Cancer Activity Of An Acid-Labile N-Alkylisatin Conjugate Targeting The Transferrin Receptor, Vineesh Indira Chandran, Lidia Matesic, Julie Locke, Danielle Skropeta, Marie Ranson, Kara Vine
Danielle Skropeta
We have previously reported a series of pH-sensitive imine-linked N-alkylisatin prodrugs that are stable at pH 7.4, but readily cleaved at pH 4.5. Herein, one of the most potent prodrugs, 5,7-dibromo-N-(pmethoxybenzyl) isatin (NAI), was functionalized with a para-phenylpropionic acid linker, and the resulting NAI–imine prodrug conjugated to transferrin (Tf) to form a NAI–imine–Tf conjugate. Cytotoxicity assays revealed the conjugate was equipotent to the free drug against MCF-7 breast cancer cells, with clear selectivity patterns based on TfR levels. These results suggest that this novel isatin-based cytotoxin conjugated to a tumor targeting protein via an acid-labile linker warrants further preclinical testing.
Synthesis And Hydrolytic Evaluation Of Acid-Labile Imine-Linked Cytoxic Isatin Model Systems, Lidia Matesic, Julie Locke, Kara Perrow, Marie Ranson, John Bremner, Danielle Skropeta
Synthesis And Hydrolytic Evaluation Of Acid-Labile Imine-Linked Cytoxic Isatin Model Systems, Lidia Matesic, Julie Locke, Kara Perrow, Marie Ranson, John Bremner, Danielle Skropeta
Danielle Skropeta
In this study a series of isatin-based, pH-sensitive aryl imine derivatives with differing aromatic substituents and substitution patterns were synthesised and their acid-catalysed hydrolysis evaluated. These derivatives were functionalised at the C3 carbonyl group of a potent N-substituted isatin cytotoxin and were stable at physiological pH but readily cleaved at pH 4.5. Observed rates of hydrolysis for the embedded imine-acid moiety were in the order para-phenylpropionic acid>phenylacetic acid (para>meta)>benzoic acid (meta>para). The ability to fine-tune hydrolysis rates in this way has potential implications for optimising imine linked, tumour targeting cytotoxin-protein conjugates
Binaphthyl-Anchored Antibacterial Tripeptide Derivatives With Hydrophobic C-Terminal Amino Acid Variations, John Bremner, Paul A. Keller, Stephen Pyne, Mark Robertson, Kandasamy Sakthivel, Kittiya Somphol, Dean Baylis, Jonathon A Coates, John Deadman, Dharshini Jeevarajah, David I. Rhodes
Binaphthyl-Anchored Antibacterial Tripeptide Derivatives With Hydrophobic C-Terminal Amino Acid Variations, John Bremner, Paul A. Keller, Stephen Pyne, Mark Robertson, Kandasamy Sakthivel, Kittiya Somphol, Dean Baylis, Jonathon A Coates, John Deadman, Dharshini Jeevarajah, David I. Rhodes
Paul Keller
The facile synthesis of seven new dicationic tripeptide benzyl ester derivatives, with hydrophobic group variations in the C-terminal amino acid component, is described. Moderate to good activity was seen against Gram-positive bacteria in vitro. One cyclohexyl-substituted compound 2c was tested more widely and showed good potency (MIC values ranging from 2–4 μg/mL) against antibiotic-resistant strains of Staphylococcus aureus and Enterococci (VRE, VSE), and against Staphylococcus epidermidis.
Crosslinking Neat Ultrathin Films And Nanofibres Of Ph-Responsive Poly(Acrylic Acid) By Uv Radiation, Adrian Gestos, Philip G. Whitten, Geoffrey Maxwell Spinks, Gordon G. Wallace
Crosslinking Neat Ultrathin Films And Nanofibres Of Ph-Responsive Poly(Acrylic Acid) By Uv Radiation, Adrian Gestos, Philip G. Whitten, Geoffrey Maxwell Spinks, Gordon G. Wallace
Gordon Wallace
Electrospun polyelectrolyte hydrogel nanofibres are being developed for many applications including artificial muscles, scaffolds for tissue engineering, wound dressings and controlled drug release. For electrospun polyelectrolytes, a post-spinning crosslinking process is necessary for producing a hydrogel. Typically, radiation or thermal crosslinking routines are employed that require multifunctional crosslinking molecules and crosslink reaction initiators (free radical producers). Here, ultraviolet subtype-C (UVC) radiation was employed to crosslink neat poly(acrylic acid) (PAA) nanofibres and films to different crosslink densities. Specific crosslink initiators or crosslinking molecules are not necessary in this fast and simple process providing an advantage for biological applications. Scanning probe microscopy …
All-Polymer Battery System Based On Polypyrrole (Ppy)/Para (Toluene Sulfonic Acid) (Pts) And Polypyrrole (Ppy)/Indigo Carmine (Ic) Free Standing Films, Irin Sultana, Md. Mokhlesur Rahman, Jiazhao Wang, Caiyun Wang, Gordon G. Wallace, Hua-Kun Liu
All-Polymer Battery System Based On Polypyrrole (Ppy)/Para (Toluene Sulfonic Acid) (Pts) And Polypyrrole (Ppy)/Indigo Carmine (Ic) Free Standing Films, Irin Sultana, Md. Mokhlesur Rahman, Jiazhao Wang, Caiyun Wang, Gordon G. Wallace, Hua-Kun Liu
Gordon Wallace
In this study, we introduce a novel all-polymer battery system based on conducting polymer (polypyrrole, PPy) doped with dopants of para (toluene sulfonic acid) (pTS) and indigo carmine (IC), respectively. The performance of the systems consisting of polypyrrole-para (toluene sulfonic acid) (PPy-pTS) as cathode and polypyrrole-indigo carmine (PPy-IC) as anode in conjunction with either a polymer based electrolyte or a commercial organic electrolyte of 1M LiPF6 in a 50:50 (v/v) mixture of ethylene carbonate (EC) and dimethyl carbonate (DMC) was evaluated. In the system, all the free-standing PPy-pTS and PPy-IC films were directly used without needing any metal substrate support …
Direct Ascorbic Acid Detection With Ferritin Immobilized On Single-Walled Carbon Nanotubes, Chonlada Dechakiatkrai, Jun Chen, Carol M. Lynam, Kwang Min Shin, Seon Jeong Kim, Sukon Phanichphant, Gordon G. Wallace
Direct Ascorbic Acid Detection With Ferritin Immobilized On Single-Walled Carbon Nanotubes, Chonlada Dechakiatkrai, Jun Chen, Carol M. Lynam, Kwang Min Shin, Seon Jeong Kim, Sukon Phanichphant, Gordon G. Wallace
Gordon Wallace
Ferritin protein was noncovalently immobilized onto single-walled carbon nanotubes (SWNTs). This SWNT/ferritin composite was characterized using cyclic voltammetry, UV-visible spectroscopy, Raman spectroscopy, and high-resolution transmission electron microscopy. The use of the SWNT/ferritin film as an amperometric biosensor was demonstrated by sensing ascorbic acid in phosphate-buffered saline solution with a sensitivity of 767 uAmg. It demonstrated that ferritin protein bound to SWNTs enhances the oxidation reaction of ascorbic acid over 11-fold.