- Glucose-responsive gel from phenylborate polymer and poly(vinyl alcohol): Prompt response at physiological pH through the interaction of berate with amino group in the gel
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Purpose. To design glucose-responsive gels based on the complexation between polymers having phenylboronic acid groups and poly (vinyl alcohol). Specifically, high-glucose sensitivity at physiological pH was achieved through the interaction of phenylborate with amino groups. Method. Terpolymers of m-acrylamidophenylbotonic acid, N,N-dimethylaminopropylacrylamide (DMAPAA), and N,N-dimethylacrylamide were prepared. DMAPAA was introduced in the terpolymer to stabilize phenylborate-polyol complex at physiological pH. The effect of amino groups on complex stabilization was estimated from viscosity as well as UV spectrum measurements. Results. A good correlation was observed between complexation rate and fraction of phenylborate as well as DMAPAA in the terpolymers. In line with this increased complexation rate, UV difference spectra measurement revealed that ionization of phenylboronic acid was facilitated in the terpolymer due to the interaction with DMAPAA. Further, sensitive change in the complexation rate was demonstrated with a variation in glucose concentration, which is in sharp contrast with the poor glucose-sensitivity of the polymer without DMAPAA. Conclusions. The introduction of an amino group into phenylborate polymers was quite effective for increasing the complexation ability and the glucose responsivity at physiological pH. These results suggest the feasibility of this complex-gel system in designing a self-regulated insulin-releasing device.
- Hisamitsu, Issei,Kataoka, Kazunori,Okano, Teruo,Sakurai, Yasuhisa
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- Glucose-sensitive holographic sensors for monitoring bacterial growth
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A glucose sensor comprising a reflection hologram incorporated into a thin, acrylamide hydrogel film bearing the cis-diol binding ligand, 3-acrylamidophenylboronic acid (3-APB), is described. The diffraction wavelength (color) of the hologram changes as t
- Lee, Mei-Ching,Kabilan, Satyamoorthy,Hussain, Abid,Yang, Xiaoping,Blyth, Jeff,Lowe, Christopher R.
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- Facile fabrication of dextran-based fluorescent nanogels as potential glucose sensors
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Glucose-responsive nanogels based on dextran and poly(3- acrylamidophenylboronic acid) (PAAPBA) were fabricated by a facile self-assembly assisted (SAA) strategy. Further introduction of the fluorescent agent 2-[4-(3-hydroxy-4-oxo-4H-chromen-2-yl)phenoxy]
- Zhou, Shuyan,Min, Xue,Dou, Hongjing,Sun, Kang,Chen, Chun-Yen,Chen, Chao-Tsen,Zhang, Zhaofeng,Jin, Yuqing,Shen, Zunli
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- Autonomous and Continuous Stimuli-Responsive Polymer Surface for Antibacterial Application through Enzymatic Self-Propagating Reactions
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Stimuli-responsive polymer materials inspired by biological materials have invoked increasing research interest; however, they still suffer from limitations such as finite amplified responses and poor sensitivity of the unstimulated parts. Herein, a new strategy for creating H+-responsive polymer surfaces that are capable of transforming specific local fleeting stimuli into global macroscopic changes is described. The introduction of self-propagating reactions into the polymer-surface systems endows them with excellent stimuli-amplifying properties and response of the unstimulated parts. On the basis of this design, a polymer and enzymatic reaction were employed to enable a specific response to a stimulus and then lead to macroscopic changes of the surface. It is further shown that the prepared H+-responsive polymer surfaces can be employed for antibacterial application. This work provides a good example of achieving autonomously reconfigurable materials that respond to local fleeting stimuli.
- Ding, Chao,Yan, Zhengqing,Ren, Jinsong,Qu, Xiaogang
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- Triply-responsive boronic acid block copolymers: Solution self-assembly induced by changes in temperature, pH, or sugar concentration
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Boronic acid-containing block copolymers capable of solution self-assembly into micelles and reverse micelles in response to changes in temperature, pH, and sugar concentration were prepared by reversible addition-fragmentation chain transfer (RAFT) polym
- Roy, Debashish,Cambre, Jennifer N.,Sumerlin, Brent S.
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- Sugar-responsive block copolymers by direct RAFT polymerization of unprotected boronic acid monomers
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Novel sugar-responsive block copolymers were prepared by RAFT block copolymerization of unprotected boronic acid monomers, providing a direct route to supramolecular assemblies that dissociate upon the addition of glucose. The Royal Society of Chemistry.
- Roy, Debashish,Cambre, Jennifer N.,Sumerlin, Brent S.
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- Boronic ester-based self-healing hydrogels formed by using intermolecular B-N coordination
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The copolymer poly(acrylamide-co-2-acrylamido glucose) (PA) and poly(acrylamide-co-N-acryloyl-3-aminophenylboronic acid-co-N-(3-dimethylaminopropyl) acrylamide) (PB) were separately prepared by radical polymerization, and the hydrogel was readily construc
- Han, Yugui,Liu, Yigang,Liu, Yusheng,Tan, Yebang,Wang, Qiuxia
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- A β-Lactamase-Imprinted Responsive Hydrogel for the Treatment of Antibiotic-Resistant Bacteria
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Antibiotics play important roles in infection treatment and prevention. However, the effectiveness of antibiotics is now threatened by the prevalence of drug-resistant bacteria. Furthermore, antibiotic abuse and residues in the environment cause serious h
- Li, Wen,Dong, Kai,Ren, Jinsong,Qu, Xiaogang
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- Tailoring uptake and release of ATP by dendritic glycopolymer/PNIPAAm hydrogel hybrids: First approaches towards multicompartment release systems
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A multicompartment release system is described which combines the advantages of dendritic architectures and hydrogels to enhance the desired delivery features in complex biological compartments. Here, a hydrogel hosts dendritic glycopolymers as nanocontai
- Polikarpov, Nikita,Appelhans, Dietmar,Welzel, Petra,Kaufmann, Anika,Dhanapal, Pranav,Bellmann, Cornelia,Voit, Brigitte
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- Therapeutic nanoplatforms with bacteria-specific activation for directional transport of antibiotics
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An entirely new strategy is explored for directional transport delivery of antibiotics to bacteria utilizing a bacteria-activated nanoplatform. The nanoplatform can effectively prevent the premature leakage of the therapeutic payload, but release was triggered when the nanoplatforms adhere to bacteria, promising potential applications for the delivery of a wide-range of antimicrobials.
- Yu, Yunjian,Zhang, Tianqi,Dai, Xijuan,Dai, Xiaomei,Wei, Xiaosong,Zhang, Xinge,Li, Chaoxing
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- Dynamic-covalent macromolecular stars with boronic ester linkages
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Macromolecular stars containing reversible boronic ester linkages were prepared by an arm-first approach by reacting well-defined boronic acid-containing block copolymers with multifunctional 1,2/1,3-diols. Homopolymers of 3-acrylamidophenylboronic acid (
- Bapat, Abhijeet P.,Roy, Debashish,Ray, Jacob G.,Savin, Daniel A.,Sumerlin, Brent S.
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- A bioinspired hierarchical nanoplatform targeting and responding to intracellular pathogens to eradicate parasitic infections
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Intracellular bacteria-mediated antibiotic tolerance, which acts as a “Trojan horse,” plays a critical and underappreciated role in chronic and recurrent infections. Failure of conventional antibiotic therapy is often encountered because infected cells pr
- Yu, Yunjian,Li, Jie,Zhang, Yufei,Ma, Zhuang,Sun, Haonan,Wei, Xiaosong,Bai, Yayun,Wu, Zhongming,Zhang, Xinge
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- PH-responsive surface charge inversion type nano-carrier as well as preparation method and application thereof
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The invention provides a pH-responsive surface charge inversion type nano-carrier as well as a preparation method and application thereof and aims to solve the technical problem that an existing drug delivery carrier cannot balance prolonging of blood cir
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Paragraph 0070; 0076-0077; 0084; 0090-0092; 0098-0099
(2021/07/10)
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- Thieno [3, 2 - c] pyridine compound, its preparation method and application
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The invention relates to a thieno-[3,2-c] pyridine type compound and an application thereof. The compound has a structure shown by a formula (I) in the specification. The compound of which the structure is shown by the formula (I), provided by the invention has a very good effect of inhibiting the activity of Bruton kinase. The invention also relates to the application of the compound in preventing and/or treating diseases which are improved by virtue of BTK (Bruton tyrosine kinase) activity inhibition.
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Paragraph 0077; 0078; 0079
(2018/09/02)
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- Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping
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The high genomic instability of non-small cell lung cancer tumors leads to the rapid development of resistance against promising EGFR tyrosine kinase inhibitors (TKIs). A recently detected triple mutation compromises the activity of the gold standard third-generation EGFR inhibitors. We have prepared a set of trisubstituted imidazoles with a rigidized 7-azaindole hinge binding motif as a new structural class of EGFR inhibitors by a target hopping approach from p38α MAPK inhibitor templates. On the basis of an iterative approach of docking, compound preparation, biological testing, and SAR interpretation, robust and flexible synthetic routes were established. As a result, we report two reversible inhibitors 11d and 11e of the clinically challenging triple mutant L858R/T790M/C797S with IC50 values in the low nanomolar range. Furthermore, we developed a kinome selective irreversible inhibitor 45a with an IC50 value of 1 nM against the EGFR L858R/T790M double mutant. Target binding kinetics and metabolic stability data are included. These potent mutant EGFR inhibitors may serve as a basis for the development of structurally novel EGFR probes, tools, or candidates.
- Juchum, Michael,Günther, Marcel,D?ring, Eva,Sievers-Engler, Adrian,L?mmerhofer, Michael,Laufer, Stefan
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supporting information
p. 4636 - 4656
(2017/06/13)
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- A glucose-sensitive autonomy type insulin release micro-gel carrier and its preparation method
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The invention provides a glucose-sensitive self-regulated insulin release micro-gel carrier and a preparation method thereof. The preparation method of the glucose-sensitive self-regulated insulin release carrier comprises the following steps: performing free radical polymerization on three monomers namely 3-acryloyl aminophenylboronic acid, hydrophilic RGD polypeptide containing ethenyl functional groups and N-isopropylacrylamide to obtain a glucose-sensitive nano gel, and then combining the glucose-sensitive nano gel with insulin to obtain a medicine-loaded micro-gel. According to the glucose-sensitive self-regulated insulin release micro-gel carrier provided by the invention, the release of insulin can be automatically 'opened and closed' according to the changes of glucose concentrations at human body temperature.
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Paragraph 0043; 0062
(2017/09/12)
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- Phenylboronate-diol crosslinked glycopolymeric nanocarriers for insulin delivery at physiological pH
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Research into polymers with glucose-sensitivity in physiological conditions has expanded recently due to their therapeutic potential in diabetes. Herein, to explore the glucose-responsive properties of a new polymer under physiological conditions, we synthesized an amphiphilic block glycopolymer based on phenylboronic acid and a carbohydrate, which was named poly(d- gluconamidoethyl methacrylate-block-3-acrylamidophenylboronic acid) (p(AAPBA-b-GAMA)). Based on the cross-linking between the diol groups of the carbohydrates and phenylboronic acid, the glycopolymers self-assembled to form nanoparticles (NPs). The glucose-sensitivity was revealed by the swelling behavior of the NPs at different glucose concentrations and was found to be dependent on the glucose level. The morphology of the NPs revealed by transmission electron microscopy showed that the NPs were spherical in shape with good dispersity. The cell viability of the NPs investigated by MTT assay was more than 90%, indicating that the glycopolymers had good cytocompatibility. Insulin could be loaded onto the glycopolymer NPs with high efficiency (up to 10%), and insulin release increased with enhancement of the glucose level in the medium. Such a glucose-responsive glycopolymer is an excellent candidate that holds great potential in the treatment of diabetes.
- Guo, Qianqian,Wu, Zhongming,Zhang, Xinge,Sun, Lei,Li, Chaoxing
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p. 911 - 920
(2014/02/14)
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- SUGAR-RESPONSIVE GEL AND MEDICINE ADMINISTERING DEVICE
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Disclosed are a sugar-responsive gel and a medicine administering device having a pKa more suitable for use in a body environment and capable of administering medicine more autonomously than before. A sugar-responsive gel and an insulin administering device having a pKa more suitable for use in a body environment and capable of administering insulin more autonomously than before, wherein under a body condition of pKa of 7.4 or less and temperature of 35° C.-40° C., when the glucose concentration increases, insulin can be released from a gel body in response thereto, and when the glucose concentration decreases, insulin release from the gel body can be suppressed.
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Paragraph 0060; 0061; 0062
(2013/03/28)
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