- NIR light controlled release of caged hydrogen sulfide based on upconversion nanoparticles
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A NIR light induced H2S release platform based on UCNPs was constructed. Under NIR light excitation, UCNPs can emit UV light which triggers H2S release in a spatial and temporal pattern. The platform was also employed to real-time monitor the delivery process in vivo, which may provide a new way for the use of H2S-based therapeutics for a variety of diseases. This journal is
- Chen, Wansong,Chen, Min,Zang, Qiguang,Wang, Liqiang,Tang, Feiying,Han, Yajing,Yang, Cejun,Deng, Liu,Liu, You-Nian
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- A fluorescent probe for fast and quantitative detection of hydrogen sulfide in blood
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The dose makes the poison: Hydrogen sulfide is an important gasotransmitter for which rapid detection agents are needed. A hydrogen sulfide probe, which allows for fast (within seconds), selective, and quantitative detection in buffer solution, serum, and whole blood is designed, synthesized, and used for detection of hydrogen sulfide (see picture). Copyright
- Peng, Hanjing,Cheng, Yunfeng,Dai, Chaofeng,King, Adrienne L.,Predmore, Benjamin L.,Lefer, David J.,Wang, Binghe
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- Dual Roles of Protein as a Template and a Sulfur Provider: A General Approach to Metal Sulfides for Efficient Photothermal Therapy of Cancer
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Fabrication of clinically translatable nanoparticles (NPs) as photothermal therapy (PTT) agents against cancer is becoming increasingly desirable, but still challenging, especially in facile and controllable synthesis of biocompatible NPs with high photothermal efficiency. A new strategy which uses protein as both a template and a sulfur provider is proposed for facile, cost-effective, and large-scale construction of biocompatible metal sulfide NPs with controlled structure and high photothermal efficiency. Upon mixing proteins and metal ions under alkaline conditions, the metal ions can be rapidly coordinated via a biuret-reaction like process. In the presence of alkali, the inert disulfide bonds of S-rich proteins can be activated to react with metal ions and generate metal sulfide NPs under gentle conditions. As a template, the protein can confine and regulate the nucleation and growth of the metal sulfide NPs within the protein formed cavities. Thus, the obtained metal sulfides such as Ag2S, Bi2S3, CdS, and CuS NPs are all with small size and coated with proteins, affording them biocompatible surfaces. As a model material, CuS NPs are evaluated as a PTT agent for cancer treatment. They exhibit high photothermal efficiency, high stability, water solubility, and good biocompatibility, making them an excellent PTT agent against tumors. This work paves a new avenue toward the synthesis of structure-controlled and biocompatible metal sulfide NPs, which can find wide applications in biomedical fields.
- Sheng, Jianping,Wang, Liqiang,Han, Yajing,Chen, Wansong,Liu, Hong,Zhang, Min,Deng, Liu,Liu, You-Nian
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- A selective fluorescent probe for thiols based on α,β- unsaturated acyl sulfonamide
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We report herein a novel fluorescent probe based on α,β- unsaturated acyl sulfonamide to detect thiols. The probe has good water solubility and reacts with thiols under aqueous conditions. It reacts selectively with cysteine but not with the other natural amino acids. The probe was subsequently applied to detect intracellular thiols.
- Zhang, Huatang,Wang, Ping,Yang, Yanxin,Sun, Hongyan
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p. 10672 - 10674,3
(2012)
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Read Online
- Protection of human retinal pigment epithelial cells from oxidative damage using cysteine prodrugs
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Age-related macular degeneration (AMD) is one of the major causes of vision loss in the elderly in most developed countries. Among other causes, oxidative stress in the retinal pigment epithelium (RPE) has been hypothesized to be a major driving force of AMD pathology. Oxidative stress could be treated by antioxidant administration into the RPE cells. However, to achieve high in-vivo efficacy of an antioxidant, it is imperative that the agent be able to penetrate the tissues and cells. Evidence suggests that lipophilicity governs cellular penetrance. Out of many antioxidant candidates, N-acetyl-L-cysteine (a prodrug of L-cysteine) (NAC) is a potent antioxidant as the bioavailability of the parent drug, L-cysteine, determines the production of glutathione; the universal antioxidant that regulates ROS. To increase the lipophilicity, four ester derivatives of N-acetylcysteine: N-acetylcysteine methyl ester, N-acetylcysteine ethyl ester, N-acetylcysteine propyl ester, and N-acetylcysteine butyl ester were synthesized. To mimic in vitro AMD conditions, hydroquinone, a component of cigarette smoke, was used as the oxidative insult. Cytosolic and mitochondrial protection against oxidative stress were tested using cytosolic and mitochondrial specific assays. The results provide evidence that these lipophilic cysteine prodrugs provide increased protection against oxidative stress in human RPE cells compared with NAC.
- Bulumulla, Chandima,Catchpole, Timothy,Christie, Abigail,Csaky, Karl G.,Kularatne, Ruvanthi N.,Stefan, Mihaela C.,Takacs, Alison
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- COMPOUNDS AND IMPLANTS FOR TREATING OCULAR DISORDERS
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The present disclosure relates to therapeutic compositions and therapies for use in the treatment of diseases and disorders of the eye. The present disclosure relates to curved, multilayer controlled-release ocular implant devices which include the therapeutic compositions of the present disclosure. The present disclosure related to methods for delivery of the therapeutic agents to the eye and the treatment of diseases and disorders of the eye.
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Paragraph 0234
(2021/05/15)
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- Unlocking Amides through Selective C–N Bond Cleavage: Allyl Bromide-Mediated Divergent Synthesis of Nitrogen-Containing Functional Groups
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We report a new set of reactions based on the unlocking of amides through simple treatment with allyl bromide, creating a common platform for accessing a diverse range of nitrogen-containing functional groups such as primary amides, sulfonamides, primary amines, N-acyl compounds (esters, thioesters, amides), and N-sulfonyl esters. The method has potential industrial applicability, as demonstrated through gram-scale syntheses in batch and in a continuous flow system.
- Govindan, Karthick,Chen, Nian-Qi,Chuang, Yu-Wei,Lin, Wei-Yu
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p. 9419 - 9424
(2021/11/30)
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- Mechanically Strong Heterogeneous Catalysts via Immobilization of Powderous Catalysts to Porous Plastic Tablets
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Main observation and conclusion: We describe a practical and general protocol for immobilization of heterogeneous catalysts to mechanically robust porous ultra-high molecular weight polyethylene tablets using inter-facial Lifshitz-van der Waals Interactions. Diverse types of powderous catalysts, including Cu, Pd/C, Pd/Al2O3, Pt/C, and Rh/C have been immobilized successfully. The immobilized catalysts are mechanistically robust towards stirring in solutions, and they worked well in diverse synthetic reactions. The immobilized catalyst tablets are easy to handle and reused. Moreover, the metal leaching of immobilized catalysts was reduced significantly.
- Li, Tingting,Xu, Bo
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supporting information
p. 2673 - 2678
(2021/08/03)
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- Fluorogenic iminosydnones: Bioorthogonal tools for double turn-on click-and-release reactions
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In this article, we report the synthesis and use of iminosydnone-based profluorophores as bioorthogonal cleavable linkers for imaging applications. These linkers react with cycloalkynes via subsequent [3+2] cycloaddition and retro Diels-Alder reactions, allowing simultaneous release of two dyes in biological media. This journal is
- Audisio, Davide,Porte, Karine,Riomet, Margaux,Taran, Frédéric,Wijkhuisen, Anne
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p. 7183 - 7186
(2020/07/14)
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- Easy-handling and low-leaching heterogeneous palladium and platinum catalysts via coating with a silicone elastomer
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We have developed a practical protocol for coating of commercial Pd/Al2O3 and Pt/Al2O3 catalysts in micro-powders with a silicone elastomer. Compared to original catalysts, the treated catalysts are easier to weight and transfer, and they are easier to recover by simple filtration. More importantly, the metal leaching of treated catalysts was significantly reduced. The treated catalysts worked very well in diverse hydrogenation reactions.
- Zhou, Mi,Li, Tingting,Xu, Bo
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supporting information
p. 948 - 952
(2019/03/08)
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- Design and Synthesis of Iminosydnones for Fast Click and Release Reactions with Cycloalkynes
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Emerging applications in the field of chemical biology are currently limited by the lack of bioorthogonal reactions allowing both removal and linkage of chemical entities on complex biomolecules. We recently discovered a novel reaction between iminosydnones and strained alkynes leading to two products resulting from ligation and fragmentation of iminosydnones under physiological conditions. We now report the synthesis of a panel of substituted iminosydnones and the structure reactivity relationship between these compounds and strained alkyne partners. This study identified the most relevant substituents, which allow to increase the rate of the transformation and to develop a bifunctional cleavable linker with improved kinetics.
- Riomet, Margaux,Decuypere, Elodie,Porte, Karine,Bernard, Sabrina,Plougastel, Lucie,Kolodych, Sergii,Audisio, Davide,Taran, Frédéric
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supporting information
p. 8535 - 8541
(2018/05/30)
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- Esterase activated carbonyl sulfide/hydrogen sulfide (H2S) donors
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Hydrogen sulfide (H2S) is a mediator of a number of cellular processes, and modulating cellular levels of this gas has emerged as an important therapeutic area. Localized generation of H2S is thus very useful but highly challenging. Here, we report pivaloyloxymethyl-based carbonothioates and carbamothioates that are activated by the enzyme, esterase, to generate carbonyl sulfide (COS), which is hydrolyzed to H2S.
- Chauhan, Preeti,Bora, Prerona,Ravikumar, Govindan,Jos, Swetha,Chakrapani, Harinath
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supporting information
p. 62 - 65
(2017/11/28)
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- SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME
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ABSTRACT The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.
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(2016/09/15)
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- Use of phosphorodithioate-based compounds as hydrogen sulfide donors
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Synthetic hydrogen sulfide (H2S) donors are useful research tools as well as potential therapeutic agents. In this chapter, we report the detailed protocols for the synthesis and evaluation of a series of phosphorodithioate-based H2S donors. Fluorescence assays were used to determine H2S release from the donors in both aqueous buffers and in cultured cells. These donors were found to be slow-release donors, much like the well-known GYY4137. These donors also showed some protective effects against hydrogen peroxide (H2O2)-induced oxidative damage in myocytes.
- Park, Chung-Min,Xian, Ming
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p. 127 - 142
(2015/03/04)
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- A new receptor with a FRET based fluorescence response for selective recognition of fumaric and maleic acids in aqueous medium
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Preferential binding of a new reagent to fumaric acid could be utilized for its estimation in aqueous medium and in commercial fruit juice.
- Upendar Reddy,Lo, Rabindranath,Roy, Sovan,Banerjee, Tanmay,Ganguly, Bishwajit,Das, Amitava
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supporting information
p. 9818 - 9820
(2013/10/21)
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- Chemosensors for Hydrogen Sulfide
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Selective chemosensing agents for hydrogen sulfide are provided. The chemosensing agents can act fast under mild conditions, are chemically stable for long-term storage, are sensitive for detection under near physiological conditions, show a linear concentration-signal relationship within physiologically relevant hydrogen sulfide concentration ranges for easy quantitation, show minimal or no interference by other anions in the blood, and are functional in aqueous solutions and blood plasma.
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(2013/11/19)
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- SUBSTITUTED SULFONAMIDES USEFUL AS ANTIAPOPTOTIC BCL INHIBITORS
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Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.
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(2012/12/13)
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