ABSTRACT
Phosphodiesterase 7 (PDE7) specifically hydrolyzes cyclic adenosine monophosphate (cAMP), a second messenger that plays essential roles in cell signaling and physiological processes. Many PDE7 inhibitors used to investigate the role of PDE7 have displayed efficacy in the treatment of a wide range of diseases, such as asthma and central nervous system (CNS) disorders. Although PDE7 inhibitors are developed more slowly than PDE4 inhibitors, there is increasing recognition of PDE7 inhibitors as potential therapeutics for no nausea and vomiting secondary. Herein, we summarized the advances in PDE7 inhibitors over the past decade, focusing on their crystal structures, key pharmacophores, subfamily selectivity, and therapeutic potential. Hopefully, this summary will lead to a better understanding of PDE7 inhibitors and provide strategies for developing novel therapies targeting PDE7.
Subject(s)
Asthma , Phosphodiesterase 4 Inhibitors , Humans , Cyclic Nucleotide Phosphodiesterases, Type 7 , Phosphodiesterase 4 Inhibitors/pharmacology , Cyclic Nucleotide Phosphodiesterases, Type 4ABSTRACT
A new calixpyridinium-based light-responsive host-guest recognition motif was found in this work. This host-guest recognition motif was further discovered to be applied as a selective turn-on fluorescent sensor for lysine over other natural amino acids.
Subject(s)
Fluorescent Dyes/chemistry , Lysine/chemistry , Macrocyclic Compounds/chemistry , Photolysis , Pyridinium Compounds/chemistry , Biosensing Techniques/methods , Hydrophobic and Hydrophilic Interactions , Molecular Conformation , Spectrometry, Fluorescence , WaterABSTRACT
In this work, cationic macrocyclic calixpyridinium was employed as a new strategy to condense DNA. Moreover, the degradation of DNA by DNase I could lead to the calixpyridinium-DNA supramolecular aggregates being dissipated. Therefore, the present system is potentially applicable as the targeted drug delivery model at DNase I-overexpressed sites.
Subject(s)
Calixarenes/chemistry , DNA/chemistry , Deoxyribonuclease I/chemistry , Animals , SalmonABSTRACT
In this work, a comparative study on the supramolecular assemblies formed by calixpyridinium and two alginates with different viscosities was performed. We found that sodium alginate (SA) with medium viscosity (SA-M) had a better capability to induce aggregation of calixpyridinium in comparison with SA with low viscosity (SA-L) because of the stronger electrostatic interactions between calixpyridinium and SA-M. Therefore, the morphology of calixpyridinium-SA-M supramolecular aggregates was a compact spherical structure, while that of calixpyridinium-SA-L supramolecular aggregates was an incompact lamellar structure. As a result, adding much more amount of 1,3,6,8-pyrenetetrasulfonic acid tetrasodium salt to calixpyridinium-SA-M solution was required to achieve the balance of the competitive binding, and in comparison with calixpyridinium-SA-L supramolecular aggregates, calixpyridinium-SA-M supramolecular aggregates were more sensitive to alkali. However, for the same reason, in comparison with calixpyridinium-SA-M supramolecular aggregates, calixpyridinium-SA-L supramolecular aggregates were much more stable in water not only at room temperature but also at a higher temperature, and even in salt solution. Therefore, in comparison with calixpyridinium-SA-L supramolecular aggregates, calixpyridinium-SA-M supramolecular aggregates exhibited a completely opposite response to acid because of the generation of salt. Because SA is an important biomaterial with excellent biocompatibility, it is anticipated that this comparative study is extremely important in constructing functional supramolecular biomaterials.
ABSTRACT
Efficiency on biodegradation of high concentration of nitrobenzene (NB) by peat-phosphate esterified polyvinyl alcohol-embedded NB-degrading bacteria Pseudomonas corrugata was conducted compared to free bacteria cells. Its biodegradation kinetics, reuse ability, degradation effect in the absence of the essential element needed for the growth of bacteria and degradation efficiency of the raw water from the contaminated site were also invested. Results show that the degradation rate when the concentration of NB was at 600, 750, and 900 mg/L reached 91.02, 83.23, and 55.9 %, which was higher than that observed in free bacteria at the same concentration levels. Biodegradation kinetics of the material could be well described by first- and zero-order kinetics when the concentration of NB was at 300, 450 mg/L and 600, 750, 900 mg/L, respectively. Stable degradation activity (stayed at a level of approximately 70 %) was displayed during the 11th repeat-batch experiment. The affect of absence of phosphorus in the medium can be abated ascribed to the addition of peat, which contributes with organic matter and other elements such as nitrogen and phosphorus necessary to maintain metabolically active the microorganisms. Effective biodegradation of the raw water from the experimental site revealed that the material can be a potential candidate for treating NB-contaminated wastewater in the practical setting.
