scholarly journals Acidity and nucleophilic reactivity of glutathione persulfide

2020 ◽  
Vol 295 (46) ◽  
pp. 15466-15481 ◽  
Author(s):  
Dayana Benchoam ◽  
Jonathan A. Semelak ◽  
Ernesto Cuevasanta ◽  
Mauricio Mastrogiovanni ◽  
Juan S. Grassano ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Biological Properties ◽  
High Electron ◽  
High Electron Density ◽  
Glutathione Disulfide ◽  
Leaving Group ◽  
Nucleophilic Reactivity ◽  
Sulfur Trafficking ◽  
Cellular Thiol

Persulfides (RSSH/RSS−) participate in sulfur trafficking and metabolic processes, and are proposed to mediate the signaling effects of hydrogen sulfide (H2S). Despite their growing relevance, their chemical properties are poorly understood. Herein, we studied experimentally and computationally the formation, acidity, and nucleophilicity of glutathione persulfide (GSSH/GSS−), the derivative of the abundant cellular thiol glutathione (GSH). We characterized the kinetics and equilibrium of GSSH formation from glutathione disulfide and H2S. A pKa of 5.45 for GSSH was determined, which is 3.49 units below that of GSH. The reactions of GSSH with the physiologically relevant electrophiles peroxynitrite and hydrogen peroxide, and with the probe monobromobimane, were studied and compared with those of thiols. These reactions occurred through SN2 mechanisms. At neutral pH, GSSH reacted faster than GSH because of increased availability of the anion and, depending on the electrophile, increased reactivity. In addition, GSS− presented higher nucleophilicity with respect to a thiolate with similar basicity. This can be interpreted in terms of the so-called α effect, i.e. the increased reactivity of a nucleophile when the atom adjacent to the nucleophilic atom has high electron density. The magnitude of the α effect correlated with the Brønsted nucleophilic factor, βnuc, for the reactions with thiolates and with the ability of the leaving group. Our study constitutes the first determination of the pKa of a biological persulfide and the first examination of the α effect in sulfur nucleophiles, and sheds light on the chemical basis of the biological properties of persulfides.

scholarly journals Structure Determination of C23H19N4OBr from Synchrotron Data

2014 ◽  
Vol 70 (a1) ◽  
pp. C141-C141
Author(s):  
Ozen Ozgen ◽  
Engin Kendi ◽  
Semra Koyunoglu ◽  
Akgul Yesilada ◽  
Hwo-Shuenn Sheu
Keyword(s):  
Powder Diffraction ◽  
Structural Information ◽  
Chemical Properties ◽  
Biological Properties ◽  
Cell Parameters ◽  
Fundamental Understanding ◽  
Physical And Chemical ◽  
Radiation Research ◽  
And Chemical Properties

A significant part of medicine is based on the discovery and development of drugs. It is very important to know the crystal structure of pharmaceutical compounds for fundamental understanding of structure, physical and chemical properties. Many of these materials are available only as powders. So any structural information must be obtained from powder diffraction. I am going to present following the stages while solving the structure of C23H19N4OBr, 2-[3-phenyl-4(m-bromophenyl)-2-pyrazolin-1-yl]-3-methyl-4(3H)-quinazolinone, from 2-pyrazolines derivatives. The compounds are known to display various biological properties such as fungicidal insecticidal, anti bacterial, anti viral activities, pharmacological properties such as antiinflammatory agents and have industral properties(1). The powder diffraction data was collected with Debye Scherrer camera at the BL01C2 beamline at room temperature in National Synchrotron Radiation Research Center(NSRRC), Taiwan. X-ray of wavelength was 1.0333Å. This compound crystallizes in orthorhombic system space group P bca, Z=8, unit cell parameters of a=25.83(1)Å, b=15.55(5)Å, c=10.63(3)Å, and V=4266.0(10)Å3. Reliability factors were reached Rwp=0.075, Rp=0.053, RB=0.086 ve S=1.31 after Rietveld refinement.

PLGA+HA/βTCP scaffold incorporating simvastatin: a promising biomaterial for bone tissue engineering

2020 ◽  
Author(s):  
Mariane Beatriz Sordi ◽  
Ariadne Cristiane Cabral da Cruz ◽  
Águedo Aragones ◽  
Mabel Mariela Rodríguez Cordeiro ◽  
Ricardo de Souza Magini
Keyword(s):  
Tissue Engineering ◽  
Bone Tissue Engineering ◽  
Bone Tissue ◽  
Thermal Analyses ◽  
Chemical Properties ◽  
Biological Properties ◽  
Scanning Calorimetry ◽  
Evaporation Technique ◽  
Porosity Analysis ◽  
Biphasic Ceramic

The aim of this study was to synthesize, characterize, and evaluate degradation and biocompatibility of poly(lactic-co-glycolic acid) + hydroxyapatite / β-tricalcium phosphate (PLGA+HA/βTCP) scaffolds incorporating simvastatin (SIM) to verify if this biomaterial might be promising for bone tissue engineering. Samples were obtained by the solvent evaporation technique. Biphasic ceramic particles (70% HA, 30% βTCP) were added to PLGA in a ratio of 1:1. Samples with SIM received 1% (m:m) of this medication. Scaffolds were synthesized in a cylindric-shape and sterilized by ethylene oxide. For degradation analysis, samples were immersed in PBS at 37 °C under constant stirring for 7, 14, 21, and 28 days. Non-degraded samples were taken as reference. Mass variation, scanning electron microscopy, porosity analysis, Fourier transform infrared spectroscopy, differential scanning calorimetry, and thermogravimetry were performed to evaluate physico-chemical properties. Wettability and cytotoxicity tests were conducted to evaluate the biocompatibility. Microscopic images revealed the presence of macro, meso, and micropores in the polymer structure with HA/βTCP particles homogeneously dispersed. Chemical and thermal analyses presented very similar results for both PLGA+HA/βTCP and PLGA+HA/βTCP+SIM. The incorporation of simvastatin improved the hydrophilicity of scaffolds. Additionally, PLGA+HA/βTCP and PLGA+HA/βTCP+SIM scaffolds were biocompatible for osteoblasts and mesenchymal stem cells. In summary, PLGA+HA/βTCP scaffolds incorporating simvastatin presented adequate structural, chemical, thermal, and biological properties for bone tissue engineering.

THE IMPORTANCE OF THE RED BOOK OF SOILS FOR MONITORING AND JUSTIFICATION OF CONSERVATION MEASURES

2020 ◽  
Author(s):  
O.S. Bezuglova ◽  
Keyword(s):  
Chemical Properties ◽  
Natural State ◽  
Soil Maps ◽  
Rostov Region ◽  
Conservation Measures ◽  
Background Data ◽  
The Russian Federation ◽  
Physical And Chemical ◽  
And Chemical Properties

Rostov Region belongs to the highly protected natural territories characterized by the continuous plowing. There territories are the only reserves with the soils preserved in their natural state. However, these areas often lack detailed information about the soils quality and composition. Surveying soils on these territories is crucial for determination of their basic physical and chemical properties. The resulted compilation of soil maps could lay a foundation for creating the Red Book of Soils and the formation of a section in the soil-geographical database of the Russian Federation. Subsequently, such information can be used as a background data for the main types of soils in the region. It will be also valuable during monitoring and justification of conservation measures.

Chitosan-Nanocellulose Composites for Regenerative Medicine Applications

2020 ◽  
Vol 27 (28) ◽  
pp. 4584-4592 ◽  
Author(s):  
Avik Khan ◽  
Baobin Wang ◽  
Yonghao Ni
Keyword(s):  
Regenerative Medicine ◽  
Preparation Method ◽  
Chemical Properties ◽  
Biological Properties ◽  
Next Generation ◽  
Structure Property ◽  
Physico Chemical ◽  
Structure Property Relationship ◽  
Attractive Candidate ◽  
Fundamental Understanding

Regenerative medicine represents an emerging multidisciplinary field that brings together engineering methods and complexity of life sciences into a unified fundamental understanding of structure-property relationship in micro/nano environment to develop the next generation of scaffolds and hydrogels to restore or improve tissue functions. Chitosan has several unique physico-chemical properties that make it a highly desirable polysaccharide for various applications such as, biomedical, food, nutraceutical, agriculture, packaging, coating, etc. However, the utilization of chitosan in regenerative medicine is often limited due to its inadequate mechanical, barrier and thermal properties. Cellulosic nanomaterials (CNs), owing to their exceptional mechanical strength, ease of chemical modification, biocompatibility and favorable interaction with chitosan, represent an attractive candidate for the fabrication of chitosan/ CNs scaffolds and hydrogels. The unique mechanical and biological properties of the chitosan/CNs bio-nanocomposite make them a material of choice for the development of next generation bio-scaffolds and hydrogels for regenerative medicine applications. In this review, we have summarized the preparation method, mechanical properties, morphology, cytotoxicity/ biocompatibility of chitosan/CNs nanocomposites for regenerative medicine applications, which comprises tissue engineering and wound dressing applications.

LC–MS/MS Determination of Apigenin in Rat Plasma and Application to Pharmacokinetic Study

2020 ◽  
Vol 21 ◽  
Author(s):  
Shixing Zhu ◽  
Jiayuan Zhang ◽  
Zhihua Lv ◽  
Mingming Yu
Keyword(s):  
Formic Acid ◽  
Pharmacokinetic Study ◽  
Ammonium Acetate ◽  
Rat Plasma ◽  
Biological Properties ◽  
Plasma Samples ◽  
Supply Rate ◽  
Natural Plant ◽  
Ammonium Acetate Buffer

Background: Apigenin, a natural plant flavone, has been shown to possess a variety of biological properties. Objective: In this report, a highly selective and sensitive LC-MS/MS method was developed and validated for the determination of apigenin in rat plasma. Methods: Analysts were separated on the HSS T3 column (1.8 μm 2.1×100 mm) using acetonitrile and 0.1% formic acid in 2 mM ammonium acetate buffer at a supply rate of 0.200 mL/min as eluent in gradient model. Results: Plasma samples were treated by protein precipitation using acetonitrile for the recovery ranging from 86.5% to 90.1% for apigenin. The calibration curves followed linearity in the concentration range of 0.50-500 ng/mL. The inter-day and intra-day precisions at different QC levels within 13.1% and the accuracies ranged from -10.6% to 8.6%. Conclusion: The assay has been successfully applied to the pharmacokinetic study of apigenin in rats.

PDO Rotonda’s Red Eggplant Extract: In vitro Determination of Biological Properties and Minerals Bioaccessibility

2020 ◽  
Vol 16 (1) ◽  
pp. 65-74
Author(s):  
Ortensia Ilaria Parisi ◽  
Mariarosa Ruffo ◽  
Fabio Amone ◽  
Rocco Malivindi ◽  
Domenico Gorgoglione ◽  
...  
Keyword(s):  
Control Sample ◽  
Specific Area ◽  
Biological Properties ◽  
Ammonium Molybdate ◽  
Antihypertensive Activity ◽  
Protected Designation Of Origin ◽  
The Family ◽  
Oil Red O Staining

Background: The Rotonda’s Red Eggplant belongs to the family of Solanum aethiopicum and it is cultivated in a specific area of Potenza (Basilicata, South of Italy) including villages of Rotonda, Viggianello, Castelluccio Superiore and Castelluccio Inferiore. The Red Eggplant cultivated in this area has gained the PDO, “Protected Designation of Origin”. Objective: The aim of this research was to evaluate the use of PDO Rotonda’s Red Eggplant extract as a possible nutraceutical supplement. The antioxidant, antihypertensive, hypoglycemic, and hypolipidemic properties were in vitro evaluated. Methods: The antioxidant activity was investigated by evaluating the scavenging properties against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-Azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals and by performing the Ammonium Molybdate and Folin-Ciocalteu assay. The hypoglycemic and antihypertensive activity was studied by evaluating the α-Amylase, α-Glucosidase and Angiotensin Converting Enzyme, respectively, inhibiting activity. In order to evaluate the hypolipidemic activity, the pancreatic lipase inhibiting property was determined and Oil Red O staining assay was performed. Finally, to evaluate the possible use of this extract as a minerals supplement, Selenium, Potassium and Chrome bioaccessibility was studied. Results: The obtained results underline the good antioxidant, hypoglycemic, antihypertensive and hypolipidemic in vitro properties of the PDO Rotonda’s Red Eggplant extract. Moreover, the obtained data show a higher minerals bioaccessibility and this higher value could be ascribable to the natural phytocomplex of PDO Rotonda’s Red Eggplant, which increases the minerals bioaccessibility if compare it with a control sample. Conclusion: The obtained results show that PDO Rotonda’s Red Eggplant extract, might be used as a possible nutraceutical supplement, along with traditional therapies, both for its biological properties and for its minerals bioaccessibility value.

Development and Pharmacokinetics Study of Antifungal Peptide Nanoliposomes by Liquid Chromatography-tandem Mass Spectrometry

2019 ◽  
Vol 15 (4) ◽  
pp. 312-318
Author(s):  
Shuoye Yang
Keyword(s):  
Mass Spectrometry ◽  
Biological Properties ◽  
Pharmacokinetic Property ◽  
Antifungal Peptide ◽  
Simple Liquid ◽  
Physico Chemical ◽  
Liquid Chromatography Tandem Mass ◽  
Pegylated Lipids

Background: The therapeutic ability and application of antifungal peptide (APs) are limited by their physico-chemical and biological properties, the nano-liposomal encapsulation would improve the in vivo circulation and stability. </P><P> Objective: To develop a long-circulating liposomal delivery systems encapsulated APs-CGA-N12 with PEGylated lipids and cholesterol, and investigated through in vivo pharmacokinetics. Methods: The liposomes were prepared and characterized, a rapid and simple liquid chromatographytandem mass spectrometry (LC-MS/MS) assay was developed for the determination of antifungal peptide in vivo, the pharmacokinetic characteristics of APs liposomes were evaluated in rats. Results: Liposomes had a large, unilamellar structure, particle size and Zeta potential ranged from 160 to 185 nm and -0.55 to 1.1 mV, respectively. The results indicated that the plasma concentration of peptides in reference solutions rapidly declined after intravenous administration, whereas the liposomeencapsulated ones showed slower elimination. The AUC(0-∞) was increased by 3.0-fold in liposomes in comparison with standard solution (20 mg·kg-1), the half-life (T1/2) was 1.6- and 1.5-fold higher compared to the reference groups of 20 and 40 mg·kg-1, respectively. Conclusion: Therefore, it could be concluded that liposomal encapsulation effectively improved the bioavailability and pharmacokinetic property of antifungal peptides.

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