scholarly journals A Novel Formononetin Derivative Promotes Anti-ischemic Effects on Acute Ischemic Injury in Mice

2021 ◽  
Vol 12 ◽  
Author(s):  
Lin Zhao ◽  
Jing Han ◽  
Jiaqi Liu ◽  
Kechen Fan ◽  
Tianjie Yuan ◽  
...  
Keyword(s):  
Myocardial Injury ◽  
Water Solubility ◽  
Oral Absorption ◽  
Lactate Dehydrogenase Level ◽  
High Water ◽  
Acute Ischemia ◽  
High Dose ◽  
Mice Model ◽  
Neuroprotective Effects ◽  
Organic Solvent Tolerant

Natural flavonoids, formononetin and ononin, possess antioxidant, antibacterial, anti-inflammatory and neuroprotective effects. Many complications caused by SARS-CoV-2 make patients difficult to recover. Flavonoids, especially formononetin and ononin, have the potential to treat SARS-CoV-2 and improve myocardial injury. However, their poor water solubility, poor oral absorption, high toxicity, and high-cost purification limit industrial practical application. Succinylation modification provides a solution for the above problems. Formononetin-7-O-β-(6″-O-succinyl)-D-glucoside (FMP), a new compound, was succinyl glycosylated from formononetin by the organic solvent tolerant bacteria Bacillus amyloliquefaciens FJ18 in a 10.0% DMSO (v/v) system. The water solubility of the new compound was improved by over 106 times compared with formononetin, which perfectly promoted the application of formononetin and ononin. The conversion rate of formononetin (0.5 g/L) was almost 94.2% at 24 h, while the yield of formononetin-7-O-β-(6″-O-succinyl)-D-glucoside could achieve 97.2%. In the isoproterenol (ISO)-induced acute ischemia mice model, the myocardial injury was significantly improved with a high dose (40 mg/kg) of formononetin-7-O-β-(6″-O-succinyl)-D-glucoside. The lactate dehydrogenase level was decreased, and the catalase and superoxide dismutase levels were increased after formononetin-7-O-β-(6″-O-succinyl)-D-glucoside treatment. Thus, formononetin-7-O-β-(6″-O-succinyl)-D-glucoside has high water solubility, low toxicity, and shows significant antimyocardial ischemia effects.

A Fluorescence Quenching Analysis of the Binding of Fluoroquinolones to Humic Acid

2017 ◽  
Vol 71 (11) ◽  
pp. 2512-2518 ◽  
Author(s):  
Ryan P. Ferrie ◽  
Gregory E. Hewitt ◽  
Bruce D. Anderson
Keyword(s):  
Humic Acid ◽  
Fluorescence Quenching ◽  
Water Solubility ◽  
Binding Constants ◽  
High Water ◽  
Static Quenching ◽  
Temperature Range ◽  
Equilibrium Binding ◽  
Quenching Analysis ◽  
High Water Solubility

Fluorescence quenching was used to investigate the interaction of six fluoroquinolones with humic acid. Static quenching was observed for the binding of ciprofloxacin, enoxacin, fleroxacin, levofloxacin, norfloxacin, and ofloxacin to humic acid. The equilibrium binding constants were found from Stern–Volmer plots of the data. The quenching experiments were repeated over a temperature range of 25–45 ℃ and van’t Hoff plots were generated. From these linear plots, thermodynamic values were calculated for Δ H, Δ G, and Δ S for each of the fluoroquinolones. The equilibrium binding constants were found to be <1 for all the antibiotics studied. The calculated ΔH values were all negative and ranged from −9.5 to −27.6 kJ/mol. The high water solubility of the antibiotics and low ΔH of binding suggests that the antibiotics will be transported easily through the environment. Finally, whether the fluoroquinolones are in a protonated, deprotonated, or partially protonated state is found to correlate to the strength of binding to humic acid.

Novel tetrazole PtII and PdII complexes with enhanced water solubility: synthesis, structural characterization and evaluation of antiproliferative activity

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Tatiyana V. Serebryanskaya ◽  
Alexander S. Lyakhov ◽  
Ludmila S. Ivashkevich ◽  
Yuri V. Grigoriev ◽  
Andreii S. Kritchenkov ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
High Performance ◽  
Water Solubility ◽  
Thermal Analyses ◽  
High Water ◽  
Acetonitrile Solution ◽  
X Ray ◽  
Molecular And Crystal Structures ◽  
Tetrazole Derivatives ◽  
High Water Solubility

AbstractNovel platinum(II) and palladium(II) chlorido complexes with tetrazole derivatives 1-(2-hydroxyethyl)tetrazole (het) and 1-[tris(hydroxymethyl)methyl]tetrazole (thm), viz. cis-[Pt(het)2Cl2], trans-[Pt(het)2Cl2], trans-[Pt(thm)2Cl2], trans-[Pd(het)2Cl2], and trans-[Pd(thm)2Cl2], were synthesized. The compounds were characterized by elemental and high-resolution electrospray ionization (HRESI) mass spectrometry, high-performance liquid chromatography (HPLC), 1H, 13C and 195Pt nuclear magnetic resonance (NMR) spectroscopy, thermal analyses, and Infrared (IR) spectroscopy. Molecular and crystal structures of trans-[PdL2Cl2] and trans-[PtL2Cl2] (L = het, thm) were established by single-crystal X-ray analysis. The complex cis-[Pt(het)2Cl2] was found to undergo cis–to–trans isomerization upon heating in acetonitrile solution and in the solid state. The synthesized complexes show rather high water solubility lying in the range of 2–10 mg/L.

scholarly journals Amphiphilic Nanocarrier Systems for Curcumin Delivery in Neurodegenerative Disorders

Medicines ◽  
2018 ◽  
Vol 5 (4) ◽  
pp. 126 ◽  
Author(s):  
Miora Rakotoarisoa ◽  
Angelina Angelova
Keyword(s):  
Neurodegenerative Disorders ◽  
Liquid Crystalline ◽  
Water Solubility ◽  
Neuronal Loss ◽  
Drug Solubility ◽  
Neuroprotective Effects ◽  
Slowing Down ◽  
Combination Treatments ◽  
Physico Chemical ◽  
Lateral Sclerosis

Neurodegenerative diseases have become a major challenge for public health because of their incurable status. Soft nanotechnology provides potential for slowing down the progression of neurodegenerative disorders by using innovative formulations of neuroprotective antioxidants like curcumin, resveratrol, vitamin E, rosmarinic acid, 7,8-dihydroxyflavone, coenzyme Q10, and fish oil. Curcumin is a natural, liposoluble compound, which is of considerable interest for nanomedicine development in combination therapies. The neuroprotective effects of combination treatments can involve restorative mechanisms against oxidative stress, mitochondrial dysfunction, inflammation, and protein aggregation. Despite the anti-amyloid and anti-tau potential of curcumin and its neurogenesis-stimulating properties, the utilization of this antioxidant as a drug in neuroregenerative therapies has huge limitations due to its poor water solubility, physico-chemical instability, and low oral bioavailability. We highlight the developments of soft lipid- and polymer-based delivery carriers of curcumin, which help improve the drug solubility and stability. We specifically focus on amphiphilic liquid crystalline nanocarriers (cubosome, hexosome, spongosome, and liposome particles) for the encapsulation of curcumin with the purpose of halting the progressive neuronal loss in Alzheimer’s, Parkinson’s, and Huntington’s diseases and amyotrophic lateral sclerosis (ALS).

scholarly journals Optimization and Modeling of an Emulsion Polymerization Reactor

2021 ◽  
Author(s):  
Narges Ghadi
Keyword(s):  
Emulsion Polymerization ◽  
Water Solubility ◽  
Monomer Conversion ◽  
High Water ◽  
Oscillatory Behavior ◽  
Operating Conditions ◽  
Polymer Properties ◽  
Continuous Polymerization ◽  
Simulation Results ◽  
The Impact

A mathematical model was developed to simulate emulsion polymerization in batch, semi-batch and continuous reactors for monomers with high water solubility and significant desorption such as vinyl acetate. The effects of operating conditions such as initiator and emulsifier concentration as well as reactor temperature have been studied. The simulation results revealed the sensitivity of polymer properties and monomer conversion to variation of these operating conditions. Furthermore, the impact of monomer soluble impurities on reduction of monomer conversion has been investigated. In order to control polymer molecular weight, application of chain transfer agents such as t-nonyl mercaptan was suggested. Generally, the simulation results fitted well [with] experimental data from the literature. Several optimizing policies were considered to enhance the reaction operation for better product quality. During continuous polymerization, the reactor demonstrates oscillatory behavior throughout the operation. A new reactor train configuration was consistent with the aim of damping the oscillations and producing high-quality latex.

scholarly journals CCN activity of organic aerosols observed downwind of urban emissions during CARES

2013 ◽  
Vol 13 (4) ◽  
pp. 9355-9399 ◽  
Author(s):  
F. Mei ◽  
A. Setyan ◽  
Q. Zhang ◽  
J. Wang
Keyword(s):  
Chemical Composition ◽  
Water Solubility ◽  
Volume Fraction ◽  
Field Studies ◽  
High Water ◽  
Carbonaceous Aerosols ◽  
Mass Spectral ◽  
Least Squares Fit ◽  
The Relationship ◽  
Aerosol Chemical Composition

Abstract. During the Carbonaceous Aerosols and Radiative Effects Study (CARES), activation fraction of size-resolved aerosol particles and aerosol chemical composition were characterized at the T1 site (~60 km downwind of Sacramento, California) from 10 June to 28 June 2010. The hygroscopicity of CCN-active particles (κCCN) with diameter from 100 to 171 nm, derived from the size-resolved activated fraction, varied from 0.10 to 0.21, with an average of 0.15, which was substantially lower than that proposed for continental sites in earlier studies. The low κCCN value was due to the high organic volume fraction, averaged over 80% at the T1 site. The derived κCCN exhibited little diurnal variation, consistent with the relatively constant organic volume fraction observed. At any time, over 90% of the size selected particles with diameter between 100 and 171 nm were CCN active, suggesting most particles within this size range were aged background particles. Due to the large organic volume fraction, organic hygroscopicity (κorg) strongly impacted particle hygroscopicity and therefore calculated CCN concentration. For vast majority of the cases, an increase of κorg from 0.03 to 0.18, which are within the typical range, doubled the calculated CCN concentration. Organic hygroscopicity was derived from κCCN and aerosol chemical composition, and its variations with the fraction of total organic mass spectral signal at m/z 44 (f44) and O : C were compared to results from previous studies. Overall, the relationships between κorg and f44 are quite consistent for organic aerosol (OA) observed during field studies and those formed in smog chamber. Compared to the relationship between κorg and f44, the relationship between κorg and O : C exhibits more significant differences among different studies, suggesting κorg may be better parameterized using f44. A least squares fit yielded κorg = 2.04 (± 0.07) × f44 − 0.11 (± 0.01) with the Pearson R2 value of 0.71. One possible explanation for the stronger correlation between κorg and f44 is that the m/z 44 signal (mostly contributed by the CO2+ ion) is more closely related to organic acids, which may dominate the overall κorg due to their relatively high water solubility and hygroscopicity.

scholarly journals Preclinical Evaluation of UDCA-Containing Oral Formulation in Mice for the Treatment of Wet Age-Related Macular Degeneration

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 561 ◽  
Author(s):  
Maharjan ◽  
Kim ◽  
Jin ◽  
Ko ◽  
Song ◽  
...  
Keyword(s):  
Macular Degeneration ◽  
Oral Delivery ◽  
Water Solubility ◽  
Vision Loss ◽  
Oral Absorption ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Preclinical Study ◽  
Age Related Macular Degeneration ◽  
Age Related

As a posterior ocular disease, wet age-related macular degeneration (WAMD) has been known to be related to vision loss, accompanying ocular complications. The intravitreous injection of VEGF antibodies has been reported to be an effective treatment to relieve symptoms of WAMD. However, the limitations of this treatment are high costs and invasiveness. For this reason, oral delivery route can be considered as a cost-effective way and the safest method to deliver drug molecules to the eyes. Accordingly, ursodeoxycholic acid (UDCA) was included in the oral formulation as the potential substance for the cure of WAMD in the animal model. Various pharmacological activities, such as antioxidant or anti-inflammatory effects, have been reported for UDCA and recent reports support the effects of UDCA in ocular treatment. However, due to poor water solubility and low pKa (around 5.0), it has been challenging to formulate aqueous solution of UDCA in the neutral pH range. In the present study, we confirmed the aqueous solubility of the oral UDCA formulation and performed a preclinical study, including pharmacokinetic profiling and WAMD model efficacy study in mice after oral administration of the drug solution. The results demonstrated that the formulation improved bioavailability of UDCA and efficiently delivered UDCA to the eye tissues after oral absorption. UDCA formulation was found to have inhibitory effects of choroidal neovascularization with a functional recovery in mice retinas. Taken together, our results suggest that the oral UDCA formulation could be used as a potent supplement for the cure of WAMD and related retinal diseases.

scholarly journals Salvianolic acid B protects against myocardial ischaemia-reperfusion injury in rats via inhibiting high mobility group box 1 protein expression through the PI3K/Akt signalling pathway

2019 ◽  
Vol 393 (8) ◽  
pp. 1527-1539 ◽  
Author(s):  
Hanqing Liu ◽  
Wei Liu ◽  
Huiliang Qiu ◽  
Dezhi Zou ◽  
Huayang Cai ◽  
...  
Keyword(s):  
Cardiac Function ◽  
Myocardial Ischaemia ◽  
Myocardial Injury ◽  
High Mobility ◽  
Salvianolic Acid B ◽  
High Mobility Group ◽  
High Dose ◽  
Dependent Manner ◽  
Salvianolic Acid ◽  
Ischaemia Reperfusion

AbstractSalvianolic acid B (Sal B) has a significant protective effect on myocardial ischaemia-reperfusion (I/R) injury. Therefore, the aims of this study were to determine the effects of Sal B on myocardial ischaemic-reperfusion (I/R) injury in rats and to explore whether its underlying mechanism of cardioprotection occurs through activating the expression of the phosphoinositide 3-kinase/protein, kinase B (PI3K/Akt) and inhibiting the expression of high mobility group protein 1 (HMGB1). Ninety Sprague-Dawley rats were randomized into five groups: group 1 (sham-operated), group 2 (myocardial I/R), group 3 (low dose of Sal B+I/R), group 4 (high dose of Sal B+I/R), and group 5 (high dose of Sal B+I/R+LY294002, which is a specific PI3k inhibitor). All I/R rats received 30 min myocardial ischaemia followed by 24-h reperfusion. Cardiac function, infarct size, myocardial injury marker levels, inflammatory response and cardiomyocyte apoptosis as well as Bcl-2, Bax, P-Akt, HMGB1 and TLR4 expression were measured. In the current study, Sal B significantly ameliorated myocardial I/R injury in a dose-dependent manner, ameliorated cardiac function, reduced myocardial infarction size, decreased myocardial injury marker expression, decreased inflammatory responses, reduced apoptosis, activated PI3K/Akt expression and inhibited HMGB1 expression. However, all effects of Sal B were significantly reversed by LY294002. Overall, the present study indicated that Sal B attenuated myocardial I/R injury by activating PI3K/Akt and inhibiting the release of HMGB1 in rats.

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