scholarly journals Design of Nanosystems for the Delivery of Quorum Sensing Inhibitors: A Preliminary Study

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5655
Author(s):  
Supandeep Singh Hallan ◽  
Paolo Marchetti ◽  
Daria Bortolotti ◽  
Maddalena Sguizzato ◽  
Elisabetta Esposito ◽  
...  
Keyword(s):  
Quorum Sensing ◽  
High Performance ◽  
Correlation Spectroscopy ◽  
Molar Ratio ◽  
In Vitro Test ◽  
Dimethyl Benzyl ◽  
Capacity Evaluation ◽  
Size And Morphology ◽  
Dicetyl Phosphate

Biofilm production is regulated by the Quorum Sensing system. Nowadays, Quorum Sensing represents an appealing target to design new compounds to increase antibiotics effects and avoid development of antibiotics multiresistance. In this research the use of liposomes to target two novel synthetic biofilm inhibitors is presented, focusing on a preformulation study to select a liposome composition for in vitro test. Five different liposome (LP) formulations, composed of phosphatidyl choline, cholesterol and charged surfactant (2:1:1, molar ratio) have been prepared by direct hydration and extrusion. As charged surfactants dicetyl phosphate didecyldimethylammonium chloride, di isobutyl phenoxy ethyl dimethyl benzyl ammonium chloride and stearylamine (SA) and have been used. Liposome charge, size and morphology were investigated by zeta potential, photon correlation spectroscopy, small angle x-ray spectroscopy and electron microscopy. LP-SA was selected for the loading of biofilm inhibitors and subjected to high performance liquid chromatography for entrapment capacity evaluation. LP-SA loaded inhibitors showed a higher diameter (223.6 nm) as compared to unloaded ones (205.7 nm) and a dose-dependent anti-biofilm effect mainly after 48 h of treatment, while free biofilm inhibitors loose activity. In conclusion, our data supported the use of liposomes as a strategy to enhance biofilm inhibitors effect.

Regional differences in catecholamine concentrations in bovine ovaries analysed by high-performance liquid chromatography

1991 ◽  
Vol 129 (2) ◽  
pp. 221-226 ◽  
Author(s):  
P. A. Denning-Kendall ◽  
M. L. Wild ◽  
Wathes D. C.
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
High Performance ◽  
Molar Ratio ◽  
Corpora Lutea ◽  
Wet Weight ◽  
High Concentrations ◽  
Highly Correlated ◽  
Very High

ABSTRACT Bovine corpora lutea and ovarian stroma were analysed by high-performance liquid chromatography for catecholamine content. High concentrations (up to 102 nmol/g wet weight) were found in both 'central' stroma, containing many blood vessels, and 'peripheral' stroma. Central stroma contained noradrenaline and some dopamine, whereas peripheral stroma contained a higher proportion of dopamine and also significant amounts of 3,4-dihydroxyphenylacetic acid (DOPAC). Occasional samples of stroma had very high amounts of dopamine, suggesting that it is stored in specific regions. Corpora lutea, although devoid of direct innervation, contained dopamine (up to 5·3 nmol/g) and noradrenaline (up to 1·2 nmol/g). The average dopamine: noradrenaline molar ratio was 1·19 : 1 and the concentrations of dopamine and noradrenaline were highly correlated (P < 0·002). The concentration of dopamine was significantly higher in the early luteal phase of the oestrous cycle than during the rest of the cycle or in pregnancy. The levels of noradrenaline and dopamine present in corpora lutea are sufficient to modulate the production of both oxytocin and progesterone by luteal cells in vitro. Journal of Endocrinology (1991) 129, 221–226

scholarly journals Synthesis, characterization and evaluation of copper nanoparticles as agrochemicals against Phytophthora spp.

2019 ◽  
Vol 2 (6) ◽  
pp. 48-56
Author(s):  
Hoang Minh Hao ◽  
Cao Van Du ◽  
Duong Thi Ngoc Dung ◽  
Cao Xuan Chuong ◽  
Nguyen Thi Phuong Phong ◽  
...  
Keyword(s):  
Copper Nanoparticles ◽  
Chemical Reduction ◽  
Trisodium Citrate ◽  
Molar Ratio ◽  
In Vitro Test ◽  
Weight Percentage ◽  
Phytophthora Spp ◽  
Transmission Electron ◽  
Xrd Techniques

By using water as a solvent, copper nanoparticles (CuNPs) have been synthesized from copper sulfate via chemical reduction method in the presence of trisodium citrate dispersant and polyvinylpyrrolidone (PVP) as capping agent. The effects of the experimental parameters such as the concentration of reducing agent (NaBH4), reaction temperature, molar ratio of citrate/Cu2+ and weight percentage ratios of Cu2+/PVP on the CuNP sizes were studied. The size of CuNPs in a range of 31 nm was obtained at NaBH4 concentration of 0.2 M, 50oC, citrate/Cu2+ molar ratio of 1.0 and Cu2+/PVP weight percentage of 5%. The colloidal CuNPs were characterized by using UV–Visible spectroscopy, transmission electron microscopy (TEM), and X-ray diffraction (XRD) techniques. The colloidal solution of CuNPs (3±1 nm) was investigated the potential against Phytophthora spp. which cause economically crop diseases. Under in vitro test conditions, the inhibition of Phytophthora spp. mycelia growth at three concentrations of CuNPs (10, 20, 30 ppm) after 48 hours are 90.18%, 91.87% and 100%, respectively. These results provided a simple and economical method to develop the CuNPs-based-fungicide.  

INTRAARTERIAL THROMBOLYSIS BY STREPTOKINASE-GLU-PLASMINOGEN

1987 ◽  
Author(s):  
E J Pilger ◽  
J Lammer ◽  
H Bertuch ◽  
H Steiner
Keyword(s):  
Artery Occlusion ◽  
Molar Ratio ◽  
In Vitro Test ◽  
Group Iii ◽  
Fibrinolytic Agent ◽  
Molar Ratios ◽  
Intraarterial Thrombolysis ◽  
Group I

In order to predict usefulness of streptokinase (SK), urokinase (UK) and streptokinase-glutamin-plasminogen (SK-Glu-Plg) for intraarterial fibrinolysis, an in vitro test was designed. Fibrin plates with and without plasminogen were incubated with SK, UK and SK-Glu-Plg (in molar ratios of 1:1, 2:1 and 1:2). On the fibrin plates containing plasminogen the highest fibrinolytic activity was observed with UK; on the fibrin plates without plasminogen, SK-Glu-Plg in a molar ratio of 1:2 was superior. We concluded, that plasmin would be synthesized by SK and Glu-Plg. In order to examine the in vivo efficacy of these different fibrinolytic agents, 120 patients suffering from peripheral artery occlusion were randomized into three treatment groups for local thrombolysis. The technique of Hess and coworkers was used for local thrombolytic therapy. In group I local fibrinolysis was performed with SK (2500 IU/5 min), in group II UK (4000 IU/5 min) was used and in group III the lytic agent consisted of SK-Glu-Plg (2500 IU/5 min). The primary recanalization rate was equal in all groups: 86%, 89% and 83% in group I, II and III respectively. However the duration required for the procedure and thus the total amount of fibrinolytic agent used was significantly different (p < 0,001) between the three groups: 2,3 ± 1,4; 2,1 ± 1,2 and 1,1 ±0,8 hours for groups I,II and III, respectively (mean ± SEM) . We conclude that SK-Glu-Plg or plasmin itself has the highest efficacy as a fibrinolytic agent for intraarterial thrombolysis. Since the intra-thrombotic concentration of Pig is unknown in an individual patient an empirically chosen dose of SK of UK may either be to high or to low for optimal thrombolysis.

scholarly journals Selecting and Characterizing Tyrosinase Inhibitors from Atractylodis macrocephalae Rhizoma Based on Spectrum-Activity Relationship and Molecular Docking

2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Yong-Qin Liu ◽  
Chang-Yan Xu ◽  
Fang-Yu Liang ◽  
Pei-Chun Jin ◽  
Zhi-Yao Qian ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
High Performance ◽  
Chemical Constituents ◽  
In Vitro Test ◽  
Least Squares Regression ◽  
Spectrum Activity ◽  
Vitro Test ◽  
Atractylenolide Iii

Atractylodis macrocephalae Rhizoma (AMR) is a famous classical Chinese traditional medicine (CTM), which has been used as a tonic for many diseases for thousands of years. In ancient China, it was used as a supplementary food for beauty in the palace. In preliminary studies, the function of whitening skin and the significant inhibiting effect on tyrosinase (TYR) which is the reactive enzyme in the composition of melanin of AMR were discovered, and the relevant research was rarely reported. In this study, high-performance liquid chromatography (HPLC) along with partial least squares regression analysis (PLS) was applied to survey the coherence between the chemical constituents and the inhibiting activity of 11 batches of AMR on TYR activity. The results of PLS showed that the chromatographic peaks 11 (atractylenolide III) and 15 could be important effective ingredients of the inhibition TYR activity as ascertained by spectrum-activity relationships. Furthermore, TYR inhibitory activity of atractylenolide III was validated by in vitro test by β-arbutin served as a positive control drug. The results of the in vitro test and the molecular docking showed that atractylenolide III has high TYR inhibitory activity and could link to the residues in TYR catalytic pocket. Therefore, bioassay, molecular docking, and spectrum-activity relationships are appropriate for linking the quality of samples with pharmaceutical-related active ingredients. And our studying would lay a theoretical foundation for applying the water extracts of AMR in whitening cosmetics.

scholarly journals Determination of the Extraction, Physicochemical Characterization, and Digestibility of Sulfated Polysaccharides in Seaweed—Porphyra haitanensis

Marine Drugs ◽  
2020 ◽  
Vol 18 (11) ◽  
pp. 539
Author(s):  
Mingshuang Dong ◽  
Yanhui Jiang ◽  
Chun Wang ◽  
Qian Yang ◽  
Xiaolu Jiang ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
High Performance ◽  
Physicochemical Characterization ◽  
Extraction Rate ◽  
Raw Material ◽  
Alpha Amylase ◽  
Molar Ratio ◽  
Sulfated Polysaccharides ◽  
Porphyra Haitanensis

The aim of the study was to extract Porphyra haitanensis polysaccharides (PHPs) using the water extraction and alcohol precipitation methods and explore their antioxidant activity and physicochemical properties. The single-factor and Box-Behnken response surface methodologies were used to optimize the extraction of polysaccharides from Porphyra haitanensis. Our results showed that the polysaccharide yield was as high as 20.48% with a raw material to water ratio of 0.04, and extraction time of 3 h at 80 °C. The extraction rate observed was similar to the actual extraction rate, thus proving the reliability of the optimization model. The extracted polysaccharides primarily consisted of galactose, glucose, and fucose in the molar ratio 76.2:2.1:1, respectively. The high performance gel permeation chromatography (HPGPC) results showed that the molecular weight of the PHPs obtained was 6.3 × 105 Da, and the sulfate content was 2.7 mg/mL. Fourier infrared spectroscopy was used to analyze the functional groups and structures of the polysaccharides. The effect of concentration, temperature, and pH on the apparent viscosity of the PHPs solution were studied using rheology experiments, which revealed that PHPs were a “non-Newtonian fluid” with shear-thinning behavior. The viscosity of the PHPs gradually increased with increasing sugar concentration, and decreased with increasing temperature, acidity, and alkalinity. Detection of the antioxidant activity of OH*, DPPH*, and ABTS* revealed that the scavenging activity of ABTS* was higher than that of OH* and DPPH* in the concentration range of 1–5 mg/mL. In the experiments of simulating gastric juice and alpha amylase in vitro, it was found that PHPs can better resist digestion of alpha amylase, and have better resistance than fructooligosaccharide (FOS), so PHPs have potential prebiotic activity. These findings demonstrate the potential of PHPs for use in the food and cosmetic industries.

scholarly journals Enhancing Dissolution Rate and Antibacterial Efficiency of Azithromycin through Drug-Drug Cocrystals with Paracetamol

Antibiotics ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 939
Author(s):  
Noor Ul Islam ◽  
Ezzat Khan ◽  
Muhammad Naveed Umar ◽  
Attaullah Shah ◽  
Muhammad Zahoor ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
High Performance ◽  
Biological Activities ◽  
Thermo Gravimetric Analysis ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Gravimetric Analysis ◽  
Pxrd Pattern ◽  
Pharmaceutical Industries

Cocrystallization is a promising approach to alter physicochemical properties of active pharmaceutical ingredients (hereafter abbreviated as APIs) bearing poor profile. Nowadays pharmaceutical industries are focused on preparing drug-drug cocrystals of APIs that are often prescribed in combination therapies by physicians. Physicians normally prescribe antibiotic with an analgesic/antipyretic drug to combat several ailments in a better and more efficient way. In this work, azithromycin (AZT) and paracetamol (PCM) cocrystals were prepared in 1:1 molar ratio using slow solvent evaporation method. The cocrystals were characterized by Fourier transform infrared (FTIR), Raman spectroscopy, powder X-ray diffraction (PXRD), differential scanning calorimeter (DSC), thermo gravimetric analysis (TGA) and high-performance liquid chromatography (HPLC). Vibrational spectroscopy and DSC confirmed that both APIs interact physically and showed chemical compatibility, while PXRD pattern of the starting material and products revealed that cocrystal have in a unique crystalline phase. The degree of hydration was confirmed by TGA analysis and result indicates monohydrate cocrystal formation. The HPLC analysis confirmed equimolar ratio of AZT:PCM in the cocrystal. The in vitro dissolution rate, saturation solubility, and antimicrobial activity were evaluated for AZT dihydrate and the resulting cocrystals. The cocrystals exhibited better dissolution rate, solubility and enhanced biological activities.

scholarly journals Sol-gel bioactive glass-ceramics Part II: Glass-ceramics in the CaO-SiO2-P2O5-MgO system

2009 ◽  
Vol 7 (3) ◽  
pp. 322-327 ◽  
Author(s):  
Lachezar Radev ◽  
Vladimir Hristov ◽  
Irena Michailova ◽  
Bisserka Samuneva
Keyword(s):  
Sol Gel ◽  
Glass Ceramics ◽  
Static Condition ◽  
Ceramic Materials ◽  
Molar Ratio ◽  
In Vitro Test ◽  
X Ray Diffraction ◽  
Vitro Test ◽  
Good Agreement

AbstractCeramics, with basic composition based on the CaO-SiO2-P2O5-MgO system with different Ca+ Mg/P+Si molar ratio (R), were prepared via polystep sol-gel technique. The structure of the obtained ceramic materials has been studied by XRD, FTIR spectroscopy, and SEM. X-ray diffraction showed the presence of akermanite and HA for the sample with R = 1.68 and Mg substituted β-TCP and silicocarnotite for the sample with R = 2.16, after thermal treatment at 1200°C/2 h. The obtained results are in good agreement with FTIR. In vitro test for bioactivity in static condition proved that the carbonate containing hydroxyapatite (CO3HA) can be formed on the surface of the synthesized samples. CO3HA consisted of both A- and B-type CO 32− ions. SEM micrographs depicted different forms of HA particles, precipitated on the surface after soaking in 1.5 simulated body fluid (SBF).

Biocompatible Delivery System for Metformin: Characterization, Radiolabeling and In Vitro Studies

2020 ◽  
Vol 20 (13) ◽  
pp. 1626-1634 ◽  
Author(s):  
Burcu Aydın ◽  
Eser Uçar ◽  
Volkan Tekin ◽  
Çiğdem İçhedef ◽  
Serap Teksöz
Keyword(s):  
Breast Cancer ◽  
Liver Cancer ◽  
Cancer Cell ◽  
High Performance ◽  
Cancer Cell Line ◽  
In Vitro Studies ◽  
Biological Behavior ◽  
Size And Morphology ◽  
Main Components

Background: In recent years, the uses of nanotechnology in medicine have an increasing potential as an effective nanocarrier system. These systems are improved with the purpose of maximizing therapeutic activity and minimizing undesirable side-effects. Moreover, radiolabeled nanoparticles can be used as agents for diagnosis and therapeutic purposes in clinical applications. They have three main components: the core, the targeting biomolecule, and the radionuclide. Objective: It is aimed to synthesize Metformin (MET) loaded Solid Lipid Nanoparticles (MET-SLN) and radiolabeled with technetium-99m tricarbonyl core. Methods: The structure of synthesized nanoparticles was characterized by Fourier Transform Infrared Spectroscopy (FTIR). The particle size and morphology of nanoparticles were examined by Dynamic Light Scattering (DLS), and Scanning Electron Microscope (SEM). Quality control studies of radiolabeled MET-SLN [99mTc(CO)3-MET-SLN] were performed by High-Performance Liquid Radiochromatography (HPLRC) and Thin Layer Radiochromatography (TLRC). Results: The radiolabeling yield of [99mTc(CO)3-MET-SLN] was found to be 88%. In vitro studies have been performed on cancer lines(MCF7, MDA-MD-231 breast, and HEPG2 liver cancer cells) to determine the biological behavior of 99mTc(CO)3-MET-SLNs. Conclusion: The results showed that higher uptake values were observed on estrogen-positive MCF7 breast cancer cell line according to estrogen negative MDA-MB-231 breast cancer and HEPG2 liver cancer cell lines.

scholarly journals Chemical Composition and Antioxidant Activities of Polysaccharides from Yingshan Cloud Mist Tea

2019 ◽  
Vol 2019 ◽  
pp. 1-11 ◽  
Author(s):  
Xiang Li ◽  
Si Chen ◽  
Jing-En Li ◽  
Ning Wang ◽  
Xin Liu ◽  
...  
Keyword(s):  
Body Weight ◽  
Chemical Composition ◽  
High Performance ◽  
Antioxidant Activities ◽  
Average Molecular Weight ◽  
Reducing Power ◽  
Gel Permeation Chromatography ◽  
The Body ◽  
Molar Ratio

The study was designed to investigate the chemical composition and antioxidant activities of polysaccharides from Yingshan Cloud Mist Tea. The chemical composition of green tea polysaccharides (GTPS) was analyzed by Fourier-transform infrared (FT-IR) spectroscopy, scanning electron microscope (SEM), thermogravimetric (TGA), gas chromatograph (GC), and high-performance gel-permeation chromatography (HPGPC). Then, the antioxidant activities in vitro of GTPS, effects of GTPS on body weight, and the antioxidant activities in chickens were studied. The results showed that GTPS were composed of rhamnose (Rha), arabinose (Ara), xylose (Xyl), mannose (Man), glucose (Glu), and galactose (Gal) in a molar ratio of 11.4 : 26.1 : 1.9 : 3.0 : 30.7 : 26.8 and the average molecular weight was 9.69×104 Da. Furthermore, GTPS exhibited obvious capacity of scavenging DPPH radical, hydroxyl radical, and superoxide radical and enhanced the ferric-reducing power in vitro. Last, GTPS significantly increased the body weight of chickens, enhanced the T-AOC, SOD, and GSH-Px level, and decreased the content of MDA in chickens. The results indicated that GTPS might be a kind of natural antioxidant, which had the potential application in feed industry.

Radiation Protection of Carboxymethylation of an Acid Polysaccharides Extracted from Auricularia Auricula against Uvb In Vitro

2011 ◽  
Vol 365 ◽  
pp. 199-204
Author(s):  
Hua Zhang ◽  
Zhen Yu Wang ◽  
Zi Luan Fan ◽  
Xin Yang ◽  
Xue Wang ◽  
...  
Keyword(s):  
Radiation Protection ◽  
High Performance ◽  
Dose Range ◽  
Chemical Characterization ◽  
Water Soluble ◽  
Molar Ratio ◽  
Ft Ir ◽  
Acid Polysaccharide ◽  
Soluble Acid

This paper reports on a water-soluble acid polysaccharide (AAP) and in how it was extracted from Auricularia auricular, acquired by CTAB, and prepared it’s carboxymethylation. Chemical characterization by high-performance liquid chromatography/gel permeation chromatograph (HPLC/GPC), Fourier transform infrared (FT-IR) spectrometer and gas chromatography–mass spectrophotometer (GC–MS) were investigated. Chemical analysis indicated that C AAAP was composed of arabinose, xylose, mannose, glucose and galactose, with the molar ratio at 0.04: 0.13: 1.00: 0.59: 0.29. Moreover, radiation protection against UVB in vitro indicated that at the dose range of 200–500 μg/mL, C AAAP enhanced the protection of HepG2 cells against UVB cytotoxicity than AAAP. However, but at the dose range of 50–150 μg/mL the result was just opposite.

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