scholarly journals Preparation and Antitumor Activity of Betulin Dipropionate and its Composites

2021 ◽  
Vol 12 (5) ◽  
pp. 6873-6894
Keyword(s):  
Cancer Cells ◽  
Water Solubility ◽  
Annexin V ◽  
Birch Bark ◽  
Natural Polymers ◽  
Wide Range ◽  
One Step ◽  
High Cytotoxicity ◽  
Betulin Dipropionate ◽  
The One

Betulin dipropionate is a natural compound with high cytotoxicity toward many cancer cells. The one-step synthesis directly from the birch bark without a separate betulin isolation stage was developed to obtain betulin dipropionate. Due to its composition, betulin dipropionate is a promising drug for treating a wide range of diseases. However, the poor water solubility of this compound has limited its applications. We prepared the composites of betulin dipropionate using two methods: ball milling of the mixtures of betulin dipropionate with synthetic and natural polymers, such as polyvinylpyrrolidone polyethylene glycol, fumed silica, arabinogalactan, and preparation of thin films with arabinogalactan by evaporating the aqueous solutions. These composites showed higher water solubility and improved antitumor properties against ascites carcinoma cells and human lung adenocarcinoma cells compared with the initial substance. Furthermore, the cell viability studies based on Annexin V and Propidium iodide probes confirmed the high proapoptotic effect of betulin dipropionate against cancer cells.

Kaempferol Improves TRAIL-Mediated Apoptosis in Leukemia MOLT-4 Cells by the Inhibition of Anti-apoptotic Proteins and Promotion of Death Receptors Expression

2019 ◽  
Vol 19 (15) ◽  
pp. 1835-1845
Author(s):  
Ali Hassanzadeh ◽  
Adel Naimi ◽  
Majid F. Hagh ◽  
Raedeh Saraei ◽  
Faroogh Marofi ◽  
...  
Keyword(s):  
Tumor Necrosis Factor ◽  
Cancer Cells ◽  
Tumor Necrosis ◽  
Lymphoblastic Leukemia ◽  
Annexin V ◽  
Death Receptors ◽  
Target Cells ◽  
Wide Range ◽  
Apoptotic Proteins ◽  
Necrosis Factor

Introduction: Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL or Apo2L) is a member of the tumor necrosis factor (TNF) superfamily, which stimulates apoptosis in a wide range of cancer cells via binding to death receptors 4 and 5 (DR4/5). Nevertheless, TRAIL has noticeable anti-cancer abilities; some cancer cells acquire resistance to TRAIL, and consequently its potential for inducing apoptosis in target cells is strongly diminished. Acute lymphoblastic leukemia MOLT-4 cell line is one of the most resistant cells to TRAIL that developed resistance to TRAIL via different pathways. We used TRAIL plus kaempferol to eliminate resistance of the MOLT-4 cells to TRAIL. Material and Methods: First, IC50 for kaempferol (95 µM) was determined by using the MTT assay. Second, the viability of the MOLT-4 cells was assayed by FACS after Annexin V/PI staining, following treatment with TRAIL (50 and 100 nM) and kaempferol (95 µM) alone and together. Finally, the expression levels of the candidate genes involved in resistance to TRAIL were assayed by real-time PCR technique. Results: Kaempferol plus TRAIL induced apoptosis robustly in MOLT-4 cells at 12, 24 and 48 hours after treatment. Additionally, we found that kaempferol could inhibit expression of the c-FLIP, X-IAP, cIAP1/2, FGF-8 and VEGF-beta, and conversely augment expression of the DR4/5 in MOLT-4 cells. Conclusion: We suggest that co-treatment of MOLT-4 cells with TRAIL plus kaempferol is a practical and attractive approach to eliminate cancers’ resistance to TRAIL via inhibition of the intracellular anti-apoptotic proteins, upregulation of DR4/5 and also by suppression of the VEGF-beta (VEGFB) and FGF-8 expressions.

Address of the President Lord Todd, O. M. at the Anniversary Meeting, 1 December 1980

1980 ◽  
Vol 211 (1182) ◽  
pp. 1-13 ◽  
Keyword(s):  
Usnic Acid ◽  
Chemical Properties ◽  
Wide Range ◽  
One Step ◽  
Oxidative Processes ◽  
The One ◽  
Physical And Chemical ◽  
Biosynthetic Studies ◽  
And Chemical Properties

The Copley Medal is awarded to Sir Derek Barton, F. R. S. Among Sir Derek Barton's many distinguished contributions to organic chemistry, outstanding is his conception and development of conformational analysis, which represents the most important advance in this century in the understanding of the stereochemistry of organic compounds, and for which he received a Nobel Prize in 1969. Originally devised for cyclohexane derivatives, the concept was rapidly extended to other ring systems, and is of major importance in interpretation of the physical and chemical properties of a wide range of natural products. Sir Derek has also contributed greatly to the understanding of biosynthesis, and in many cases demonstrated the validity of his hypotheses by labelling experiments in vivo . In particular, his ideas on the nature of phenolic coupling, involving one-electron oxidative processes, formed the basis of a very large number of successful biosynthetic studies, especially in the alkaloid field. He has also applied his ideas to the simulation of natural biosynthetic sequences, the one-step synthesis of the complex usnic acid from a simple monocyclic precursor providing one of the most striking examples.

scholarly journals A Straightforward Substitution Strategy to Tune BODIPY Dyes Spanning the Near-Infrared Region via Suzuki–Miyaura Cross-Coupling

Materials ◽  
2018 ◽  
Vol 11 (8) ◽  
pp. 1297 ◽  
Author(s):  
Guanglei Li ◽  
Yu Otsuka ◽  
Takuya Matsumiya ◽  
Toshiyuki Suzuki ◽  
Jianye Li ◽  
...  
Keyword(s):  
Near Infrared ◽  
Cross Coupling ◽  
Cumulus Cells ◽  
Infrared Region ◽  
Quantum Yields ◽  
Nir Dyes ◽  
Wide Range ◽  
One Step ◽  
The One ◽  
First Time

In this study, a series of new red and near-infrared (NIR) dyes derived from 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) were developed by introducing thiophene and its derivatives to the 3- and 5- positions of the dichloroBODIPY core. For the first time, cyclictriol boronates and N-methyliminodiacetic acid (MIDA) boronate were used as organoboron species to couple with 3,5-dichloroBODIPY via the one-step Suzuki–Miyaura cross-coupling. Six kinds of thieno-expended BODIPY dyes were synthesized in acceptable yields ranging from 31% to 79%. All six dyes showed different absorption and emission wavelengths spanning a wide range (c.a. 600–850 nm) in the red and NIR regions with relatively high quantum yields (19–85%). Cellular imaging of 8-(2,6-dimethylphenyl)-re3,5-di(2-thienyl)-BODIPY (dye 1) was conducted using bovine cumulus cells, and the fluorescence microscopy images indicated that the chromophore efficiently accumulated and was exclusively localized in the cytoplasm, suggesting it could be utilized as a subcellular probe. All six dyes were characterized using 1H-NMR and mass spectrometry.

scholarly journals The role of thermal activation in motion and force generation by molecular motors

2000 ◽  
Vol 355 (1396) ◽  
pp. 511-522 ◽  
Author(s):  
R. Dean Astumian
Keyword(s):  
Molecular Motors ◽  
Atp Hydrolysis ◽  
Force Production ◽  
Hand Model ◽  
Small Load ◽  
Wide Range ◽  
One Step ◽  
The One ◽  
Kinesin Molecule ◽  
Stochastic Properties

The currently accepted mechanism for ATP–driven motion of kinesin is called the hand–over–hand model, where some chemical transition during the ATP hydrolysis cycle stretches a spring, and motion and force production result from the subsequent relaxation. It is essential in this mechanism for the moving head of kinesin to dissociate, while the other head remains firmly attached to the microtubule. Here we propose an alternative Brownian motor model where the action of ATP modulates the interaction potential between kinesin and the microtubule rather than a spring internal to the kinesin molecule alone. In this model neither head need dissociate (which predicts that under some circumstances a single–headed kinesin can display processive motion) and the transitions by which the motor moves are best described as thermally activated steps. This model is consistent with a wide range of experimental data on the force–velocity curves, the one ATP to one–step stoichiometry observed at small load, and the stochastic properties of the stepping.

scholarly journals One-Step Green Synthesis of Metallic Nanoparticles Using Sodium Alginate

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Jesus Valdez ◽  
Idalia Gómez
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Particle Size Distribution ◽  
Size Distribution ◽  
Sodium Alginate ◽  
Metallic Nanoparticles ◽  
Natural Polymers ◽  
Vis Spectroscopy ◽  
Wide Range ◽  
One Step

Metallic nanoparticles have been focus of research because of their characteristic properties, specifically the LSPR which can have wide applications in biomedical sciences and engineering. Currently, traditional physical and chemical methods can synthesize these nanoparticles but their disadvantages such as costs, time, effectiveness, and toxicity of precursors provide a wide range of problems for the synthesis of these nanoparticles. Recently, some natural polymers and organic compounds have been used for the synthesis of nanoparticles by green methods. In this study, we synthesize copper, silver, and gold nanoparticles using sodium alginate as reducing and stabilizing agent under microwave irradiation. The LSPR for each system was observed by UV-vis spectroscopy. Particle size distribution and zeta potential demonstrate the size and stability for these nanoparticles. FESEM and TEM microscopies have shown the size and morphology of these systems correlated with UV-vis, particle size distribution, and zeta potential analyses. The study demonstrates a rapid, facile, cheaper, and one-step green method of synthesis for these metallic nanoparticles being an alternative to the conventional methods used for synthesis of metallic nanoparticles.

scholarly journals Biotin Transport-Targeting Polysaccharide-Modified PAMAM G3 Dendrimer as System Delivering α-Mangostin into Cancer Cells and C. elegans Worms

2021 ◽  
Vol 22 (23) ◽  
pp. 12925
Author(s):  
Joanna Markowicz ◽  
Łukasz Uram ◽  
Stanisław Wołowiec ◽  
Wojciech Rode
Keyword(s):  
Cancer Cells ◽  
Delivery System ◽  
Water Solubility ◽  
Model Organism ◽  
Amide Bond ◽  
C Elegans ◽  
Wide Range ◽  
Amine Groups

The natural xanthone α-mangostin (αM) exhibits a wide range of pharmacological activities, including antineoplastic and anti-nematode properties, but low water solubility and poor selectivity of the drug prevent its potential clinical use. Therefore, the targeted third-generation poly(amidoamine) dendrimer (PAMAM G3) delivery system was proposed, based on hyperbranched polymer showing good solubility, high biocompatibility and low immunogenicity. A multifunctional nanocarrier was prepared by attaching αM to the surface amine groups of dendrimer via amide bond in the ratio 5 (G32B12gh5M) or 17 (G32B10gh17M) residues per one dendrimer molecule. Twelve or ten remaining amine groups were modified by conjugation with D-glucoheptono-1,4-lactone (gh) to block the amine groups, and two biotin (B) residues as targeting moieties. The biological activity of the obtained conjugates was studied in vitro on glioma U-118 MG and squamous cell carcinoma SCC-15 cancer cells compared to normal fibroblasts (BJ), and in vivo on a model organism Caenorhabditis elegans. Dendrimer vehicle G32B12gh at concentrations up to 20 µM showed no anti-proliferative effect against tested cell lines, with a feeble cytotoxicity of the highest concentration seen only with SCC-15 cells. The attachment of αM to the vehicle significantly increased cytotoxic effect of the drug, even by 4- and 25-fold for G32B12gh5M and G32B10gh17M, respectively. A stronger inhibition of cells viability and influence on other metabolic parameters (proliferation, adhesion, ATP level and Caspase-3/7 activity) was observed for G32B10gh17M than for G32B12gh5M. Both bioconjugates were internalized efficiently into the cells. Similarly, the attachment of αM to the dendrimer vehicle increased its toxicity for C. elegans. Thus, the proposed α-mangostin delivery system allowed the drug to be more effective in the dendrimer-bound as compared to free state against both cultured the cancer cells and model organism, suggesting that this treatment is promising for anticancer as well as anti-nematode chemotherapy.

scholarly journals Hydrothermal Synthesis of CeO2-SnO2 Nanoflowers for Improving Triethylamine Gas Sensing Property

Nanomaterials ◽  
2018 ◽  
Vol 8 (12) ◽  
pp. 1025 ◽  
Author(s):  
Dongping Xue ◽  
Yan Wang ◽  
Jianliang Cao ◽  
Zhanying Zhang
Keyword(s):  
Gas Sensing ◽  
Hydrothermal Reaction ◽  
Pure Sno2 ◽  
Characterization Methods ◽  
Working Temperature ◽  
Wide Range ◽  
Sensitivity And Selectivity ◽  
One Step ◽  
The One ◽  
Optimum Working

Developing the triethylamine sensor with excellent sensitivity and selectivity is important for detecting the triethylamine concentration change in the environment. In this work, flower-like CeO2-SnO2 composites with different contents of CeO2 were successfully synthesized by the one-step hydrothermal reaction. Some characterization methods were used to research the morphology and structure of the samples. Gas-sensing performance of the CeO2-SnO2 gas sensor was also studied and the results show that the flower-like CeO2-SnO2 composite showed an enhanced gas-sensing property to triethylamine compared to that of pure SnO2. The response value of the 5 wt.% CeO2 content composite based sensor to 200 ppm triethylamine under the optimum working temperature (310 °C) is approximately 3.8 times higher than pure SnO2. In addition, CeO2-SnO2 composite is also significantly more selective for triethylamine than pure SnO2 and has better linearity over a wide range of triethylamine concentrations. The improved gas-sensing mechanism of the composites toward triethylamine was also carefully discussed.

General Trend of Negative Transference Number in Li Salt/Ionic Liquid Mixtures

2019 ◽  
Author(s):  
Nicola Molinari ◽  
Jonathan P. Mailoa ◽  
Boris Kozinsky
Keyword(s):  
Ionic Liquid ◽  
Transference Number ◽  
Liquid Mixtures ◽  
Single Linkage ◽  
Self Diffusion ◽  
Wide Range ◽  
Single Linkage Cluster ◽  
Concentrated Solution ◽  
The One ◽  
Dynamics Simulations

We show that strong cation-anion interactions in a wide range of lithium-salt/ionic liquid mixtures result in a negative lithium transference number, using molecular dynamics simulations and rigorous concentrated solution theory. This behavior fundamentally deviates from the one obtained using self-diffusion coefficient analysis and agrees well with experimental electrophoretic NMR measurements, which accounts for ion correlations. We extend these findings to several ionic liquid compositions. We investigate the degree of spatial ionic coordination employing single-linkage cluster analysis, unveiling asymmetrical anion-cation clusters. Additionally, we formulate a way to compute the effective lithium charge that corresponds to and agrees well with electrophoretic measurements and show that lithium effectively carries a negative charge in a remarkably wide range of chemistries and concentrations. The generality of our observation has significant implications for the energy storage community, emphasizing the need to reconsider the potential of these systems as next generation battery electrolytes.<br>

Complexation with Hydroxypropyl-gama-Cyclodextrin of Birch Tree Extract Physico-chemical Characterisation of their Binary Products

2008 ◽  
Vol 59 (6) ◽  
Author(s):  
Codruta Soica ◽  
Cristina A. Dehelean ◽  
Valentin Ordodi ◽  
Diana Antal ◽  
Vicentiu Vlaia
Keyword(s):  
Inclusion Complexes ◽  
Water Solubility ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Bark Extract ◽  
Birch Bark ◽  
Preparation Methods ◽  
Birch Tree ◽  
Physico Chemical

Birch bark contains important pentacyclic triterpens that determine an anticancer, anti-inflammatory and antiviral activity. The compounds can be extracted by simple procedures with organic solvents. The major problem of this type of triterpens is their low water solubility which can be increased by physical procedures like cyclodextrin complexation. The aim of present study was to analyse the products between birch bark extract and hydroxypropyl-g -cyclodextrin. Hydroxypropyl-g -cyclodextrin (HPGCD) was used as a host to improve its solubility in water, via inclusion complex formation. In order to obtain the inclusion complexes, 1:2 molar ratio and two preparation methods (physical mixing, kneading) were used. The inclusion complexes were analyzed by in vitro dissolution tests, thermal analysis and X-ray diffraction.

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