scholarly journals Water-Soluble Substances of Arglabin

2020 ◽  
Vol 22 (3) ◽  
pp. 205
Author(s):  
S.M. Adekenov ◽  
А.N. Zhabayeva ◽  
G.М. Baisarov
Keyword(s):  
Complex Formation ◽  
Sesquiterpene Lactone ◽  
Glycyrrhizic Acid ◽  
Water Solubility ◽  
Magnesium Carbonate ◽  
Complex Compounds ◽  
Disodium Salt ◽  
Water Soluble ◽  
Mechanochemical Treatment ◽  
Complexing Agents

The article discusses the results of a study of the water solubility of natural sesquiterpene lactone arglabin, in particular, its ability to complex formation with complexing agents polyvinylpyrrolidone, the disodium salt of glycyrrhizic acid, magnesium carbonate. Mechanocomposites with polyvinylpyrrolidone and disodium salt of glycyrrhizic acid, which have increased water solubility, were obtained by the method of mechanochemical treatment of arglabin native. At the same time, the best result of dissolution in water is achieved by a two-hour treatment with polyvinylpyrrolidone and with disodium salt of glycyrrhizic acid. The water solubility of complex compounds of arglabin with polyvinylpyrrolidone increases by 4.61 times, and with disodium salt of glycyrrhizic acid by 4.42 times.

scholarly journals COMPLEX COMPOUNDS BASED ON PINOSTROBIN OXIME

2021 ◽  
pp. 219-226
Author(s):  
Sergazy Mynzhasarovich Adekenov ◽  
Gabiden Maratovich Baysarov ◽  
Anar Nikhanbaevna Zhabayeva ◽  
Lyubov' Petrovna Suntsova ◽  
Aleksandr Valer'yevich Dushkin
Keyword(s):  
Intermolecular Interaction ◽  
Glycyrrhizic Acid ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Magnesium Carbonate ◽  
Complex Compounds ◽  
Disodium Salt ◽  
Mechanochemical Treatment ◽  
Melting Peak ◽  
Scanning Calorimetry

The article studied the structural features of solid dispersions of pinostrobin oxime with arabinogalactan, disodium salt of glycyrrhizic acid, polyvinylpyrrolidone and basic magnesium carbonate obtained by mechanochemical treatment. The obtained complexes of pinostrobin oxime with arabinogalactan, disodium salt of glycyrrhizic acid, polyvinylpyrrolidone, and basic magnesium carbonate have increased water solubility in comparison with the initial pinostrobin oxime. The thermal effects of pinostrobin oxime and its complex compounds have been studied by differential scanning calorimetry. At the same time, on the DSC-curve, the melting peak of solid dispersions of pinostrobin oxime with disodium salt of glycyrrhizated acid and pinostrobin oxime with arabinogalactan is not displayed, which is associated with the intermolecular interaction of the components of the complex, where the molecule of pinostrobin oxime forms a bond with a complexformation agent during mechanochemical treatment. The complex of pinostrobin oxime with magnesium carbonate is not formed, as evidenced by the thermal curve, where the melting of the sample begins at 182 °C, and complete destruction occurs at a temperature of 782 °C, which is similar to the melting peak of the initial pinostrobin oxime. The results of studying intermolecular bonds in complexes of pinostrobin oxime by the method of NMR-relaxation indicate that the times of spin-lattice and spin-spin relaxation are very sensitive to intermolecular interaction and to the diffusion mobility of molecules.

Development and Characterization of the Neuroregenerative Xanthohumol C/Hydroxypropyl-β-cyclodextrin Complex Suitable for Parenteral Administration

Planta Medica ◽  
2019 ◽  
Vol 85 (16) ◽  
pp. 1233-1241
Author(s):  
Michael Kirchinger ◽  
Lara Bieler ◽  
Julia Tevini ◽  
Michael Vogl ◽  
Elisabeth Haschke-Becher ◽  
...  
Keyword(s):  
Water Solubility ◽  
Pharmaceutical Research ◽  
Water Soluble ◽  
Complexing Agents ◽  
Cyclodextrin Complex ◽  
Scanning Calorimetry ◽  
In Vivo Experiments ◽  
Strong Candidate

AbstractThe chroman-like chalcone Xanthohumol C, originally found in hops, was demonstrated to be a potent neuroregenerative and neuroprotective natural product and therefore constitutes a strong candidate for further pharmaceutical research. The bottleneck for in vivo experiments is the low water solubility of this chalcone. Consequently, we developed and validated a suitable formulation enabling in vivo administration. Cyclodextrins were used as water-soluble and nontoxic complexing agents, and the complex of Xanthohumol C and 2-hydroxypropyl-β-cyclodextrin was characterized using HPLC, HPLC-MS, NMR, and differential scanning calorimetry. The water solubility of Xanthohumol C increases with increasing concentrations of cyclodextrin. Using 50 mM 2-hydroxypropyl-β-cyclodextrin, solubility was increased 650-fold. Furthermore, in vitro bioactivity of Xanthohumol C in free and complexed form did not significantly differ, suggesting the release of Xanthohumol C from 2-hydroxypropyl-β-cyclodextrin. Finally, a small-scaled in vivo experiment in a rat model showed that after i. p. administration of the complex, Xanthohumol C can be detected in serum, the brain, and the cerebrospinal fluid at 1 and 6 h post-administration. Mean (± SD) Xanthohumol C serum concentrations after 1, 6, and 12 h were determined as 463.5 (± 120.9), 61.9 (± 13.4), and 9.3 (± 0.8) ng/mL upon i. v., and 294.3 (± 22.4), 45.5 (± 0.7), and 13 (± 1.0) ng/mL after i. p. application, respectively. Accordingly, the formulation of Xanthohumol C/2-hydroxypropyl-β-cyclodextrin is suitable for further in vivo experiments and further pharmaceutical research aiming for the determination of its neuroregenerative potential in animal disease models.

scholarly journals Development of decontamination and detergents for the nuclear industry

2021 ◽  
Vol 5 (4) ◽  
pp. 192-200
Author(s):  
Kudryavtsev P
Keyword(s):  
Nuclear Power ◽  
High Efficiency ◽  
Complex Compounds ◽  
Nuclear Industry ◽  
Water Soluble ◽  
Complexing Agents ◽  
Fabric Materials ◽  
Research Equipment ◽  
Water Soluble Complex ◽  
Processing Aids

At the enterprises of the radiochemical industry in the world, the task is to clean the technological and research equipment, overalls, and personnel from contamination with radioactive products. This task is especially relevant in case of emergencies, for example, such as an accident at a nuclear power plant in Fukushima, Japan. A review of the deactivation methods currently used is reviewed. It has been shown that the most typical pollutants are mixtures of radionuclides 137Cs, 144Ce, 144Pr, 90Sr, and 239Pu. All these elements are prone to the formation of chelate complexes. Therefore, complexing substances should be an essential component of deactivation solutions that form stable, water-soluble complex compounds with these radionuclides. When creating the recipe, we chose those complexing agents with the most persistent complex compounds with the expected pollutants. For research and testing in real conditions, we have prepared three types of technical detergents of various compositions with the code name MDS for decontaminating various surfaces, equipment, and workwear. The composition of these preparations consists mainly of an optimized mixture of surfactants, complexing agents, corrosion inhibitors, and processing aids. The studies were conducted to evaluate the possibility of using these funds for deactivation of premises, equipment, washing clothes in the Federal Unitary Enterprise "Mayak" and at its branch NIKIET in town Zarechny at Beloyarskyaya Nuclear Power Station in Russia. The effectiveness of deactivation was judged by the amount of residual contamination of the surface of the samples. The deactivating ability of MDS preparations for stainless, carbon steel, and plastic contaminated with β- and α-emitting nuclides was tested. The possibility of using MDS detergents for the deactivation of platinum ampoules stored as radioactive waste was assessed. The possibility of using MDS detergents for the deactivation of fabric materials, including underwear and work clothes, was also evaluated. The tests showed the high efficiency of the developed detergent MDS compared to the existing and currently used deactivation agents.

scholarly journals Encapsulation of Carotenoids as Food Colorants via Formation of Cyclodextrin Inclusion Complexes: A Review

2021 ◽  
Vol 2 (2) ◽  
pp. 454-476
Author(s):  
Carlos A. Fuenmayor ◽  
Omar G. Baron-Cangrejo ◽  
Paula A. Salgado-Rivera
Keyword(s):  
Complex Formation ◽  
Water Solubility ◽  
Scale Up ◽  
Complexing Agents ◽  
Cyclodextrin Complex ◽  
Food Colorants ◽  
Published Evidence ◽  
Food Matrices ◽  
Multiple Challenges ◽  
Key Aspects

The use of natural carotenoids as food colorants is an important trend of innovation in the industry due to their low toxicity, their potential as bio-functional ingredients, and the increasing demand for natural and organic foods. Despite these benefits, their inclusion in food matrices presents multiple challenges related to their low stability and low water solubility. The present review covers the main concepts and background of carotenoid inclusion complex formation in cyclodextrins as a strategy for their stabilization, and subsequent inclusion in food products as color additives. The review includes the key aspects of the molecular and physicochemical properties of cyclodextrins as complexing agents, and a detailed review of the published evidence on complex formation with natural carotenoids from different sources in cyclodextrins, comparing complex formation methodologies, recovery, inclusion efficiency, and instrumental characterization techniques. Moreover, process flow diagrams (PFD), based on the most promising carotenoid-cyclodextrin complex formation methodologies reported in literature, are proposed, and discussed as a potential tool for their future scale-up. This review shows that the inclusion of carotenoids in complexes with cyclodextrins constitutes a promising technology for the stabilization of these pigments, with possible advantages in terms of their stability in food matrices.

scholarly journals Orthogonal self-assembly of an organoplatinum(II) metallacycle and cucurbit[8]uril that delivers curcumin to cancer cells

2018 ◽  
Vol 115 (32) ◽  
pp. 8087-8092 ◽  
Author(s):  
Sougata Datta ◽  
Santosh K. Misra ◽  
Manik Lal Saha ◽  
Nabajit Lahiri ◽  
Janis Louie ◽  
...  
Keyword(s):  
Complex Formation ◽  
Cancer Cells ◽  
Self Assembly ◽  
Water Solubility ◽  
Therapeutic Potential ◽  
Water Soluble ◽  
Spectroscopic Techniques ◽  
Guest Complex ◽  
Host Guest Complex ◽  
Stat3 Phosphorylation

Curcumin (Cur) is a naturally occurring anticancer drug isolated from the Curcuma longa plant. It is known to exhibit anticancer properties via inhibiting the STAT3 phosphorylation process. However, its poor water solubility and low bioavailability impede its clinical application. Herein, we used organoplatinum(II) ← pyridyl coordination-driven self-assembly and a cucurbit[8]uril (CB[8])-mediated heteroternary host–guest complex formation in concert to produce an effective delivery system that transports Cur into the cancer cells. Specifically, a hexagon 1, containing hydrophilic methyl viologen (MV) units and 3,4,5-Tris[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]benzoyl groups alternatively at the vertices, has been synthesized and characterized by several spectroscopic techniques. The MV units of 1 underwent noncovalent complexation with CB[8] to yield a host–guest complex 4. Cur can be encapsulated in 4, via a 1:1:1 heteroternary complex formation, resulting in a water-soluble host–guest complex 5. The host–guest complex 5 exhibited ca. 100-fold improved IC50 values relative to free Cur against human melanoma (C32), melanoma of rodents (B16F10), and hormone-responsive (MCF-7) and triple-negative (MDA-MB231) breast cancer cells. Moreover, strong synergisms of Cur with 1 and 4 with combinatorial indexes of <1 across all of the cell lines were observed. An induced apoptosis with fragmented DNA pattern and inhibited expression of phosphor-STAT3 supported the improved therapeutic potential of Cur in heteroternary complex 5.

scholarly journals Encapsulation of Carotenoids as Food Colorants via Formation of Cyclodextrin Inclusion Complexes: A Review

2021 ◽  
Author(s):  
Carlos Alberto Fuenmayor ◽  
Omar Giovanny Baron Cangrejo ◽  
Paula Andrea Salgado Rivera
Keyword(s):  
Complex Formation ◽  
Water Solubility ◽  
Scale Up ◽  
Complexing Agents ◽  
Cyclodextrin Complex ◽  
Food Colorants ◽  
Published Evidence ◽  
Food Matrices ◽  
Multiple Challenges ◽  
Key Aspects

The use of natural carotenoids as food colorants is an important trend of innovation in the industry due to their low toxicity, their potential as bio-functional ingredients, and the increasing demand for natural and organic foods. Despite these benefits, their inclusion in food matrices presents multiple challenges related to their low stability and low water solubility. The present review covers the main concepts and background of carotenoid inclusion complex formation in cyclodextrins as a strategy for their stabilization, and subsequent inclusion in food products as color additives. The review includes the key aspects of the molecular and physicochemical properties of cyclodextrins as complexing agents, and a detailed review of the published evidence on complex formation with natural carotenoids from different sources in cyclodextrins, comparing complex formation methodologies, recovery, inclusion efficiency, and instrumental characterization techniques. Moreover, process flow diagrams (PFD), based on the most promising carotenoid-cyclodextrin complex formation methodologies, are proposed, and discussed as a potential tool for their future scale-up. This review shows that the inclusion of carotenoids in complexes with cyclodextrins constitutes a promising technology for the stabilization of these pigments, with possible advantages in terms of their stability in food matrices.

BODIPY Fluorophores for Membrane Potential Imaging

2019 ◽  
Author(s):  
Jenna Franke ◽  
Benjamin Raliski ◽  
Steven Boggess ◽  
Divya Natesan ◽  
Evan Koretsky ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Water Solubility ◽  
Water Soluble ◽  
Voltage Sensitivity ◽  
Chemical Transformations ◽  
Direct Modification ◽  
Biological Compatibility ◽  
Meso Position ◽  
Ionizable Groups ◽  
Boron Center

Fluorophores based on the BODIPY scaffold are prized for their tunable excitation and emission profiles, mild syntheses, and biological compatibility. Improving the water-solubility of BODIPY dyes remains an outstanding challenge. The development of water-soluble BODIPY dyes usually involves direct modification of the BODIPY fluorophore core with ionizable groups or substitution at the boron center. While these strategies are effective for the generation of water-soluble fluorophores, they are challenging to implement when developing BODIPY-based indicators: direct modification of BODIPY core can disrupt the electronics of the dye, complicating the design of functional indicators; and substitution at the boron center often renders the resultant BODIPY incompatible with the chemical transformations required to generate fluorescent sensors. In this study, we show that BODIPYs bearing a sulfonated aromatic group at the meso position provide a general solution for water-soluble BODIPYs. We outline the route to a suite of 5 new sulfonated BODIPYs with 2,6-disubstitution patterns spanning a range of electron-donating and -withdrawing propensities. To highlight the utility of these new, sulfonated BODIPYs, we further functionalize them to access 13 new, BODIPY-based voltage-sensitive fluorophores. The most sensitive of these BODIPY VF dyes displays a 48% ΔF/F per 100 mV in mammalian cells. Two additional BODIPY VFs show good voltage sensitivity (≥24% ΔF/F) and excellent brightness in cells. These compounds can report on action potential dynamics in both mammalian neurons and human stem cell-derived cardiomyocytes. Accessing a range of substituents in the context of a water soluble BODIPY fluorophore provides opportunities to tune the electronic properties of water-soluble BODIPY dyes for functional indicators.

scholarly journals Synthesis, Characterization and Bactericidal Activity of a 4-Ammoniumbuthylstyrene-Based Random Copolymer

Polymers ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1140
Author(s):  
Silvana Alfei ◽  
Gabriella Piatti ◽  
Debora Caviglia ◽  
Anna Maria Schito
Keyword(s):  
Antibacterial Activity ◽  
Bactericidal Activity ◽  
Antimicrobial Agents ◽  
Water Solubility ◽  
Physicochemical Characterization ◽  
Random Copolymer ◽  
Water Soluble ◽  
Cationic Polymers ◽  
Severe Infections

The growing resistance of bacteria to current chemotherapy is a global concern that urgently requires new and effective antimicrobial agents, aimed at curing untreatable infection, reducing unacceptable healthcare costs and human mortality. Cationic polymers, that mimic antimicrobial cationic peptides, represent promising broad-spectrum agents, being less susceptible to develop resistance than low molecular weight antibiotics. We, thus, designed, and herein report, the synthesis and physicochemical characterization of a water-soluble cationic copolymer (P5), obtained by copolymerizing the laboratory-made monomer 4-ammoniumbuthylstyrene hydrochloride with di-methyl-acrylamide as uncharged diluent. The antibacterial activity of P5 was assessed against several multi-drug-resistant clinical isolates of both Gram-positive and Gram-negative species. Except for strains characterized by modifications of the membrane charge, most of the tested isolates were sensible to the new molecule. P5 showed remarkable antibacterial activity against several isolates of genera Enterococcus, Staphylococcus, Pseudomonas, Klebsiella, and against Escherichia coli, Acinetobacter baumannii and Stenotrophomonas maltophilia, displaying a minimum MIC value of 3.15 µM. In time-killing and turbidimetric studies, P5 displayed a rapid non-lytic bactericidal activity. Due to its water-solubility and wide bactericidal spectrum, P5 could represent a promising novel agent capable of overcoming severe infections sustained by bacteria resistant the presently available antibiotics.

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