scholarly journals The Water-Soluble Chitosan Derivative, N-Methylene Phosphonic Chitosan, Is an Effective Fungicide against the Phytopathogen Fusarium eumartii

2021 ◽  
Vol 37 (6) ◽  
pp. 533-542
Author(s):  
Florencia Anabel Mesas ◽  
María Cecilia Terrile ◽  
María Ximena Silveyra ◽  
Adriana Zuñiga ◽  
María Susana Rodriguez ◽  
...  
Keyword(s):  
Water Solubility ◽  
Water Soluble ◽  
Phytopathogenic Fungus ◽  
Oxygen Species ◽  
Chitosan Derivative ◽  
Solubility In Water ◽  
Environmental Friendly ◽  
Antifungal Effects ◽  
Species Production ◽  
Low Solubility

Chitosan has been considered an environmental-friendly polymer. However, its use in agriculture has not been extended yet due to its relatively low solubility in water. N-Methylene phosphonic chitosan (NMPC) is a water-soluble derivative prepared by adding a phosphonic group to chitosan. This study demonstrates that NMPC has a fungicidal effect on the phytopathogenic fungus Fusarium solani f. sp. eumartii (F. eumartii) judged by the inhibition of F. eumartti mycelial growth and spore germination. NMPC affected fungal membrane permeability, reactive oxygen species production, and cell death. Also, this chitosan-derivative exerted antifungal effects against two other phytopathogens, Botrytis cinerea, and Phytophthora infestans. NMPC did not affect tomato cell viability at the same doses applied to these phytopathogens to exert fungicide action. In addition to water solubility, the selective biological cytotoxicity of NMPC adds value in its application as an antimicrobial agent in agriculture.

scholarly journals The water-soluble chitosan derivative, N-methylene phosphonic chitosan, is an effective fungicide against the phytopathogen Fusarium eumartii

2021 ◽  
Author(s):  
Florencia Anabel Mesas ◽  
María Cecilia Terrile ◽  
María Ximena Silveyra ◽  
Adriana Zuñiga ◽  
Maria Susana Rodriguez ◽  
...  
Keyword(s):  
Water Soluble ◽  
Added Value ◽  
In Vivo Studies ◽  
Phytopathogenic Fungus ◽  
Chitosan Derivative ◽  
Industry Waste ◽  
Argentinean Patagonia ◽  
Ic50 Values ◽  
Low Solubility

Chitosan has been considered an environmental-friendly polymer. However, its use in agriculture has not been extended yet due to its relatively low solubility in water. In an attempt to improve such chemical characteristics, a chitosan-derivative prepared by adding a phosphonic group to chitosan N-methylene phosphonic chitosan, NMPC, was obtained from shrimp fishing industry waste from Argentinean Patagonia. This study showed that NMPC had a fungicidal effect on the phytopathogenic fungus Fusarium solani f. sp. eumartii (F. eumartii). NMPC inhibited F. eumartti mycelial growth and spore germination with low IC50 values. In vivo studies showed that NMPC affected fungal membrane permeability, ROS production, and cell death. NMPC also exerted antifungal effects against two other phytopathogens, Botrytis cinerea, and Phytophthora infestans. NMPC did not affect tomato cell viability at the same doses applied to these phytopathogens. Furthermore, the selective cytotoxicity of NMPC could give it added value in its application as an antimicrobial agent in agriculture.

scholarly journals Synthesis of morpholinium salts based on chloroacylated derivatives of dihydroquercetin

2019 ◽  
Vol 59 (7) ◽  
pp. 37-42
Author(s):  
Anton O. Pozdeev ◽  
◽  
Alexander M. Koroteev ◽  
Sofia N. Pimankina ◽  
Mikhail P. Koroteev ◽  
...  
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
High Water ◽  
Water Soluble ◽  
Synthetic Approach ◽  
Solubility In Water ◽  
Natural Amino Acids ◽  
Synthetic Approaches ◽  
Derivatives Of ◽  
Low Solubility

The flavonoid dihydroquercetin and its esterified derivatives possess various biological activities and are widely used as dietary supplements and in pharmacology. A significant disadvantage of this flavonoid is its low solubility in water at ordinary temperatures of up to 0.03%, which negatively affects its biological activity. Nature overcomes this problem by glycosylation, sulfation, and phosphorylation. In chemistry and pharmacology to overcome this problem, there are several synthetic approaches. For dihydroquercetin (DHQ) is the inclusion of DHQ in the cyclodextrin matrix or the formation of a complex of DHQ with basic natural amino acids. In this paper, a method is proposed for obtaining water-soluble morpholinium salts based on chloroacylated derivatives of DHQ. The acylation reaction was carried out in dioxane, pyridine was used as an acceptor of choric hydrogen. The target compounds were obtained with a yield of 68-79%. As a result, chlorinated derivatives based on DHQ and its acyl and benzyl derivatives were synthesized. These derivatives in the interaction with morpholine form its salts, which, as it turned out, have a high water solubility. Pentamorpholine salt of DHQ had the highest solubility in water, up to 6.5% at room temperature, which is 200 times more soluble than the original DHQ. The proposed synthetic approach to increase the water solubility of acyl derivatives of DHQ can be extended using other nitrogenous bases and other haloacyl derivatives of DHQ.

scholarly journals New Active Pharmaceutical Ingredient-Ionic Liquids (API-ILs) Derived from Indomethacin and Mebendazole

Proceedings ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 48 ◽  
Author(s):  
◽  
Emilia Tojo
Keyword(s):  
Ionic Liquids ◽  
Water Solubility ◽  
Methanesulfonic Acid ◽  
Active Pharmaceutical Ingredient ◽  
High Water ◽  
Solubility In Water ◽  
Pharmaceutical Ingredients ◽  
Low Toxicity ◽  
Low Solubility ◽  
High Water Solubility

The transformation of two solid Active Pharmaceutical Ingredients (APIs) into new ionic liquids (IL)s that incorporate APIs (API-ILs) is reported. The structures of the APIs (indomethacin and mebendazole) were selected by their susceptibility to being transformed into API-ILs (either to form the cation or the anion) and their limited bioavailability due to their low solubility in water. The counterions, such as those derived from 2-dimethylaminoethanol (DMEA), tetramethylguanidine (TMG), 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), 1,4-diazabicyclo[2.2.2] (TED), <i>p</i>-toluensulfonic acid, glycolic acid, methanesulfonic acid, and saccharin, were carefully chosen, aiming for high biocompatibility, low toxicity, and high water solubility. The synthesis was carried out by direct treatment of the API with the corresponding selected acid or base. Finally, the solubility in water of all the synthesized salts was determined.

scholarly journals Temperature-Responsive Pyraclostrobin-Loaded Octadecane Submicrocapsules with Lowered Toxicity

Nanomaterials ◽  
2020 ◽  
Vol 10 (12) ◽  
pp. 2374
Author(s):  
Aiym Tleuova ◽  
VSSL Prasad Talluri ◽  
Rohitesh Kumar ◽  
František Štěpánek
Keyword(s):  
Melting Point ◽  
Artemia Salina ◽  
In Vitro Tests ◽  
Technical Grade ◽  
Aquatic Life ◽  
Solubility In Water ◽  
Agricultural Industry ◽  
Antifungal Effects ◽  
Low Solubility

Pyraclostrobin (Pyr) is one of the most effective fungicides. However, it can degrade via photolysis in water, it is toxic to aquatic life and if inhaled, it has a low solubility in water, that leads to difficulties when applying to plants by spraying. Additionally, the necessity of repeated (weekly) sprays of fungicides when the pathogen growth risk is the highest, such as at the temperature range of 24 to 36 °C and increased humidity of about 95%, leads to loss of efficiency of the fungicide and overdose of chemicals. In the present study, pyraclostrobin was microencapsulated to solve the abovementioned issues. As a core of capsules octadecane (OD) with a melting point of 28 °C was used, thus, the release of pyraclostrobin was controlled via temperature change. Pyraclostrobin-loaded submicrocapsules (PyrSMCs) were characterized using SEM, DLS, TGA/DSC, HPLC, FTIR methods; stimuli-responsivity was tested employing in vitro tests with pathogenic culture (Fungal strain of Pyrenophora teres - CPPF-453) grown in Petri dishes. Toxicity of PyrSMCs to Artemia salina was studied as well. Size of capsules was 200–600 nm along with the presence of bigger capsules with a diameter of 1–4 µm. PyrSMCs showed excellent antifungal effects above the melting point of octadecane. PyrSMCs demonstrated 29 times less toxicity than pyraclostrobin of technical grade. Overall, results show the potential of such capsules to be applied in the agricultural industry for precise agriculture strategies.

scholarly journals An Approach to the Use of Glycol Alkoxysilane–Polysaccharide Hybrids in the Conservation of Historical Building Stones

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 938
Author(s):  
Miguel Meléndez-Zamudio ◽  
Ileana Bravo-Flores ◽  
Eulalia Ramírez-Oliva ◽  
Antonio Guerra-Contreras ◽  
Gilberto Álvarez-Guzmán ◽  
...  
Keyword(s):  
Water Solubility ◽  
High Water ◽  
Water Soluble ◽  
Building Stones ◽  
Historical Building ◽  
Solubility In Water ◽  
Angle Measurements ◽  
Historical Monuments ◽  
Contact Angle Measurements ◽  
Stone Consolidants

Stone consolidants have been widely used to protect historical monuments. Consolidants and hydrophobic formulations based on the use of tetraethoxysilane (TEOS) and alkylalkoxysilanes as precursors have been widely applied, despite their lack of solubility in water and requirement to be applied in organic media. In the search for a “greener” alternative based on silicon that has potential use in this field, the use of tetrakis(2-hydroxyethyl)silane (THEOS) and tris(2-hydroxyethyl)methyl silane (MeTHEOS) as precursors, due their high water solubility and stability, is proposed in this paper. It is already known that THEOS and MeTHEOS possess remarkable compatibility with different natural polysaccharides. The investigated approach uses the water-soluble silanes THEOS–chitosan and MeTHEOS–chitosan as a basis for obtaining hybrid consolidants and hydrophobic formulations for the conservation of siliceous and calcareous stones. In the case of calcareous systems, their incompatibility with alkoxysilanes is known and is expected to be solved by the developed hybrid consolidant. Their application in the conservation of building stones from historical and archeological sites from Guanajuato, México was studied. The evaluation of the consolidant and hydrophobic formulation treatment was mainly conducted by determining the mechanical properties and contact angle measurements with satisfactory results in terms of the performance and compatibility with the studied stones.

scholarly journals HSAF-induced antifungal effects in Candida albicans through ROS-mediated apoptosis

RSC Advances ◽  
2016 ◽  
Vol 6 (37) ◽  
pp. 30895-30904 ◽  
Author(s):  
Yanjiao Ding ◽  
Zhenyu Li ◽  
Yaoyao Li ◽  
Chunhua Lu ◽  
Haoxin Wang ◽  
...  
Keyword(s):  
Reactive Oxygen Species ◽  
Candida Albicans ◽  
Antifungal Agent ◽  
Reactive Oxygen Species Production ◽  
Reactive Oxygen ◽  
Oxygen Species ◽  
Binding Model ◽  
Antifungal Effects ◽  
Species Production ◽  
Β Tubulin

HSAF, a potent antifungal agent, induced the apoptosis of Candida albicans through reactive oxygen species production. The binding model of HSAF to β-tubulin was simulated by Amber 12 and shown by PyMoL.

scholarly journals Characterization and Applications of Colloidal Systems as Versatile Drug Delivery Carriers for Parenteral Formulations

2021 ◽  
Vol 14 (2) ◽  
pp. 108
Author(s):  
Lakshmi Kolluru ◽  
Prachi Atre ◽  
Syed Rizvi
Keyword(s):  
Drug Delivery ◽  
Water Solubility ◽  
Water Soluble ◽  
Cell Membrane Permeability ◽  
Low Permeability ◽  
Colloidal Systems ◽  
Drug Candidates ◽  
Nano Emulsion ◽  
Stability Issues ◽  
Low Solubility

Preparing a suitable formulation for parenteral administration is already a difficult task; this, coupled with poor water-soluble new chemical entity (NCE), complicates this situation even further. There are several methodologies available to enhance water solubility, but this alone does not entail successful formulation. Making a micro/nano emulsion with a suitable surfactant not only increases the drug solubility but also the cell membrane permeability. Thus, not only biopharmaceutic classification system (BCS)-II (low solubility compounds) but also BCS-III (low permeability) and BCS-IV drugs (low solubility and low permeability) can be further exploited. Those drug candidates otherwise will not move further in NCE evaluation or clinical trials. This succinct review article delves into various aspects of biphasic micro/nano emulsion systems for parenteral drug delivery including the structure of the biphasic colloidal systems, characterization parameters, stability issues, regulatory considerations, and applications in life sciences.

UV LED Curing Formulation for Polyacrylamide Hydrogels

2015 ◽  
Vol 1125 ◽  
pp. 84-88
Author(s):  
Nur Farizah Ayub ◽  
Shahrir Hashim ◽  
Jamarosliza Jamaluddin ◽  
Roshafima Rasit Ali ◽  
Nadia Adrus
Keyword(s):  
Water Solubility ◽  
Monochromatic Light ◽  
Green Technology ◽  
Water Soluble ◽  
Light Sources ◽  
Water Addition ◽  
Solubility In Water ◽  
Polyacrylamide Hydrogels ◽  
Uv Led ◽  
Trade Name

Current studies showed that UV LED system is a green technology and highly efficient as compared to UV Mercury (UV Hg) system. In this study, the UV LED curing formulations of polyacrylamide (PAAm) hydrogels were developed. The formulations consisted of acrylamide (AAm) as a main monomer,N,N’-methylenebisacrylamide as a crosslinker and photoinitiator. UV LED emits monochromatic light sources only (365 nm or 385 nm). Thus, in order to developed formulation of UV LED curable hydrogels, a suitable water soluble photoinitiator (i.e. λ ~ 365 nm) has to be employed. A commercially available photoinitiator Oligo [2-hydroxy-2-methyl-1-[4-(1-methylvinyl) phenyl] propanone] under the trade name Chivacure 300 (λ ~ 330 nm) was chosen in the first formulations. However, due to limited solubility in water, addition of tetrahydrofuran (THF) at 9.5:0.5 ratio of water/THF was required for Chivacure 300. We also synthesized a photoinitiator based on 2,2-dimethoxy-2-phenyl acetophenone (DMPA) and methylated-β-cyclodextrin (MβCD) to be used in the second formulation. The complexation of DMPA and MβCD resulted in transparent and water-soluble supramolecular-structured photoinitiator (SSPI) (λ ~ 330 nm). Both formulations were irradiated using UV LED system (Hoenle AG, Germany, 365 nm) for 15 min. Synthesis of PAAm hydrogels with both photoinitiators has yielded almost complete conversion of hydrogels (> 80 %). Clearly, this study has revealed that enhanced formulation of UV LED curable hydrogels are due to appropriate choice of excellent water-solubility photoinitiators (Chivacure 300 and modified DMPA). We concluded that UV LED is an important tool for curing hydrogel formulations of various acrylate water-based monomers.

scholarly journals Current Applications of Nanoemulsions in Cancer Therapeutics

Nanomaterials ◽  
2019 ◽  
Vol 9 (6) ◽  
pp. 821 ◽  
Author(s):  
Elena Sánchez-López ◽  
Mariana Guerra ◽  
João Dias-Ferreira ◽  
Ana Lopez-Machado ◽  
Miren Ettcheto ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Water Solubility ◽  
Cancer Therapeutics ◽  
Pharmaceutical Formulations ◽  
Water Soluble ◽  
Hydrophobic Core ◽  
Research Areas ◽  
Reduce Tumor Growth ◽  
Tumoral Cells ◽  
Low Solubility

Nanoemulsions are pharmaceutical formulations composed of particles within a nanometer range. They possess the capacity to encapsulate drugs that are poorly water soluble due to their hydrophobic core nature. Additionally, they are also composed of safe gradient excipients, which makes them a stable and safe option to deliver drugs. Cancer therapy has been an issue for several decades. Drugs developed to treat this disease are not always successful or end up failing, mainly due to low solubility, multidrug resistance (MDR), and unspecific toxicity. Nanoemulsions might be the solution to achieve efficient and safe tumor treatment. These formulations not only solve water-solubility problems but also provide specific targeting to cancer cells and might even be designed to overcome MDR. Nanoemulsions can be modified using ligands of different natures to target components present in tumor cells surface or to escape MDR mechanisms. Multifunctional nanoemulsions are being studied by a wide variety of researchers in different research areas mainly for the treatment of different types of cancer. All of these studies demonstrate that nanoemulsions are efficiently taken by the tumoral cells, reduce tumor growth, eliminate toxicity to healthy cells, and decrease migration of cancer cells to other organs.

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