scholarly journals Synthesis, Physicochemical Properties, and Biological Activities of 4-(S-Methyl-N-(2,2,2-Trifluoroacetyl)Sulfilimidoyl) Anthranilic Diamide

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3451 ◽  
Author(s):  
Hwan Jung Lim ◽  
Won Hyung Lee ◽  
Seong Jun Park
Keyword(s):  
Physicochemical Properties ◽  
Physical Properties ◽  
Strong Correlation ◽  
Biological Activities ◽  
Organosulfur Compounds ◽  
Anthranilic Diamide ◽  
New Crop ◽  
Insecticidal Activities

Novel anthranilic diamides with sulfilimidoyl and sulfoximidoyl functionalities were successfully prepared. Among newly-prepared organosulfur compounds, 3-bromo-1-(3-chloropyridin-2-yl)-N-(2-methyl-6-(methylcarbamoyl)-4-(methylthio)phenyl)-1H-pyrazole-5-carboxamide and (S,E)-3-bromo-1-(3-chloropyridin-2-yl)-N-(2-methyl-4-(S-methyl-N-(2,2,2-trifluoroacetyl)sulfinimidoyl)-6-(methylcarbamoyl)phenyl)-1H-pyrazole-5-carboxamide showed good levels of efficacy and a strong correlation between insecticidal activities and physical properties, respectively. In particular, available data indicated that the N-trifluoroacetyl sulfilimine moiety could be an appealing structural scaffold for the discovery of a new crop-protecting agent.

Physicochemical Characterization and Antinociceptive Effect of β-cyclodextrin/Lippia pedunculosa Essential Oil in Mice

2018 ◽  
Vol 18 (9) ◽  
pp. 797-807 ◽  
Author(s):  
Paula dos Passos Menezes ◽  
Francielly de Oliveira Araujo ◽  
Tatianny Araujo Andrade ◽  
Igor Araujo Santos Trindade ◽  
Heitor Gomes de Araujo-Filho ◽  
...  
Keyword(s):  
Essential Oil ◽  
Physicochemical Properties ◽  
Water Solubility ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Antinociceptive Effect ◽  
Physicochemical Characterization ◽  
Good Tool ◽  
Main Challenge ◽  
Higher Temperature

Background: Some research studies have shown that Lippia pedunculosa essential oil (EOLP) has interesting biological activities. However, its low water solubility is the main challenge to achieve its therapeutic potential. In this context, Cyclodextrins (CDs) have been widely used in order to overcome this problem due to your capability to improve the physicochemical properties of drugs. Objective: In this perspective, the main goal of this study was to investigate how the improvement of the physicochemical properties of inclusion complexes (EOLP and β-CD) enhance the antinociceptive effect in mice. Methods: To achieve that, we prepared samples by Physical Mixture (PM), Paste Complexation (PC) and Slurry Complexation (SC) methods, followed by their physicochemical characterization. In addition, it was evaluated if the use of β-CD enhances the antinociceptive effect of EOLP in mice. Results: The analysis showed that rotundifolone (72.02%) was the major compound of EOLP and we found out based on DSC results that β-CD protected it from oxidation. In addition, TG techniques demonstrated that the best inclusion methods were PC and SC, due to their greater weight loss (10.8 and 11.6%, respectively) in the second stage (171-312°C), indicating that more complexed oil was released at the higher temperature than oil free. Other characteristics, such as changes in the typical crystalline form, and reduced particle size were observed by SEM and laser diffraction, respectively. The SC was the most effective complexation method, once the presence of rotundifolone was detected by FTIR. Based on that, SC method was used in all mice tests. In this regard, the number of paw licks was reduced for both compounds (all doses), but EOLP was more effective in reducing the nociceptive behavior. Conclusion: Therefore, CDs seem not to be a good tool to enhance the pharmacological properties of EOs rich in peroxide compounds such as rotundifolone.

scholarly journals Hepatoprotective Effect of Mixture of Dipropyl Polysulfides in Concanavalin A-Induced Hepatitis

Nutrients ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 1022
Author(s):  
Dragana Arsenijevic ◽  
Bojana Stojanovic ◽  
Jelena Milovanovic ◽  
Aleksandar Arsenijevic ◽  
Milos Simic ◽  
...  
Keyword(s):  
Concanavalin A ◽  
Messenger Rna ◽  
T Regulatory Cells ◽  
Mononuclear Cells ◽  
Biological Activities ◽  
Biologically Active ◽  
Organosulfur Compounds ◽  
Liver Inflammation ◽  
Regulatory Cells ◽  
Active Components

The main biologically active components of plants belonging to the genus Allium, responsible for their biological activities, including anti-inflammatory, antioxidant and immunomodulatory, are organosulfur compounds. The aim of this study was to synthetize the mixture of dipropyl polysulfides (DPPS) and to test their biological activity in acute hepatitis. C57BL/6 mice were administered orally with DPPS 6 h before intravenous injection of Concanavalin A (ConA). Liver inflammation, necrosis and hepatocytes apoptosis were determined by histological analyses. Cytokines in liver tissue were determined by ELISA, expression of adhesive molecules and enzymes by RT PCR, while liver mononuclear cells were analyzed by flow cytometry. DPPS pretreatment significantly attenuated liver inflammation and injury, as evidenced by biochemical and histopathological observations. In DPPS-pretreated mice, messenger RNA levels of adhesion molecules and NADPH oxidase complex were significantly reduced, while the expression of SOD enzymes was enhanced. DPPS pretreatment decreased protein level of inflammatory cytokines and increased percentage of T regulatory cells in the livers of ConA mice. DPPS showed hepatoprotective effects in ConA-induced hepatitis, characterized by attenuation of inflammation and affection of Th17/Treg balance in favor of T regulatory cells and implicating potential therapeutic usage of DPPS mixture in inflammatory liver diseases.

scholarly journals Physicochemical Properties and Biological Activity of Active Films Based on Corn Peptide Incorporated Carboxymethyl Chitosan

Coatings ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 604
Author(s):  
Liyan Wang ◽  
Liang Lei ◽  
Kang Wan ◽  
Yuan Fu ◽  
Hewen Hu
Keyword(s):  
Antioxidant Activity ◽  
Physicochemical Properties ◽  
Food Packaging ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Carboxymethyl Chitosan ◽  
Vapor Permeability ◽  
Zone Method ◽  
Oil Resistance

Active films based on carboxymethyl chitosan incorporated corn peptide were developed, and the effect of the concentration of corn peptide on films was evaluated. Physicochemical properties of the films, including thickness, opacity, moisture content, color, mechanical properties, water vapor permeability, and oil resistance, were measured. Biological activities of the films, including the antioxidant and antibacterial activities, were characterized in terms of 2, 2-diphenyl-1-picrylhydrazyl free radical scavenging activity, reducing power, the total antioxidant activity, and the filter disc inhibition zone method. The results indicated that the incorporation of corn peptide caused interactions between carboxymethyl chitosan and corn peptide in Maillard reaction and gave rise to the films light yellow appearance. Compared with the Control, the degree of glycosylation, browning intensity, thickness, opacity, tensile strength, antioxidant activity, and antibacterial activity of films were increased, but the elongation, vapor permeability, and oil resistance of films were decreased. The films based on corn peptide and carboxymethyl chitosan can potentially be applied to food packaging.

scholarly journals Synthesis and biological activities of two camptothecin derivatives against Spodoptera exigua

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Fulai Yang ◽  
Liping Wang ◽  
Lan Zhang ◽  
Yanning Zhang ◽  
Liangang Mao ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Spodoptera Exigua ◽  
Insect Pests ◽  
Biological Activities ◽  
Beet Armyworm ◽  
Esterification Reaction ◽  
Contact Toxicity ◽  
Compound A ◽  
High Concentrations ◽  
Insecticidal Activities

AbstractCamptothecin (CPT), a natural alkaloid isolated from Camptotheca acuminata Decne, is found to show potential insecticidal activities with unique action mechanisms by targeting at DNA-topoisomease I (Top1) complex and inducing cell apoptosis. To improve the efficacy against insect pests, two camptothecin (CPT) derivatives were synthesized through introducing two functional groups, 2-nitroaminoimidazoline and 1-chloro-2-isocyanatoethane by esterification reaction. The insecticidal activities of these two derivatives were evaluated at contact toxicity, cytotoxicity and topoisomerase I (Top1) inhibitory activities comparing with CPT and hydroxyl-camptothecin (HCPT). Results showed that compound a, synthesized by introducing 2-nitroaminoimidazoline to CPT, apparently increased contact toxicity to the third larvae of beet armyworm, Spodoptera exigua, and cytotoxicity to IOZCAS-Spex-II cells isolated from S. exigua. However, the inhibition on DNA relaxation activity of Top1 was reduced to less than 5 percentage even at high concentrations (50 and 100 μM). For introducing 1-chloro-2-isocyanatoethane to HCPT, the contact toxicity, cytotoxicity and Top1 inhibitory activity of synthesized compound b were increased significantly compared to CPT and HCPT. These results suggested that both synthesized compounds possessed high efficacy against S. exigua by targeting at Top1 (compound b) or novel mechanism of action (compound a).

scholarly journals Preliminary Studies Regarding the Physicochemical Characteristics of Some Balsamic Vinegars

1970 ◽  
Vol 66 (2) ◽  
Author(s):  
Delia Mihaela TRUTA ◽  
Maria TOFANA ◽  
Sonia Ancuţa SOCACI ◽  
Rowena CHELEMAN
Keyword(s):  
Physicochemical Properties ◽  
Physical Properties ◽  
Quality Evaluation ◽  
Physicochemical Characteristics ◽  
Production Method ◽  
Chemical Information ◽  
Grape Must ◽  
The Third ◽  
The Future ◽  
Balsamic Vinegar

The aim of this work is to analyze the chemical and physical properties of balsamic vinegar, in order to improve the chemical information about this product, useful for its authentication and quality evaluation. Using three balsamic vinegars purchased in local markets as samples, this study investigated the labeling and the physicochemical properties of commercial concentrated balsamic vinegar in order to understand their production method and quality. Two of the samples were balsamic vinegars from Modena (BVM) and the third was a balsamic vinegar from Kalamata (BVK). According to the labels, all the balsamic vinegars samples were made of grape must and had an acidity of 6%. The appearance of the samples of vinegar differed significantly, but the acidity from the label was the same for all. Since people are paying much more attention to health, the number of concentrated vinegar products is expected to increase in the future. Thus, appropriate rules and physicochemical properties are required to regulate vinegar production and quality.

scholarly journals Effect of physicochemical properties and phenolic compounds of bifloral propolis on antioxidant and antimicrobial capacity

Nova Scientia ◽  
2020 ◽  
Vol 12 (24) ◽  
Author(s):  
Rey David Vargas Sánchez ◽  
Evelin Martínez Benavidez ◽  
Javier Hernández ◽  
Gastón Ramón Torrescano Urrutia ◽  
Armida Sánchez Escalante
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Phenolic Compounds ◽  
Physicochemical Properties ◽  
Phenolic Content ◽  
Biological Activities ◽  
Sensory Characteristics ◽  
Total Phenolic ◽  
Gram Positive ◽  
Phenolic Components

In this study the effect of pollen source (mesquite and catclaw) on the sensory characteristics (appearance, color, aroma, taste, consistency and visible impurities), and physicochemical properties of raw propolis, and the phenolic content and biological activities of propolis extracts (PEs) was determined. The phenolic composition of PEs was determined by the total phenolic (TPC), flavone and flavonol (FFC), and flavanone and dihydroflavonol content (FDC). The individual phenolic components were analyzed by HPLC-DAD. The antioxidant activity was determined by the ferric-reducing power (FRAP) and free-radical scavenging activity (FRS). The antibacterial activity was evaluated against Gram-positive (Staphylococcus aureus and Listeria innocua) and Gram-negative (Echerichia coli and Salmonella thyphimurium) bacteria. The results showed that sensory characteristic and physicochemical properties of mesquite and catclaw propolis complied with international quality regulations. Fifteen phenolic compounds were identified, of which pinocembrin, naringenin, galangin, chrysin and quercetin were found a high concentration (> 3 mg/g). Mesquite propolis had the highest phenolic content (TFC and FDC), as well as antioxidant activity (> 2.5 mg Fe (II) equivalent/g; > 40% of DPPH radical inhibition) and antibacterial activity against Gram-positive bacterias in the order S. aureus > L. innocua (> 50% of inhibition for both bacterias at 500 µg/mL). These results indicating that pollen source affect the sensory characteristics and physicochemical properties of propolis, as well as the biological activity of their extracts.

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