scholarly journals Discovery of New Cyclopentaquinoline Analogues as Multifunctional Agents for the Treatment of Alzheimer’s Disease

2019 ◽  
Vol 20 (3) ◽  
pp. 498 ◽  
Author(s):  
Kamila Czarnecka ◽  
Małgorzata Girek ◽  
Paweł Kręcisz ◽  
Robert Skibiński ◽  
Kamil Łątka ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Molecular Modeling ◽  
Physicochemical Properties ◽  
Amyloid Beta ◽  
Mixed Type ◽  
Biological Assessment ◽  
Assay Method ◽  
Compound A ◽  
Receptor Interactions ◽  
Multifunctional Agents

Here we report the two-step synthesis of 8 new cyclopentaquinoline derivatives as modifications of the tetrahydroacridine structure. Next, the biological assessment of each of them was performed. Based on the obtained results we identified 6-chloro-N-[2-(2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylamino)-hexyl]]-nicotinamide hydrochloride (3e) as the most promising compound with inhibitory potencies against EeAChE and EqBuChE in the low nanomolar level 67 and 153 nM, respectively. Moreover, 3e compound is non-hepatotoxic, able to inhibit amyloid beta aggregation, and shows a mix-type of cholinesterase’s inhibition. The mixed type of inhibition of the compound was confirmed by molecular modeling. Then, yeast three-hybrid (Y3H) technology was used to confirm the known ligand-receptor interactions. New derivatives do not show antioxidant activity (confirmed by the use of two different tests). A pKa assay method was developed to identify the basic physicochemical properties of 3e compound. A LogP assay confirmed that 3e compound fulfills Lipinsky’s rule of five

scholarly journals Development of Novel 2-Acetylphenol-O-Alkylhydroxyethylamine Derivatives as Multifunctional Agents for Alzheimer’s Disease Treatment

2021 ◽  
Author(s):  
Gaofeng zhu ◽  
xinfeng li ◽  
Jing Yang ◽  
ying he ◽  
jing mi ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Metal Ions ◽  
Blood Brain Barrier ◽  
Mixed Type ◽  
Ache Inhibition ◽  
Disease Treatment ◽  
Neuroprotective Effects ◽  
Mao B ◽  
Multifunctional Agents

Abstract Due to the complex pathogenesis of AD, the multi-target-directed ligands (MTDLs) strategy presented the best pharmacological option for AD treatment. Herein, a series of novel 2-acetylphenol-O-alkylhydroxyethylamine derivatives was rationally designed and synthesized. Of these derivatives, 5c was a good multifunctional agent (eeAChE IC50 =7.9 μM, MAO-B IC50 = 9.9 μM, BACE1 IC50 = 8.3 μM) in vitro and displayed a mixed-type AChE inhibition, which could bind to the CAS and PAS of AChE. Compound 5c also exhibited good antioxidant activity (ORAC = 2.5 eq) and neuroprotective effects. Furthermore, compound 5c was a selective metal ions chelator. And it could cross blood-brain barrier in vitro and complied with drug-like properties rule of 5. Therefore, compound 5c was a promising multifunctional agent for the treatment of AD.

scholarly journals In vitro activities of Acacia nilotica (L.) Delile bark fractions against Oral Bacteria, Glucosyltransferase and as antioxidant

2020 ◽  
Vol 20 (1) ◽  
Author(s):  
Ali Mahmoud Muddathir ◽  
Ebtihal Abdalla M. Mohieldin ◽  
Tohru Mitsunaga
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Gallic Acid ◽  
Crude Extract ◽  
Inhibitory Activity ◽  
Oral Bacteria ◽  
Acacia Nilotica ◽  
Assay Method ◽  
Medicinal Uses ◽  
Wide Range

Abstract Background Dental caries and periodontal disease are the most common chronic infectious oral diseases in the world. Acacia nilotica was commonly known in Sudan as Garad or Sunt has a wide range of medicinal uses. In the present study, antibacterial activity of oral bacteria (Streptococcus sobrinus and Porphyromonas gingivalis), inhibitory activity against glucosyltransferase (GTF) enzyme and antioxidant activity were assayed for methanolic crude extract of A. nilotica bark and its fractions. Methods Methanoilc crude extract of A. nilotica bark was applied to a Sephadex LH-20 column and eluted with methanol, aqueous methanol, and finally aqueous acetone to obtain four fractions (Fr1- Fr4). Furthermore, the crude extract and fractions were subjected to analytical high performance liquid chromatography (HPLC). The crude extract and its fractions were assayed for antibacterial activity against S. sobrinus and P. gingivalis using a microplate dilution assay method to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC), as well as GTF inhibition and antioxidant activity using ABTS radical scavenging method. Results Fractions (Fr1 and Fr2) exhibited MIC values of 0.3 mg/ml against the P. gingivalis. Additionally, Fr2 displayed MBC value of 1 mg/ml against two types of bacteria. Fr4 showed an especially potent GTF inhibitory activity with IC50 value of 3.9 μg/ml. Fr1 displayed the best antioxidant activity with IC50 value of 1.8 μg/ml. The main compound in Fr1 was identified as gallic acid, and Fr2 was mostly a mixture of gallic acid and methyl gallate. Conclusions The results obtained in this study provide some scientific rationale and justify the use of this plant for the treatment of dental diseases in traditional medicine. A. nilotica bark, besides their antibacterial potentiality and GTF inhibitory activity, it may be used as adjuvant antioxidants in mouthwashes. Further studies in the future are required to identify the rest of the active compounds.

scholarly journals Relationships Linking the Colour and Elemental Concentrations of Blossom Honeys with Their Antioxidant Activity: A Chemometric Approach

Agriculture ◽  
2021 ◽  
Vol 11 (8) ◽  
pp. 702
Author(s):  
Monika Kędzierska-Matysek ◽  
Anna Teter ◽  
Małgorzata Stryjecka ◽  
Piotr Skałecki ◽  
Piotr Domaradzki ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Physicochemical Properties ◽  
Black Locust ◽  
Antioxidant Properties ◽  
Principal Component ◽  
Botanical Origin ◽  
Antioxidant Parameters ◽  
Colour Parameters ◽  
Hue Angle ◽  
Chemometric Approach

The antioxidant activity of honey depends on the botanical origin, which also determines their physicochemical properties. In this study, a multivariate analysis was used to confirm potential relationships between the antioxidant properties and colour parameters, as well as the content of seven elements in five types of artisanal honey (rapeseed, buckwheat, linden, black locust, and multifloral). The type of honey was found to significantly influence most of its physicochemical properties, colour parameters, and the content of potassium, manganese and copper. Antioxidant parameters were shown to be significantly positively correlated with redness and concentrations of copper and manganese, but negatively correlated with the hue angle and lightness. The principal component analysis confirmed that the darkest buckwheat honey had the highest antioxidant activity in combination with its specific colour parameters and content of antioxidant minerals (manganese, copper and zinc). The level of these parameters can be potentially used for the identification of buckwheat honey.

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 SIFAT FISIKOKIMIA HAND AND BODY CREAM DENGAN PEMANFAATAN EKSTRAK ETANOL BUNGA GEMITIR (Tagetes erecta L.) DAN BUNGA PACAR AIR MERAH (Impatiens balsamina L.) DARI LIMBAH CANANG

2017 ◽  
Vol 5 (1) ◽  
pp. 1
Author(s):  
Dewa Ayu Ika Paramitha ◽  
James Sibarani ◽  
Ni Made Suaniti
Keyword(s):  
Antioxidant Activity ◽  
Physicochemical Properties ◽  
National Standard ◽  
Tagetes Erecta ◽  
Basic Formula ◽  
Impatiens Balsamina ◽  
Ethanol Extracts ◽  
Tagetes Erecta L ◽  
Microbial Numbers

ABSTRAK: Pada penelitian ini dilakukan pengembangan formula sediaan hand and body cream dengan memanfaatkan sumber antioksidan yang dimiliki oleh dua jenis ekstrak etanol yaitu ekstrak bunga pacar air merah (Impatiens balsamina L.) dan bunga gemitir (Tagetes erecta L.) dengan taraf perlakuan sebesar 1% dari masing-masing ekstrak (FPM dan FG) dan campuran 0,5% ekstrak pacar air merah dan 0,5% ekstrak gemitir (FCPMG). Pengujian terhadap  produk dilakukan pada sifat fisikokimia  meliputi pH, viskositas, aktivitas antioksidan, angka lempeng total mikroba, dan ukuran partikel. Berdasarkan hasil pengujian produk hand and body cream yang dihasilkan memiliki antioksidan yang cukup tinggi sebagai produk perawatan tubuh dengan penambahan 1% ekstrak etanol pacar air merah, gemitir dan campuran dari kedua ekstrak etanol. Kualitas produk hand and body cream yang dihasilkan baik dan memenuhi standar mutu SNI dari aspek nilai pH, viskositas, dan nilai ALT. Warna yang dihasilkan mulai dari warna kuning kemerahan sampai dengan warna kuning, dan partikel yang dimiliki oleh produk adalah nanopartikel dengan sistem polidispersi. ABSTRACT: Formulations of hand and body creams using ethanol extracts of flowers of red Impatiens balsamina L. And Tagetes erecta L. As antioxidant sources have been developed.  One percent of  extracts (FPM and FG) and the mixture of 0.5% each extracts (FCPMG) were added to the basic formula. The analysis of physicochemical properties of the products was conducted including pH, viscosity, antioxidant activity, the size of the particles, and total microbial plate numbers. Based on the results, the quality of the hand and body creams meet the national standard of Indonesia (SNI) regarding to pH, viscosity, and the total microbial numbers. The colours of the hand and body creams resulted are reddish yellow to yellow with polydispersion nanoparticles.

Sign in / Sign up

Export Citation Format

Share Document