scholarly journals Synthesis and Evaluation of Biological Activity of New Arylphosphoramidates

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Amal Thebti ◽  
M. A. K. Sanhoury ◽  
H-I. Ouzari ◽  
T. Barhoumi-slimi
Keyword(s):  
Biological Activity ◽  
Ir Spectroscopy ◽  
Acetylcholinesterase Activity ◽  
Inhibitory Effect ◽  
Bacterial Strains ◽  
Significant Inhibitory Effect ◽  
Subsequent Addition

The synthesis of new substituted arylphosphoramidates is performed in two steps through phosphorylation of the corresponding alcohols followed by aminolysis. The formation of the desired phosphoramidates depends on the subsequent addition of the two alcohols with the amine being added at the last step. The products were obtained in 58–95% yields. They were characterized mainly by multinuclear (1H, 13C, 31P, and 19F) NMR and IR spectroscopy. In addition, the antimicrobial and antiacetylcholinesterase activities were evaluated. The results showed acetylcholinesterase activity by some compounds, whilst no significant inhibitory effect against the tested bacterial strains has been recorded.

scholarly journals In Vitro Evaluation and Docking Studies of 5-oxo-5H-furo[3,2-g]chromene-6-carbaldehyde Derivatives as Potential Anti-Alzheimer’s Agents

2019 ◽  
Vol 20 (21) ◽  
pp. 5451
Author(s):  
Malose J. Mphahlele ◽  
Samantha Gildenhuys ◽  
Emmanuel N. Agbo
Keyword(s):  
Breast Cancer ◽  
Biological Activity ◽  
Active Sites ◽  
Kinetic Studies ◽  
Inhibitory Effect ◽  
Docking Studies ◽  
Significant Inhibitory Effect ◽  
Anti Oxidant ◽  
Mcf 7

A series of novel 2-carbo–substituted 5-oxo-5H-furo[3,2-g]chromene-6-carbaldehydes and their 6-(4-trifluoromethyl)phenylhydrazono derivatives have been prepared and evaluated for biological activity against the human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The most active compounds from each series were, in turn, evaluated against the following enzyme targets involved in Alzheimer’s disease, β-secretase (BACE-1) and lipoxygenase-15 (LOX-15), as well as for anti-oxidant potential. Based on the in vitro results of ChE and β-secretase inhibition, the kinetic studies were conducted to determine the mode of inhibition by these compounds. 2-(4-Methoxyphenyl)-5-oxo-5H-furo[3,2-g]chromene-6-carbaldehyde (2f), which exhibited significant inhibitory effect against all these enzymes was also evaluated for activity against the human lipoxygenase-5 (LOX-5). The experimental results were complemented with molecular docking into the active sites of these enzymes. Compound 2f was also found to be cytotoxic against the breast cancer MCF-7 cell line.

Preliminary in Vitro Investigations on The Inhibitory Activity of The Original Dietary Supplement Oxidal® on Pathogenic Bacterial Strains

2020 ◽  
Vol 11 ◽  
pp. 37-43
Author(s):  
Prof. Teodora P. Popova ◽  
Toshka Petrova ◽  
Ignat Ignatov ◽  
Stoil Karadzhov
Keyword(s):  
Dietary Supplement ◽  
Broad Spectrum ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Clinical Effectiveness ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Microbial Strains

The antimicrobial action of the dietary supplement Oxidal® was tested using the classic Bauer and Kirby agar-gel diffusion method. Clinical and reference strains of Staphylococcus aureus and Escherichia coli were used in the studies. The tested dietary supplement showed a well-pronounced inhibitory effect against the microbial strains commensurable with that of the broad-spectrum chemotherapeutic agent Enrofloxacin and showed even higher activity than the broad spectrum antibiotic Thiamphenicol. The proven inhibitory effect of the tested dietary supplement against the examined pathogenic bacteria is in accordance with the established clinical effectiveness standards for antimicrobial agents.

Potential antidiarrheal agents: 1-(11-Cyano-6,11-dihydrodibenzo[b,e]thiepin-11-yl-alkyl)- and 1-(10-cyano-10,11-dihydrodibenzo[b,f]thiepin-10-yl-alkyl)-4-substituted piperidines

1985 ◽  
Vol 50 (5) ◽  
pp. 1089-1096 ◽  
Author(s):  
Karel Šindelář ◽  
Jan Metyš ◽  
Miroslav Protiva
Keyword(s):  
Inhibitory Effect ◽  
Substitution Reactions ◽  
Significant Inhibitory Effect

Substitution reactions of 11-(2-bromoethyl)- and 11-(3-bromopropyl)-6,11-dihydrodibenzo[b,e]thiepin-11-carbonitrile and further of 10-(2-bromoethyl)- and 10-(3-bromopropyl)-10,11-dihydrodibenzo[b,f]thiepin-10-carbonitrile with ethyl 4-phenylpiperidine-4-carboxylate, 4-phenylpiperidin-4-ol, 4-(2-tolyl)piperidin-4-ol, 4-(4-fluorophenyl)piperidin-4-ol, 4-(2-oxobenzimidazolin-1-yl)-piperidine and 1-phenyl-1,3,8-triazaspiro[4,5]decan-4-one afforded the tricyclic piperidinoalkyl nitriles IV-XIII which are cyclic analogues of the antidiarrheal agents diphenoxylate (I) and loperamide (III). Out of the compounds prepared only IV and XI showed a significant inhibitory effect towards diarrhea elicited by intravenously administered serotonin in mice.

scholarly journals A novel BRD4 inhibitor suppresses osteoclastogenesis and ovariectomized osteoporosis by blocking RANKL-mediated MAPK and NF-κB pathways

2021 ◽  
Vol 12 (7) ◽  
Author(s):  
Ying Liu ◽  
Wenjie Liu ◽  
Ziqiang Yu ◽  
Yan Zhang ◽  
Yinghua Li ◽  
...  
Keyword(s):  
Bone Loss ◽  
Osteoporosis Treatment ◽  
Inhibitory Effect ◽  
Specific Gene ◽  
Actin Ring ◽  
Treatment Target ◽  
Significant Inhibitory Effect ◽  
Promising Treatment

AbstractBromodomain-containing protein 4 (BRD4) has emerged as a promising treatment target for bone-related disorders. (+)-JQ1, a thienotriazolodiazepine compound, has been shown to inhibit pro-osteoclastic activity in a BRD4-dependent approach and impede bone loss caused by ovariectomy (OVX) in vivo. However, clinical trials of (+)-JQ1 are limited because of its poor druggability. In this study, we synthesized a new (+)-JQ1 derivative differing in structure and chirality. One such derivative, (+)-ND, exhibited higher solubility and excellent inhibitory activity against BRD4 compared with its analogue (+)-JQ1. Interestingly, (-)-JQ1 and (-)-ND exhibited low anti-proliferative activity and had no significant inhibitory effect on RANKL-induced osteoclastogenesis as compared with (+)-JQ1 and (+)-ND, suggesting the importance of chirality in the biological activity of compounds. Among these compounds, (+)-ND displayed the most prominent inhibitory effect on RANKL-induced osteoclastogenesis. Moreover, (+)-ND could inhibit osteoclast-specific gene expression, F‐actin ring generation, and bone resorption in vitro and prevent bone loss in OVX mice. Collectively, these findings indicated that (+)-ND represses RANKL‐stimulated osteoclastogenesis and averts OVX-triggered osteoporosis by suppressing MAPK and NF-κB signalling cascades, suggesting that it may be a prospective candidate for osteoporosis treatment.

New Galantamine Derivatives with Inhibitory Effect on Acetylcholinesterase Activity

2021 ◽  
Vol 83 (3) ◽  
pp. 1211-1220 ◽  
Author(s):  
Maria I. Lazarova ◽  
Daniela S. Tsekova ◽  
Lyubka P. Tancheva ◽  
Kiril T. Kirilov ◽  
Diamara N. Uzunova ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Memory Performance ◽  
Acetylcholinesterase Activity ◽  
Inhibitory Effect ◽  
Long Term Memory ◽  
Molegro Virtual Docker ◽  
Ache Inhibitors ◽  
Hybrid Molecules ◽  
Ache Inhibitory Activity ◽  
Biological Assessments

Background: Inhibitors of acetylcholinesterase (AChE) are used to treat many disorders, among which are neurodegenerative upsets, like Alzheimer’s disease (AD). One of the limited licensed AChE inhibitors (AChEIs) used as drugs is the natural compound galantamine (Gal). Objective: As Gal is a toxic compound, here we expose data about its four derivatives in hybrid peptide-norgalantamine molecules, which have shown 100 times lower toxicity. Methods: Four newly synthesized galantamine derivatives have been involved in docking analysis made by Molegro Virtual Docker. Biological assessments were performed on ICR male mice. The change in short and long-term memory performance was evaluated by passive avoidance test. AChE activity and levels of main oxidative stress parameters: lipid peroxidation, total glutathione (GSH), enzyme activities of catalase (CAT), superoxide dismutase, and glutathione peroxidase were measured in brain homogenates. Results: Our experimental data revealed that the new hybrid molecules did not impair memory performance in healthy mice. Two of the compounds demonstrated better than Gal AChE inhibitory activity in the brain. None of them changed the level of lipid peroxidation products, one of the compounds increased GSH levels, and all of them increased CAT enzyme activity. Conclusion: The new galantamine-peptide hybrids demonstrated a potential for inhibition of AChE and antioxidant activity and deserve further attention.

scholarly journals Isolasi dan Identifikasi Senyawa Fenolik dari Kulit Akar Tumbuhan Artocarpus Dadah Miq 63-74

2015 ◽  
Vol 4 (2) ◽  
pp. 205
Author(s):  
Indarto Indarto
Keyword(s):  
Biological Activity ◽  
Phenolic Compounds ◽  
Ir Spectroscopy ◽  
The Other ◽  
Flash Chromatography ◽  
Rare Plant ◽  
Isolation And Purification ◽  
Phenolic Group ◽  
The Village ◽  
Murine Leukemia

Artocarpus plant  dadah  Miq.  is one of the species of Artocarpus of the Moraceae family that belongs to a rare plant in nature. This plant is known as the main source of phenolic derivative compound that is flavone compound  in  or  tri-oxygenated and terisoprenilasi in C-3 position ,  and also known as the main source of phenolic compound derived flavonoids, aryl-benzofuran, stilbenoid and xanthane flavonoida, which have biological activity as promoters antitumor, antibacterial, antifungal, antiimflamatori, antikanker and others. This study aimed to isolate and identify the phenolic compounds contained in plant  A .  dadah obtained from the village of Purwoasri, North Metro District, Metro City, Lampung Province. Research stages include collection and sample preparation and extraction, isolation, and purification of compounds using KCV method, flash chromatography  , KKG, and TLC, while the identification of compounds is performed using ultraviolet-visible (UV-VIS) and infrared (IR) spectroscopy. In the present study, three compounds were isolated, one of which was estimated to be flavonoid compounds based on UV-VIS and IR spectra data which also had high activity against murine leukemia P-388 cells with IC 50  3.1 μg / mL. Based on the IR spectral data for the other two compounds there is a -OH uptake in the region of 3200-3500 cm -1, C = C aromatic uptake in the area of 1600-1400 cm -1 , so it is estimated that both compounds are phenolic group compounds.Tumbuhan Artocarpus dadah Miq.merupakan salah satu spesies Artocarpus dari famili Moraceae yang termasuk tumbuhan langka di alam. Tumbuhan ini dikenal sebagai sumber utama senyawa turunan fenolik yaitu senyawa flavon di atau tri-oksigenasi dan terisoprenilasi pada posisi C-3, dan juga dikenal sebagai sumber utama senyawa fenolik turunan flavonoid, aril-benzofuran, stilbenoid dan santon turunan flavonoida, yang memiliki aktivitas biologi sebagai promotor antitumor, antibakteri, antifungal, antiimflamatori, antikanker dan lain-lain.Penelitian ini bertujuan untuk mengisolasi dan mengidentifikasi senyawa fenolik yang terkandung dalam tumbuhan A. dadah yang diperoleh dari desa Purwoasri, Kecamatan Metro Utara, Kota Metro, Provinsi Lampung.Tahapan penelitian yang dilakukan meliputi pengumpulan dan persiapan sampel kemudian ekstraksi, isolasi, dan pemurnian senyawa menggunakan metode KCV, kromatografi flash, KKG, dan KLT, sedangkan identifikasi senyawa dilakukan menggunakan spektroskopi ultraungu-tampak (UV-VIS) dan inframerah (IR). Pada penelitian ini telah berhasil diisolasi tiga senyawa, yang salah satunya diperkirakan senyawa flavonoid berdasarkan data spektrum UV-VIS dan IR yang juga memiliki aktivitas tinggi terhadap sel murine leukemia P-388 dengan IC50 3,1 μg/mL. Berdasarkan data spektrum IR untuk dua senyawa yang lain terdapat serapan –OH pada daerah 3200-3500 cm-1, serapan C=C aromatik di daerah 1600-1400 cm-1, sehingga diperkirakan kedua senyawa tersebut merupakan senyawa golongan fenolik.

scholarly journals Effects of fragrance compounds on growth of the silkworm Bombyx mori

PeerJ ◽  
2021 ◽  
Vol 9 ◽  
pp. e11620
Author(s):  
Zhen-peng Kai ◽  
Yanwei Qiu ◽  
Xue-wei Zhang ◽  
Shan-shan Chen
Keyword(s):  
Bombyx Mori ◽  
Endocrine System ◽  
Inhibitory Effect ◽  
Ethyl Vanillin ◽  
Abnormal Growth ◽  
Significant Inhibitory Effect ◽  
Ecological Problems ◽  
Musk Xylene ◽  
Fragrance Compounds

Due to the contamination and biological toxicity of some fragrance compounds, the environmental and ecological problems of such compounds have attracted more and more attention. However, studies of the toxicity of fragrance compounds for insects have been limited. The toxicity of 48 fragrance compounds for the silkworm Bombyx mori were investigated in this study. All of the fragrance compounds examined had no acute toxicity for B. mori larvae, but eight of them (menthol, maltol, musk xylene, musk tibeten, dibutyl sulfide, nerolidol, ethyl vanillin, and α-amylcinnamaldehyde) exhibited chronic and lethal toxicity with LC50 values from 20 to 120 µM. In a long-term feeding study, musk tibeten, nerolidol, and musk xylene showed significant growth regulatory activity. They were also extremely harmful to the cocooning of B. mori, resulting in small, thin, and loose cocoons. Two important insect hormones, namely, juvenile hormone (JH) and 20-hydroxyecdysone (20-E), were quantified in hemolymph following chronic exposure to musk tibeten, nerolidol, and musk xylene, respectively. Musk tibeten significantly increased JH titer and decreased the 20-E titer in hemolymph, and musk xylene had a significant inhibitory effect on JH titer and increased 20-E titer. Although nerolidol had no effect on hormone levels, exogenous JH mimic nerolidol increased the physiological effects of JH and significantly slowed the growth rate of B. mori larvae. The results showed that these fragrance compounds could interfere with the insect endocrine system, leading to death and abnormal growth. The risk to insects of residual fragrance compounds in the environment is worthy of attention.

scholarly journals Antibacterial activity of plant extracts against Listeria monocytogenes isolated from ready-to-eat salads

2020 ◽  
Vol 13 (1) ◽  
pp. 131-143
Author(s):  
É. György ◽  
É. Laslo ◽  
E. Csató
Keyword(s):  
Listeria Monocytogenes ◽  
Essential Oils ◽  
Antibacterial Effect ◽  
Storage Conditions ◽  
Inhibitory Effect ◽  
Listeria Innocua ◽  
Foodborne Diseases ◽  
Bacterial Strains ◽  
Antibacterial Effects ◽  
Growth Environment

Abstract Ready-to-eat salads are becoming more and more popular. However, due to their ingredients, they represent a suitable growth environment for different microbes. In the prevention of foodborne diseases, hygienic food preparation and appropriate storage conditions are very important. During this study, ten different ready-to-eat salads were analysed for the presence of Listeria monocytogenes. Five different selective agar mediums were used for the enumeration and isolation of Listeria monocytogenes. The isolated bacterial strains were subjected to morphological and biochemical confirmation tests. The antibacterial effects of five different freshly squeezed vegetable juices (carrots, celery, beets, horseradish, and onions) and of five essential oils (dill, thyme, oregano, lemongrass, and sage) were determined against Listeria monocytogenes, Listeria innocua, and L. monocytogenes strains isolated from ready-to-eat salads. Based on the results obtained from fresh vegetable juices, carrot juice exerted the highest antibacterial effect, while the others showed no or slight inhibitory effect (horseradish, beets, onions) against Listeria species. Among the essential oils, thyme, lemongrass, and oregano showed the strongest antibacterial effect against the studied Listeria species.

scholarly journals Using Lactobacillus as Probiotic to Inhibit Growth and Adhesion of Proteus mirabilis Causing Urinary Tract Infection

2008 ◽  
Vol 2 (1) ◽  
pp. 19-32
Author(s):  
Ghydaa H. A al-jeboury ◽  
Abdul Wahed Baker
Keyword(s):  
Urinary Tract Infection ◽  
Lactic Acid ◽  
Urinary Tract ◽  
Epithelial Cell ◽  
Tract Infection ◽  
Proteus Mirabilis ◽  
Inhibitory Effect ◽  
Adhesion Property ◽  
Significant Inhibitory Effect ◽  
Urine Specimens

The aim of the study was to use lactic acid bacteria (LAB), as probiotic, to treat growth and adhesion property of Proteus mirabilis isolated from patients suffering from urinary tract infection (UTI). For this purpose, one P. mirabilis isolate (P.M.9) was selected out of 9 isolates obtained from 150 urine specimens. Due to its resistance to 11 antibiotics tested, this isolate was treated with three-fold concentrated filtrates of two lactobacillus isolates (as probiotic). Results after treatment, showed that the filtrates exhibited significant inhibitory effect against the pathogenic P.M.9 and its adhesion property especially when only an average of 3-10 bacteria /cell were adhered to each epithelial cell compared to 44-55 bacteria/cell.

scholarly journals Searching for Antagonistic Activity of Bacterial Isolates Derived from Food Processing Environments on Some Food-Borne Pathogenic Bacteria

2020 ◽  
Vol 49 (4) ◽  
pp. 415-423
Author(s):  
B. Baráti-Deák ◽  
Cs. Mohácsi-Farkas ◽  
Á. Belák
Keyword(s):  
Escherichia Coli ◽  
Food Processing ◽  
Pathogenic Bacteria ◽  
Inhibitory Effect ◽  
Antagonistic Activity ◽  
Bacterial Isolates ◽  
Bacterial Strains ◽  
Food Borne ◽  
Time Period ◽  
Growth Decline

Bacterial strains with inhibitory effect on Salmonella Hartford, Listeria monocytogenes, Yersinia enterocolitica, and Escherichia coli, respectively, were isolated. Out of the 64 bacteria originated from food processing environments, 20 could inhibit at least one of the tested pathogens, and it was proved that growth decline of the pathogenic bacteria was more remarkable by co-culturing than by using cell-free supernatants of the isolates. Seven different genera (Pseudomonas, Bacillus, Paenibacillus, Macrococcus, Staphylococcus, Serratia, and Rothia) reduced the pathogens’ growth during the time period of analysis, and the strongest inhibitory effect was observed after 24 h between 15 and 30 °C. Sensitivity of the tested human pathogenic bacteria against the inhibitory strains was distinct, as Y. enterocolitica could be inhibited by numerous isolates, while S. Hartford proved to be the most resistant. Our results reveal that the isolated bacteria or their excreted metabolites could hinder pathogen growth when used in sufficient quantities.

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