scholarly journals ACETYLCHOLINESTERASE INHIBITORY EFFECT OF 3-(1H-INDOL-3-YL)-1, 3-DIPHENYLPROPAN-1-ONE DERIVATIVES

2017 ◽  
Vol 10 (8) ◽  
pp. 83
Author(s):  
Manjunatha K S ◽  
Manu Cp ◽  
Satyanarayan Nd ◽  
Vinay Kn ◽  
Vineetha Ms ◽  
...  
Keyword(s):  
Hydrochloric Acid ◽  
Mode Of Action ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Considerable Degree ◽  
Ache Inhibition ◽  
Ache Inhibitors ◽  
Ellman’S Method ◽  
Inhibition Ability

Objective: The objective of the study is acetylcholinesterase (AChE) inhibitory effect of 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives by Ellman’s method, physostigmine is used as positive control.Method: 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were synthesized by the addition of chalcone (0.25 g, 1 mmol), indole (0.12 g, 1 mmol) in ethanol (5 ml), and concentrated hydrochloric acid (5 mmol %). These earlier synthesized compounds were screened for AChE inhibitors by modifying Ellman’s method.Results: Among the tested compounds, 3a and 3j were found to be having more potential than other compounds with half maximal inhibitory concentration values of 13.64 and 14.3 μg/ml, respectively. Whereas, compounds 3c, 3e, 3g, and 3i exhibited an average AChE inhibition of 16.4, 17.9, 17.6, and 21.1 μg/ml, respectively.Conclusion: The compounds 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were found to be possible lead molecules in AChE inhibition and even though, the molecules were structurally dissimilar to that of the standard, still they exhibited a considerable degree of inhibition and encourage the researchers to look into the mode of action of their inhibition ability against AChE.

scholarly journals Synthesis and bioactivity of novel C2-glycosyl oxadiazole derivatives as acetylcholinesterase inhibitors

2018 ◽  
Vol 24 (6) ◽  
pp. 333-338 ◽  
Author(s):  
Lei Wang ◽  
Yu-Ran Wu ◽  
Shu-Ting Ren ◽  
Long Yin ◽  
Xiu-Jian Liu ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Acetylcholinesterase Inhibitors ◽  
Inhibition Activity ◽  
Ache Inhibition ◽  
Active Compounds ◽  
Oxadiazole Derivatives ◽  
Inhibitory Activities ◽  
Ellman’S Method

Abstract A series of glycosyl-substituted 1,3,4-oxadiazoles were synthesized by cyclization of glycosyl-acylthiosemicarbazides via a base-catalyzed reaction. The starting glycosyl-acylthiosemicarbazide derivatives were obtained by the reaction of glycosyl isothiocyanate with various hydrazides. The acetylcholinesterase (AChE) inhibitory activities of the products were tested by Ellman’s method. The most active compounds were subsequently evaluated for the 50% inhibitory concentration (IC50) values. N-(1,3,4,6-tetra-O-benzyl-2-deoxy-β-D-glucopyranosyl)-5-(4-fluorophenyl)-1,3,4-oxadiazole-2-amine (6i) possesses the best AChE -inhibition activity with an IC50 of 1.61±0.34 μm.

scholarly journals In Vitro Effects of Doxycycline on Replication of Feline Coronavirus

Pathogens ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 312
Author(s):  
Magdalena Dunowska ◽  
Sayani Ghosh
Keyword(s):  
Inhibitory Concentration ◽  
Infectious Virus ◽  
Treatment Options ◽  
Inhibitory Effect ◽  
Virus Titration ◽  
Reverse Transcription Quantitative Pcr ◽  
In Vitro Effects ◽  
Dose Dependent ◽  
Feline Coronavirus

Feline infectious peritonitis (FIP) is a sporadic fatal disease of cats caused by a virulent variant of feline coronavirus (FCoV), referred to as FIP virus (FIPV). Treatment options are limited, and most of the affected cats die or are euthanized. Anecdotally, doxycycline has been used to treat FIP-affected cats, but there are currently no data to support or discourage such treatment. The aim of this study was to establish whether doxycycline inhibits replication of FIPV in vitro. The virus was cultured in Crandell-Rees feline kidney cells with various concentrations of doxycycline (0 to 50 µg/mL). The level of FIPV in cultures was determined by virus titration and FCoV-specific reverse-transcription quantitative PCR. Cell viability was also monitored. There was no difference in the level of infectious virus or viral RNA between doxycycline-treated and untreated cultures at 3, 12- and 18-hours post-infection. However, at 24 h, the growth of FIPV was inhibited by approximately two logs in cultures with >10 µg/mL doxycycline. This inhibition was dose-dependent, with inhibitory concentration 50% (IC50) 4.1 µg/mL and IC90 5.4 µg/mL. Our data suggest that doxycycline has some inhibitory effect on FIPV replication in vitro, which supports future clinical trials of its use for the treatment of FIP-affected cats.

scholarly journals In Vitro α-Glucosidase and α-Amylase Inhibitory Activities of Free and Bound Phenolic Extracts from the Bran and Kernel Fractions of Five Sorghum Grain Genotypes

Foods ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 1301
Author(s):  
Yun Xiong ◽  
Ken Ng ◽  
Pangzhen Zhang ◽  
Robyn Dorothy Warner ◽  
Shuibao Shen ◽  
...  
Keyword(s):  
Digestive System ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Phenolic Contents ◽  
Inhibitory Activities ◽  
Sorghum Grain ◽  
Global Health Challenge ◽  
Phenolic Extracts

Diabetes is a global health challenge. Currently, an effective treatment for diabetes is to reduce the postprandial hyperglycaemia by inhibiting the carbohydrate hydrolysing enzymes in the digestive system. In this study, we investigated the in vitro α-glucosidase and α-amylase inhibitory effects of free and bound phenolic extracts, from the bran and kernel fractions of five sorghum grain genotypes. The results showed that the inhibitory effect of sorghum phenolic extracts depended on the phenolic concentration and composition. Sorghum with higher phenolic contents generally had higher inhibitory activity. Among the tested extracts, the brown sorghum (IS131C)-bran-free extract (BR-bran-free, half-maximal inhibitory concentration (IC50) = 18 ± 11 mg sorghum/mL) showed the strongest inhibition against α-glucosidase which was comparable to that of acarbose (IC50 = 1.39 ± 0.23 mg acarbose/mL). The red sorghum (Mr-Buster)-kernel-bound extract (RM-kernel-bound, IC50 = 160 ± 12 mg sorghum/mL) was the most potent in inhibiting α-amylase but was much weaker compared to acarbose (IC50 = 0.50 ± 0.03 mg acarbose/mL).

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 Enhanced Antibacterial Activity of Meropenem against Extensively Drug-Resistant Acinetobacter baumannii by Myrtaceae Plant Extracts

2020 ◽  
Vol 17 (11) ◽  
pp. 1168-1176
Author(s):  
Dennapa SAELOH ◽  
Monton VISUTTHI ◽  
Marisa LEEHA ◽  
Surasak LIMSUWAN ◽  
Supayang Piyawan VORAVUTHIKUNCHAI
Keyword(s):  
Acinetobacter Baumannii ◽  
Bacterial Infections ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Drug Resistant ◽  
Microdilution Method ◽  
Extensively Drug Resistant ◽  
Resistant Phenotype ◽  
Bacterial Growth Inhibition ◽  
Mic Value

Acinetobacter baumannii (A. baumannii) has been known as a major cause of nosocomial bacterial infections worldwide. The bacteria are increasingly associated with a broad spectrum of antibiotic resistance, and this has become a widespread concern in a variety of hospitals.Antibiotic development and alternative treatment have become priorities for the treatment of bacterial infections.This study investigated the efficacy of meropenem in combination with five ethanolic extracts of plants in Myrtaceae against extensively drug-resistant (XDR) A. baumannii. The resistant phenotype was previously determined by microdilution method. XDR-A. baumannii strains showed resistance to meropenem with the minimum inhibitory concentration (MIC) in a range of 16 - 128 µg/mL, whereas the MIC value of all extracts, including Calistemon lancealatus, Eucalyptus citridora, Rhodomytus tomentasa, Syzygium cumini, and Xanthortemon chrysanthus, was over 1,000 µg/mL. Interestingly, all extracts potentiated the activity of the antibiotic by reducing the MIC values of the antibiotic. Xanthortemon chrysanthus extract displayed excellent synergism against the bacteria by decreasing the MIC value of the drug greater than 8-fold. In addition, the extract, at concentrations of 31.25, 62.5, 125, 250, 500, and 1,000 µg/mL, obviously increased the inhibitory effect of meropenem (1/4´MIC) against A. baumannii. The percentage of bacterial growth inhibition by combination was 87.9, 88.8, 91.8, 93.6, 99.9, and 100, respectively. The results supported that the extract could improve the activity of ineffective antibiotics against drug-resistant pathogens.Therefore, the findings may serve as therapeutic options for XDR-A. baumannii infections in the future.

scholarly journals Nisin and ε-poly-L-lysine as natural antimicrobials towards spoilage-associated Lactobacillus plantarum

2021 ◽  
Vol 51 (2) ◽  
Author(s):  
Fernanda Cristina Kandalski Bortolotto ◽  
Maria Helena da Rosa Farfan ◽  
Nathalia Cristina Kleinke Jede ◽  
Gabriela Maia Danielski ◽  
Renata Ernlund Freitas de Macedo
Keyword(s):  
Lactic Acid ◽  
Lactic Acid Bacteria ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Minimal Bactericidal Concentration ◽  
Natural Antimicrobials ◽  
Food Preservatives ◽  
Spoilage Bacteria ◽  
Mass Spectrometry Identification

ABSTRACT: Sausages are highly susceptible to microbial spoilage. Lactic acid bacteria (LAB) is the main group of spoilage bacteria in vacuum packed cooked sausages. To control microbial growth natural antimicrobials have been used as food preservatives. The aim of this study was to identify strains of lactic acid bacteria isolated from spoiled commercial Calabresa sausages and use them in an in vitro challenge with the natural antimicrobials, nisin (NI) and ε-poly-L-lysine (ε-PL). Mass spectrometry identification of LAB isolated from sausages using MALDI-TOF revealed a predominance of L. plantarum in the LAB population. RAPD-PCR of L. plantarum strains showed four different genetic profiles. Minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of NI and ε-PL, alone and in combination, against a pool of different profiles L. plantarum were determined. MIC of NI and ε-PL were 0.468 mg/ L and 75 mg/ L; respectively, whereas MBC of NI and ε-PL were 12.48 mg/L and 150 mg/L, respectively. The combined effect of NI and ε-PL was determined using concentrations at 1/4 and 1/8 of individual MICs. Synergistic effect was confirmed at both concentrations showing a fractional inhibitory concentration index of 0.5 and 0.2, respectively. The combination of NI and ε-PL at a small concentration of 0.05 mg/L and 9.375 mg/L, respectively, showed inhibitory effect towards spoilage L. plantarum Results show the potential of the combined use of NI and ε-PL to control sausage spoilage-associated with lactobacilli.

Evaluation of Phytochemicals and Pharmacological Activities of Ben-Cha-Lo-Ka-Wi-Chian Remedy

2019 ◽  
Vol 891 ◽  
pp. 52-59
Author(s):  
Chanai Noysang ◽  
Teerarat Pummarin
Keyword(s):  
Antioxidant Activity ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Propionibacterium Acnes ◽  
Ethanolic Extract ◽  
Inhibition Zone ◽  
Inhibitory Effect ◽  
Pharmacological Activities ◽  
Ethanolic Extracts ◽  
Reaction Test

Benchalokawichian (BLW) remedy is a Thai traditional medicine that has been notified in the List of Medicine Products of the National List of Essential Drugs A.D. 2006 and has long been used as an antipyretic. The phytochemicals of the 70% and 95% ethanolic extracts of were studied by color reaction test and HPTLC analysis. The BLW remedy showed a highest amounts of 70% ethanolic extractives (ca. 3.99 ± 0.60% of dry material weight). The several ethanolic extracts showed similar qualitative phytochemicals. The major of phytochemicals identified in these extracts were alkaloids, flavonoids, tannins, and polyphenols. The antioxidant activity was assessed using the 2,2-diphenyl-1-picrylhydrazyl assay. The analysed 70% ethanolic extract showed a highest antioxidant activity at IC50= 526.09 µg/ml and both extracts not showed tyrosinase inhibitory effect. The 95% ethanolic extract showed the greatest anti-propionibacterium acnes activity with inhibition zone of 10.10 ± 0.45 mm and minimum inhibitory concentration (MIC) was 5.05 mg/ml

Na+ transport in normal and CF human bronchial epithelial cells is inhibited by BAY 39-9437

2001 ◽  
Vol 281 (1) ◽  
pp. L16-L23 ◽  
Author(s):  
Robert J. Bridges ◽  
Ben B. Newton ◽  
Joseph M. Pilewski ◽  
Daniel C. Devor ◽  
Christopher T. Poll ◽  
...  
Keyword(s):  
Serine Protease ◽  
Half Life ◽  
Inhibitory Concentration ◽  
Therapeutic Potential ◽  
Short Circuit ◽  
Short Circuit Current ◽  
Inhibitory Effect ◽  
Human Bronchial Epithelial Cells ◽  
Na Transport ◽  
Bronchial Epithelial

To test the hypothesis that Na+ transport in human bronchial epithelial (HBE) cells is regulated by a protease-mediated mechanism, we investigated the effects of BAY 39-9437, a recombinant Kunitz-type serine protease inhibitor, on amiloride-sensitive short-circuit current of normal [non-cystic fibrosis (CF) cells] and CF HBE cells. Mucosal treatment of non-CF and CF HBE cells with BAY 39-9437 decreased the short-circuit current, with a half-life of ∼45 min. At 90 min, BAY 39-9437 (470 nM) reduced Na+ transport by ∼70%. The inhibitory effect of BAY 39-9437 was concentration dependent, with a half-maximal inhibitory concentration of ∼25 nM. Na+ transport was restored to control levels, with a half-life of ∼15 min, on washout of BAY 39-9437. In addition, trypsin (1 μM) rapidly reversed the inhibitory effect of BAY 39-9437. These data indicate that Na+transport in HBE cells is activated by a BAY 39-9437-inhibitable, endogenously expressed serine protease. BAY 39-9437 inhibition of this serine protease maybe of therapeutic potential for the treatment of Na+ hyperabsorption in CF.

scholarly journals Psoromic Acid, a Lichen-Derived Molecule, Inhibits the Replication of HSV-1 and HSV-2, and Inactivates HSV-1 DNA Polymerase: Shedding Light on Antiherpetic Properties

Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 2912 ◽  
Author(s):  
Sherif T. S. Hassan ◽  
Miroslava Šudomová ◽  
Kateřina Berchová-Bímová ◽  
Karel Šmejkal ◽  
Javier Echeverría
Keyword(s):  
Dna Polymerase ◽  
Active Sites ◽  
Inhibitory Action ◽  
Inhibitory Concentration ◽  
Competitive Inhibition ◽  
Inhibitory Effect ◽  
Standard Drug ◽  
Key Enzyme ◽  
Hsv 1

Psoromic acid (PA), a bioactive lichen-derived compound, was investigated for its inhibitory properties against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2), along with the inhibitory effect on HSV-1 DNA polymerase, which is a key enzyme that plays an essential role in HSV-1 replication cycle. PA was found to notably inhibit HSV-1 replication (50% inhibitory concentration (IC50): 1.9 μM; selectivity index (SI): 163.2) compared with the standard drug acyclovir (ACV) (IC50: 2.6 μM; SI: 119.2). The combination of PA with ACV has led to potent inhibitory activity against HSV-1 replication (IC50: 1.1 µM; SI: 281.8) compared with that of ACV. Moreover, PA displayed equivalent inhibitory action against HSV-2 replication (50% effective concentration (EC50): 2.7 μM; SI: 114.8) compared with that of ACV (EC50: 2.8 μM; SI: 110.7). The inhibition potency of PA in combination with ACV against HSV-2 replication was also detected (EC50: 1.8 µM; SI: 172.2). Further, PA was observed to effectively inhibit HSV-1 DNA polymerase (as a non-nucleoside inhibitor) with respect to dTTP incorporation in a competitive inhibition mode (half maximal inhibitory concentration (IC50): 0.7 μM; inhibition constant (Ki): 0.3 μM) compared with reference drugs aphidicolin (IC50: 0.8 μM; Ki: 0.4 μM) and ACV triphosphate (ACV-TP) (IC50: 0.9 μM; Ki: 0.5 μM). It is noteworthy that the mechanism by which PA-induced anti-HSV-1 activity was related to its inhibitory action against HSV-1 DNA polymerase. Furthermore, the outcomes of in vitro experiments were authenticated using molecular docking analyses, as the molecular interactions of PA with the active sites of HSV-1 DNA polymerase and HSV-2 protease (an essential enzyme required for HSV-2 replication) were revealed. Since this is a first report on the above-mentioned properties, we can conclude that PA might be a future drug for the treatment of HSV infections as well as a promising lead molecule for further anti-HSV drug design.

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