scholarly journals Screening and Application of Chitin Synthase Inhibitors

Processes ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 1029
Author(s):  
Xiaozai Shi ◽  
Shuo Qiu ◽  
Yingling Bao ◽  
Hanchi Chen ◽  
Yuele Lu ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Chitin Synthase ◽  
Fungal Cell ◽  
Ic50 Value ◽  
Further Development ◽  
Fungicide Target ◽  
Better Than

Chitin is an important part of the fungal cell wall, but is not found in plants and mammals, so chitin synthase (CHS) can be a green fungicide target. In this paper, 35 maleimide compounds were designed and synthesized as CHS inhibitors. All the screened compounds showed different degrees of CHS inhibitory activity and antifungal activity in vitro. In particular, the half–inhibitory concentration (IC50) value of compound 20 on CHS was 0.12 mM, and the inhibitory effect was better than that of the control polyoxin B (IC50 = 0.19 mM). At the same time, this compound also showed good antifungal activity and has further development value.

scholarly journals Synthesis of Highly Potent Anti-Inflammatory Compounds (ROS Inhibitors) from Isonicotinic Acid

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1272
Author(s):  
Sana Yaqoob ◽  
Nourina Nasim ◽  
Rahila Khanam ◽  
Yan Wang ◽  
Almas Jabeen ◽  
...  
Keyword(s):  
Isonicotinic Acid ◽  
Docking Studies ◽  
Fine Tuning ◽  
Standard Drug ◽  
Ic50 Value ◽  
Anti Inflammatory ◽  
Further Development ◽  
Insight Into ◽  
Better Than

In search of anti-inflammatory compounds, novel scaffolds containing isonicotinoyl motif were synthesized via an efficient strategy. The compounds were screened for their in vitro anti-inflammatory activity. Remarkably high activities were observed for isonicotinates 5–6 and 8a–8b. The compound 5 exhibits an exceptional IC50 value (1.42 ± 0.1 µg/mL) with 95.9% inhibition at 25 µg/mL, which is eight folds better than the standard drug ibuprofen (11.2 ± 1.9 µg/mL). To gain an insight into the mode of action of anti-inflammatory compounds, molecular docking studies were also performed. Decisively, further development and fine tuning of these isonicotinates based scaffolds for the treatment of various aberrations is still a wide-open field of research.

Synthesis and biological activity of aldehyde derivatives of isopimaric acid

2021 ◽  
Vol 18 ◽  
Author(s):  
Yanju Lu ◽  
Zhendong Zhao ◽  
Yuxiang Chen ◽  
Jing Wang
Keyword(s):  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Klebsiella Pneumonia ◽  
Hep G2 ◽  
Isopimaric Acid ◽  
Streptococcus Pneumonia ◽  
Derivatives Of ◽  
Better Than

: Four series of acylhydrazone derivatives, including halogenated aryl modified acylhydrazone, thiophene, pyrrole and quinoline, were synthesized and characterized. The minimum inhibitory concentrations of the compounds against five bacteria were determined and most of the compounds displayed some degree of antibacterial activity. Isopimaric acid (pyrrole-3-carboxaldehyde) acylhydrazone (3j) exhibited the most potent activity against Streptococcus pneumonia and Klebsiella Pneumonia, with the minimum inhibitory concentration being 3.91 μg/mL. The antimicrobial activity against S. pneumoniae was improved when the pyrrole structure was introduced into isopimaric acid. All heterocyclic acylhydrazone derivatives of isopimaric acid exhibited a good in vitro antitumorial activity at 100 μM. It is concluded that the inhibitory effect of isopimaric acid (2-fluoro-6-methoxybenzaldehyde) acylhydrazone (3d) on Hep G2 and isopimaric acid (3-bromothiophene-2-carbaldehyde) acylhydrazone (3g) on Hep G2 and MDAMB 231 is better than that of the positive control 5-fluorouracil (5-FU) (76.51%), which is a widely used clinical anticancer agent, at 100 μM.

Synthesis and Assessment of Novel Anti-chlamydial Benzylidene Acylhydrazides Derivatives

2018 ◽  
Vol 15 (1) ◽  
pp. 31-36 ◽  
Author(s):  
Xiaofeng Bao ◽  
Ying Xue ◽  
Chao Xia ◽  
Yin Lu ◽  
Ningjing Yang ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Dependent Manner ◽  
Iron Starvation ◽  
Hydrochloride Salt ◽  
Obligate Intracellular ◽  
Biphasic Life Cycle ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Dose Dependent ◽  
Better Than

Background: Chlamydiae, characterized by a unique biphasic life cycle, are a group of Gram-negative obligate intracellular bacterial pathogens responsible for diseases in a range of hosts including humans. Benzylidene acylhydrazide CF0001 could inhibit chlamydiae independent of iron starvation and T3SS inhibition. This finding promoted us to design and synthesize more benzylidene acylhydrazides to find novel anti-chlamydial agents. Methods: The carboxylic acids 1a-1d were coupled with Boc-hydrazide inpresence of EDCI and DMAP to obtain the intermediate 2a-2d in 60-62% yields. N-Boc deprotections were performed to obtain hydrazide hydrochloride salt 3a-3d. Nextly, the hydrazides were subjected to condensation with aldehydes to obtain benzylidene acylhydrazides 4a-4g in 30-52% yields in two steps. Results: Compound 4d exhibited best inhibitory effect on the formation and growth of chlamydial inclusions. The IC50 value of compound 4d for infectious progenies was 3.55 µM, better than 7.30 µM of CF0001. Conclusion: To find novel anti-chlamydial agents, we have designed and synthesized benzylidene acylhydrazides 4a-4g. Compounds 4a, 4d, 4g showed inhibitory activity on C. muridarum with the IC50 values from 3.55-12 µM. The 3,5-dibromo-4-hydroxyl substitutes on ring B are critical to keep their anti-chlamydial activity. Compound 4d inhibited C. muridarum in a dose-dependent manner without apparent cytotoxicity.

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).

scholarly journals The "in vitro" antifungal activity evaluation of propolis G12 ethanol extract on Cryptococcus neoformans

2007 ◽  
Vol 49 (2) ◽  
pp. 93-95 ◽  
Author(s):  
Fabrício Freitas Fernandes ◽  
Amanda Latercia Tranches Dias ◽  
Cíntia Lacerda Ramos ◽  
Masaharu Ikegaki ◽  
Antonio Martins de Siqueira ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Cryptococcus Neoformans ◽  
Ethanol Extract ◽  
Inhibitory Effect ◽  
Biological Properties ◽  
Standard Strain ◽  
Antiviral Activities ◽  
Prolonged Antibiotic Therapy ◽  
In Vitro Antifungal Activity

Cryptococcosis is a worldwide disease caused by the etiological agent Cryptococcus neoformans. It affects mainly immunocompromised humans. It is relatively rare in animals only affecting those that have received prolonged antibiotic therapy. The propolis is a resin that can present several biological properties, including antibacterial, antifungal and antiviral activities. The standard strain C. neoformans ATTC 90112 was used to the antifungal evaluation. The tests were realized with propolis ethanol extract (PEE) G12 in concentrations from 0.1 to 1.6 mg mL-1. The evaluation of MIC and MFC were done according to DUARTE (2002)5. The inhibitory effect of PEE G12 on the fungal growing was seen at the concentration of 0.2 mg mL-1 and 1.6 mg mL-1 was considered a fungicidal one.

scholarly journals DIFFERENCE BETWEEN ANTIMICROBIAL EFFECTS OF PAPACARIE AND PAPAIN ON STREPTOCOCCUS MUTANS IN VITRO

2019 ◽  
pp. 79-83
Author(s):  
TITTY SULIANTI ◽  
NILAKESUMA DJAUHARI ◽  
BAMBANG NURSASONGKO
Keyword(s):  
Inhibitory Concentration ◽  
Minimum Bactericidal Concentration ◽  
Zone Of Inhibition ◽  
Antimicrobial Effects ◽  
Treatment Groups ◽  
Group Control ◽  
Caries Removal ◽  
And Diffusion ◽  
Better Than

Objective: The aim is to compare the antimicrobial effects of papain and Papacarie with dilution and diffusion tests.Methods: There were two treatment groups and one Group control. The treatment group received papain and Papacarie, and the control groupreceived chlorhexidine, in five liquids with different concentrations of 0.5%, 0.25%, 0.125%, 0.0625%, and 0.03%. The dilution and diffusion testswere used to determine the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and zone of inhibition for eachtreatment material.Results: MICs of papain and Papacarie were 12.5%, indicating that at a concentration of 12.5%, the material can inhibit the growth of Streptococcusmutans. Papain does not have an MBC value but the Papacarie has an MBC at 25%, which indicating that at a concentration of 25%, Papacarie hasbactericidal effects on S. mutans. The zone of inhibition of papain was lower than Papacarie.Conclusion: Based on chemomechanical caries removal materials, the antimicrobial effects of Papacarie were better than those of papain.

scholarly journals Potential Effect of Pomegranate Peels Extract (Punica Granatum.) against Covid-19 Virus .

2021 ◽  
Author(s):  
Ashraf fawzy mosa ◽  
Mostafa abo Elhoda Mohamed
Keyword(s):  
Tissue Culture ◽  
Water Extract ◽  
Punica Granatum ◽  
Inhibitory Effect ◽  
Potential Effect ◽  
Laboratory Methods ◽  
Global Epidemic ◽  
Ic50 Value ◽  
The World

Abstract Background: Covid-19 Virus infection poses significant global health challenges and considered a global epidemic sweeping all countries of the world Which prompted scientists around the world to search for a quick or safe treatment to preserve people's lives .So far, options for controlling and treating the disease have not been revealed. The current study was conducted to evaluate the effectiveness of pomegranate peels extract against the Covid-19 virus in the laboratory. Methods: In this research, tow methods of extraction are carried out ethyl alcohol and distal water extract of pomegranate peels . activity of the extract assessed using 50% Tissue Culture Infectious Doses (TCID50) method in Vero E6 cells. Results: Pomegranate peels extract had the highest inhibitory effect against Covid -19 virus with IC50 value of 0.125, 0.0625 and 0.031256 μl in Vero E6 cells. Conclusion: Based on our results, the aqueous extract of pomegranate peels can inhibit Covid-19 virus replication in vitro.

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.

Inhibitory activity of isoniazid and ethionamide against Cryptococcus biofilms

2015 ◽  
Vol 61 (11) ◽  
pp. 827-836 ◽  
Author(s):  
Rossana de Aguiar Cordeiro ◽  
Rosana Serpa ◽  
Francisca Jakelyne de Farias Marques ◽  
Charlline Vládia Silva de Melo ◽  
Antonio José de Jesus Evangelista ◽  
...  
Keyword(s):  
Cell Membrane ◽  
Biofilm Formation ◽  
Inhibitory Effect ◽  
Cell Membrane Permeability ◽  
Planktonic Cells ◽  
Fungal Cell ◽  
Antituberculosis Drugs ◽  
Opportunistic Mycoses ◽  
Cryptococcus Spp

In recent years, the search for drugs to treat systemic and opportunistic mycoses has attracted great interest from the scientific community. This study evaluated the in vitro inhibitory effect of the antituberculosis drugs isoniazid and ethionamide alone and combined with itraconazole and fluconazole against biofilms of Cryptococcus neoformans and Cryptococcus gattii. Antimicrobials were tested at defined concentrations after susceptibility assays with Cryptococcus planktonic cells. In addition, we investigated the synergistic interaction of antituberculosis drugs and azole derivatives against Cryptococcus planktonic cells, as well as the influence of isoniazid and ethionamide on ergosterol content and cell membrane permeability. Isoniazid and ethionamide inhibited both biofilm formation and viability of mature biofilms. Combinations formed by antituberculosis drugs and azoles proved synergic against both planktonic and sessile cells, showing an ability to reduce Cryptococcus biofilms by approximately 50%. Furthermore, isoniazid and ethionamide reduced the content of ergosterol in Cryptococcus spp. planktonic cells and destabilized or permeabilized the fungal cell membrane, leading to leakage of macromolecules. Owing to the paucity of drugs able to inhibit Cryptococcus biofilms, we believe that the results presented here might be of interest in the designing of new antifungal compounds.

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