Strong Inhibitory Effect, Low Cytotoxicity and High Plasma Stability of Steroidal Inhibitors of N-Methyl-D-Aspartate Receptors With C-3 Amide Structural Motif

Lactic acid bacteria have functions in immunoregulation, antagonism, and pathogen inhibition. The purpose of this study was to evaluate the effectiveness of lactic acid bacteria (LAB) in countering oral pathogens and develop related products. After a series of assays to 450 LAB strains, 8 heat-inactivated strains showed a strong inhibitory effect on a caries pathogen, Streptococcus mutans, and 308 heat-inactivated LAB strains showed a strong inhibitory effect on a periodontal pathogen, Porphyromonas gingivalis. The key reasons for inhibiting oral pathogens were bacteriocins produced by LAB and the coaggregation effect of the inactivated cells. We selected Lacticaseibacillus (Lb) paracasei 111 and Lb.paracasei 141, which had the strongest inhibitory effects on the above pathogens, was the main oral health food source. The optimal cultural conditions of Lb. paracasei 111 and Lb. paracasei 141 were studied. An oral tablet with a shelf life of 446 days made of the above strains was developed. A 40 volunteers’ clinical study (CSMUH IRB number: CS05065) was conducted with this tablet in the Periodontological Department of the Stomatology Research Center, Affiliated Hospital of Chung Shan Medical University (Taiwan). After 8 weeks of testing, 95% and 78.9% of patients showed an effect on reducing periodontal pathogens and improving probing pocket depth, respectively, in the oral tablet group.

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Caffeine does not inhibit substance P-evoked intracellular Ca2+ mobilization in rat salivary acinar cells

AJP Cell Physiology ◽

10.1152/ajpcell.1999.276.4.c915 ◽

1999 ◽

Vol 276 (4) ◽

pp. C915-C922 ◽

Cited By ~ 23

Author(s):

J. T. Seo ◽

H. Sugiya ◽

S. I. Lee ◽

M. C. Steward ◽

A. C. Elliott

Keyword(s):

Signal Transduction ◽

Substance P ◽

G Protein ◽

Acinar Cells ◽

Inhibitory Effect ◽

Structural Motif ◽

Stimulus Response ◽

Inhibit Substance ◽

Prior Application ◽

G Protein Coupled

We used the Ca2+-sensitive fluorescent dye fura 2, together with measurements of intracellulard- myo-inositol 1,4,5-trisphosphate [Ins(1,4,5) P 3], to assess the inhibitory effects of caffeine on signal transduction via G protein-coupled receptor pathways in isolated rat mandibular salivary acinar cells. ACh, norepinephrine (NE), and substance P (SP) all evoked substantial increases in the intracellular free Ca2+ concentration ([Ca2+]i). Responses to ACh and NE were markedly inhibited by prior application of 20 mM caffeine. The inhibitory effect of caffeine was not reproduced by phosphodiesterase inhibition with IBMX or addition of cell-permeant dibutyryl cAMP. In contrast to the ACh and NE responses, the [Ca2+]iresponse to SP was unaffected by caffeine. Despite this, SP and ACh appeared to mobilize Ca2+ from a common intracellular pool. Measurements of agonist-induced changes in Ins(1,4,5) P 3levels confirmed that caffeine inhibited the stimulus-response coupling pathway at a point before Ins(1,4,5) P 3generation. Caffeine did not, however, inhibit [Ca2+]iresponses evoked by direct activation of G proteins with 40 mM F−. These data show that caffeine inhibits G protein-coupled signal transduction in these cells at some element that is common to the muscarinic and α-adrenergic signaling pathways but is not shared by the SP signaling pathway. We suggest that this element might be a specific structural motif on the G protein-coupled muscarinic and α-adrenergic receptors.

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Isolation, Identification, and Antibacterial Mechanisms of Bacillus amyloliquefaciens QSB-6 and Its Effect on Plant Roots

Frontiers in Microbiology ◽

10.3389/fmicb.2021.746799 ◽

2021 ◽

Vol 12 ◽

Author(s):

Yanan Duan ◽

Ran Chen ◽

Rong Zhang ◽

Weitao Jiang ◽

Xuesen Chen ◽

...

Keyword(s):

Bacillus Amyloliquefaciens ◽

Fermentation Broth ◽

Biological Control Agent ◽

Lateral Roots ◽

Dna Gyrase ◽

Inhibitory Effect ◽

Dilution Method ◽

Fertilizer Treatment ◽

Strong Inhibitory Effect ◽

Subunit B

Apple replant disease (ARD) is a common problem in major apple planting areas, and biological factors play a leading role in its etiology. Here, we isolated the bacterial strain QSB-6 from the rhizosphere soil of healthy apple trees in a replanted orchard using the serial dilution method. Strain QSB-6 was provisionally identified as Bacillus amyloliquefaciens based on its morphology, physiological and biochemical characteristics, carbon source utilization, and chemical sensitivity. Maximum likelihood analysis based on four gene sequences [16S ribosomal RNA gene (16S rDNA), DNA gyrase subunit A (gyrA), DNA gyrase subunit B (gyrB), and RNA polymerase subunit B (rpoB)] from QSB-6 and other strains indicated that it had 100% homology with B. amyloliquefaciens, thereby confirming its identification. Flat standoff tests showed that strain QSB-6 had a strong inhibitory effect on Fusarium proliferatum, Fusarium solani, Fusarium verticillioides, Fusarium oxysporum, Alternaria alternata, Aspergillus flavus, Phoma sp., Valsa mali, Rhizoctonia solani, Penicillium brasilianum, and Albifimbria verrucaria, and it had broad-spectrum antibacterial characteristics. Extracellular metabolites from strain QSB-6 showed a strong inhibitory effect on Fusarium hyphal growth and spore germination, causing irregular swelling, atrophy, rupture, and cytoplasmic leakage of fungal hyphae. Analysis of its metabolites showed that 1,2-benzenedicarboxylic acid and benzeneacetic acid, 3- hydroxy-, methyl ester had good inhibitory effects on Fusarium, and increased the length of primary roots and the number of lateral roots of Arabidopsis thaliana plantlet. Pot experiments demonstrated that a QSB-6 bacterial fertilizer treatment (T2) significantly improved the growth of Malus hupehensis Rehd. seedlings. It increased root length, surface area, tips, and forks, respiration rate, protective enzyme activities, and the number of soil bacteria while reducing the number of soil fungi. Fermentation broth from strain QSB-6 effectively prevented root damage from Fusarium. terminal restriction fragment length polymorphism (T-RFLP) and quantitative PCR (qPCR) assays showed that the T2 treatment significantly reduced the abundance of Fusarium in the soil and altered the soil fungal community structure. In summary, B. amyloliquefaciens QSB-6 has a good inhibitory effect on Fusarium in the soil and can significantly promote plant root growth. It has great potential as a biological control agent against ARD.

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Stromal Cells from Human Decidua Exert a Strong Inhibitory Effect on NK Cell Function and Dendritic Cell Differentiation

PLoS ONE ◽

10.1371/journal.pone.0089006 ◽

2014 ◽

Vol 9 (2) ◽

pp. e89006 ◽

Cited By ~ 34

Author(s):

Daniele Croxatto ◽

Paola Vacca ◽

Francesca Canegallo ◽

Romana Conte ◽

Pier Luigi Venturini ◽

...

Keyword(s):

Cell Differentiation ◽

Dendritic Cell ◽

Stromal Cells ◽

Cell Function ◽

Nk Cell ◽

Inhibitory Effect ◽

Dendritic Cell Differentiation ◽

Strong Inhibitory Effect ◽

Human Decidua

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Design, synthesis and antibacterial evaluation of ocotillol derivatives with polycyclic nitrogen-containing groups

Future Medicinal Chemistry ◽

10.4155/fmc-2020-0364 ◽

2021 ◽

Author(s):

Yucheng Cao ◽

Kaiyi Wang ◽

Jiali Wang ◽

Haoran Cheng ◽

Mengxin Ma ◽

...

Keyword(s):

Antibacterial Activity ◽

Multidrug Resistant ◽

Inhibitory Effect ◽

Resistant Bacteria ◽

Design Synthesis ◽

In Vitro Antibacterial Activity ◽

Strong Inhibitory Effect ◽

Hospital Acquired ◽

Derivatives Of

Aim: With the increasing abuse of antibacterial drugs, multidrug-resistant bacteria have become a burden on human health and the healthcare system. To find alternative compounds effective against hospital-acquired methicillin-resistant Staphylococcus aureus (HA-MRSA), novel derivatives of ocotillol were synthesized. Methods & Results: Ocotillol derivatives with polycyclic nitrogen-containing groups were synthesized and evaluated for in vitro antibacterial activity. Compounds 36–39 exhibited potent antibacterial activity against hospital-acquired MRSA, with MIC = 8–64 μg/ml. Additionally, a combination of compound 37 and the commercially available antibiotic kanamycin showed synergistic inhibitory effects, with a fractional inhibitory concentration index of ≤0.375. Conclusion: Compound 37 has a strong inhibitory effect, and this derivative has potential for use as a pharmacological tool to explore antibacterial mechanisms.

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The Ovistatic Effect of Saprotrophic Soil Fungi on Ascaris suum Eggs

Folia Biologica ◽

10.3409/fb_67-3.11 ◽

2019 ◽

Vol 67 (3) ◽

pp. 109-118

Author(s):

Lidia Kołodziejczyk ◽

Kinga Mazurkiewicz-Zapałowicz ◽

Magdalena Twarużek ◽

Jan Grajewski ◽

Łukasz Łopusiewicz ◽

...

Keyword(s):

Mtt Assay ◽

Soil Fungi ◽

Developmental Stages ◽

Ascaris Suum ◽

Hydrolytic Activity ◽

Inhibitory Effect ◽

Penicillium Expansum ◽

Fungal Enzymes ◽

Low Cytotoxicity ◽

High Cytotoxicity

The aim of the study was to evaluate the potential use of selected species of soil fungi (Fusarium oxysporum, F. sulphureum, F. verticillioides, and Penicillium expansum) for the bioregulation of the dispersive stages of a parasitic nematode – the large roundworm of pig (Ascaris suum). Experimental cultures containing A. suum eggs with soil fungi and control cultures without fungi were incubated at 26°C for 28 days. Microscopic observations of the developmental stages of the A. suum eggs (zygote, 2-8 blastomeres, morula/blastula, gastrula, and larva) were performed at 7, 14, 21, and 28 days. The API-ZYM test was used to semi-quantitatively determine the activity of 19 hydrolytic fungal enzymes. The cytotoxicity of the fungi was determined with a tetrazole salt MTT assay. Microscopic observations of A. suum eggs incubated in the presence of fungi up to day 28 did not show any signs of destruction to egg shells and/or penetration of the fungi into the eggs. The ovistatic effect of all tested fungi (F. sulphureum, P. expansum, F. verticillioides, and F. oxysporum; p<0.05) was seen only on the 7th day of incubation, whereas on the 14th day, only F. verticillioides and F. oxysporum showed an inhibitory effect on the embryogenesis of A. suum, and by the 28th day, only P. expansum. The API-ZYM test showed differences in the hydrolytic activity of the tested strains, while the MTT assay showed the high cytotoxicity of F. sulphureum, the moderate cytotoxicity of F. verticillioides and P. expansum, and the low cytotoxicity of F. oxysporum. Among the fungal strains studied, F. sulphureum showed the highest ovistatic effect, which may be related to its enzymatic activity and cytotoxicity.

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Effect of Some Flavonic Compounds and Ascorbic Acid on Lactoferrin Stimulation of Erythrocyte Glycolysis and Na+/K+-ATPase Activity

Zeitschrift für Naturforschung C ◽

10.1515/znc-2008-9-1025 ◽

2008 ◽

Vol 63 (9-10) ◽

pp. 773-779 ◽

Cited By ~ 1

Author(s):

Ana Maneva ◽

Borislava Taleva

Keyword(s):

Ascorbic Acid ◽

Atpase Activity ◽

Specific Binding ◽

Lactate Production ◽

Inhibitory Effect ◽

High Concentration ◽

Transport Chain ◽

Strong Inhibitory Effect ◽

Lactate Formation ◽

Stimulation Of

The aim of the present study was to assess if some flavonic compounds (quercetin, piceatannol and apigenin) and ascorbic acid could interfere with the Lf stimulatory effect on the erythrocyte function. Quercetin (1.5 μm) and piceatannol (30 μm) showed an additive effect on Lf stimulation of Na+/K+-ATPase when used together with Lf. The enhancement of Lf stimulation on Na+/K+-ATPase in the presence of flavonoids was probably due to their antioxidative properties and/or to their involvement in the erythrocyte signaling. None of the estimated flavonoids showed an effect on Lf stimulation of the lactate production. Quercetin itself enhanced the ATPase activity but did not affect the lactate formation. Apigenin (1.5 μm) enhanced reliably the lactate generation, but it did not exert any effect on the ATPase activity. High concentration of ascorbic acid (60 mm) did not change the Lf stimulatory effect on Na+/K+-ATPase, but decreased the Lf-specific-binding. A significantly strong inhibitory effect on the Lf-specific binding exerted the electron acceptors NAD+ (2 mm) and FAD (2 mm). These effects concern most likely the competition with Lf for electron(s) which is (are) provided from the erythrocyte intercellular electron transport chain(s).

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Inhibitory Effect of New Semisynthetic Usnic Acid Derivatives on Human Tyrosyl-DNA Phosphodiesterase 1

Planta Medica ◽

10.1055/a-0681-7069 ◽

2018 ◽

Vol 85 (02) ◽

pp. 103-111 ◽

Cited By ~ 6

Author(s):

Nadezhda Dyrkheeva ◽

Olga Luzina ◽

Aleksandr Filimonov ◽

Olga Zakharova ◽

Ekaterina Ilina ◽

...

Keyword(s):

Biological Activity ◽

Usnic Acid ◽

Inhibitory Effect ◽

Repair Enzyme ◽

Topoisomerase 1 ◽

Anticancer Properties ◽

Human Dna ◽

Whole Number ◽

Ic50 Values ◽

Low Cytotoxicity

AbstractUsnic acid, a lichen secondary metabolite produced by a whole number of lichens, has attracted the interest of researchers owing to its broad range of biological activity, including antiviral, antibiotic, anticancer properties, and it possessing a certain toxicity. The synthesis of new usnic acid derivatives and the investigation of their biological activity may lead to the discovery of compounds with better pharmacological and toxicity profiles. In this context, a series of new usnic acid derivatives comprising a terpenoid moiety were synthesized, and their ability to inhibit the catalytic activity of the human DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 was investigated. The most potent compounds (15a, 15b, 15g, and 16a, 16b, 16g) had IC50 values in the range of 0.33 – 2.7 µM. The inhibitory properties were mainly dependent on the flexibility and length of the terpenoid moiety, but not strongly dependent on the configuration of the asymmetric centers. The synthesized derivatives showed low cytotoxicity against human cell lines in an MTT assay. They could be used as a basis for the development of more effective anticancer therapies when combined with topoisomerase 1 inhibitors.

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Study on the Effect of Magesium Ion on the Crystal Phase of Calcium Carbonate

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.554-556.35 ◽

2012 ◽

Vol 554-556 ◽

pp. 35-38

Author(s):

Zhen Fa Liu ◽

Mei Fang Yan ◽

Li Hui Zhang ◽

Hai Hua Li

Keyword(s):

Magnetic Field ◽

Calcium Carbonate ◽

Inhibitory Effect ◽

Crystal Phase ◽

Strong Inhibitory Effect ◽

Blank Solution

Morphology and crystal phase of calcium carbonate, which formed with the presence of Mg2+, were characterized by SEM and XRD. The effect of Mg2+ on crystallization and crystal phase of calcium carbonate was studied. The results showed that the crystal phase of calcium carbonate were mainly calcite and aragonite and the content of aragonite was higher after adding Mg2+ to the blank solution. With the increase of Mg2+ concentration, the content of aragonite increased. The calcium carbonate crystals grain became more fine and the content of aragonite was higher by synergistic treatment between Mg2+ and magnetic field. There was a strong inhibitory effect on calcite when the concentration of Mg2+ was more than 0.50mmol.L-1. The calcite could be transformed into aragonite in the presence of Mg2+ in solution.

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