A bioassay for systemic fungicides using axenic cultures of the carnation rust fungus, Uromyces dianthi

1973 ◽  
Vol 51 (10) ◽  
pp. 2004-2006 ◽  
Author(s):  
D. R. Jones
Keyword(s):  
Inhibitory Action ◽  
Agar Medium ◽  
Rust Fungus ◽  
Screening Programs ◽  
Systemic Fungicides ◽  
Low Concentrations ◽  
Wide Range ◽  
Axenic Cultures ◽  
High Concentrations

The inhibitory action of three systemic fungicides (Benlate, Hoe 6053, and Milstem) on the growth of axenic cultures of the carnation rust fungus, Uromyces dianthi, was assessed. The rust- and smut-specific fungicide (Hoe 6053) was found to inhibit growth when present in the agar medium in very low concentrations, while moderate concentrations of the wide range fungicide (Benlate), and high concentrations of the powdery mildew-specific fungicide (Milstem) were needed for inhibition. The results indicated the possible use of U. dianthi in future in vitro fungicide screening programs and mode-of-action studies.

Effects of polymethoxylated flavone metabolites on apoB100 secretion and MTP activity in Huh7.5 cells

2021 ◽  
Vol 18 ◽  
Author(s):  
Danielle R. Gonçalves ◽  
Thais B. Cesar ◽  
John A. Manthey ◽  
Paulo I. Costa
Keyword(s):  
Lipid Synthesis ◽  
Dependent Manner ◽  
Transfer Protein ◽  
Low Concentrations ◽  
Wide Range ◽  
Cell Assays ◽  
Polymethoxylated Flavones ◽  
High Concentrations

Background: Citrus polymethoxylated flavones (PMFs) reduce the synthesis of liver lipoproteins in animal and in vitro cell assays, but few studies have evaluated the direct effects of their metabolites on this highly regulated process. Objective: To investigate the effects of representative metabolites of PMF on the secretion of liver lipoproteins using the mammalian cell Huh7.5. Method: In this study, the influences of three PMFs and five previously isolated PMF metabolites on hepatic apoB-100 secretion and microsomal transfer protein (MTP) activity were evaluated. Tangeretin (TAN), nobiletin (NOB) and 3,5,6,7,8,3′,4′-heptamethoxyflavone (HMF), and their glucuronides (TAN-Gluc, NOB-Gluc and HMF-Gluc) and oxidatively demethylated metabolites (TAN-OH, NOB-OH, HMF-OH) were incubated with Huh7.5 cells to measure their inhibitory effects on lipid synthesis. Results: The results showed that TAN, HMF and TAN-OH reduced the secretion of apoB-100 in a dose-dependent manner, while NOB and the other tested metabolites showed no inhibition. MTP activity in the Huh7.5 cells was significantly reduced in the presence of low concentrations of TAN, and in high concentrations of NOB-OH. This study also showed that PMFs and PMF metabolites produced a wide range of effects on apoB-100 secretion and MTP activity. Conclusion: The results suggest that while PMFs and their metabolites control dyslipidemia in vivo, the inhibition of MTP activity cannot be the only pathway influenced by these compounds.

In Vitro Effects of Ethanol on Rabbit Platelet Aggregation, Secretion of Granule Contents, and Cyclic AMP Levels in the Presence of Prostacyclin

1989 ◽  
Vol 61 (02) ◽  
pp. 254-258 ◽  
Author(s):  
Margaret L Rand ◽  
Peter L Gross ◽  
Donna M Jakowec ◽  
Marian A Packham ◽  
J Fraser Mustard
Keyword(s):  
Cyclic Amp ◽  
Inhibitory Effect ◽  
Rabbit Platelet ◽  
Inhibitory Effects ◽  
Low Concentrations ◽  
Rabbit Platelets ◽  
High Concentrations ◽  
In Vitro Effects ◽  
Aggregation Of Platelets

SummaryEthanol, at physiologically tolerable concentrations, inhibits platelet responses to low concentrations of collagen or thrombin, but does not inhibit responses of washed rabbit platelets stimulated with high concentrations of ADP, collagen, or thrombin. However, when platelet responses to high concentrations of collagen or thrombin had been partially inhibited by prostacyclin (PGI2), ethanol had additional inhibitory effects on aggregation and secretion. These effects were also observed with aspirin- treated platelets stimulated with thrombin. Ethanol had no further inhibitory effect on aggregation of platelets stimulated with ADP, or the combination of ADP and epinephrine. Thus, the inhibitory effects of ethanol on platelet responses in the presence of PGI2 were very similar to its inhibitory effects in the absence of PGI2, when platelets were stimulated with lower concentrations of collagen or thrombin. Ethanol did not appear to exert its inhibitory effects by increasing cyclic AMP above basal levels and the additional inhibitory effects of ethanol in the presence of PGI2 did not appear to be brought about by further increases in platelet cyclic AMP levels.

Aggregation of Cat Platelets in Vitro

1970 ◽  
Vol 23 (03) ◽  
pp. 601-620 ◽  
Author(s):  
Th. B Tschopp
Keyword(s):  
Adenosine Monophosphate ◽  
Blood Collection ◽  
Base Line ◽  
Reversible Aggregation ◽  
Low Concentrations ◽  
Irreversible Aggregation ◽  
High Concentrations ◽  
Two Phases ◽  
Improved Technique

SummaryAggregation of cat platelets in the citrated plasma is examined by means of Born’s absorptiometer. A marked tendency of the platelets of this species to spontaneous aggregation necessitated first of all the development of an improved technique of blood collection.A hypothesis according to which 5-HT is released from the platelets, explains the absence of oscillations on the base line of the absorptiometer, the absence of platelet swelling, when ADP is added, and the effect of stirring on the aggregation curves in cat PRP. The average volume of cat platelets amounts to 10.46 μ3 when directly fixed in the blood, when fixed from PRP to 12.17 μ3, when fixed from stirred PRP to 13.51 μ3.In low concentrations (0.3-2 μM) ADP produce reversible aggregation; in narrowly restricted, individually dissimilar mean concentrations irreversible aggregation in two phases and in high concentrations, irreversible aggregation in one phase. Like ADP serotonin produces 2 phase irreversible aggregation in concentrations of 3-10 μM, but unlike ADP, the aggregation velocity decreases again with high 5-HT concentrations (>100 μM). Adrenaline does not produce aggregation and it is likely that adenosine and adenosine monophosphate inhibit the aggregation by serotonin but not by ADP. Species differences in the aggregation of human, rabbit and cat platelets are discussed.

Application of the EYTEX™ System to the Evaluation of Cosmetic Products and their Ingredients

1992 ◽  
Vol 20 (1) ◽  
pp. 146-163
Author(s):  
Francis H. Kruszewski ◽  
Laura H. Hearn ◽  
Kyle T. Smith ◽  
Janice J. Teal ◽  
Virginia C. Gordon ◽  
...  
Keyword(s):  
Double Blind ◽  
Eye Irritation ◽  
Ocular Irritation ◽  
Rabbit Eye ◽  
Wide Range ◽  
High Concentrations ◽  
Alkaline Membrane ◽  
Positive Agreement

465 cosmetic product formulations and raw ingredients were evaluated with the EYTEX™ system to determine the potential of this in vitro alternative for identifying eye irritation potential. The EYTEX™ system is a non-animal, biochemical procedure developed by Ropak Laboratories, Irvine, CA, that was designed to approximate the Draize rabbit eye irritation assay for the evaluation of ocular irritation. Avon Products Inc. provided all the test samples, which included over 30 different product types and represented a wide range of eye irritancy. All the EYTEX™ protocols available at the time of this study were used. Samples were evaluated double-blind with both the membrane partition assay (MPA) and the rapid membrane assay (RMA). When appropriate, the standard assay (STD) and the alkaline membrane assay (AMA) were used, as well as specific, documented protocol modifications. EYTEX™ results were correlated with rabbit eye irritation data which was obtained from the historical records of Avon Products Inc. A positive agreement of EYTEX™ results with the in vivo assay was demonstrated by an overall concordance of 80%. The assay error was 20%, of which 18% was due to an overestimation of sample irritancy (false positives) and 2% was attributed to underestimation (false negatives). Overestimation error in this study was due in part to the inability of the protocols to accurately classify test samples with very low irritation potential. Underestimation of sample irritancy was generally associated with ethoxylated materials and high concentrations of specific types of surfactants. 100% sensitivity and 85% predictability were described by the data, indicating the efficiency of EYTEX™ in identifying known irritants. A specificity rate of 39% showed the EYTEX™ assay to be weak in discerning non-irritants. However, the EYTEX™ protocols used in this study were not designed to identify non-irritants. A compatibility rate of 99% proved the effectiveness of the EYTEX™ assay in accommodating a diversity of product types. The EYTEX™ system protocols, when used appropriately, can provide a conservative means of assessing the irritant potential of most cosmetic formulations and their ingredients.

scholarly journals In Vitro Synergistic Interactions of Isavuconazole and Echinocandins against Candida auris

Antibiotics ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 355
Author(s):  
Unai Caballero ◽  
Sarah Kim ◽  
Elena Eraso ◽  
Guillermo Quindós ◽  
Valvanera Vozmediano ◽  
...  
Keyword(s):  
Interaction Model ◽  
Antifungal Drugs ◽  
Health Concern ◽  
Candida Auris ◽  
Fungistatic Activity ◽  
Drug Concentrations ◽  
Low Concentrations ◽  
Wide Range ◽  
Time Kill

Candida auris is an emergent fungal pathogen that causes severe infectious outbreaks globally. The public health concern when dealing with this pathogen is mainly due to reduced susceptibility to current antifungal drugs. A valuable alternative to overcome this problem is to investigate the efficacy of combination therapy. The aim of this study was to determine the in vitro interactions of isavuconazole with echinocandins against C. auris. Interactions were determined using a checkerboard method, and absorbance data were analyzed with different approaches: the fractional inhibitory concentration index (FICI), Greco universal response surface approach, and Bliss interaction model. All models were in accordance and showed that combinations of isavuconazole with echinocandins resulted in an overall synergistic interaction. A wide range of concentrations within the therapeutic range were selected to perform time-kill curves. These confirmed that isavuconazole–echinocandin combinations were more effective than monotherapy regimens. Synergism and fungistatic activity were achieved with combinations that included isavuconazole in low concentrations (≥0.125 mg/L) and ≥1 mg/L of echinocandin. Time-kill curves revealed that once synergy was achieved, combinations of higher drug concentrations did not improve the antifungal activity. This work launches promising results regarding the combination of isavuconazole with echinocandins for the treatment of C. auris infections.

THE SELECTIVE PROTEOLYTIC ENZYME INHIBITORY ACTION OF BENZETHONIUM CHLORIDE

1960 ◽  
Vol 38 (1) ◽  
pp. 25-32 ◽  
Author(s):  
Ivan T. Beck ◽  
E. Pinter ◽  
R. D. McKenna ◽  
H. Griff
Keyword(s):  
Subcutaneous Injection ◽  
Proteolytic Enzyme ◽  
Inhibitory Action ◽  
Hemorrhagic Pancreatitis ◽  
Benzethonium Chloride ◽  
Tryptic Activity ◽  
High Concentrations ◽  
Acute Hemorrhagic Pancreatitis ◽  
Very High

Acute hemorrhagic pancreatitis in humans is thought to be perpetuated by the autolytic processes catalyzed by trypsin and lipase. This study is an integral part of our search for trypsin and lipase inhibitors to be used in the treatment of this disease.Benzethonium chloride was found to inhibit tryptic activity in vitro. The proteolytic activity of rabbit's serum was inhibited, and the inhibition was most pronounced 6 to 12 hours after the subcutaneous injection of the compound. Fibrinolysin was also inhibited in vitro but benzethonium chloride had no inhibitory action on chymotrypsin, pepsin, or lipase.Serum proteins in vitro were precipitated only with very high concentrations of the compound. No significant protein changes were observed in sera of rabbits after the subcutaneous injection of the compound.

Prostacyclin and cerebral vessel relaxation

1982 ◽  
Vol 57 (3) ◽  
pp. 334-340 ◽  
Author(s):  
Kamal S. Paul ◽  
Eric T. Whalley ◽  
Christine Forster ◽  
Richard Lye ◽  
John Dutton
Keyword(s):  
Angiotensin Ii ◽  
Arterial Spasm ◽  
Cerebral Vessel ◽  
Content Type ◽  
Wide Range ◽  
Potent Vasodilator ◽  
Dose Dependent Fashion ◽  
Basilar Arteries ◽  
High Concentrations

✓ The authors have studied the ability of prostacyclin to reverse contractions of human basilar arteries in vitro that were induced by a wide range of substances implicated in the etiology of cerebral arterial spasm. Prostacyclin (10−10 to 10−6M) caused a dose-related reversal of contractions induced by 5-hydroxytryptamine, noradrenaline, angiotensin II, prostaglandin (PG)F2α, and U-46619 (a thromboxane-A2 mimetic). These agents were tested at concentrations or volumes that produced almost maximum or maximum responses and those that produced approximately 50% of the maximum response. Contractions induced by maximum concentrations of angiotensin II and U-46619 were least affected by prostacyclin. In addition, contractions induced by thromboxane-A2 generated from guinea-pig lung were reversed in a dose-dependent fashion by prostacyclin. This ability of prostacyclin to physiologically antagonize contractions of the human basilar artery in vitro induced by high concentrations of various spasmogenic agents suggests that such a potent vasodilator agent or more stable analogue may be of value in the treatment of such disorders as cerebral arterial spasm following subarachnoid hemorrhage.

scholarly journals In vitro antimicrobial activity of the organic extract of Cladonia substellata Vainio and usnic acid against Staphylococcus spp. obtained from cats and dogs

2017 ◽  
Vol 37 (4) ◽  
pp. 368-378 ◽  
Author(s):  
Jusciêne B. Moura ◽  
Agueda C. de Vargas ◽  
Gisele V. Gouveia ◽  
João J. de S. Gouveia ◽  
Juracy C. Ramos-Júnior ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biological Activities ◽  
Meca Gene ◽  
Usnic Acid ◽  
Organic Extract ◽  
In Vitro Antimicrobial Activity ◽  
Low Concentrations ◽  
Wide Range ◽  
Staphylococcus Spp

ABSTRACT: Cladonia substellata Vainio is a lichen found in different regions of the world, including the Northeast of Brazil. It contains several secondary metabolites with biological activity, including usnic acid, which has exhibited a wide range of biological activities. The aim of this study was to evaluate the in vitro antimicrobial activity of the organic extract of C. substellata and purified usnic acid. Initially, Staphylococcus spp., derived from samples of skin and ears of dogs and cats with suspected pyoderma and otitis, were isolated and analyzed. In antimicrobial susceptibility testing against Staphylococcus spp., 77% (105/136) of the isolates were resistant to the antimicrobials tested. In the assessment of biofilm production, 83% (113/136) were classified as producing biofilm. In genetic characterization, 32% (44/136) were positive for blaZ, no isolate (0/136) was positive for the mecA gene, and 2% (3/136) were positive for the icaD gene. The in vitro antimicrobial activity of the organic extract of C. substellata and purified usnic acid against Staphylococcus spp. ranged from 0.25mg/mL to 0.0019mg/mL, inhibiting bacterial growth at low concentrations. The substances were more effective against biofilm-producing bacteria (0.65mg/mL-0.42mg/mL) when compared to non-biofilm producing bacteria (2.52mg/mL-2.71mg/mL). Usnic acid and the organic extract of C. substellata can be effective in the treatment of pyoderma and otitis in dogs and cats caused by Staphylococcus spp.

An evaluation of potential seed treatments to control Fusarium solani f.sp. phaseoli, the cause of foot and root rot of Phaseolus vulgaris

1977 ◽  
Vol 89 (1) ◽  
pp. 235-238 ◽  
Author(s):  
P. E. Russell ◽  
A. E. A. Mussa
Keyword(s):  
Phaseolus Vulgaris ◽  
Fusarium Solani ◽  
Root Rot ◽  
Similar Pattern ◽  
Fungal Growth ◽  
Systemic Fungicide ◽  
Product Concentration ◽  
Low Concentrations ◽  
High Concentrations

SummaryTwo systemic fungicides, benomyl and thiabendazole, were more active than the non-systemic fungicide Drazoxolon in inhibiting fungal growth in vitro. A similar pattern was obtained in glasshouse trials with benomyl and thiabendazole giving adequate protection at low concentrations while Drazoxolon was ineffective unless applied at 50% the commercial product concentration. A field trial using thiabendazole, Drazoxolon and a mixture of benomyl and thiram confirmed the glasshouse results.Some phytotoxicity was noticed with high concentrations of both benomyl and thiabendazole, but satisfactory disease control was achieved using fungicide concentrations which did not induce phytotoxicity.

scholarly journals Colchicine-binding protein of the liver. Its characterization and relation to microtubules.

1975 ◽  
Vol 66 (3) ◽  
pp. 609-620 ◽  
Author(s):  
C Patzelt ◽  
A Singh ◽  
Y L Marchand ◽  
L Orci ◽  
B Jeanrenaud
Keyword(s):  
High Speed ◽  
Specific Binding ◽  
Electrophoretic Analysis ◽  
Binding Activity ◽  
Low Concentrations ◽  
Electrophoretic Behavior ◽  
High Affinity Binding Site ◽  
High Concentrations

Colchicine-binding activity of mouse liver high-speed supernate has been investigated. It has been found to be time and temperature dependent. Two binding activities with different affinities for colchicine seem to be present in this high-speed supernate, of which only the high-affinity binding site (half maximal binding at 5 x 10(-6) M colchicine) can be attributed to microtubular protein by comparison with purified tubulin. Vinblastine interacted with this binding activity by precipitating it when used at high concentrations (2 x 10(-3) M), and by stabilizing it at low concentrations (10(-5) M). Lumicolchicine was found not to compete with colchicine. The colchicine-binding activity was purified from liver and compared with that of microtubular protein from brain. The specific binding activity of the resulting preparation, its electrophoretic behavior, and the electron microscope appearance of the paracrystals obtained upon its precipitation with vinblastine permitted its identification as microtubular protein (tubulin). Electrophoretic analysis of the proteins from liver supernate that were precipitated by vinblastine indicated that this drug was not specific for liver tubulin. Preincubation of liver supernate with 5 mM EGTA resulted in a time-dependent decrease of colchicine-binding activity, which was partly reversed by the addition of Ca++. However, an in vitro formation of microtubules upon lowering the Ca++ concentration could not be detected. Finally, a method was developed enabling that portion of microtubular protein which was present as free tubulin to be measured and to be compared with the total amount of this protein in the tissue. This procedure permitted demonstration of the fact that, under normal conditions, only about 40% of the tubulin of the liver was assemled as microtubules. It is suggested that, in the liver, rapid polymerization and depolymerization of microtubules occur and may be an important facet of the functional role of the microtubular system.

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