scholarly journals Effect of dimethylmaleate and phorone on glutathione content of Setaria cervi (Nematoda: Filarioidea) during in vitro incubation

2007 ◽  
Vol 44 (1) ◽  
pp. 14-17 ◽  
Author(s):  
S. Gupta ◽  
N. Banu ◽  
A. Srivastava
Keyword(s):  
Drug Design ◽  
Incubation Period ◽  
Salt Solution ◽  
Glutathione Metabolism ◽  
Setaria Cervi ◽  
Short Incubation Period ◽  
In Vitro Incubation ◽  
Dose Dependent

AbstractGlutathione metabolism represents a prospective target for antifilarial drug design, and therefore, the alterations in glutathione (GSH) content of filarial worms by known mammalian GSH depletors i.e. dimethylmaleate (DMM) and phorone were first thought for investigation in model filarial worms Setaria cervi. The dose dependent GSH depletion was achieved when these worms were incubated at 37°C for 6 h in Hanks balanced salt solution with varying concentrations (10–250 μM) of DMM or phorone. During the short incubation period of 6 h, 250 μM of DMM and phorone declined more than 90 % of the GSH content of filarial worms.

scholarly journals Antifilarial Screening and Oxidative Role of Isolated Fraction from Aegle Marmelos Corr. Leaves Extract

2021 ◽  
Vol 18 (2) ◽  
pp. 395-401
Author(s):  
Sahare K N
Keyword(s):  
Control Level ◽  
Chloroform Extract ◽  
Aegle Marmelos ◽  
Setaria Cervi ◽  
Parasite Motility ◽  
Antifilarial Activity ◽  
Dose Dependent ◽  
Mtt Assays

In the present work antifilarial active fraction was isolated from the leaves Chloroform extract of Aegle marmelos Corr. evaluated in vitro for antifilarial activity and studied the possible oxidative role against Setaria cervi parasite. Antifilarial study was carried out with isolated fractions by worm motility and MTT assays. Complete parasite motility inhibition was observed at 0.002 to 0.08 mg/mL in motility assay and in MTT assay plant fraction gave > 50% reduction 58.9, 74.6 and 97.2% at concentrations 0.02, 0.04 and 0.08 mg/mL at 10, 6 and 2 hours incubation period respectively (p< 0.05). Inhibitory concentration (IC50) was found to be 0.015 mg/mL. Oxidative parameters levels for MDA, Carbonyl content and Nitric oxide were identified as antifilarial activity achieved. The level of oxidative parameters was calculated in dose dependent manners as compared to the control level. The antifilarial activity of isolated fraction is associated with the oxidative mechanism in this study.

Are ovine Leydig cells able to aromatize androgens?

1997 ◽  
Vol 9 (2) ◽  
pp. 193 ◽  
Author(s):  
Barbara Biliska ◽  
Marcin Le´sniak ◽  
Barbara Schmalz
Keyword(s):  
Aromatase Inhibitor ◽  
Incubation Period ◽  
Immunohistochemical Staining ◽  
Leydig Cells ◽  
Culture Medium ◽  
Aromatase Activity ◽  
Dependent Manner ◽  
Dose Dependent ◽  
Testosterone Synthesis

The conversion of testosterone into oestradiol by ovine Leydig cells culturedin vitrowas studied using the non-steroidal aromatase inhibitor CGS 16949A. Additionally, aromatase activity was detected by immunohistochemical staining of cultured Leydig cells or cryosections. The cells were obtained from testes of Polish Mountain rams 5–6 months old (immature) or 12–15 months old (mature). Leydig cells were cultured alone (controls) or incubated for 6 h in the presence of testosterone. Aromatase inhibitor was then added to the cultures which were incubated for a further 18 h. After a 24-h incubation period, testosterone and oestradiol secretion were determined by testing the culture medium using radioimmunological methods. The addition of testosterone to the culture medium enhanced oestradiol synthesis, suggesting that exogenous testosterone could also be aromatized to oestradiol by ovine Leydig cells in vitro. In the presence of CGS 16949A, the conversion of testosterone to oestradiol was significantly suppressed in a dose-dependent manner. All Leydig cells obtained from testes of mature rams and stained immunohistochemically were positive for aromatase, whereas Leydig cells from immature males were negative. The localization of immunoreactive aromatase appeared to be dependent on the age of the donor ram. It is suggested therefore, that mature Leydig cells in the ram are not only the site for testosterone synthesis, they are also capable of converting androgens into oestrogens.

Drug Design Structural Alert

2011 ◽  
Vol 30 (5) ◽  
pp. 546-550 ◽  
Author(s):  
Martin E. Dowty ◽  
George Hu ◽  
Fengmei Hua ◽  
F. Barclay Shilliday ◽  
Heather V. Dowty
Keyword(s):  
Drug Design ◽  
Dependent Manner ◽  
Safety Testing ◽  
Cellular Debris ◽  
Safety Studies ◽  
Structural Alerts ◽  
Testicular Injury ◽  
Dose Dependent

In the process of drug design, it is important to consider potential structural alerts that may lead to toxicosis. This work illustrates how using trifluoroethane as a part of a novel chemical entity led to cytochrome P450 – mediated N-dealkylation and the formation of trifluoroacetaldehyde, a known testicular toxicant, in exploratory safety studies in rats. Testicular toxicosis was noted microscopically in a dose-dependent manner as measured by testicular spermatocytic degeneration and necrosis and excessive intratubular cellular debris in the epididymis. This apparent toxic effect correlated well with the dose-dependent formation of trifluoroacetaldehyde, identified from in vitro rat liver microsome metabolism studies. A similar safety study performed with an N-tetrazole substitution in place of the N-trifluoroethane showed no evidence of testicular injury, implicating further the role of trifluoroacetaldehyde in the testicular lesion observed. These results highlight the relevance of early metabolic and safety testing in assessing potential structural alerts in drug design.

Effect of Temperature on ADP-Induced Platelet Aggregation

1973 ◽  
Vol 29 (01) ◽  
pp. 183-189
Author(s):  
C. A Praga ◽  
E. M Pogliani
Keyword(s):  
Platelet Aggregation ◽  
Incubation Period ◽  
Room Temperature ◽  
Important Variable ◽  
Practical Significance ◽  
Effect Of Temperature ◽  
Induce Platelet Aggregation ◽  
Cuvette Holder ◽  
Exact Temperature

SummaryTemperature represents a very important variable in ADP-induced platelet aggregation.When low doses of ADP ( < 1 (μM) are used to induce platelet aggregation, the length of the incubation period of PRP in the cuvette holder of the aggregometer, thermostatted at 37° C, is very critical. Samples of the same PRP previously kept at room temperature, were incubated for increasing periods of time in the cuvette of the aggregometer before adding ADP, and a significant decrease of aggregation, proportional to the length of incubation, was observed. Stirring of the PRP during the incubation period made these changes more evident.To measure the exact temperature of the PRP during incubation in the aggre- gometer, a thermocouple device was used. While the temperature of the cuvette holder was stable at 37° C, the PRP temperature itself increased exponentially, taking about ten minutes from the beginning of the incubation to reach the value of 37° C. The above results have a practical significance in the reproducibility of the platelet aggregation test in vitro and acquire particular value when the effect of inhibitors of ADP induced platelet aggregation is studied.Experiments carried out with three anti-aggregating agents (acetyl salicyclic acid, dipyridamole and metergoline) have shown that the incubation conditions which influence both the effect of the drugs on platelets and the ADP breakdown in plasma must be strictly controlled.

Increased Protein Synthesis by Human Platelets during Phagocytosis of Latex Particles in Vitro

1976 ◽  
Vol 35 (02) ◽  
pp. 350-357 ◽  
Author(s):  
Hana Bessler ◽  
Galila Agam ◽  
Meir Djaldetti
Keyword(s):  
Protein Synthesis ◽  
Fold Increase ◽  
Human Platelets ◽  
Polystyrene Latex ◽  
Latex Particles ◽  
The Third ◽  
Platelet Protein ◽  
Dose Dependent ◽  
Phagocytotic Activity

SummaryA three-fold increase of protein synthesis by human platelets during in vitro phagocytosis of polystyrene latex particles was detected. During the first two hours of incubation, the percentage of phagocytizing platelets and the number of latex particles per platelet increased; by the end of the third hour, the first parameter remained stable, while the number of latex particles per cell had decreased.Vincristine (20 μg/ml of cell suspension) inhibited platelet protein synthesis. This effect was both time- and dose-dependent. The drug also caused a decrease in the number of phagocytizing cells, as well as in their phagocytotic activity.

The Effect of Adrenaline Infusions on Blood Coagulation in Normal and Haemophilia B Dogs

1966 ◽  
Vol 15 (03/04) ◽  
pp. 349-364 ◽  
Author(s):  
A.H Özge ◽  
H.C Rowsell ◽  
H.G Downie ◽  
J.F Mustard
Keyword(s):  
Body Weight ◽  
Factor Viii ◽  
Factor Ix ◽  
Clotting Factor ◽  
Blood Ph ◽  
Order Of Magnitude ◽  
Dose Dependent ◽  
Generation Test ◽  
Plasma Activity

SummaryThe addition of trace amounts of adrenaline to whole blood in plasma in vitro increased factor VIII, factor IX and whole plasma activity in the thromboplastin generation test. This was dose dependent.Adrenaline infusions less than 22 (μg/kg body weight in normal dogs accelerated clotting, increased factor IX, factor VIII and whole plasma activity in the thromboplastin generation test and caused a fall in blood pH. In a factor IX deficient dog, there was no increase in factor IX activity. After adrenaline infusions, however, the other changes occurred and were of the same order of magnitude as in the normal. Adrenaline in doses greater than 22 μg/kg body weight did not produce as great an effect on clotting in normal or factor IX deficient dogs. The platelet count in the peripheral blood was increased following the infusion of all doses of adrenaline. These observations suggest that the accelerating effect of adrenaline on clotting is not mediated through increase in activity of a specific clotting factor.

Soluble Thrombomodulin Purified from Human Urine Exhibits a Potent Anticoagulant Effect In Vitro and In Vivo

1995 ◽  
Vol 73 (05) ◽  
pp. 805-811 ◽  
Author(s):  
Yasuo Takahashi ◽  
Yoshitaka Hosaka ◽  
Hiromi Niina ◽  
Katsuaki Nagasawa ◽  
Masaaki Naotsuka ◽  
...  
Keyword(s):  
Human Urine ◽  
Specific Activity ◽  
Anticoagulant Activity ◽  
Rabbit Lung ◽  
Soluble Thrombomodulin ◽  
Molecular Weights ◽  
Dose Dependent Fashion ◽  
Dose Dependent

SummaryWe examined the anticoagulant activity of two major molecules of soluble thrombomodulin purified from human urine. The apparent molecular weights of these urinary thrombomodulins (UTMs) were 72,000 and 79,000, respectively. Both UTMs showed more potent cofactor activity for protein C activation [specific activity >5,000 thrombomodulin units (TMU)/mg] than human placental thrombomodulin (2,180 TMU/mg) and rabbit lung thrombomodulin (1,980 TMU/mg). The UTMs prolonged thrombin-induced fibrinogen clotting time (>1 TMU/ml), APTT (>5 TMU/ml), TT (>5 TMU/ml) and PT (>40 TMU/ml) in a dose-dependent fashion. These effects appeared in the concentration range of soluble thrombomodulins present in human plasma and urine. In the rat DIC model induced by thromboplastin, administration of UTMs by infusion (300-3,000 TMU/kg) restored the hematological abnormalities derived from DIC in a dose-dependent fashion. These results demonstrate that UTMs exhibit potent anticoagulant and antithrombotic activities, and could play a physiologically important role in microcirculation.

Oxygenation of 18-hydroxycorticosterone as the final reaction for aldosterone biosynthesis

1984 ◽  
Vol 107 (3) ◽  
pp. 395-400 ◽  
Author(s):  
Itaru Kojima ◽  
Etsuro Ogata ◽  
Hiroshi Inano ◽  
Bun-ichi Tamaoki
Keyword(s):  
Carbon Monoxide ◽  
Hydroxysteroid Dehydrogenase ◽  
Dependent Manner ◽  
In Vitro Production ◽  
Mitochondrial Preparation ◽  
Final Reaction ◽  
Vitro Production ◽  
Dose Dependent ◽  
Cytochrome P 450

Abstract. Incubation of 18-hydroxycorticosterone with the sonicated mitochondrial preparation of bovine adrenal glomerulosa tissue leads to the production of aldosterone, as measured by radioimmunoassay. The in vitro production of aldosterone from 18-hydroxycorticosterone requires both molecular oxygen and NADPH, and is inhibited by carbon monoxide. Cytochrome P-450 inhibitors such as metyrapone, SU 8000. SU 10603, SKF 525A, amphenone B and spironolactone decrease the biosynthesis of aldosterone from 18-hydroxycorticosterone. These results support the conclusion that the final reaction in aldosterone synthesis from 18-hydroxycorticosterone is catalyzed by an oxygenase, but not by 18-hydroxysteroid dehydrogenase. By the same preparation, the production of [3H]aldosterone but not [3H]18-hydroxycorticosterone from [1,2-3H ]corticosterone is decreased in a dose-dependent manner by addition of non-radioactive 18-hydroxycorticosterone.

Differences between antigenic determinants of pig and cat zona pellucida proteins

Reproduction ◽  
2000 ◽  
pp. 15-23 ◽  
Author(s):  
K Jewgenow ◽  
M Rohleder ◽  
I Wegner
Keyword(s):  
In Vitro Fertilization ◽  
Zona Pellucida ◽  
Antigenic Determinants ◽  
Vitro Fertilization ◽  
Contraceptive Vaccine ◽  
Sperm Binding ◽  
Dependent Inhibition ◽  
Dose Dependent Inhibition ◽  
Dose Dependent

Despite many efforts, the control of reproduction in feral cat populations is still a problem in urban regions around the world. Immunocontraception is a promising approach; thus the present study examined the suitability of the widely used pig zona pellucida proteins (pZP) for contraception in feral domestic cats. Purified zona pellucida proteins obtained from pig and cat ovaries were used to produce highly specific antisera in rabbits. Antibodies against pZP raised in rabbits or lions were not effective inhibitors of either in vitro sperm binding (cat spermatozoa to cat oocytes) or in vitro fertilization in cats, whereas antibodies against feline zona pellucida proteins (fZP) raised in rabbits showed a dose-dependent inhibition of in vitro fertilization. Immunoelectrophoresis, ELISA and immunohistology of ovaries confirmed these results, showing crossreactivity of anti-fZP sera to fZP and to a lesser extent to pZP, but no interaction of anti-pZP sera with fZP. It is concluded that cat and pig zonae pellucidae express a very small number of shared antigenic determinants, making the use of pZP vaccine in cats questionable. A contraceptive vaccine based on feline zona pellucida determinants will be a better choice for the control of reproduction in feral cats if immunogenity can be achieved.

Effect of Jatropha curcas Latex on L3 Haemonchus contortus Larval Motility

2017 ◽  
Vol 9 (3) ◽  
Author(s):  
Noorzaid Muhamad ◽  
Syahirah Sazeli ◽  
Resni Mona ◽  
Jannathul Firdous
Keyword(s):  
Larvicidal Activity ◽  
Jatropha Curcas ◽  
Haemonchus Contortus ◽  
Anthelmintic Resistance ◽  
Small Ruminants ◽  
Gastrointestinal Nematodes ◽  
Dose Dependent ◽  
Plants Extract

The anthelmintic resistance has limited the control of gastrointestinal nematodes of small ruminants and thus has awakened interest in the study of plants extract as a source of anthelmintics. These experiments were carried out to evaluate the in vitro efficacy of Jatrophacurcas latex extract against Haemonchuscontortus larval motility. To evaluate the larvicidal activity, H.contortus L3 were incubated with the extracts with varying concentration of 5 mg/mL, 10 mg/mL, 15 mg/mL and 20 mg/mL at 27°C for 48, 72 and 96 hrs. The results were subjected to the Kruskal-Wallis test (P less than 0.05). The extracts showed dose-dependent larvicidal effects. These results suggest that J.curcas can be used to control gastrointestinal nematodes of small ruminants.

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