scholarly journals Short Communication:In VitroEfficacy Testing of Praziquantel, Ivermectin, and Oxfendazole againstTaenia SoliumCysts

2012 ◽  
Vol 2012 ◽  
pp. 1-4 ◽  
Author(s):  
S. Cederberg ◽  
C. S. Sikasunge ◽  
Å. Andersson ◽  
M. V. Johansen
Keyword(s):  
Culture Media ◽  
Taenia Solium ◽  
Effective Concentration ◽  
Effect Measurement ◽  
Recommended Dose ◽  
Drug Of Choice ◽  
Porcine Cysticercosis ◽  
Half Maximal Effective Concentration ◽  
Brain Cysts

Oxfendazole is recommended as the drug of choice for treating porcine cysticercosis. The drug does not kill brain cysts and is not registered for use in pigs. Latest its safety in the recommended dose has been questioned. The aim of this study was to investigate two alternative anthelminthics. The efficacy of praziquantel and ivermectin was compared to oxfendazoleIn VitroonTaenia solium. Cysts ofT. soliumwere isolated from infected pork and incubated in culture media together with the drugs. The degree of evagination was used as effect measurement and determined after 6 hours. Praziquantel had a half maximal effective concentration (EC50) of value 0.006 ± 0.001 μg/mL. Ivermectin did not show any impact on the evagination in concentrations from 0.001 to 30 μg/mL and neither did oxfendazole in concentrations from 0.001 to 50 μg/mL.

scholarly journals Impact of L-carnitine supplementation on the in vitro developmental competence and cryotolerance of buffalo embryos

2021 ◽  
pp. 3164-3169
Author(s):  
Mohamed M. M. El-Sokary ◽  
Al-Shimaa Al-H. H. El-Naby ◽  
Amal R. Abd El Hameed ◽  
Karima Gh. M. Mahmoud ◽  
T. H. Scholkamy
Keyword(s):  
Embryo Culture ◽  
In Vitro Maturation ◽  
Culture Media ◽  
Effective Concentration ◽  
Developmental Competence ◽  
Carnitine Supplementation ◽  
Oocyte Developmental Competence ◽  
High Lipid ◽  
Significant Difference

Background and Aim: Despite many trials, buffalo embryos have poor cryosurvivability because of their high lipid content. L-carnitine was found to be a lipid-reducing agent when added to oocyte and embryo culture media. The study aimed to determine the most effective concentration of L-carnitine to improve the oocyte developmental competence and cryotolerance of buffalo embryos. Materials and Methods: In vitro maturation and embryo culture media were supplemented with four concentrations of L-carnitine: 0 (control), 0.25, 0.5, and 1 mM. Good-quality embryos on 7 days were vitrified using mixtures of dimethyl sulfoxide and ethylene glycol at two concentrations (3.5 and 7 M). Results: The result showed that the cleavage and morula rates were significantly (p<0.05) higher in the 0.5 mM group. Blastocyst rates were significantly (p<0.05) higher at both 0.5 and 1 mM. The rates of viable embryos directly after thawing were significantly (p<0.05) increased in the 0.5 mM group. No significant difference was found in embryos cultured for 24 h after warming among all the groups. Conclusion: The addition of L-carnitine at a concentration of 0.5 mM to the culture media improves the oocyte developmental competence and cryotolerance of buffalo embryos directly after warming but not after 24 h of culture. Nevertheless, further studies must identify how L-carnitine exerts its beneficial micromechanisms.

scholarly journals In VitroEfficacy of Brincidofovir against Variola Virus

2014 ◽  
Vol 58 (9) ◽  
pp. 5570-5571 ◽  
Author(s):  
Victoria A. Olson ◽  
Scott K. Smith ◽  
Scott Foster ◽  
Yu Li ◽  
E. Randall Lanier ◽  
...  
Keyword(s):  
Animal Models ◽  
Effective Concentration ◽  
Variola Virus ◽  
Half Maximal Effective Concentration ◽  
Animal Rule ◽  
Virus Strains ◽  
Lipid Conjugate

ABSTRACTBrincidofovir (CMX001), a lipid conjugate of the acyclic nucleotide phosphonate cidofovir, is under development for smallpox treatment using “the Animal Rule,” established by the FDA in 2002. Brincidofovir reduces mortality caused by orthopoxvirus infection in animal models. Compared to cidofovir, brincidofovir has increased potency, is administered orally, and shows no evidence of nephrotoxicity. Here we report that the brincidofovir half-maximal effective concentration (EC50) against five variola virus strainsin vitroaveraged 0.11 μM and that brincidofovir was therefore nearly 100-fold more potent than cidofovir.

scholarly journals Amnestic Concentrations of Etomidate Modulate GABAA,slowSynaptic Inhibition in Hippocampus

2009 ◽  
Vol 111 (4) ◽  
pp. 766-773 ◽  
Author(s):  
Shuiping Dai ◽  
Misha Perouansky ◽  
Robert A. Pearce
Keyword(s):  
Time Constant ◽  
Hippocampal Slices ◽  
Effective Concentration ◽  
Detectable Effect ◽  
Gamma Aminobutyric Acid ◽  
Gaba A ◽  
Phasic Inhibition ◽  
Half Maximal Effective Concentration

Background Gamma-aminobutyric acid type A (GABA(A)) receptor-mediated inhibition in the central nervous system exists in two forms: phasic (inhibitory postsynaptic currents, IPSCs) and tonic (nonsynaptic). Phasic inhibition is further subdivided into fast (GABA(A,fast)) and slow (GABA(A,slow)) IPSCs. By virtue of its dendritic location and kinetics, GABA(A,slow) has been proposed to control synaptic plasticity and memory. Etomidate is a nonbarbiturate, intravenous anesthetic that selectively modulates GABA(A) receptors and produces amnesia at low doses in vivo. This study tested whether correspondingly low concentrations of etomidate in vitro alter GABA(A,fast) and GABA(A,slow) phasic inhibition. Methods Electrophysiological recordings were obtained from hippocampal slices prepared from postnatal day 3-8 mice and maintained in organotypic culture for 10-14 days. Etomidate was applied at concentrations corresponding to one-half to four times the half maximal effective concentration that impairs hippocampus-dependent learning and memory--i.e., 0.125-1.0 microm. Results Etomidate 0.25 microm (the half maximal effective concentration) doubled the time constant of decay of GABA(A,slow) IPSCs, but it had no detectable effect on GABA(A,fast) IPSCs. Higher concentrations of etomidate had stronger effects on both types of phasic inhibition: 0.5 and 1 microm etomidate prolonged the time constant of decay by 310% and 410% for GABA(A,slow) and by 25% and 78% for GABA(A,fast). Concentrations of etomidate up to 1 microm had no significant effects on the amplitudes of either GABA(A,fast) or GABA(A,slow) IPSCs. Conclusions At concentrations that impair hippocampus-dependent memory, etomidate modulates GABA(A,slow) more strongly than GABA(A,fast) IPSCs. Effects of etomidate on GABA(A,slow) IPSCs may contribute to etomidate-induced amnesia.

scholarly journals In vitro anti-motility and antispasmodic effects of Garcinia mangostana extracts in isolated chicken ileum preparation

2019 ◽  
Vol 10 (2) ◽  
pp. 1444-1447
Author(s):  
Michelle Ooi Yi Ching ◽  
Sasikala Chinnappan ◽  
Mogana Sundari Rajagopal
Keyword(s):  
Effective Concentration ◽  
Aqueous Extracts ◽  
Inhibitory Effects ◽  
Garcinia Mangostana ◽  
Response Curves ◽  
Half Maximal Effective Concentration ◽  
Set Up ◽  
Smooth Muscle Contractions ◽  
Significant Concentration

Garcinia mangostana pericarps have been traditionally used in Southeast Asia for a variety of medicinal conditions. The present study was carried out to determine the anti-motility and antispasmodic effects of methanolic and aqueous G. mangostana extracts (MEM and AEM) on isolated chicken ileum. Extracts were prepared from the pericarp of G. mangostana using maceration technique with methanol and distilled water. Isolated ileum preparations were set up for recording in Tyrode’s solution at 37°C. Dose-response curves were plotted using various doses of agonist as control such as acetylcholine (ACh) and histamine. Atropine, mepyramine and extracts were used as an antagonist. The results showed that methanolic and aqueous extracts possess significant concentration-dependent inhibitory effects (p<0.05) on agonist-induced contractions. The half maximal effective concentration (EC50) of extracts and standard antagonists were higher than the agonist alone. Both methanolic and aqueous extract of G. mangostana exerts anti-motility and antispasmodic effects on smooth muscle contractions. The study provides findings that support G. mangostana can be the potential treatment for diarrhoea and spasm.

scholarly journals Investigation of Fertilizing Capacity of Zebrafish (Danio rerio) Sperm Exposed to Heavy Metals

Dose-Response ◽  
2020 ◽  
Vol 18 (2) ◽  
pp. 155932582091959
Author(s):  
Flóra Kerekes ◽  
Tímea Kollár ◽  
Gyöngyi Gazsi ◽  
Eszter Kása ◽  
Béla Urbányi ◽  
...  
Keyword(s):  
Heavy Metals ◽  
Embryonic Development ◽  
Danio Rerio ◽  
Aquatic Environment ◽  
Fertilization Rate ◽  
Effective Concentration ◽  
Toxicological Studies ◽  
Half Maximal Effective Concentration ◽  
The Given

The objective of our study was to investigate the effects of heavy metals on the fertilizing capacity of exposed zebrafish sperm, on embryonic survival, and on occurrence of embryonic deformities following fertilization with exposed sperm. It is important to test heavy metals because they are well-known pollutants. Sperm of externally fertilizing species can get in contact with pollutants found in aquatic environment. Zebrafish sperm, despite its advantages, has seldom been used in in vitro toxicological studies and no reports are available regarding the fertilizing capacity of exposed sperm. Zebrafish sperm was stripped and exposed to concentrations of the tested heavy metals (Zn2+, Cd2+, Cr3+, Cu2+, Ni2+, Hg2+, As3+) for 30 or 120 minutes. Calculated half-maximal effective concentration (EC50) values do not differ significantly from those calculated for motility for any of the tested heavy metals, which means fertilization rate can indicate the toxicity of the given substance following exposure of sperm. Thus, its application as in vitro toxicological end point is reasonable. The survival of embryos and embryonic development have not been affected by the exposure of spermatozoa, which means all alterations in spermatozoa caused by heavy metals have been expressed before 24 hours post fertilization.

Differential in vitro effects of insulin on Taenia crassiceps and Taenia solium cysticerci

2009 ◽  
Vol 83 (4) ◽  
pp. 403-412 ◽  
Author(s):  
G. Escobedo ◽  
M.C. Romano ◽  
J. Morales-Montor
Keyword(s):  
Insulin Receptor ◽  
Molecular Mechanisms ◽  
Taenia Solium ◽  
Normal Female ◽  
Taenia Crassiceps ◽  
Larval Stages ◽  
Porcine Cysticercosis ◽  
In Vitro Effects ◽  
Specific Insulin

AbstractHormones play a significant role in murine cysticercosis (Taenia crassiceps), and increase the frequency of porcine cysticercosis caused by Taenia solium. In the present study, we report the in vitro effect of insulin on the larval stages of T. crassiceps (ORF strain) and T. solium. In vitro exposure of T. crassiceps cysticerci to insulin was found to stimulate this parasite's reproduction twofold with respect to control values, while the same treatment had no effect on T. solium cysticerci. Moreover, normal female mice (BALB/cAnN) infected with T. crassiceps cysticerci previously exposed to insulin presented larger parasite loads than mice inoculated with vehicle-treated cysticerci. To determine the possible molecular mechanisms by which insulin affects T. crassiceps, the insulin receptor was amplified by means of reverse transcriptase-polymerase chain reaction (RT-PCR). Interestingly, both T. crassiceps and T. solium expressed the insulin receptor, although insulin had effects only on T. crassiceps. These results demonstrate that insulin has a dichotomistic effect; it acts directly only on T. crassiceps cysticerci reproduction, possibly through its binding to a specific insulin receptor synthesized by the parasite. Thus, insulin may be recognized by T. crassiceps cysticercus cells as a mitogenic factor, and contribute to parasite proliferation inside the host, as well as to the female mouse susceptibility to T.crassiceps. This phenomenon has not been reported for cysticercosis caused by T. solium, which could, in part, be related to the poor effect of insulin upon the human parasite.

scholarly journals Distribution, Pathotypes, and Metalaxyl Sensitivity of Phytophthora sojae from Heilongjiang and Fujian Provinces in China

Plant Disease ◽  
2010 ◽  
Vol 94 (7) ◽  
pp. 881-884 ◽  
Author(s):  
Linkai Cui ◽  
Weixiao Yin ◽  
Qinghua Tang ◽  
Suomeng Dong ◽  
Xiaobo Zheng ◽  
...  
Keyword(s):  
Root Rot ◽  
Phytophthora Sojae ◽  
Effective Concentration ◽  
Effective Management ◽  
Population Status ◽  
The Past ◽  
Metalaxyl Sensitivity ◽  
Half Maximal Effective Concentration ◽  
Soybean Leaf

Phytophthora sojae causes root and stem rot, one of the most devastating diseases of soybean worldwide. In Heilongjiang and Fujian provinces in China, serious cases of Phytophthora stem and root rot have occurred and caused heavy losses in the past several years. To determine the current population status of this pathogen, we investigated the pathogen's distribution, pathotypes, and metalaxyl sensitivity in both provinces. P. sojae was baited and isolated from 258 soil samples in both provinces using the soybean leaf bait method. The pathotypes of all isolates were characterized on 13 differential soybean cultivars using the hypocotyl slit inoculation method, and the sensitivity of all isolates to metalaxyl was tested in vitro. In all, 75 isolates were recovered from 75 fields in 33 counties; of these, 31 counties were in Heilongjiang Province and 2 counties were in Fujian Province. Thirty-five new pathotypes were identified compared with the previously defined races. Less than 5% of the isolates were virulent to cultivars with individual Rps genes 1a, 1c, or 1k. No metalaxyl-resistant isolates were found; the half maximal effective concentration values of all isolates ranged from 0.04 to 0.22 μg ml–1. These results suggest that effective management of the disease in both provinces can be accomplished through the use of resistant cultivars with Rps genes 1a, 1c, or 1k and the fungicide metalaxyl.

scholarly journals Effect of selected nonsteroidal anti-inflammatory drugs on the viability of canine osteosarcoma cells of the D-17 line: in vitro studies

2019 ◽  
Vol 63 (3) ◽  
pp. 399-403 ◽  
Author(s):  
Dominik Poradowski ◽  
Bożena Obmińska-Mrukowicz
Keyword(s):  
Effective Concentration ◽  
Tolfenamic Acid ◽  
Osteosarcoma Cells ◽  
Anticancer Effect ◽  
Canine Osteosarcoma ◽  
Half Maximal Effective Concentration ◽  
Analysis Of Results ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Abstract Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used in veterinary medicine. They are used in pain control and in anti-inflammatory and antipyretic therapies. Some NSAIDs, e.g piroxicam, also have a documented anticancer effect. The objective of this study was to evaluate which of the commonly used NSAIDs (etodolac, flunixin, tolfenamic acid, carprofen, and ketoprofen) are cytotoxic to the D-17 cell line of canine osteosarcoma. Material and Methods The viability of the cells was evaluated using the MTT assay. Four independent repetitions were performed and the results are given as the average of these values; EC50 values (half maximal effective concentration) were also calculated. Results The analysis of results showed that carprofen and tolfenamic acid displayed the highest cytotoxicity. Other drugs either did not provide such effects or they were very poor. For carprofen, it was possible to determine an EC50 which fell within the limits of concentrations obtainable in canine serum after the administration of routinely used doses. Conclusion The results are promising but further studies should be conducted to confirm them, since this study is only preliminary. The possibility of introducing carprofen and tolfenamic acid into the routine treatment of osteosarcoma in dogs should be considered.

scholarly journals Emetine, Ipecac, Ipecac Alkaloids and Analogues as Potential Antiviral Agents for Coronaviruses

2020 ◽  
Vol 13 (3) ◽  
pp. 51 ◽  
Author(s):  
Martin Bleasel ◽  
Gregory Peterson
Keyword(s):  
Side Effects ◽  
Treatment Options ◽  
Antiviral Agents ◽  
Effective Concentration ◽  
Potential Treatment ◽  
Optimal Method ◽  
Half Maximal Effective Concentration ◽  
Related Compounds ◽  
Old Drugs

The COVID-19 coronavirus is currently spreading around the globe with limited treatment options available. This article presents the rationale for potentially using old drugs (emetine, other ipecac alkaloids or analogues) that have been used to treat amoebiasis in the treatment of COVID-19. Emetine had amongst the lowest reported half-maximal effective concentration (EC50) from over 290 agents screened for the Middle East respiratory syndrome (MERS) and severe acute respiratory syndrome (SARS) coronaviruses. While EC50 concentrations of emetine are achievable in the blood, studies show that concentrations of emetine can be almost 300 times higher in the lungs. Furthermore, based on the relative EC50s of emetine towards the coronaviruses compared with Entamoeba histolytica, emetine could be much more effective as an anti-coronavirus agent than it is against amoebiasis. This paper also discusses the known side effects of emetine and related compounds, how those side effects can be managed, and the optimal method of administration for the potential treatment of COVID-19. Given the serious and immediate threat that the COVID-19 coronavirus poses, our long history with emetine and the likely ability of emetine to reach therapeutic concentrations within the lungs, ipecac, emetine, and other analogues should be considered as potential treatment options, especially if in vitro studies confirm viral sensitivity.

Erythromycin contracts rabbit colon myocytes via occupation of motilin receptors

1992 ◽  
Vol 262 (1) ◽  
pp. G50-G55 ◽  
Author(s):  
W. L. Hasler ◽  
A. Heldsinger ◽  
O. Y. Chung
Keyword(s):  
Dissociation Constant ◽  
Effective Concentration ◽  
Rabbit Colon ◽  
Colonic Motor ◽  
Half Maximal Effective Concentration ◽  
Gastroduodenal Motility ◽  
Maximal Binding ◽  
Motilin Receptor ◽  
Dissociation Constant Kd

Erythromycin stimulates gastroduodenal motility via action on motilin receptors. We evaluated erythromycin as a colonic muscle motilin agonist using in vitro rabbit colon studies. Isolated myocytes contracted to erythromycin with a half-maximal effective concentration of 2 pM and peak shortening of 22.4 +/- 2.5% at 1 nM, which was superimposable with the response to motilin. 125I-labeled motilin binding to colon muscle homogenates was saturable and specific with a dissociation constant (Kd) of 0.39 nM and maximal binding (Bmax) of 41 +/- 3 fmol/mg protein. Motilin displaced specifically bound 125I-motilin, with a Kd of 0.31 nM. Erythromycin displaced 125I-motilin but was less potent, with an inhibitory constant of 84.0 nM. Bmax values from displacement studies were similar to the Scatchard data. Motilin receptor protection from alkylation by N-ethylmaleimide preserved contraction to motilin and erythromycin but not acetylcholine or cholecystokinin, whereas protection with erythromycin preserved contraction to motilin but not other agonists. In conclusion, erythromycin binds to colon muscle motilin receptors present in densities similar to reported values for the upper gut. Furthermore, erythromycin contracts colonic myocytes via specific action on motilin receptors. Thus erythromycin may have colonic motor-stimulating properties by action on motilin receptors.

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