scholarly journals Effects of single and 7-fold administration of a complex of albendazole with disodium salt of glycyrrhizic acid to hamsters infected with Opisthorchis felineus

2021 ◽  
Vol 15 (3) ◽  
pp. 83-92
Author(s):  
D. F. Avgustinovich ◽  
M. N. Lvova ◽  
M. A. Tsyganov ◽  
D. V. Ponomarev ◽  
V. A. Mordvinov ◽  
...  
Keyword(s):  
Alanine Aminotransferase ◽  
Glycyrrhizic Acid ◽  
Solid Phase ◽  
Anthelmintic Activity ◽  
Disodium Salt ◽  
Pure Substance ◽  
Daily Consumption ◽  
Opisthorchis Felineus ◽  
Alanine Aminotransferase Activity ◽  
Anthelmintic Effect

The purpose of the research is to evaluate the effect of albendazole as part of the supramolecular complex with disodium salt of glycyrrhizic acid obtained by solid-phase mechanical treatment.Materials and methods. The anthelmintic activity of the complex and its effect on the host organism was assessed on hamsters infected with Opisthorchis felineus by single and 7-fold administration at 45 days after infection. After 21 days, we counted the number of helminthes in the liver, and conducted a morphometric analysis of the liver and spleen, and detected biochemically the activity of alanine aminotransferase and aspartate aminotransferase in the animals’ blood serum.Results and discussion. The number of O. felineus significantly decreased after 7-fold, but not a single, administration of albendazole (ABZ) and ABZ-Na2GA complex (1 : 10). The administrated substances had no effect on the weight gain of the animals and the daily consumption of the pellets. At the same time, ABZ only as part of the complex normalized the weight of the liver and spleen in hamsters infected with O. felineus and reduced the alanine aminotransferase activity. Consequently, a longer administration of ABZ as part of the complex with disodium glycyrrhizinate has not only a pronounced anthelmintic effect, but also improves some of the physiological parameters of hamsters to a greater extent than a pure substance.

scholarly journals Anthelmintic Efficacy of Supramolecular Complex of Praziquantel Obtained by Mechanochemical Technology

2020 ◽  
Author(s):  
Ivan ARKHIPOV ◽  
Salavat KHALIKOV ◽  
Alexander DUSHKIN ◽  
Konstantin SADOV ◽  
Elizaveta METELEVA ◽  
...  
Keyword(s):  
Glycyrrhizic Acid ◽  
Chemical Properties ◽  
Anthelmintic Activity ◽  
Disodium Salt ◽  
Supramolecular Complex ◽  
Laboratory Model ◽  
Mechanochemical Processing ◽  
Anthelmintic Efficacy ◽  
Physico Chemical ◽  
Therapeutic Doses

Background: A supramolecular complex of praziquantel (PZQ) with disodium salt of glycyrrhizic acid (Na2GA) was obtained by mechanochemical technology to increase solubility, absorption rate and hence bioavailability of the drug and reduction its therapeutic doses. The aim of our study was evaluation of anthelmintic efficacy of supramolecular complex of PZQ. Methods: Different samples of PZQ with Na2GA were obtained by mechanochemical processing and examined for some physico-chemical properties. The anthelmintic activity of the most perspective samples was studied on the laboratory model of Hymenolepis nana infection of mice and Moniezia expansa infection of sheep by the results of helminthological necropsy of the small intestines (the controlled test). Results: A high efficacy (> 98%) of supramolecular complex of PZQ with Na2GA (1/10) was shown at doses of 3; 2 and 1 mg/kg of body weight at single oral administration against H. nana in mice and M. expansa in sheep. While the basic PZQ had 27.19% and 36.64% efficacy respectively at the dose of 1 mg/kg. The PZQ:Na2GA 1/10 physical mixture (without mechanochemical processing) revealed no anthelmintic efficacy. Conclusion: Joint mechanochemical treatment the PZQ substance and Na2GA led to increased solubility, reduction of particle sizes, amorphization of substance, incorporating it with micelles of glycyrrhizic acid and high anthelmintic efficacy in reduced dose. The supramolecular complex of praziquantel was found to be a perspective anthelminthic with enhanced pharmacological activity that needs further research.

Correlation of Melting Results for Both Pure Substances and Impure Substances

1986 ◽  
Vol 108 (3) ◽  
pp. 649-653 ◽  
Author(s):  
E. M. Sparrow ◽  
G. A. Gurtcheff ◽  
T. A. Myrum
Keyword(s):  
Solid Phase ◽  
Equilibrium Phase ◽  
Equilibrium Phase Diagram ◽  
Vertical Tube ◽  
Step Change ◽  
Pure Substance ◽  
Characteristic Temperatures ◽  
Pure Substances ◽  
T Values ◽  
Melting Experiments

Melting experiments were performed encompassing both pure and impure substances. The pure substances included n-octadecane paraffin and n-eicosane paraffin, while the impure substances were mixtures synthesized from the pure paraffins. The experiments were carried out in a closed vertical tube whose wall was subjected to a step-change increase in temperature to initiate the melting. For each impure substance, supplementary measurements were made of two characteristic temperatures: the temperature T** at which melting of the solid phase first begins and the lowest temperature T* at which the melting can go to completion. For a pure substance, T** = T*. The time-dependent melting results for all the investigated substances, both pure and impure, were well correlated as a function of FoSte**(Gr**)1/8 alone, where the ** signifies the presence of T** in the temperature difference which appears in Ste and Gr. This correlation enables melting rates for impure substances to be determined from melting rates for pure substances. The T** values needed for the implementation of the correlation can be obtained from simple experiments, obviating the need for the complete equilibrium phase diagram.

scholarly journals Essential Oils and Their Bioactive Compounds in the Control of Gastrointestinal Nematodes of Small Ruminants

2018 ◽  
Vol 46 (1) ◽  
pp. 14 ◽  
Author(s):  
Weibson Paz Pinheiro André ◽  
Wesley Lyeverton Correia Ribeiro ◽  
Lorena Mayana Beserra de Oliveira ◽  
Iara Tersia Freitas Macedo ◽  
Fernanda Cristina Macedo Rondon ◽  
...  
Keyword(s):  
Natural Products ◽  
Essential Oils ◽  
Bioactive Compounds ◽  
Small Ruminant ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
In Vivo Tests ◽  
Anthelmintic Effect

Background: Gastrointestinal nematodes are one of the major health and economic problem of sheep and goats in the world. The control of these nematodes is carried out conventionally with synthetic anthelminths, which favored the selection of gastrointestinal nematode (GIN) populations multiresistant to anthelmintics. The emergence of anthelmintic resistance has stimulated the search for new alternatives to control small ruminant GIN, standing out the use of plants and their bioactives compounds, such as essential oils (EO). The objective of this review was to present the main characteristics and anthelmintic activity of EO, their isolated compounds and drug delivery systems in the control of GIN.Review: Essential oils are a complex blend of bioactive compounds with volatile, lipophilic, usually odoriferous and liquid substances. EO are composed of terpenes, terpenoids, aromatic and aliphatic constituents. EO has various pharmacological activities of interest in preventive veterinary medicine such as antibacterials, antifungals, anticoccicids, insecticides and anthelmintics. In vitro and in vivo tests are used to validate the anthelmintic activity of EO on GIN. In vitro tests are low cost screening tests that allow the evaluation of the anthelmintic activity of a large amount of bioactive compounds on eggs, first (L1) and third stage larvae (L3), and adult nematodes. The antiparasitic effect of EO is related to its main compound or to the interaction of the compounds. These bioactive compounds penetrate the cuticle of the nematodes by transcuticular diffusion, altering the mechanisms of locomotion, besides causing cuticular lesions. Following in vitro evaluation, the acute and sub-chronic toxicity test should be performed to assess the toxicity of the bioactive compounds and to define the dose to be used in in vivo tests. In vivo tests are more reliable because the anthelmintic effectiveness of bioactive compounds is evaluated after the metabolization process. The metabolization process of the bioactive compounds can generate metabolites that exhibit or not anthelmintic effectiveness. The in vivo tests assessing the anthelmintic effectiveness of bioactive compounds in sheep and goats are the fecal egg count reduction test and the controlled test.  OE promoted reduction of egg elimination in faeces which may be related to cuticular and reproductive alterations in GIN, and reduction of parasite burden in in vivo tests. Due to the promising results obtained with OE in the in vivo tests, interest has been aroused in using nanotechnology as an alternative to increase the bioavailability of OE and consequently, potentializing its anthelmintic effect, reducing the dose and  toxicity of the biocompounds. In addition to nanotechnology, the isolation and chemical modification of compounds isolated from OE have been employed to obtain new molecules with anthelmintic action and understand the mechanism of action of EO on the small ruminant GIN.Conclusion: The use of EO and their compound bioactive in the control of resistant populations of GIN is a promising alternative. The adoption of strategies in which natural products can replace synthetic anthelmintics, such as in dry periods and use synthetic anthelmintics in the rainy season when the population in refugia in the pasture is high, thus reducing the dissemination of GIN resistant populations. As perspective, the evaluation of pharmacokinetics and pharmacodynamics of these natural products should be performed so that one defines treatment protocols that optimize the anthelmintic effect.

Delayed onset of acute renal failure after significant paracetamol overdose: A case series

2009 ◽  
Vol 29 (1) ◽  
pp. 63-68 ◽  
Author(s):  
WS Waring ◽  
H. Jamie ◽  
GE Leggett
Keyword(s):  
Renal Failure ◽  
Acute Renal Failure ◽  
Serum Creatinine ◽  
Alanine Aminotransferase ◽  
Paracetamol Overdose ◽  
Peak Serum ◽  
Wilcoxon Test ◽  
Aminotransferase Activity ◽  
Baseline Serum ◽  
Alanine Aminotransferase Activity

Acute renal failure is a recognized manifestation of paracetamol toxicity, but comparatively little data is available concerning its onset and duration. The present study sought to characterize the time course of rising serum creatinine concentrations in paracetamol nephrotoxicity. Renal failure was defined by serum creatinine concentration ≥150 μmol/L (1.69 mg/dL) or ≥50% increase from baseline. Serum creatinine concentrations and alanine aminotransferase activity were considered with respect to the interval after paracetamol ingestion. There were 2068 patients with paracetamol overdose between March 2005 and October 2007, and paracetamol nephrotoxicity occurred in 8 (0.4%). All had significant hepatotoxicity, and peak serum alanine aminotransferase activity occurred at 2.5 days (2.2 to 2.9 days) after ingestion. Peak serum creatinine concentrations did not occur until 5.5 days (4.4 to 5.9 days) after ingestion (p = .031 by Wilcoxon test). Serum creatinine concentrations slowly restored to normal, and renal replacement was not required. In this patient series, rising serum creatinine concentrations only became detectable after more than 48 hours after paracetamol ingestion. Therefore, renal failure might easily be missed if patients are discharged home before this. Further work is required to establish the prevalence of paracetamol-induced nephrotoxicity, and its clinical significance.

Physicochemical Properties and Anti-Opisthorchosis Effect of Mechanochemically Synthesized Solid Compositions of Praziquantel with Glycyrrhizic Acid Disodium Salt

2018 ◽  
Vol 481 (1) ◽  
pp. 228-231 ◽  
Author(s):  
E. S. Meteleva ◽  
Yu. S. Chistyachenko ◽  
L. P. Suntsova ◽  
M. A. Tsyganov ◽  
G. B. Vishnivetskaya ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Glycyrrhizic Acid ◽  
Disodium Salt

Effect of Lactate Dehydrogenase Isoenzymes on the Coupled Enzymatic Assay for Alanine Aminotransferase Activity

1975 ◽  
Vol 21 (3) ◽  
pp. 330-333 ◽  
Author(s):  
Michael M Chang ◽  
Tai Wha Chung
Keyword(s):  
Lactate Dehydrogenase ◽  
Dehydrogenase Activity ◽  
Alanine Aminotransferase ◽  
Rabbit Muscle ◽  
Aminotransferase Activity ◽  
Lactate Dehydrogenase Activity ◽  
Enzymatic Assays ◽  
Substrate Specificities ◽  
Lactate Dehydrogenase Isoenzymes ◽  
Alanine Aminotransferase Activity

Abstract We show an example of the importance of specifying the form of isoenzyme and source of indicator enzymes to be used in coupled enzymatic assays. When we compared H4 (pig heart) and M4 (rabbit muscle) isoenzymes of lactate dehydrogenase for their suitability as indicator enzymes in the assay for alanine aminotransferase activity, we found that about fourfold as much M4 as H4 was required in terms of lactate dehydrogenase activity to reflect accurately equivalent amounts of alanine aminotransferase activity. Moreover, the substrate specificities of the two isoenzymes differed quantitatively.

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