In vitro and ex vivo antiparasitic effect of Rheum ribes L. extract against the hydatid cyst protoscoleces

2020 ◽  
Vol 20 ◽  
Author(s):  
Hossein Mahmoudvand ◽  
Mojgan Saki ◽  
Ali Asghar Kiani ◽  
Tina Taban ◽  
Mohammad Kazem Shahmoradi
Keyword(s):  
Ex Vivo ◽  
Biological Activities ◽  
Herbal Medicines ◽  
Modern Medicine ◽  
Infected Sheep ◽  
Hydatid Cysts ◽  
Zoonotic Infection ◽  
Worldwide Distribution ◽  
Ex Vivo Assay

Background: Cystic echinococcosis is a zoonotic infection in humans and herbivorous animals with worldwide distribution which caused by larva stage of Echinococcus granulosus. Rhubarb (Rheum ribes L.) as an herbal medicines has various therapeutics properties such as the antioxidant, anticancer, and antimicrobial ones. With respect to the potential of the biological activities of this plant in traditional and modern medicine, we aim to examine its protoscolicidal effects against E. granulosus protoscolecess in vitro and ex vivo. Methods: Collected protoscoleces from liver hydatid cysts of infected sheep were exposed to the different concentrations of the extract (225, 450, 900 mg/mL) for 5-60 min in vitro and ex vivo. Then using the eosin exclusion assay the viability of protoscoleces was studied. Results: R. ribes extract had a potent protoscolicidal activity in vitro so that at the 450 and 900 mg/ml killed 56.3 and 100% of protoscoleces after 10 min exposure. Ex vivo assay, the extract needed more time to kill the protoscoleces than the in vitro; so that at the concentration of 900 mg/mL, all protoscoleces were killed after 15 minutes Conclusion: The obtained results exhibited the potent protoscolicidal effects of R. ribes extract particularly at the concentration of 900 mg/ml which completely killed the parasite after <15 min exposure. However, more and supplementary studies are required to verify these findings through assessing in animal models and clinical subjects.

In Vitro and Ex Vivo Evaluation of Capparis Spinosa Extract to Inactivate Protoscoleces During Hydatid cyst Surgery

2020 ◽  
Vol 17 ◽  
Author(s):  
Hossein Mahmoudvand ◽  
Amal Khudair Khalaf ◽  
Mania Beyranvand
Keyword(s):  
Hydatid Cyst ◽  
Ex Vivo ◽  
Infected Sheep ◽  
Phytochemical Analysis ◽  
Phytochemical Screening ◽  
Hydatid Cysts ◽  
The World ◽  
Capparis Spinosa ◽  
Ex Vivo Assay

Background:: Hydatidosis is one of the most dangerous zoonosis diseases in the world caused by the larval stage of the broad-worm or Echinococcus granulosus parasite. Today, cysts' rupture or content leakage during surgery and in-volvement of organs adjacent to the organ involved, and consequently secondary cysts, are the major concern for hydatid cyst surgeons. Therefore, using scolicidal substances such as hypertonic saline 20%, silver nitrate and formalin has been considered to reduce the risk of protoscoleces spread and recurrence of disease in recent years. The current work designed to assess the antiparasitic effects of Capparis spinose L. extract against hydatid cyst protoscoleces. Methods:: Collected protoscoleces from liver fertile hydatid cysts of infected sheep were exposed to the different concentra-tions of the essential oil (150, 300, 600 mg/mL) for 5-60 min in vitro and ex vivo. Then by using the eosin exclusion assay the viability of protoscoleces was studied. The primary phytochemical analysis of the C. spinosa extract was done to assess the presence of tannins, alkaloids, saponins, flavonoids, terpenoids and glycosides. Results:: C. spinosa extract had a powerful protoscolicidal activity in vitro so that at the 300 and 600 mg/ml entirely elimi-nates the parasite after 10 and 5 minutes; whereas at lower doses demonstrated weak protoscolicidal activity. Ex vivo assay, no similar effect with in vitro was observed, so that requiring a more time to show a potent protoscolicidal activity. C. spi-nosa extract at the concentrations of 300 and 600 mg/mL after exposure time of 20 and 12 min, killed 100% of protoscole-ces within the hydatid cyst, respectively. The findings of primary phytochemical screening of the C. spinosa extract demon-strated the existance of flavonoids, tannins, terpenoids, glycosides and alkaloids in this plant. Conclusion:: The obtained results in vitro and ex vivo exhibited that potent protoscolicidal effects of C. spinosa extract particu-larly at the concentrations of 600 and 300 mg/ml which entirely eliminates the parasite after 5-20 min exposure. However, more and supplementary works are required to verify these findings through assessing in animal models and clinical subjects.

A Comparative Ex Vivo Study of Plasminogen Activators and Proteases for Fibrinolytic Activity and Side Effects in Rabbits

1977 ◽  
Vol 37 (01) ◽  
pp. 154-161 ◽  
Author(s):  
B. A Janik ◽  
S. E Papaioannou
Keyword(s):  
Side Effects ◽  
Effective Dose ◽  
Fibrinolytic Activity ◽  
Ex Vivo ◽  
Plasminogen Activators ◽  
Assay System ◽  
Coagulation Parameters ◽  
Ex Vivo Assay

SummaryUrokinase, streptokinase, Brinase, trypsin, and SN 687, a bacterial exoprotease, have been evaluated in an ex vivo assay system. These enzymes were injected into rabbits and the fibrinolytic activity as well as other coagulation parameters were measured by in vitro techniques. Dose-response correlations have been made using the euglobulin lysis time as a measure of fibrinolytic activity and the 50% effective dose has been determined for each enzyme. Loading doses, equal to four times the 50% effective dose, were administered to monitor potential toxicity revealing that Brinase, trypsin, and SN 687 were very toxic at this concentration.Having established the 50% effective dose for each enzyme, further testing was conducted where relevant fibrinolytic and coagulation parameters were measured for up to two days following a 50% effective dose bolus injection of each enzyme. Our results have demonstrated that urokinase and streptokinase are plasminogen activators specifically activating the rabbit fibrinolytic system while Brinase, trypsin and SN 687 increase the general proteolytic activity in vivo.The advantages of this ex vivo assay system for evaluating relative fibrinolytic potencies and side effects for plasminogen activators and fibrinolytic proteases have been discussed.

scholarly journals Development of Novel Indole-Based Bifunctional Aldose Reductase Inhibitors/Antioxidants as Promising Drugs for the Treatment of Diabetic Complications

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2867
Author(s):  
Lucia Kovacikova ◽  
Marta Soltesova Prnova ◽  
Magdalena Majekova ◽  
Andrej Bohac ◽  
Cimen Karasu ◽  
...  
Keyword(s):  
Aldose Reductase ◽  
Diabetic Complications ◽  
Therapeutic Potential ◽  
Ex Vivo ◽  
Biological Activities ◽  
In Vivo Models ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Promising Therapeutic Approach

Aldose reductase (AR, ALR2), the first enzyme of the polyol pathway, is implicated in the pathophysiology of diabetic complications. Aldose reductase inhibitors (ARIs) thus present a promising therapeutic approach to treat a wide array of diabetic complications. Moreover, a therapeutic potential of ARIs in the treatment of chronic inflammation-related pathologies and several genetic metabolic disorders has been recently indicated. Substituted indoles are an interesting group of compounds with a plethora of biological activities. This article reviews a series of indole-based bifunctional aldose reductase inhibitors/antioxidants (ARIs/AOs) developed during recent years. Experimental results obtained in in vitro, ex vivo, and in vivo models of diabetic complications are presented. Structure–activity relationships with respect to carboxymethyl pharmacophore regioisomerization and core scaffold modification are discussed along with the criteria of ‘drug-likeness”. Novel promising structures of putative multifunctional ARIs/AOs are designed.

scholarly journals Determination of in Vivo Biological Activities of Dodonaea Viscosa Flowers Against CCL4 Toxicity in Albino Mice With Bioactive Compound Detection

2021 ◽  
Author(s):  
Hina Gul ◽  
Muhammad Awais ◽  
Salina Saddick ◽  
Falak Sher Khan ◽  
Muhammad Gulfraz ◽  
...  
Keyword(s):  
Protective Effect ◽  
Biological Activities ◽  
Hematological Parameters ◽  
Octadecenoic Acid ◽  
Radical Scavenging ◽  
Herbal Medicines ◽  
Bioactive Compound ◽  
Dodonaea Viscosa

Abstract Dodonaea viscosa L. Jacq. is an evergreen shrub and native to Asia, Africa and Australia. It has been used as traditional medicine in different countries. The foremost objective of the current study was to discover protective potential of D. Viscosa flowers Methanol (DVM) and Chloroform (DVC) extracts against CCL4 induced toxicity in mice. This study was intended to identify phytochemicals through HPLC, GCMS and FT-IR as well as in vitro antioxidant and in vitro antituberculosis activity. Our comprehensive findings indicate that Dodonaea viscosa is valuable and widespread herbal medicines through therapeutic potentials for curing various ailments. Dodonaea viscosa flowers are found to have protective effect against oxidative stress produced by CCL4 in liver, kidney and spleen. The level of hepatic enzymes (ALP, AST ALT and Direct bilirubin), hematological parameters (RBCs, WBCs and Platelets), total protein and liver antioxidant enzymes (SOD, GPx and CAT) were restored by the intake of DV extracts after decline in levels by CCL4. Histopathological results discovered the defensive effect of 300mg/kg of DVM extract against CCL4 induced damage, thus having improved protective effect as compared to DVC and control. As a result of analysis total flavonoids and total phenolics were also revealed. Phytochemical investigation by HPLC identified gallic acid, epicatechin, cumeric acid, flavonoids while Oleic acid (Octadecenoic acid) (C18H34O2), Stearic acid (C18H36O2), Ricinoleic acid (C18H34O3) and Cedrol (C15H26O) was estimated by GCMS. DVM extract exhibited resistance against in vitro Mycobacterium tuberculosis strains. This study proposed that protective effect of DV against oxidative damage induced in Liver, Kidney and Spleen can possibly be correlated to their antioxidant as well as free radical scavenging property.

scholarly journals In vitro and in vivo activities of flavonoids – apigenin, baicalin, chrysin, scutellarin – in regulation of hypertension – a review for their possible effects in pregnancy-induced hypertension

2019 ◽  
Vol 65 (1) ◽  
pp. 55-70 ◽  
Author(s):  
Marcin Ożarowski ◽  
Radosław Kujawski ◽  
Przemysław Ł. Mikołajczak ◽  
Karolina Wielgus ◽  
Andrzej Klejewski ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Chemical Compounds ◽  
New Drugs ◽  
Future Application ◽  
Mediators Of Inflammation ◽  
And Function

Summary Flavonoids and their conjugates are the most important group of natural chemical compounds in drug discovery and development. The search for pharmacological activity and new mechanisms of activity of these chemical compounds, which may inhibit mediators of inflammation and influence the structure and function of endothelial cells, can be an interesting pharmacological strategy for the prevention and adjunctive treatments of hypertension, especially induced by pregnancy. Because cardiovascular diseases have multi-factorial pathogenesis these natural chemical compounds with wide spectrum of biological activities are the most interesting source of new drugs. Extracts from one of the most popular plant used in Traditional Chinese Medicine, Scutellaria baicalensis Georgi could be a very interesting source of flavonoids because of its exact content in quercetin, apigenin, chrysin and scutellarin as well as in baicalin. These flavonoids exert vasoprotective properties and many activities such as: anti-oxidative via several pathways, anti-in-flammatory, anti-ischaemic, cardioprotective and anti-hypertensive. However, there is lack of summaries of results of studies in context of potential and future application of flavonoids with determined composition and activity. Our review aims to provide a literature survey of in vitro, in vivo and ex vivo pharmacological studies of selected flavonoids (apigenin, chrysin and scutellarin, baicalin) in various models of hypertension carried out in 2008–2018.

scholarly journals Distinct in vitro Complement Activation by Various Intravenous Iron Preparations

2016 ◽  
Vol 45 (1) ◽  
pp. 49-59 ◽  
Author(s):  
Julia Cordelia Hempel ◽  
Felix Poppelaars ◽  
Mariana Gaya da Costa ◽  
Casper F.M. Franssen ◽  
Thomas P.G. de Vlaam ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Complement Activation ◽  
Ex Vivo ◽  
Ferric Carboxymaltose ◽  
Hypersensitivity Reactions ◽  
Iron Dextran ◽  
Iv Iron ◽  
Ex Vivo Assay

Background: Intravenous (IV) iron preparations are widely used in the treatment of anemia in patients undergoing hemodialysis (HD). All IV iron preparations carry a risk of causing hypersensitivity reactions. However, the pathophysiological mechanism is poorly understood. We hypothesize that a relevant number of these reactions are mediated by complement activation, resulting in a pseudo-anaphylactic clinical picture known as complement activation-related pseudo allergy (CARPA). Methods: First, the in-vitro complement-activating capacity was determined for 5 commonly used IV iron preparations using functional complement assays for the 3 pathways. Additionally, the preparations were tested in an ex-vivo model using the whole blood of healthy volunteers and HD patients. Lastly, in-vivo complement activation was tested for one preparation in HD patients. Results: In the in-vitro assays, iron dextran, and ferric carboxymaltose caused complement activation, which was only possible under alternative pathway conditions. Iron sucrose may interact with complement proteins, but did not activate complement in-vitro. In the ex-vivo assay, iron dextran significantly induced complement activation in the blood of healthy volunteers and HD patients. Furthermore, in the ex-vivo assay, ferric carboxymaltose and iron sucrose only caused significant complement activation in the blood of HD patients. No in-vitro or ex-vivo complement activation was found for ferumoxytol and iron isomaltoside. IV iron therapy with ferric carboxymaltose in HD patients did not lead to significant in-vivo complement activation. Conclusion: This study provides evidence that iron dextran and ferric carboxymaltose have complement-activating capacities in-vitro, and hypersensitivity reactions to these drugs could be CARPA-mediated.

Hypotensive effects of the triterpene oleanolic acid for cardiovascular prevention

2020 ◽  
Vol 13 ◽  
Author(s):  
A. Sureda ◽  
M. Monserrat-Mesquida ◽  
S. Pinya ◽  
P. Ferriol ◽  
S. Tejada
Keyword(s):  
Blood Pressure ◽  
Oleanolic Acid ◽  
Ex Vivo ◽  
Biological Activities ◽  
Cardiovascular Prevention ◽  
In Vivo Studies ◽  
Antihypertensive Activity ◽  
In Vitro Tests

Background:: Hypertension is a high prevalent chronic disease worldwide and a major cardiovascular risk factor. Oleanolic acid (3β-hydroxy-olea-12-en-28-oic acid) is a wide distributed bioactive pentacyclic triterpenoid with diverse biological activities such as anti-inflammatory, hepaprotective anti-diabetic or anti-hypertensive. Objective:: The aim of this study was to review and highlight the available data about antihypertensive activity of oleanolic acid and the described mechanisms of action. Method:: Extensive searches were made in the available literature on oleanolic acid and the data investigating its antihypertensive effects were analysed. Results:: Most of research has been performed on animal models of hypertension, ex vivo studies with aortic ring and some in vitro tests with cell cultures, whereas clinical trials are still lacking. Treatment of hypertensive animals with oleanolic acid significantly ameliorated the rise in the systolic blood pressure. In addition, the hypotensive effects of oleanolic acid are also related to a potent diuretic-natriuretic activity and nephroprotection. In vitro studies have characterized the participation of various signalling pathways that modulate the release of vasodilation mediators. Conclusion:: In vitro and in vivo studies suggest that oleanolic acid effectively reduce blood pressure and could be an interesting co-adjuvant to conventional treatment of hypertension.

scholarly journals Restricted immune activation and internalisation of anti-idiotype complexes between drug and antidrug antibodies

2018 ◽  
Vol 77 (10) ◽  
pp. 1471-1479 ◽  
Author(s):  
Karin A van Schie ◽  
Simone Kruithof ◽  
Pleuni Ooijevaar-de Heer ◽  
Ninotska I L Derksen ◽  
Fleur S van de Bovenkamp ◽  
...  
Keyword(s):  
Adverse Events ◽  
Immune Activation ◽  
Immune Complexes ◽  
Ex Vivo ◽  
Biological Activities ◽  
Size Exclusion ◽  
Exclusion Chromatography ◽  
Soluble Immune Complexes ◽  
High Concentrations

ObjectivesTherapeutic antibodies can provoke an antidrug antibody (ADA) response, which can form soluble immune complexes with the drug in potentially high amounts. Nevertheless, ADA-associated adverse events are usually rare, although with notable exceptions including infliximab. The immune activating effects and the eventual fate of these ‘anti-idiotype’ complexes are poorly studied, hampering assessment of ADA-associated risk of adverse events. We investigated the in vitro formation and biological activities of ADA-drug anti-idiotype immune complexes using patient-derived monoclonal anti-infliximab antibodies.MethodsSize distribution and conformation of ADA-drug complexes were characterised by size-exclusion chromatography and electron microscopy. Internalisation of and immune activation by complexes of defined size was visualised with flow imaging, whole blood cell assay and C4b/c ELISA.ResultsSize and conformation of immune complexes depended on the concentrations and ratio of drug and ADA; large complexes (>6 IgGs) formed only with high ADA titres. Macrophages efficiently internalised tetrameric and bigger complexes in vitro, but not dimers. Corroborating these results, ex vivo analysis of patient sera demonstrated only dimeric complexes in circulation.No activation of immune cells by anti-idiotype complexes was observed, and only very large complexes activated complement. Unlike Fc-linked hexamers, anti-idiotype hexamers did not activate complement, demonstrating that besides size, conformation governs immune complex potential for triggering effector functions.ConclusionsAnti-idiotype ADA-drug complexes generally have restricted immune activation capacity. Large, irregularly shaped complexes only form at high concentrations of both drug and ADA, as may be achieved during intravenous infusion of infliximab, explaining the rarity of serious ADA-associated adverse events.

FIBRINOLYTIC POTENCY OF NON ANTICOAGULANT, OXI-EEDUCED SLOW AND FAST MOVING HEPARINS

1987 ◽  
Author(s):  
R Porta ◽  
R Pescador ◽  
R Niada ◽  
M Mantovani ◽  
G Prino
Keyword(s):  
Fast Moving ◽  
Fibrinolytic Activity ◽  
Animal Species ◽  
Ex Vivo ◽  
Biological Activities ◽  
Anticoagulant Activity ◽  
Risk Patients ◽  
Slow Moving ◽  
Different Doses

It is well known that heparin is able to induce an increase of fibrinolytic activity when i.v. administered in man and in several animal species. Nevertheless, its anticoagulant properties can cause serious problems of bleeding and this restricts the therapeutic use of heparin. An oxi-reductive process applied to heparin leads to a conpound with reduced anticoagulant activity. Moreover, heparin can be separated into slow moving (SM) and fast moving (FM) components on the basis of electrcphoretic properties. The SM and FM components display quantitatively different biological activities. The aim of this paper was to verify if the oxi-reduction could affect or not the fibrinolytic activities of SM and FM. SM and FM, prepared by ethanolic precipitation from parent heparin, were oxidized by periodate and stabilized by reduction (RO-SM and RO-FM). The USP, APTT and anti Xa titres were determined in vitro using sheep plasma and kits from Boehrirger Biochemia (APTT) and Sigpia (Anti Xa). Fibrinolytic activities were assessed ex vivo after i.v. injection into rabbits at different doses to find out the effective dose hundred (ED100). The euglobulin fraction obtained from plasma was applied on human fibrin plates and the lysis areas were measured. The Table gives the resultsThe oxi-reduction decreased dramatically the anticoagulant activities of SM and FM heparins while their fibrinolytic activities were practically unaffected. Tne oxi-reduced heparins could be helpful therapeutic agents in pathological conditions characterized by a diminished fibrinolytic activity. They could represent an effective alternative to heparin; the very lew anticoagulant activities reduce the risk of bleeding, specially in the high risk patients, while the good fibrinolytic activity, comparable to heparin, could allow the dissolution of fibrin clots.

Protective Effect of Rosmarinic Acid is Through Regulation of Inflammatory Cytokine in Cadmium-Induced Ototoxicity

2013 ◽  
Vol 41 (02) ◽  
pp. 391-404 ◽  
Author(s):  
Su-Jin Kim ◽  
Jae-Young Um ◽  
Sung-Hoon Kim ◽  
Seung-Heon Hong
Keyword(s):  
Auditory System ◽  
Rosmarinic Acid ◽  
Ex Vivo ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Cadmium Toxicity ◽  
Reactive Oxygen Species Generation ◽  
Protective Effects ◽  
Pharmacological Mechanism

Cadmium ( Cd2+ ) is an environmental contaminant that causes a variety of adverse effects. Auditory cells are sensitive to cadmium, and the cochlea is more vulnerable to cadmium toxicity than the other parts of the auditory system. Rosmarinic acid (RA) exhibits a wide spectrum of biological activities, mainly antioxidant and anti-inflammatory activities. However, the regulatory effects of RA in the auditory system have not been elucidated. In this study, we investigated the protective effects of RA on Cd2+ -induced ototoxicity in vitro and ex vivo. The findings showed that RA inhibited Cd2+ -mediated cell toxicity, reactive oxygen species generation, interleukin (IL)-6 and IL-1β production, the translocation of the apoptosis inducing factor into the nucleus and activation of caspases-3 in an auditory cell line, HEI-OC1. In addition, RA prevented the destruction of hair cell arrays in the rat organ of Cortiprimary explants in the presence of Cd2+ . These results are expected to improve our understanding of the pharmacological mechanism of RA, and help develop potential therapeutic strategies against ototoxicity.

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