scholarly journals In vitro action of Mimosa caesalpinifolia ketone extract on Haemonchus contortus and Trichostrongylus colubriformis

2017 ◽  
Vol 38 (4) ◽  
pp. 1963 ◽  
Author(s):  
Danilo Rodrigues Barros Brito ◽  
Livio Martins Costa Júnior ◽  
João Luis Garcia ◽  
Suzana Gomes Lopes ◽  
Giselle Cutrim de Oliveira Santos ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
In Vivo Studies ◽  
In Vitro Assays ◽  
Trichostrongylus Colubriformis ◽  
Lower Efficiency ◽  
Egg Hatchability

This study aimed to evaluate the in vitro anthelmintic activity of Mimosa caesalpinifolia (sabiá) ketone extract, which is rich in condensed tannins (CT), on Haemonchus contortus and Trichostrongylus colubriformis. The leaves and stems of M. caesalpinifolia were collected, dried in the shade, and ground to a dry powder from which ketone extracts were obtained for in vitro assays. The extracts were diluted in 5% acetone and PBS to concentrations in the range 0.25-2.80 mg mL-¹ and the inhibition of egg hatchability was assayed. Feces collected from goats naturally infected with H. contortus (55%) and T. colubriformis (45%) were macerated and the helminth eggs were collected to conduct in vitro egg hatchability tests. Nematode larvae collected from the feces were used for a larval exsheathment inhibition assay of M. caesalpinifolia leaf and M. caesalpinifolia leaf and stem ketone extracts at concentrations of 0.6 and 1.2 mg mL-¹; three replicates were performed for each concentration. PBS was used as a negative control. Polyvinylpolypyrrolidone (PVPP) was added to the extracts to assess the effect of phenolic compounds on anthelmintic activity. An inhibitory effect of 80.7% and 82.3% was observed on hatchability after treatment with 1.0 and 2.0 mg mL-¹ M. caesalpinifolia leaf ketone extract, respectively. An inhibition rate lower than 75% was observed for 1.0 mg mL-¹ M. caesalpinifolia leaf and stem ketone extract. The M. caesalpinifolia leaf ketone extract larval exsheathment assay resulted in inhibition of 97.3% and 99.8% at concentrations of 0.6 and 1.2 mg mL-¹, respectively. For the leaf and stem ketone extract, the larval exsheathment inhibition was 94.3% at 1.2 mg mL-¹. The leaf and leaf and stem extracts showed no inhibitory effects on larval exsheathment after the addition of PVPP. These results showed that cuticular loss was related to the action of the phenolic compounds in the M. caesalpinifolia extracts. M. caesalpinifolia leaf ketone extract inhibited egg hatchability, but the leaf and stem extract showed lower efficiency, which indicated a greater abundance of active compounds in the leaves. The M. caesalpinifolia ketone extracts were effective in the inhibition of larval exsheathment at the highest concentration tested. Based on these results, in vivo studies should be performed to demonstrate the anthelmintic activity of this plant in goats.

In-silico Studies of Isolated Phytoalkaloid Against Lipoxygenase: Study Based on Possible Correlation

2018 ◽  
Vol 21 (3) ◽  
pp. 215-221
Author(s):  
Haroon Khan ◽  
Muhammad Zafar ◽  
Helena Den-Haan ◽  
Horacio Perez-Sanchez ◽  
Mohammad Amjad Kamal
Keyword(s):  
In Silico ◽  
Docking Studies ◽  
In Vivo Studies ◽  
In Vitro Assays ◽  
Chronic Obstructive ◽  
Lipoxygenase Inhibitors ◽  
Lipoxygenase Inhibition ◽  
In Silico Studies

Aim and Objective: Lipoxygenase (LOX) enzymes play an important role in the pathophysiology of several inflammatory and allergic diseases including bronchial asthma, allergic rhinitis, atopic dermatitis, allergic conjunctivitis, rheumatoid arthritis and chronic obstructive pulmonary disease. Inhibitors of the LOX are believed to be an ideal approach in the treatment of diseases caused by its over-expression. In this regard, several synthetic and natural agents are under investigation worldwide. Alkaloids are the most thoroughly investigated class of natural compounds with outstanding past in clinically useful drugs. In this article, we have discussed various alkaloids of plant origin that have already shown lipoxygenase inhibition in-vitro with possible correlation in in silico studies. Materials and Methods: Molecular docking studies were performed using MOE (Molecular Operating Environment) software. Among the ten reported LOX alkaloids inhibitors, derived from plant, compounds 4, 2, 3 and 1 showed excellent docking scores and receptor sensitivity. Result and Conclusion: These compounds already exhibited in vitro lipoxygenase inhibition and the MOE results strongly correlated with the experimental results. On the basis of these in vitro assays and computer aided results, we suggest that these compounds need further detail in vivo studies and clinical trial for the discovery of new more effective and safe lipoxygenase inhibitors. In conclusion, these results might be useful in the design of new and potential lipoxygenase (LOX) inhibitors.

scholarly journals TGFβ signalling acts as a molecular brake of myoblast fusion

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Julie Melendez ◽  
Daniel Sieiro ◽  
David Salgado ◽  
Valérie Morin ◽  
Marie-Julie Dejardin ◽  
...  
Keyword(s):  
Dynamic Control ◽  
Muscle Growth ◽  
Myoblast Fusion ◽  
In Vivo Studies ◽  
In Vitro Assays ◽  
Receptor Complex ◽  
Tgfβ Signalling ◽  
Molecular Brake

AbstractFusion of nascent myoblasts to pre-existing myofibres is critical for skeletal muscle growth and repair. The vast majority of molecules known to regulate myoblast fusion are necessary in this process. Here, we uncover, through high-throughput in vitro assays and in vivo studies in the chicken embryo, that TGFβ (SMAD2/3-dependent) signalling acts specifically and uniquely as a molecular brake on muscle fusion. While constitutive activation of the pathway arrests fusion, its inhibition leads to a striking over-fusion phenotype. This dynamic control of TGFβ signalling in the embryonic muscle relies on a receptor complementation mechanism, prompted by the merging of myoblasts with myofibres, each carrying one component of the heterodimer receptor complex. The competence of myofibres to fuse is likely restored through endocytic degradation of activated receptors. Altogether, this study shows that muscle fusion relies on TGFβ signalling to regulate its pace.

Isolation of hydroxytyrosol from olive leaves extract, radioiodination and investigation of bioaffinity using in vivo/in vitro methods

2013 ◽  
Vol 101 (9) ◽  
pp. 585-593 ◽  
Author(s):  
M. Ozkan ◽  
F. Z. Biber Muftuler ◽  
A. Yurt Kilcar ◽  
E. I. Medine ◽  
P. Unak
Keyword(s):  
Small Intestine ◽  
Phenolic Compounds ◽  
Biological Activities ◽  
In Vivo Studies ◽  
Flavonoid Content ◽  
Olive Leaves ◽  
In Vitro Methods ◽  
Extraction And Purification

Summary It is known that medicinal plants like olive have biological activities due to their flavonoid content such as olueropein, tyrosol, hydroxytyrosol etc. In current study, hydroxytrosol (HT) which is one of the major phenolic compounds in olive, olive leaves and olive oil, was isolated after methanol extraction and purification of olive leaves which are grown in the northern Anatolia region of Turkey. The isolated HT was radiolabeled with 131I (131I-HT) and the bioaffinity of this radiolabeled component of olive leaves extract was investigated by using in vivo/in vitro methods. It was found that HT could be radiolabeled with 131I in yields of 95.6±4.4% (n = 8), and in vivo studies showed that 131I-HT is taken up by urinary bladder, stomach, small intestine, large intestine, breast and prostate. Significant incorporation of activity was observed in cell lines via in vitro studies.

scholarly journals Pleiotropic Biological Effects of Dietary Phenolic Compounds and their Metabolites on Energy Metabolism, Inflammation and Aging

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 596 ◽  
Author(s):  
María del Carmen Villegas-Aguilar ◽  
Álvaro Fernández-Ochoa ◽  
María de la Luz Cádiz-Gurrea ◽  
Sandra Pimentel-Moral ◽  
Jesús Lozano-Sánchez ◽  
...  
Keyword(s):  
Energy Metabolism ◽  
Phenolic Compounds ◽  
Molecular Mechanisms ◽  
Biological Effects ◽  
Biological Properties ◽  
In Vivo Studies ◽  
Wide Range ◽  
High Prevalence

Dietary phenolic compounds are considered as bioactive compounds that have effects in different chronic disorders related to oxidative stress, inflammation process, or aging. These compounds, coming from a wide range of natural sources, have shown a pleiotropic behavior on key proteins that act as regulators. In this sense, this review aims to compile information on the effect exerted by the phenolic compounds and their metabolites on the main metabolic pathways involved in energy metabolism, inflammatory response, aging and their relationship with the biological properties reported in high prevalence chronic diseases. Numerous in vitro and in vivo studies have demonstrated their pleiotropic molecular mechanisms of action and these findings raise the possibility that phenolic compounds have a wide variety of roles in different targets.

STUDIES ON THE ANTICOAGULANT AND ANTITHROMBOTIC ACTIONS OF DERMATANS AND THEIR SULFATED DERIVATIVES

1987 ◽  
Author(s):  
D Hoppensteadt ◽  
A Kumar ◽  
J Fareed ◽  
J Mardigian
Keyword(s):  
Antithrombin Iii ◽  
Femoral Vein ◽  
In Vivo Studies ◽  
In Vitro Assays ◽  
Protease Inhibition ◽  
Thrombosis Model ◽  
Antithrombotic Effects ◽  
Activated Prothrombin Complex Concentrates

Non-antithrombin III mediated effects such as interaction with heparin cofactor II, modulation of endothelium and polymorphonuclear leukocytes contribute to the overall antithrombotic effects of glycosaminoglycans. In order to study the role of these dermatans, we investigated their in vitro anticoagulant effects using the clot based (PT, APTT, TT, and Heptest), antiprotease (anti IIa and anti Xa) and Thromboplastin C activated fibrinopeptide A generation test. The in vivo antithrombotic actions were investigated, against activated and non activated prothrombin complex concentrates, and in combination with Russells viper venom in jugular and femoral vein stasis thrombosis models (rabbit). The dermatans studied consisted of a standard dermatan of porcine intestinal origin and four sulfated dermatans with varying degrees of sulfation. All of the dermatans studied showed weak anticoagulant effects on the routinely performed clot based assays. Marked variability was seen on the protease inhibition (anti Xa and anti IIa) assays. In the in vivo studies all dermatans studied showed varying degrees of antithrombotic actions against various thrombogenic agents in a modified stasis thrombosis model. Sulfation appeared to produce stronger anticoagulant effects as determined by in vitro assays, whereas the intravenous antithrombotic actions of native dermatan were stronger than sulfated derivatives. This data suggests that dermatans produce their antithrombotic actions via non-antithrombin III mediated pathways. Furthermore, in vitro testing methods are of limited value in the evaluation of the biologic actions of dermatans and their derivatives.

Can in vitro assays substitute for in vivo studies in assessing the pulmonary hazards of fine and nanoscale materials?

2008 ◽  
Vol 11 (2) ◽  
pp. 421-431 ◽  
Author(s):  
Christie M. Sayes ◽  
Kenneth L. Reed ◽  
Shekhar Subramoney ◽  
Lloyd Abrams ◽  
David B. Warheit
Keyword(s):  
In Vivo Studies ◽  
In Vitro Assays ◽  
Nanoscale Materials

Haemonchus contortus: In vitro and in vivo anthelmintic activity of aqueous and hydro-alcoholic extracts of Hedera helix

2007 ◽  
Vol 116 (4) ◽  
pp. 340-345 ◽  
Author(s):  
T. Eguale ◽  
G. Tilahun ◽  
A. Debella ◽  
A. Feleke ◽  
E. Makonnen
Keyword(s):  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
Hedera Helix

scholarly journals Anthelmintic activity of Cymbopogon citratus against Haemonchus contortus

2015 ◽  
Vol 24 (3) ◽  
pp. 268-275 ◽  
Author(s):  
Iara Tersia Freitas Macedo ◽  
Lorena Mayana Beserra de Oliveira ◽  
Wesley Lyeverton Correia Ribeiro ◽  
Jessica Maria Leite dos Santos ◽  
Kaline das Chagas Silva ◽  
...  
Keyword(s):  
Essential Oil ◽  
Haemonchus Contortus ◽  
Anthelmintic Activity ◽  
Meriones Unguiculatus ◽  
Parasitic Nematodes ◽  
Control Group ◽  
Cymbopogon Citratus ◽  
Egg Hatching

Parasitic nematodes are of major economic importance in livestock. An alternative for the control of parasites is phytotherapy. This study evaluated the efficacy of Cymbopogon citratus decoction (CcD), C. citratus essential oil (CcEo) and citral against Haemonchus contortus using in vitro egg hatch test (EHT) and larval development test (LDT) and an in vivo test using a Meriones unguiculatus (gerbil) model. The effect of 800 mg/kg CcEo was evaluated in gerbils that had been artificially infected with 5,000 third-stage H. contortus larvae. The effective concentrations required to inhibit 50% (EC50) of egg hatching were 0.46, 0.14 and 0.13 mg/mL for CcD, CcEo and citral, respectively. The EC50 values in the LDT were 5.04, 1.92 and 1.37 mg/mL for CcD, CcEo and citral, respectively. H. contortus population in the group treated with C. citratus essential oil was reduced by 38.5% (P< 0.05) in comparison to the control group. These results suggest that it may be possible to use C. citratusessential oil to control of H. contortus parasite of small ruminant.

The anthelmintic activity of 1,10-phenanthroline, a metalloenzyme inhibitor

2019 ◽  
Author(s):  
S.M.A. Abidi ◽  
Kavita Singh ◽  
A. Rehman ◽  
R. Ullah ◽  
L. Rehman ◽  
...  
Keyword(s):  
Enzyme Inhibitor ◽  
Anthelmintic Activity ◽  
In Vivo Studies ◽  
Parasitic Helminths ◽  
Tegumental Surface ◽  
Biochemical Assays ◽  
Direct Exposure ◽  
Surface Changes

Paramphistomosis is a chronic, debilitating parasitic disease of livestock prevalent in the tropical and sub-tropical countries. Globally there is a heavy reliance on anthelmintics but concerns over drug resistance encourage the search for new leads. Metalloproteinases play a significant role in the biology and life cycle of parasitic helminths. The efficacy of metalloproteinase inhibitor, 1,10-Phenanthroline (1,10-phe) which is commonly used as a specific enzyme inhibitor in biochemical assays, was tested in vitro on Gigantocotyle explanatum tegument as a marker of anthelmintic action. The scanning electron microscopy revealed that the tegumental surface exhibited considerable changes in the worms treated with the metalloenzyme inhibitor, 1,10-phe. The untreated control worms appeared normal showing smooth tegumental surface with abundant dome shaped papillae in the anterior to mid region, while their density was less around the acetabulum which serves as a hold-fast organ helping the worms to remain attached in biliary passage. The 1,10-phe produced significant tegumental damage when the liver amphistomes were in vitro exposed to this compound at 12.5 µM concentration. The surface changes appeared in the form of edematous ridges with prominent furrows and erosion of the dome shaped papillae with rosette shaped deep lesions as a result of which deep parenchymatous tissues were exposed. The collapse of sensory bulbs as well as sloughing of tegument, particularly in the anterior-mid region was observed. The nature of damage could be comparable to various anthelmintics used in previous studies. To the best of our knowledge this is the first report of direct exposure of amphistome worms to zinc metallo-enzyme inhibitor, however, further in vivo studies are required to ascertain the anthelmintic efficacy of 1,10-phe.

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