Biological effects and assessment of acute toxicity of anticoagulants extracted from plants

2020 ◽  
Vol 21 (4) ◽  
pp. 27-29
Author(s):  
E. P. Kalinin ◽  
◽  
N. N. Buslaeva ◽  
D. I. Boyarintsev ◽  
◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Biological Effect ◽  
Leaf Extract ◽  
Biological Effects ◽  
Inhibitory Effect ◽  
Anticoagulant Effect ◽  
Laboratory Animals ◽  
Plasma Coagulation ◽  
Direct Acting

The aim of the study – was to study the biological effects and assess acute toxicity in an in vivo experimental study when injecting plant-derived effectors with an anticoagulant effect to laboratory animals. Materials and methods. As the studied effectors, plant anticoagulants obtained from the leaves of blueberry (Vaccinium myrtillus) and peloid, which were obtained in the previous studies, were used. The biological effect of effectors was evaluated by indicators characterizing coagulation and platelet hemostasis when administered to laboratory animals. Acute toxicity was assessed by the survival rate of animals after administration of effectors. Results. Blueberry leaf extract demonstrated an inhibitory effect on the development of reactions of the internal pathway of plasma coagulation and ADP – induced platelet aggregation. The effector obtained from sapropel significantly inhibits both plasma coagulation and platelet reactions. None of the effectors showed acute toxicity. Conclusion. As a result of this study, we consider the most promising peptide for further study, derived from peloid, as a promising direct-acting anticoagulant that affects the final pathway of plasma coagulation. The anticoagulant from blueberry leaves did not demonstrate the expected activity in the in vivo experiment, presumably due to the presence of impurities that neutralize its anticoagulant effect, and needs additional purification and evaluation.

Aqueous extracts of avocado pear (Persea americana Mill.) leaves and seeds exhibit anti-cholinesterases and antioxidant activities in vitro

2016 ◽  
Vol 27 (2) ◽  
Author(s):  
Ganiyu Oboh ◽  
Veronica O. Odubanjo ◽  
Fatai Bello ◽  
Ayokunle O. Ademosun ◽  
Sunday I. Oyeleye ◽  
...  
Keyword(s):  
Leaf Extract ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Seed Extract ◽  
Persea Americana ◽  
Dependent Manner ◽  
Natural Treatment

AbstractAvocado pear (The inhibitory effects of extracts on AChE and BChE activities and antioxidant potentials (inhibition of FeThe extracts inhibited AChE and BChE activities and prooxidant-induced TBARS production in a dose-dependent manner, with the seed extract having the highest inhibitory effect and the leaf extract exhibiting higher phenolic content and radical scavenging abilities, but lower Fe chelation ability compared with that of the seed. The phytochemical screening revealed the presence of saponins, alkaloids, and terpenoids in both extracts, whereas the total alkaloid profile was higher in the seed extract than in the leaf extract, as revealed by GC-FID.The anti-cholinesterase and antioxidant activities of avocado leaf and seed could be linked to their phytoconstituents and might be the possible mechanisms underlying their use as a cheap and natural treatment/management of AD. However, these extracts should be further investigated in vivo.

Biochemical and pharmacological effects of the direct thrombin inhibitor AR-H067637

2009 ◽  
Vol 101 (06) ◽  
pp. 1051-1059 ◽  
Author(s):  
Christer Mattsson ◽  
Tord Inghardt ◽  
Margareta Elg ◽  
Johanna Deinum
Keyword(s):  
Competitive Inhibitor ◽  
Direct Thrombin Inhibitor ◽  
Anticoagulant Effect ◽  
Thrombin Inhibitor ◽  
Thrombin Time ◽  
Clotting Time ◽  
Binding Studies ◽  
Plasma Coagulation ◽  
Coagulation Assays

SummaryAZD0837 is in development as a new oral anticoagulant for use in thromboembolic disorders. In vivo, AZD0837 is converted to AR-H067637, a selective and reversible direct thrombin inhibitor. Established biochemical methods were used to assess and measure the biochemical and pharmacological properties of AR-H067637. Both direct Biacore binding studies of AR-H067637 with immobilised α-thrombin and inhibition studies using pre-steady state kinetics with thrombin in the fluid phase confirmed that AR-H067637 is a rapid-binding, reversible and potent (inhibition constant K i = 2–4 nM), competitive inhibitor of thrombin, as well as of thrombin bound to fibrin (clot-bound thrombin) or to thrombomodulin. The total amount of free thrombin generated in platelet-poor clotting plasma was inhibited concentration-dependently by AR-H067637, with a concentration giving half maximal inhibition (IC50) of 0.6 μM. Moreover, AR-H067637 is, with the exception of trypsin, a se-lective inhibitor for thrombin without inhibiting other serine proteases involved in haemostasis. Furthermore, no anticoagulant effect of the prodrug was found. AR-H067637 prolonged the clotting time concentration-dependently in a range of plasma coagulation assays including activated partial thromboplastin time, prothrombin time, prothrombinase-induced clotting time, thrombin time and ecarin clotting time. The two latter assays were found to be most sensitive for assessing the anticoagulant effect of AR-H067637 (plasma IC50 93 and 220 nM, respectively). AR-H067637 also inhibited thrombin-induced platelet activation (by glycoprotein IIb/IIIa exposure, IC50 8.4 nM) and aggregation (IC50 0.9 nM). In conclusion, AR-H067637 is a selective, reversible, competitive inhibitor of α-thrombin, with a predictable anticoagulant effect demonstrated in plasma coagulation assays.

scholarly journals In vivo Pharmacological investigation of leaf of Polygonum hydropiper (L.)

2014 ◽  
Vol 12 (2) ◽  
pp. 165-169
Author(s):  
Rumana Akhter ◽  
Md Aminul Haque ◽  
Mohiuddin Ahmed Bhuiyan ◽  
Mohamad Shahriar
Keyword(s):  
Acute Toxicity ◽  
Intestinal Motility ◽  
Leaf Extract ◽  
Methanol Extract ◽  
Diclofenac Sodium ◽  
Chloroform Extract ◽  
Polygonum Hydropiper ◽  
Albino Mice ◽  
Higher Doses

The present study was planned to evaluate the anti-nociceptive, gastro intestinal motility, anti-pyretic and acute toxicity studies of leaf extract of Polygonum hydropiper leaves in albino mice following oral administration. The results showed that the anti-nociceptive activity in the scale of ethanol > n-hexane > petroleum ether > chloroform > methanol extract showed a significant result compared to diclofenac sodium. Chloroform extract showed significant results on gastro intestinal motility test. Ethanol & chloroform extracts showed considerable reduction of temperature at higher doses within 1st hour on yeast induced pyrexia in albino mice. Highest dose introduced as 1000, 2000 & 4000 mg/kg body weight of each extracts in acute toxicity test did not shown any sign of toxicity in albino mice in one week observation. Dhaka Univ. J. Pharm. Sci. 12(2): 165-169, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17619

scholarly journals Antivenom Effects of 1,2,3-Triazoles againstBothrops jararacaandLachesis mutaSnakes

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Thaisa F. S. Domingos ◽  
Laura de A. Moura ◽  
Carla Carvalho ◽  
Vinícius R. Campos ◽  
Alessandro K. Jordão ◽  
...  
Keyword(s):  
Biological Effects ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Snake Venoms ◽  
Concentration Dependent Manner ◽  
Biological Assays ◽  
Snake Bites ◽  
Lachesis Muta

Snake venoms are complex mixtures of proteins of both enzymes and nonenzymes, which are responsible for producing several biological effects. Human envenomation by snake bites particularly those of the viperid family induces a complex pathophysiological picture characterized by spectacular changes in hemostasis and frequently hemorrhage is also seen. The present work reports the ability of six of a series of 1,2,3-triazole derivatives to inhibit some pharmacological effects caused by the venoms ofBothrops jararacaandLachesis muta.In vitroassays showed that these compounds were impaired in a concentration-dependent manner, the fibrinogen or plasma clotting, hemolysis, and proteolysis produced by both venoms. Moreover, these compounds inhibited biological effectsin vivoas well. Mice treated with these compounds were fully protected from hemorrhagic lesions caused by such venoms. But, only theB. jararacaedema-inducing activity was neutralized by the triazoles. So the inhibitory effect of triazoles derivatives against somein vitroandin vivobiological assays of snake venoms points to promising aspects that may indicate them as molecular models to improve the production of effective antivenom or to complement antivenom neutralization, especially the local pathological effects, which are partially neutralized by antivenoms.

scholarly journals PHYTOTOXIC ACTIVITY OF MORINGA OLEIFERA LEAF EXTRACT ON GERMINATION AND SEEDLING GROWTH OF TOMATO

2021 ◽  
Vol 21 (No 1) ◽  
Author(s):  
Ruchi Vyas ◽  
Kanika Sharma
Keyword(s):  
Seed Germination ◽  
Seedling Growth ◽  
Crude Extract ◽  
Extraction Method ◽  
Leaf Extract ◽  
Moringa Oleifera ◽  
Inhibitory Effect ◽  
Phytotoxic Activity ◽  
Young Leaves

The aim of this study was to evaluate the phytotoxic potential of 50% alcoholic crude extract as well as benzene fraction of young leaves of Moringa oleifera Both determine the growth bioassay of seed germination and seedling growth of tomato (Solanum lycopersicon). The crude extract was prepared by cold extraction method and benzene fraction was prepared by hot extraction method with soxhlet assembly. Extraction was carried out with healthy young leaves (in powder form) and organic solvent. Concentrations are used for phytotoxicity assay is 5,10,15,20 and 25mg/ml. Phytotoxicity was done by standard blotter method. The Result exhibited that 5, 10 and 15 mg/ml concentration of extract was non phytotoxic and were further used for in vivo experiments using chambered Thick Paper Glass. The phytotoxic potential of the crude as well as partially purified extract of leaves of Moringa oleifera varied according to concentration and it is called concentration depended inhibitory effect. The greatest inhibitory effect on the seed germination that is 37% in crude extract and 30% in a partially purified extract of 25mg/ml concentration of leaf extract. Equally, 25 mg/ml concentration detected to be toxic against a seedling growth of tomato and demonstrating that the compound responsible for the phytotoxic

scholarly journals Acute and Subacute Toxicity Assessment of Ethyl Acetate Extracts from Aerial Parts of Clerodendrum thomsoniae Balf.f in Rodents

2021 ◽  
Vol 11 (6) ◽  
pp. 13952-13961
Keyword(s):  
Acute Toxicity ◽  
Ethyl Acetate ◽  
Human Subjects ◽  
Female Rats ◽  
Laboratory Animals ◽  
Oral Toxicity ◽  
Subacute Toxicity ◽  
Toxicity Studies ◽  
Male And Female Rats

Clerodendrum is a genus of about 500 species belongs to the family Lamiaceae. Several species of this genus have been proved for the treatment of various diseases. Clerodendrum thomsoniae Balf.f were selected in this study; according to the literature available, there is no systematic toxicity studies for this plant were described. The current study was therefore carried out to evaluate the acute and sub-acute toxicity in mice and rats. The acute oral toxicity study was performed in mice following OECD guidelines 425, and the sub-acute toxicity was performed in male and female rats following OECD guidelines 407. The results showed that mice given a single dose of up to 2000 mg/kg orally did not show any toxicity signs or mortality. In the sub-acute toxicity analysis in rats, 3 specific daily doses of 150, 300, and 600 mg/kg for 28 days did not induce any major changes to the hematological and biochemical parameters. Histopathological studies revealed normal architecture that did not indicate any morphological disturbances. In our study, no deaths or any signs of toxicity were found in acute and subacute toxicity studies after oral administration according to OECD guidelines, which concluded that ethyl acetate extract of Clerodendrum thomsoniae Balf (EACT) could use for in vivo biological activity studies in laboratory animals to explore its various medicinal activity before study in human subjects.

On the Release of the Three Locust (Locusta migratoria) Adipokinetic Hormones: Effect of Crustacean Cardioactive Peptide and Inhibition by Sugars

1999 ◽  
Vol 54 (1-2) ◽  
pp. 110-118 ◽  
Author(s):  
James E. Flanigan ◽  
Gerd Gäde
Keyword(s):  
Biological Effects ◽  
Locusta Migratoria ◽  
Inhibitory Effect ◽  
Test System ◽  
Hormone Release ◽  
Adipokinetic Hormone ◽  
High Potassium ◽  
Crustacean Cardioactive Peptide

An existing test to monitor the rate of adipokinetic hormone release from the corpora cardiaca (C C) of Locusta migratoria in vitro was improved, so that a constant basal rate of release was achieved and the amount of released Lom-AKH-I, II and III could be quantified by HPLC . This test system was subsequently used to demonstrate that a small peptide, which has been found in a few insect species including L. migratoria, crustacean cardioactive peptide (CCAP), induces release of all three AKHs. Moreover, 80 mᴍ trehalose reduces CCAP-induced release of AKHs in vitro, and 160 mᴍ glucose reduces this release even further. Glucose also had a greater inhibitory effect than trehalose on the spontaneous release and inhibited the high potassium-stimulated release of AKH from the CC in vitro. Eighty mᴍ sucrose, on the other hand, had no effect on the release of AKH . The effect of trehalose and glucose could be due to their use as an energy source, with trehalose first having to be converted to glucose. Whatever the stimulus, the three AKHs are released in the same proportions as they are found in the CC, which in vivo would make Lom-AKH-I, the most abundant AKH, the major effector of the biological effects of AKHs in adult locusts

scholarly journals Anthelmintic effect of thymol and thymol acetate on sheep gastrointestinal nematodes and their toxicity in mice

2017 ◽  
Vol 26 (3) ◽  
pp. 323-330 ◽  
Author(s):  
Weibson Paz Pinheiro André ◽  
Géssica Soares Cavalcante ◽  
Wesley Lyeverton Correia Ribeiro ◽  
Jessica Maria Leite dos Santos ◽  
Iara Tersia Freitas Macedo ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Biological Effects ◽  
Anthelmintic Activity ◽  
Gastrointestinal Nematodes ◽  
In Vitro Tests ◽  
Egg Hatch ◽  
In Vivo Test ◽  
Anthelmintic Effect

Abstract Thymol is a monoterpene and acetylation form of this compound can reduce the toxicity and enhance its biological effects. The objective of this study was to evaluate the effect of thymol and thymol acetate (TA) on egg, larva and adult Haemonchus contortus and the cuticular changes, acute toxicity in mice and the efficacy on sheep gastrointestinal nematodes. In vitro tests results were analyzed by analysis of variance (ANOVA) and followed by comparison with Tukey test or Bonferroni. The efficacy of in vivo test was calculated by the BootStreet program. In the egg hatch test (EHT), thymol (0.5 mg/mL) and TA (4 mg/mL) inhibited larval hatching by 98% and 67.1%, respectively. Thymol and TA (8 mg/mL) inhibited 100% of larval development. Thymol and TA (800 µg/mL) reduced the motility of adult worms, by 100% and 83.4%, respectively. Thymol caused cuticular changes in adult worm teguments. In the acute toxicity test, the LD50 of thymol and TA were 1,350.9 mg/kg and 4,144.4 mg/kg, respectively. Thymol and TA reduced sheep egg count per gram of faeces (epg) by 59.8% and 76.2%, respectively. In in vitro tests thymol presented better anthelmintic activity than TA. However TA was less toxic and in in vivo test efficacy was similar.

scholarly journals UTILIZATION OF SAMBUNG NYAWA LEAF EXTRACTS Gynura procumbens (Lour) Merr. FOR TREATMENT OF Vibrio alginolyticus IN TIGER GROUPER (Epinephelus fuscoguttatus Forsskal, 1775)

2019 ◽  
Vol 47 (2) ◽  
pp. 134
Author(s):  
Novi Santika ◽  
Wardiyanto Wardiyanto ◽  
Esti Harpeni
Keyword(s):  
Leaf Extract ◽  
Sea Water ◽  
Economic Value ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Vibrio Alginolyticus ◽  
Leaf Extracts ◽  
Tiger Grouper

Tiger Grouper is one of the sea water fish commodities that is quite popular with the community and has a high economic value. The problem faced by farmers is the attack of Vibriosis, one of which is caused by the Vibrio alginolyticus bacteria. The use of synthetic antibiotics has been widely used but has many adverse effects, so it needs new alternatives for the treatment of Vibriosis disease. One of them is by using the extract of lifelong leaf extract. Life-sustaining plants (Gynura procumbens) contain secondary metabolites such as flavonoids, tannins, and antibacterial saponins. This study aims to determine the best dosage of lifelong leaf extract for the treatment of Vibriosis disease in tiger grouper. The study was conducted in two stages, namely in vitro and in vivo. Before the fish were treated with feed that had been given a sambung deca leaf extract, the fish were challenged using Vibrio alginolyticus with a density of 108 CFU / mL as much as 0.1 mL / head and then fed with treatment and maintained for 21 days. The results of the in vitro study showed that the life of sambung leaf extract at a dose of 700 ppm had a broad inhibitory effect on V. alginolyticus, which amounted to 10.47 mm compared to other treatments. Whereas when continued for in vivo testing, a dose of 350 ppm in general has been applied for the treatment of attacks of Vibrio alginolyticus in tiger grouper.

scholarly journals Chrysophyllum cainito: A Tropical Fruit with Multiple Health Benefits

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Hau V. Doan ◽  
Thao P. Le
Keyword(s):  
Human Health ◽  
Leaf Extract ◽  
Viral Infections ◽  
Inflammatory Responses ◽  
Biological Effects ◽  
Antioxidant Properties ◽  
Tropical Fruit ◽  
Chrysophyllum Cainito

Chrysophyllum cainito is a tropical fruit tree with multiple benefits to human health. C. cainito possesses strong antioxidant properties either in vitro or in vivo. Extracts from the leaves, stem bark, fruits, peel, pulp, or seed of C. cainito are promising candidates in traditional medicine for curing diabetes and fighting against bacterial, fungal, and viral infections. C. cainito leaf extract alone or in a complex formula exhibits anti-inflammatory responses by reducing hypersensitivity, acts as inflammatory markers, and has antinociceptive effects. The leaf extract also increases wound healing speed and assists in regulating fat uptake. In addition, the C. cainito fruit shows anticancer activity against osteosarcoma. In conclusion, the aerial parts of C. cainito have strong beneficial biological effects on human health.

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