Thrombolytic Potential Research Articles

In vitro Thrombolytic Activity of Flowers of Nerium oleander

The study was carried out to investigate the in vitro thrombolytic potential of crude methanolic extract of flowers of Nerium oleander, a plant widely employed in traditional medicine to treat cardiovascular diseases. Using the blood of selected sixteen individuals, the thrombolytic activity was assessed in four different concentrations of the crude plant extract where streptokinase and normal saline were used as the positive and negative control respectively. The clot lysis percentage was calculated using weight reduction of the blood clot in comparison to the initial clot weight. The highest thrombolytic potential was observed at 10 mg/mL concentration of the extract and there was no significant difference between mean clot lysis percentages of streptokinase and this extract. Therefore, 10.0 mg/mL concentration of methanolic extract of flowers of N. oleander has a good thrombolytic ability, however, further investigations on its chemical profile and toxic properties are required before developing it as a therapeutic agent.

Enhanced activity of an ADAMTS‐13 variant (R568K/F592Y/R660K/Y661F/Y665F) against platelet agglutination in vitro and in a murine model of acute ischemic stroke

Summary Essentials ADAMTS13 requires a substrate‐induced conformational change to attain full activity in vitro.The efficacy of wild type ADAMTS13 in models of thrombosis/stroke may be enhanced by pre‐activation.A pre‐activated ADAMTS13 variant exhibits enhanced proteolysis of platelet agglutinates.This ADAMTS13 variant is protective in a murine model of stroke at a lower dose than WT ADAMTS13. SummaryBackgroundADAMTS‐13 circulates in a closed conformation, only achieving full proteolytic activity against von Willebrand factor (VWF) following a substrate‐induced conformational change. A gain‐of‐function (GoF) ADAMTS‐13 variant (R568K/F592Y/R660K/Y661F/Y665F) is conformationally preactivated.ObjectivesTo establish how the hyperactivity of GoF ADAMTS‐13 is manifested in experimental models mimicking the occlusive arterial thrombi present in acute ischemic stroke.MethodsThe ability of GoF ADAMTS‐13 to dissolve VWF–platelet agglutinates was examined with an assay of ristocetin‐induced platelet agglutination and in parallel‐flow models of arterial thrombosis. A murine model of focal ischemia was used to assess the thrombolytic potential of GoF ADAMTS‐13.ResultsWild‐type (WT) ADAMTS‐13 required conformational activation to attain full activity against VWF‐mediated platelet capture under flow. In this assay, GoF ADAMTS‐13 had an EC50 value more than five‐fold lower than that of WT ADAMTS‐13 (0.73 ± 0.21 nm and 3.81 ± 0.97 nm, respectively). The proteolytic activity of GoF ADAMTS‐13 against preformed platelet agglutinates under flow was enhanced more than four‐fold as compared with WT ADAMTS‐13 (EC50 values of 2.5 ± 1.1 nm and 10.2 ± 5.6 nm, respectively). In a murine stroke model, GoF ADAMTS‐13 restored cerebral blood flow at a lower dose than WT ADAMTS‐13, and partially retained the ability to recanalize vessels when administration was delayed by 1 h.ConclusionsThe limited proteolytic activity of WT ADAMTS‐13 in in vitro models of arterial thrombosis suggests an in vivo requirement for conformational activation. The enhanced activity of the GoF ADAMTS‐13 variant translates to a more pronounced protective effect in experimental stroke.

Unveiling novel 2-cyclopropyl-3-ethynyl-4-(4-fluorophenyl)quinolines as GPCR ligands via PI3-kinase/PAR-1 antagonism and platelet aggregation valuations; development of a new class of anticancer drugs with thrombolytic effects

In the present study, novel 2-cyclopropyl-3-ethynyl-4-(4-fluorophenyl) quinolines (4a-l) were recognized and evaluated as G-Protein Coupled Receptor (GPCR) ligands through molecular evaluations. Thrombin mediates adhesion of mast cell, a type of cell abundantly found in connective tissue and releasing histamine and other substances during inflammatory and allergic reactions, through phosphoinositol 3-kinase pathway. With this background, as preliminary, 4a-l are resolute to be potential leads, designated from their effective phosphoinositol 3-kinase (PI3-Kinase) inhibition potentials, best-docked scores, comparative ligand efficiency, and significant structural attributes evaluated by ab initio simulations. Since thrombin is one of the main reason for various cancer invasion in association with PI3Kinase, a thrombolytic potential of the compounds also analyzed. The experimental in vitro studies confirmed the significant enhancement as PI3Kinase inhibitors and appreciable enhancement in MTT assay of breast and skin cancer cell lines. Significantly, acetophenone substituent in the quinoline scaffold could be coherent to note the significant binding affinity to all the evaluated drug targets.

Investigation of biological activities of the flowers of Lagerstroemia speciosa, the Jarul flower of Bangladesh

BackgroundLagerstroemia speciosa (L.) Pers. (Family: Lythraceae) is used in traditional medicine in the treatment of diarrhea, diabetes and other diseases. The study was performed to conduct antioxidant, cytotoxic, thrombolytic, membrane stabilizing, antimicrobial, peripheral and central analgesic and hypoglycemic activity assays and phenobarbitone sodium–induced sleeping time test using crude methanol extract of flowers of L. speciosa and its different partitionates.MethodThe antioxidant potential was evaluated by determining the ability of the samples to scavenge 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical. The cytotoxic potential was examined following the procedures of brine shrimp lethality bioassay. Thrombolytic potential was assayed using streptokinase as standard. The samples were subjected to membrane stabilizing activity assay under heat induced condition. Antimicrobial potential was observed by disc diffusion method. The ability of the extract to inhibit writhing induced by acetic acid was determined in peripheral analgesic activity assay. The extract was also tested for central analgesic and hypoglycemic activities by tail flicking and tail tipping methods in Swiss albino mice model, respectively. CNS depressant activity was evaluated by an assay in which sleep was induced in mice using phenobarbitone sodium.ResultsThe chloroform soluble fraction of L. speciosa extract demonstrated the highest antioxidant activity (IC50 = 4.20 ± 0.41 μg/ml) while the most prominent cytotoxic potency was showed by hexane soluble fraction (LC50 = 2.00 ± 0.31 μg/ml). Among the test samples, the carbon tetrachloride soluble fraction induced clot lysis (64.80 ± 0.27%) and prevented heat induced haemolysis (41.90 ± 0.10%) to the maximum extent. The largest zone of inhibition (19.0 mm) against Staphylococcus aureus, was also observed for the same fraction. In peripheral analgesic activity assay, 16.68% inhibition of writhing was documented for the L. speciosa extract (400 mg/kg body weight dose). The extract (400 mg/kg dose) also reduced blood sugar level by 56.12% after three hours of administration of glucose solution. In CNS depressant activity assay, mice of the sample group slept for shorter period of time compared to control group.ConclusionsFrom our investigation, it can be suggested that, the extract should be further studied for possible phytochemicals responsible for the observed biological activities.

Evaluation of anticoagulant and thrombolytic activity of Berberis orthobotrys in animal model

Fundamental to this research was the evaluation of anticoagulant and thrombolytic potential of Berberis orthobotrys using clotting time, prothrombin time and activated partial thromboplastin time performed at 2.5, 5, 10% concentration. Aqueous-methanol extract significantly (p<0.05) increased the coagulation parameters both in human blood as well as in rabbit blood and exhibited the more salient effect on prolongation of these coagulation parameters at 10% concentration. Aqueous methanol extract (25, 50 and 100 mg/kg) produced the preferential increase in bleeding time and clotting time nevertheless the effect was more perceptible after 90 min at 100 mg/kg. Moreover, the crude extract presented a substantial increase in coagulation parameters after 7 days of administration in rabbits with more pronounced effects at the highest dose. HPLC profile of aqueous methanol extract revealed the presence of quercetin, p-coumaric acid, gallic acid, vanillic acid, 4-hydroxy-3-methoxy benzoic acid. Thus, the present study provides the pharmacological basis for its medical use in cardiovascular and other thrombotic disorders.

Cytotoxic Activity on Brine Shrimp, MCF-7 Cell Line and Thrombolytic Potential: Seven Different Medicinal Plant Leaves Extract

The aim of our study was to find out the preliminary cytotoxic and thrombolytic effect of the seven selected medicinal plant leaves extract. In cytotoxic activity, out of the seven leaves extract three of them exhibited stronger brine shrimp lethality with LC50 122.548 (Uncaria acida), 170.861 (Leea indica) and 175.469 (Piper porphyrophyllum) μg /mL respectively, and on MCF-7 cell line, they also exhibited moderate cytotoxic activity with different concentration of the extract of the same plant leaves such as,Uncaria acida (72.31, 56.22, 38.12 and 9.24%), Leea indica (67.31, 58.22, 43.12 and 15.24%), Piper porphyrophyllum (65.88, 48.12, 40.12 and 21.34%). In thrombolytic assessments, all the leaves extract showed moderate (considering > 20% moderate; **p < 0.01; *p < 0.05) clot lysis activity, but among the extracts, Uncaria cordata (27.36 ± 0.10%) showed the highest and Stachytarpheta indica the lowest (6.14 ± 0.20%) percent clot lysis as compared with the standard streptokinase (65.15 ± 0.16%). This study was conducted to legalize the folkloric use of seven medicinal plant leaves.

Investigation of Preliminary Phytochemicals, Analgesic, Anti-Arthritic, Thrombolytic and Cytotoxic Activities of Begonia Roxburghii (Miq.) DC. Leaves

Background: The study was designed to investigate the phytochemical, analgesic, anti-arthritic, thrombolytic and cytotoxic evaluation of the Begonia roxburghii (Miq.) DC leaves extract (nHBR) using both in vitro and in vivo methods.Methods: The acetic acid induced writhing test and formalin induced pain test was used to perform anti-nociceptive activity on mice. In vitro anti-arthritic activity was assessed using protein denaturation method. The clot lysis activity was considered to evaluate thrombolytic potentials of the plant extract. The cytotoxic study was performed using brine shrimp larvae.Results: The phytochemical study has shown the abundance of flavonoids, alkaloids, glycosides, tannins, saponins and reducing sugars in the plant extract. In acetic acid-induced writhing test, the extract at different doses (100-400 mg/kg) reduced the number of writhing by 26.42 ± 1.13, 43.64 ± 2.50 and 55.42 ± 1.83 % respectively. The nHBR inhibited the licking response in both the early phase (56.52 ± 2.55 %) and the late phase (62.52 ± 2.57 %) in the formalin induced pain test. Moreover, the results revealed concentration dependent anti-arthritic effect in protein denaturation method with maximum inhibition 69.61 ± 2.15 % at doses 1000 μg/ml. The nHBR also showed (47.77 ± 1.80 %) clot lytic activity and cytotoxicity with LC50 67.61 μg/ml in the brine shrimp larvae bioassay.Conclusion: The study demonstrated phytochemical, anti-nociceptive, anti-arthritic, clot lysis and cytotoxic activities of the Begonia roxburghii (Miq.) DC.

Production of Fibrinolytic Enzyme by the Marine Isolate Serratia marcescens subsp. sakuensis and its In-vitro Anticoagulant and Thrombolytic Potential

Production of Fibrinolytic Enzyme by the Marine Isolate Serratia marcescens subsp. sakuensis and its In-vitro Anticoagulant and Thrombolytic Potential

In-vivo antiemetic and antinociceptive, cytotoxic and in-vitro thrombolytic potential of hydro-alcoholic stem and leaves extract of jatropha gossypiifolia.

This study describes the biological investigations of hydro-alcoholic leaves and stem extract of Jatropha gossypiifolia, a plant belonging to the family Euphorbiaceae, to reveal their possible contribution as an antiemetic, antinociceptives, cytotoxic and thrombolytic factor. The leaves and stems of Jatropha gossypiifolia were extracted with methanol. The leaves extracts were used for the observation of thrombolytic potential. Result reveals that the leaves at a concentration of 2.5mg/mL, showed maximum activity (27.255 ± 0.90%), whereas 20 mg/mL sample solution showed the lowest activity (7.722 ± 0.26%), when comparing positive control streptokinase. The extracts were used for the investigation of cytotoxic activity considering vincristine sulfate as a positive control. The leaves and the stems portion have considerable cytotoxic property (LC50 are 0.00532 µg/ml for stems and 0.000109 µg/ml for leaves, respectively) when comparing with positive control. The methanolic extract showed potent antiemetic activity at the highest concentration both at leaves and stem extracts as compared to positive control metoclopramide. Where metoclopramide shows 73% of inhibition, there leaves and the stem portion of the plant shows 90% and 91% of emesis inhibition respectively. By using a standard protocol, the crude methanolic stem and leaves extract of J. gossypiifolia was conducted to attempt for antinociceptives activities, where Diclofenac Na is used as a standard. The crude methanolic extract of leaves and stem exhibit 31.07% and 30.79% writhing inhibition in test animals respectively, which are statistically significant. The results of the study showed that the plant extract has potential thrombolytic, cytotoxic, antiemetic and antinociceptive activities.

Therapeutic investigations of novel indoxyl-based indolines: A drug target validation and Structure-Activity Relationship of angiotensin-converting enzyme inhibitors with cardiovascular regulation and thrombolytic potential

A family of 12 members of Naphthalene-2-ol-indolin-2-one-thiocarbamides (5a-l) with pharmacological potentials of cardiovascular modulator were efficiently synthesized and evaluated. These compounds show inhibitory activity on angiotensin-converting enzyme (ACE), which is a principal constituent of the renin–angiotensin system and causative source for hypertension (HTN) (elevated blood pressure) and congestive heart failure (CHF), a parameter that was tested in this report. Prior to this, to get more insight into the binding mode and inhibition of human ACE C-domain (PDB ID: 2XY9) and N-domain (PDB ID: 3NXQ) compounds 5a-l was docked into the active site of them. The established inhibitory constant (Ki) (range 40–500 nM) and least binding affinities (−18.52 to −30.57 kcal/mol) indicated the therapeutic selectivity of compounds 5a-l towards ACE C-domain inhibition over ACE N-domain. The cytotoxicity effect of most potent compounds among 5a-l were tested in normal breast cells and MCF-7 cell lines. Simultaneously, H2O2 induced antioxidant and DNA damage assessment was executed. Eventually, a thrombolytic activity followed by a human red blood cell (HRBC) membrane stabilization study to ensure the relaxation of blood and stabilization of RBC was executed. Structure-Activity Relationship (SAR) study discloses the potential of 5c, 5h, and 5k as cardiovascular protective therapeutic agents among 5a-l.

THROMBOLYTIC ACTIVITY OF C.AMADA AND C.CAESIA

Objective: To compare the thrombolytic activity of C.amada and C. caesia.Methods: Hydro alcoholic extractions of C.amada and C. caesia were prepared. Clot lysis potential of the extracts was checked and the results were statistically analysed.Result and Conclusion: On comparing the thrombolytic potential, the % of clot lysis of silver nanoparticle synthesized using C. caesia (51%) was found to be higher than C.amada (34.7%) extract. Similarly C. caesia extract (38.75 ± 2.217) showed higher % of clot lysis than C.amada (34.74 ± 6.074). The mean percentage of clot lysis of rhizome extracts and synthesized silver nanoparticle were statistically more significant (p value < 0.05) when compared to the positive control streptokinase and negative control water. Active component involvement analysis will be helpful to utilize the C.amada and C. caesia as potent therapeutic agent.Key words: C.amada, C. caesia, thrombolytic potential.

In vitro Thrombolytic Potential of Actinoprotease from Marine Streptomyces violaceus VITYGM.

The main aim of the study was to isolate, screen, characterize and produce an extracellular thrombolytic protease from marine actinomycetes. Marine actinomycete was isolated and characterized on the basis of morphological, biochemical, and molecular characterization. The primary screening for protease activity was done by casein hydrolysis method followed by radial caseinolytic assay. The actinoprotease was partially purified using ammonium sulfate precipitation technique followed by dialysis and Sephadex G-50 gel permeation chromatography. 16srDNA sequencing and BLAST search analysis of the sequence revealed close affiliation with Streptomyces genera and identified as Streptomyces violaceus VITYGM with 99% similarity. The specific activity of purified protease was found to be 1437 units/mg along with purification fold up to 1.5 times. The blood clot lysis activity was compared with the standard and found to lyse the blood clot with 97.43%. Till now very less evidences have been reported on actinoprotease. A single peak at retention time 0.9 min observed on high performance liquid chromatography (HPLC) confirmed the homogeneity of the preparation. This is the first study to report on actinoprotease from Streptomyces violaceus VITYGM. This study emphasizes the potency of novel actinoproteases as active compound in drugs for the treatment of cardiovascular diseases.

Exploring hemostatic and thrombolytic potential of heynein - A cysteine protease from Ervatamia heyneana latex

Ethnopharmacological relevanceThe latex of Ervatamia heyneana (Wall.) T. Cooke plant has been used for wound healing and various skin diseases by Indian tribes and folklore. Aim of the studyTo validate the scientific basis of heynein – a key protease of Ervatamia heyneana, in hemostasis and wound healing process. Materials and methodsThe latex from E. heyneana was processed and subjected to two step purification. The purified heynein was assayed for proteolytic activity using casein as substrate and also attested by zymography. The inhibition studies confirmed the nature of heynein. Pure fibrinogen was used for fibrinogenolytic activity and citrated plasma was used for coagulant and fibrinolytic activities. The edema inducing action and hemorrhagic activity of heynein were assessed on mice model. ResultsThe purified heynein exhibited proteolytic activity, which was confirmed by caseinolytic assay and zymography. The inhibition studies confirmed heynein to be a cysteine protease. Heynein showed complete hydrolysis of all the three subunits of human fibrinogen (Aα, Bβ, γ). It exhibited strong pro-coagulant activity by reducing plasma clotting time from 248 to 39s at 40µg concentration. Heynein cleaved α polymer subunit in fibrin clot and did not induce edema and hemorrhage in mice models. The non-hemorrhagic nature was supported with histopathological studies of skin samples. ConclusionHeynein displays strong pro-coagulant action associated with fibrin(ogen)olytic activity. This provides basis for the observed pharmacological action of Ervatamia heyneana and thereby justifies its use in folk medicine.

Assessment of in-vitro cholinesterase inhibitory and thrombolytic potential of bark and seed extracts of Tamarindus indica (L.) relevant to the treatment of Alzheimer's disease and clotting disorders.

Low level of acetylcholine (ACh) is an important hallmark of Alzheimer's disease (AD), a common type of progressive neurodegenerative disorder. Effective treatment strategies rely mostly on either enhancing the cholinergic function of the brain by improving the level of ACh from being a breakdown by cholinesterase enzymes. Again atherothrombosis is major life-threatening cerebral diseases. Traditionally Tamarindus indica (L.) has widely known for its medicinal values. Our aim is to investigate the cholinesterase inhibitory activities as well as thrombolytic activities of the bark and seeds crude methanolic extracts (CMEs) in the treatment of AD and clotting disorder. The crude methanol extract was prepared by cold extraction method and was assessed for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities by the Ellman's method. For thrombolytic activity clot lysis method was applied. To compare both the fractions, extracts from the bark got more AChE inhibitory activity than the seed with the inhibitory concentration 50% IC50 values of 268.09 and 287.15 µg/ml, respectively. The inhibitory activity of BuChE was quiet similar to that of AChE as IC50 values of both the fractions were 201.25 and 254.71 µg/ml. Again in-vitro thrombolytic activity of bark was 30.17% and of seed it was 22.53%. The results revealed that the CME of bark and seed both have moderate cholinesterases inhibitory activities as well as thrombolytic activities, worth of further investigations to identify the promising molecule(s) potentially useful in the treatment of AD as well as in clotting disorders.

Impaired thrombolytic status predicts adverse cardiac events in patients undergoing primary percutaneous coronary intervention.

Antithrombotic medications reduce thrombosis but increase bleeding. Identification of ST-elevation myocardial infarction (STEMI) patients at risk of recurrent thrombosis could allow targeted treatment with potent antithrombotic medications, with less potent agents in others, to reduce bleeding. Conventional platelet function tests assess platelet reactivity only, yet there is increasing evidence that endogenous thrombolytic potential determines outcome following thrombus initiation. We investigated whether assessing both platelet reactivity and endogenous thrombolysis, could identify STEMI patients at high-risk of recurrent thrombotic events. Thrombotic status was assessed in STEMI patients, before and after primary percutaneous coronary intervention (PPCI), at discharge and at 30 days; with 12 months' follow-up. The time to form an occlusive thrombus under high shear (occlusion time, OT), and time to restore flow by endogenous thrombolysis (lysis time, LT) was measured using the point-of-care Global Thrombosis Test (GTT) in the cardiac catheterisation laboratory. Impaired endogenous thrombolysis (prolonged LT ≥ 3000 s), seen in 13 % patients pre-PPCI, was related to major adverse cardiac events, MACE (HR: 3.31, 95 %CI: 1.02-10.78, p = 0.045), driven by cardiovascular death (HR: 4.17, 95 %CI: 0.99-17.51, p = 0.05). Enhanced (rapid) endogenous thrombolysis (LT < 1000 s) was associated with spontaneous reperfusion, ST-segment resolution and Thrombolysis In Myocardial Infarction 3 flow pre-PPCI. Baseline OT was shorter in those with MACE (especially recurrent myocardial infarction and stroke) than those without (253 ± 150 s vs 354 ± 134 s, p=0.017). Endogenous thrombolysis, when impaired, is associated with increased cardiovascular risk, and when enhanced, with spontaneous reperfusion. Endogenous thrombolysis may be a novel target for pharmacological intervention, and allow targeting of potent antithrombotic medications to high-risk patients.

In vivo analgesic, anti-inflammatory potential in Swiss albino mice and in vitro thrombolytic activity of hydroalcoholic fruits extract from Daemonorops robusta Warb

Objectives: The analgesic, anti-inflammatory and thrombolytic potential of Daemonorops robusta Warb, a Bangladeshi tribal medicinal plant was studied for the first time. So our aim was to evaluate analgesic, anti-inflammatory and thrombolytic activities of fruit extract of D. robusta. Methods: Fresh fruits of plant were extracted with methanol and then subjected to preliminary phytochemical screening. Analgesic activity of the extract was performed against acetic acid induced writhing, hot plate and formalin induced test. Anti-inflammatory effect was evaluated using carrageenan induced paw edema in mice. An in vitro thrombolytic model was used to check the clot lysis potential of the extract. Results: Phytochemical screening showed the presence of alkaloid, carbohydrate, flavonoids, steroid, phlobatanin and saponin. The extract exhibited significant analgesic effect (P

Preliminary study on thrombolytic property of thirty six different extracts of eight Bangladeshi medicinal plants with folkloric relevance

Traditional medicinal practitioners or Kavirajes use a variety of medicinal plants for treatment of thrombus ailments-cardiovascular problems. In this study, thrombolytic activity of 36 extracts of different solvents of eight Bangladeshi medicinal plants traditionally used in cardiovascular problems were evaluated to justify their use in folklore medicinal practitice. Extraction was conceded using methanol. Five grams of the concentrated methanol extract of each crude extract were then fractionated to provide n-hexane and carbon tetrachloride fractions. Phytochemically important groups like reducing sugars, tannins, saponins, steroids, gums, flavonoids and alkaloids were tested using standard chromogenic reagents. In vitro thrombolytic potential of extracts was assayed for analyzing the clot lyses by adding the extracts to the pre-clotted blood. The results were compared with the results obtained from streptokinase as standard and water as a negative control. Thrombolytic effect of the extracts ranged from 0.73 ± 2.44 % to 45.81 ± 0.34 % clot lysis whereas the standard streptokinase showed 65.13 ± 0.96 % and the negative control water showed 2.50 ± 0.67 % clot lysis. The highest thrombolytic effect was shown by the crude extract of Melastoma malabathricum leaves and the lowest by the CCl4 fractionate of Litsea glutinosa leaves. Most of the results were found relevant to the traditional use of the plants. Plants traditionally used in thrombus ailments may be an interesting source for further drug development.

TRIAGEM FITOQUÍMICA E AVALIAÇÃO DAS ATIVIDADES TROMBOLÍTICA E CITOTÓXICA DE CECROPIA HOLOLEUCA MIQ. (URTICACEAE), LIPPIA ALBA (MILL.) N.E.BR. EX P. WILSON (VERBENACEAE) E ZANTHOXYLUM RHOIFOLIUM LAM (RUTACEAE)

&lt;em&gt;Cecropia hololeuca&lt;/em&gt;, &lt;em&gt;Lippia alba&lt;/em&gt;, e &lt;em&gt;Zanthoxylum rhoifolium&lt;/em&gt; são espécies vegetais de ocorrência natural no Brasil, características de regiões de Mata Atlântica e, dentro de suas finalidades medicinais, estão incluídas ação anti-hipertensiva, digestiva e no tratamento de malária. Neste estudo, foram avaliados o perfil químico e as atividades citotóxica e trombolítica do extrato etanólico das folhas destas espécies vegetais. O perfil químico dos extratos foi obtido através de ensaios fitoquímicos clássicos, a fim de identificar as classes químicas presentes. A atividade citotóxica foi avaliada frente a &lt;em&gt;Artemia salina&lt;/em&gt; e a atividade trombolítica foi determinada &lt;em&gt;in vitro&lt;/em&gt; a partir da lise em coágulo de sangue humano. Os testes fitoquímicos indicaram a presença de alcaloides e flavonoides nos três extratos investigados. Saponinas, triterpenos e naftoquinonas foram detectados apenas em &lt;em&gt;C. hololeuca&lt;/em&gt;. Esta não demonstrou citotoxicidade frente &lt;em&gt;Artemia salina&lt;/em&gt; (DL&lt;sub&gt;50&lt;/sub&gt; &amp;gt;1000 ppm), enquanto &lt;em&gt;Z. rhoifolium&lt;/em&gt; apresentou DL&lt;sub&gt;50&lt;/sub&gt; igual a 719,44 ppm e &lt;em&gt;L. alba&lt;/em&gt; &amp;lt;250 ppm, o que indica atenção quanto a segurança no uso desta planta medicinal. A atividade trombolítica de &lt;em&gt;L. alba&lt;/em&gt; e &lt;em&gt;C. hololeuca&lt;/em&gt; foi de 6,43 ±2,08 e 9,64 ±1,83 %, respectivamente, demonstrando baixa atividade. Já &lt;em&gt;Z. rhoifolium&lt;/em&gt; alcançou lise de 24,71 ±10,52 %, indicando promissora atividade (p &amp;lt;0,001). A atividade trombolítica de &lt;em&gt;Z. rhoifolium&lt;/em&gt; justifica novos estudos, a fim de investigar os componentes responsáveis pela atividade. Perante a literatura, este é o primeiro relato da avaliação da atividade trombolítica destas espécies vegetais. Os resultados encontrados neste trabalho contribuem para o conhecimento químico-biológico das respectivas espécies.

Molecular processes in the streptokinase thrombolytic therapy

The aim of this research is to evaluate the current streptokinase thrombolytic treatment and to identify or improve new techniques that will base new approaches with a higher efficiency in this area of expertise. In order to be as realistic as possible a new method was set up using magnetic vectorized nanoparticles streptokinase and human blood thrombus. The experimental data confirm the maximum 83% thrombus lyses whenever increase streptokinase concentration. It is very probable to happen because of the presence of high concentration of antiplasmin in the blood that neutralizes around half of the thrombolytic potential of the sanguine plasminogen. The experiment shows also that only free serum plasminogen are available for streptokinase action in order to generate plasmin.

In vitro thrombolytic potential of bioactive compounds from marine Streptomyces sp. VITJS4

The most practical approach to reduce morbidity and mortality of c oronary heart disease (CHD) is to delay the process of thrombus by usage of clot-dissolving agents . The necessities of such safer compounds are to be critically examined for thrombolytic activity especially, from marine sources. Thrombolytic agents have been investigated as a possible treatment for thrombus. The aim of this study was to investigate the in vitro thrombolytic potential of Streptomyces sp.VITJS4 (NCIM No. 5574); (ACC No: JQ234978.1) active compounds. The fibrin degradation revealed a clear transparent zone of clearance with 500μg/mL concentration showing 24mm hydrolysis. The thrombolytic effect of Streptomyces sp.VITJS4 compounds was also demonstrated in vitro clot lysis assay where The percent of thrombolysis by the crude extract showed 90±1.7% at the concentration of 1000µg/mL, whereas percent of thrombolysis by streptokinase was found 100± 00%%. The bioactive compounds were further studied for spectrophotometric analysis. The UV-VIS profile showed different peaks ranging from 400-700 nm with different absorption respectively. The data confirmed the presence of both analogues with absorption maxima at 210 and 310 nm. A sensitive method using LC-MS technique was optimized for the separation and identification of bioactive metabolites which was indicated by the fingerprints. The results of the LC-MS analysis provided different peaks determining the presence of compounds with different therapeutic activities. The current study refers the bioactive compound as impressive thrombolytic agent for further laboratory study. Further studies should be conducted to ensure the efficacy and safety of different concentration of bioactive compounds for drug development. Hence the results reported perhaps useful for the discovery of novel thrombolytic drugs from marine origin.