scholarly journals Therapeutic Potentials of Syzygium fruticosum Fruit (Seed) Reflected into an Array of Pharmacological Assays and Prospective Receptors-Mediated Pathways

Life ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 155
Author(s):  
Jannatul Nasma Rupa Moni ◽  
Md. Adnan ◽  
Abu Montakim Tareq ◽  
Md. Imtiazul Kabir ◽  
A.S.M. Ali Reza ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Integrated Approach ◽  
Gas Chromatography Mass Spectrometry ◽  
Clot Lysis ◽  
Lipinski’S Rule ◽  
Lysis Activity ◽  
In Silico Studies ◽  
Immobility Time

Syzygium fruticosum (SF), a valuable Bangladeshi fruit, is considered an alternative therapeutic agent. Mainly, seeds are used as nutritional phytotherapy to ease physical and mental status by preventing chronic diseases. Here, we scrutinized the S. fruticosum seed’s fundamental importance in traditional medicine by following an integrated approach combining in vivo, in vitro, and in silico studies. The SF was fractionated with different solvents, and the ethyl acetate fraction of SF (EaF-SF) was further studied. Mice treated with EaF-SF (200 and 400 mg/kg) manifested anxiolysis evidenced by higher exploration in elevated plus maze and hole board tests. Similarly, a dose-dependent drop of immobility time in a forced swimming test ensured significant anti-depressant activity. Moreover, higher dose treatment exposed reduced exploratory behaviour resembling decreased movement and prolonged sleeping latency with a quick onset of sleep during the open field and thiopental-induced sleeping tests, respectively. In parallel, EaF-SF significantly (p < 0.001) and dose-dependently suppressed acetic acid and formalin-induced pain in mice. Also, a noteworthy anti-inflammatory activity and a substantial (p < 0.01) clot lysis activity (thrombolytic) was observed. Gas chromatography-mass spectrometry (GC–MS) analysis resulted in 49 bioactive compounds. Among them, 12 bioactive compounds with Lipinski’s rule and safety confirmation showed strong binding affinity (molecular docking) against the receptors of each model used. To conclude, the S. fruticosum seed is a prospective source of health-promoting effects that can be an excellent candidate for preventing degenerative diseases.

scholarly journals Exploration of in vitro thrombolytic, anthelminthic, cytotoxic and in vivo anxiolytic potentials with phytochemical screening of flowers of Brassica nigra

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Mohammad Sarowar Uddin ◽  
Md. Shalahuddin Millat ◽  
Mohammad Safiqul Islam ◽  
Md. Saddam Hussain ◽  
Md. Giash Uddin ◽  
...  
Keyword(s):  
Brassica Nigra ◽  
Anxiolytic Activity ◽  
Clot Lysis ◽  
Dependent Manner ◽  
Standard Drug ◽  
Lead Compounds ◽  
Lysis Activity ◽  
Test Models

Abstract Background Brassica nigra is a plant of Brassicaceae family, which possesses numerous medicinal values. Our present study is intended to assess the potential in vitro thrombolytic, anthelminthic, cytotoxic and in vivo anxiolytic properties of MCE of B. nigra flowers. MCE was fractioned for separating the compound on the basis of polarity by using chloroform, n-hexane and ethyl acetate solvent. Thrombolytic and anthelminthic activities were explained by collecting human erythrocytes and earthworms as test models, respectively. Anxiolytic activity was evaluated by elevated plus maze and hole board models while cytotoxic test was conducted through brine shrimp lethality bioassay. Results MCE revealed the presence of alkaloids, flavonoids, tannin, diterpenes, glycosides, carbohydrates, phenols, fixed oils and fat. In case of thrombolytic test, the MCE, CSF, ASF and n-HSF had produced maximum clot lysis activity at 5 and 10 mg/ml dose conditions. Two different concentrations (10 and 20 mg/ml) of MCE and its fractions showed significant (p < 0.05) anthelminthic activities in a dose-dependent manner. Significant anxiolytic activity was observed for all fractions which was comparable to the standard drug diazepam (p < 0.05). Again, the cytotoxic screening also presented good potentials for all fractions. Conclusion From the findings of present study, we can conclude that MCE of B. nigra flowers and its fraction possess significant anxiolytic, anthelmintic, anticancer and thrombolytic properties which may be a good candidate for treating these diseases through the determination of bio-active lead compounds.

scholarly journals Docking against Lung cancer protein and Drug-likeliness of Bioactive Compounds from Phymatosorus scolopendria (Burm.F.) Pic. Serm.

2020 ◽  
pp. 437-441
Author(s):  
Sujatha Srinivasan ◽  
Catharin S. Sivaraman ◽  
Ramya R. Issac ◽  
Gayathiri Mahalingam ◽  
Gnana D. R. Roke
Keyword(s):  
Lung Cancer ◽  
Bioactive Compounds ◽  
Vinyl Ester ◽  
In Vivo Studies ◽  
Lipinski’S Rule ◽  
Lipinski’S Rule Of Five ◽  
Gas Chromatography Mass Spectroscopy ◽  
Nitrophenyl Ester

Phymatosorus scolopendria (Burm.F.) Pic. Serm. is a medicinally important fern which is used traditionally by various people all over the World. The aim of this research focuses on the docking against lung cancer protein (2ITO) with bioactive compounds of Phymatosorus scolopendria (Burm.F.) Pic. Serm. which is obtained by using Gas Chromatography Mass Spectroscopy.  The same compounds were analysed using Lipinski’s rule of five for its pharmacological prediction. The bioactive compounds were further referred for ADMET property to find its pharmacokinetic potency and prediction towards its potential as drug in future.   Among the four compounds docked with the Lung cancer protein (2ITO) 4-Nitrophenyl laurate shows high docking score followed by Hexadecanoic acid, 4 Nitrophenyl ester and Myristic acid Vinyl ester. Out of four compounds studied three compounds satisfied the  drug-likeliness based on Lipinski’s rule of five. The present work suggests the bioactive compounds of Phymatosorus scolopendria (Burm.F.) Pic. Serm.  for further in vitro and in vivo studies for its anticancer benefits especially related to lung cancer.

scholarly journals Prediksi Protein Target Bioaktif Ekstrak Metanol Buah Belimbing (Averrhoa carambola) dalam Regulasi Tekanan Darah

2019 ◽  
Vol 8 (1) ◽  
pp. 9-22
Author(s):  
Siti Munawaroh ◽  
Dian Laila Purwaningroom ◽  
Dianita Rifqia Putri ◽  
Cholik Harun Rosjidi
Keyword(s):  
Mass Spectrometry ◽  
Blood Pressure ◽  
Gas Chromatography ◽  
Bioactive Compounds ◽  
Methanol Extract ◽  
Gas Chromatography Mass Spectrometry ◽  
Pressure Regulation ◽  
Averrhoa Carambola

AbstractBlood pressure regulation is basically control of amount of blood flow to certain tissues according to their metabolic needs. The complexity of the mechanisms involved leading to the assumption that there are many functional and structural proteins involved in blood pressure regulation. Indonesian people, especially those living on the island of Java, usually consume star fruit Averrhoa carambola to reduce blood pressure, but the content of bioactive compounds and the mechanism of their interference with proteins is still unknown. This study aimed to determine the bioactive compound content of Averrhoa carambola's methanol extract and its mechanism of interference with the target proteins. An amount of 200 g Averrhoa carambola dried simplicia was extracted by the maceration method using absolute methanol. The extract was then subjected to phytochemical tests using the Gas Chromatography-Mass Spectrometry (GC-MS) method. Based on the results obtained from the GC-MS phytochemical test, the names of the bioactive compounds found in the Averrhoa carambola methanol extract were obtained. The compounds are then analyzed for their target protein in the human body using the STITCH database (http://stitch.embl.de/). The proteins that had been predicted to be the target of active compounds of Averrhoa carambola methanol extract were analyzed for interactions between proteins using the STRINGdb database (https://string-db.org/cgi/input.pl). Based on this research, it can be concluded that Averrhoa carambola fruit methanol extract can help lower blood pressure by producing NO and acting as antioxidants. However, further research (in-vitro and in-vivo) needs to be done to prove the mechanism. AbstrakRegulasi tekanan darah adalah jumlah kontrol aliran darah ke jaringan tertentu sesuai dengan kebutuhan metabolismenya. Kompleksnya mekanisme yang terlibat, memunculkan asumsi terdapat banyak protein fungsional maupun struktural yang terlibat dalam regulasi tekanan darah. Masyarakat Indonesia, terutama yang tinggal di pulau Jawa biasa mengkonsumsi buah belimbing untuk menurunkan tekanan darah, namun kandungan senyawa bioaktif dan mekanisme intervensinya terhadap protein-protein belum diketahui. Tujuan penelitian ini adalah untuk mengetahui kandungan senyawa bioaktif ekstrak metanol buah Averrhoa carambola dan mekanisme intervensinya terhadap protein-protein targetnya. Simplisia kering buah Averrhoa carambola sebanyak 200 g diekstraksi dengan metode maserasi menggunakan metanol absolut. Dari ekstrak tersebut dilakukan uji fitokimia dengan metode Gas chromatography–mass spectrometry (GC-MS) sehingga didapatkan nama-nama senyawa bioaktif yang terdapat pada ekstrak metanol Averrhoa carambola. Senyawa-senyawa tersebut kemudian dianalisis protein targetnya dalam tubuh manusia menggunakan database STITCH (http://stitch.embl.de/). Kemudian dianalisis interaksi antar protein menggunakan database STRINGdb (https://string-db.org/cgi/input.pl). Berdasarkan penelitian ini, ekstrak metanol buah Averrhoa carambola dapat membantu menurunkan tekanan darah dengan memproduksi NO dan berperan sebagai antioksidan. Namun, penelitian lebih lanjut (in-vitro dan in-vivo) perlu dilakukan untuk membuktikan mekanismenya

scholarly journals MOLECULAR DOCKING OF SELECTED BIOACTIVE COMPOUNDS FROM AZADIRACHTA INDICA FOR THE INHIBITION OF COVID19 PROTEASE

2020 ◽  
pp. 71-77
Author(s):  
S. FEBINA BERNICE SHARON
Keyword(s):  
Bioactive Compounds ◽  
Azadirachta Indica ◽  
Binding Energies ◽  
Global Public Health ◽  
Lipinski’S Rule ◽  
Novel Drug ◽  
Native Ligand ◽  
Autodock 4.2

Objective: COVID-19 caused by novel SARS-coronavirus 2 belonging to family Coronaviridae, is a global public health emergency infecting many people all around the world, especially in India with more than 2,98,000 cases. Hence there is a need for a novel drug that counters SARS-CoV2 is the prime requirement at this time. Methods: The present study aimed to assess bioactive compounds found in Azadirachta indica as a potential inhibitor of COVID-19 Mpr °(6Y2E, 6LU7, and 2GTB) by Autodock 4.2, with the Lamarckian Genetic Algorithm. COVID-19 Mpr ° was docked with thirteen bioactive compounds, and docking was analyzed by Autodock 4.2 and Pymol. Nelfinavir and Saquinavir were used as positive standards for comparison. Results: Azadirachtanin, Azadirachtol, and Salannolide, were left out because of the violation of Lipinski’s rule. The binding energies obtained from the docking of 6Y2E with a native ligand, Azadiradione, Beta-sitosterol, Epiazadiradione, Epoxyazadiradione, Kaempferol, Meldenin, Myricetin, Nimbaflavone, Nimbinene, Nimbione, Nimbocinolide, Quercitrin, Vepnin, Saquinavir, and Nelfinavir were-7.32,-6.63,-6.69,-7.52,-5.27,-4.54,-6.07,-4.19,-5.02,-5.58,-6.23,-4.71, -3.72,-6.4,-7.14 and-4.67 kcal/mol respectively. The binding energies obtained from the docking of 6LU7 with the native ligand, Azadiradione, Nimbione, Vepnin, and Saquinavir were-6.14,-6.48,-6.79 and-6.49 kcal/mol correspondingly. The binding energies obtained from the docking of 2GTB with the native ligand, Azadiradione, Epiazadiradione, Epoxyazadiradione, Kaempferol, Meldenin, Myricetin, Nimbaflavone, Nimbione, Nimbocinolide, Quercitrin, Vepnin, Saquinavir, and Nelfinavir were-6.96,-7.13,-6.69,-5.22,-6.44,-5.06,-5.93,-6.66,-5.3,-5.63,-7.11,-6.89 and-5.42kcal/mol, respectively. Conclusion: Azadiradione, Epiazadiradione, Nimbione, and Vepnin seemed to have the greatest potential to act as COVID-19 protease inhibitors. However, further research is necessary to explore their prospective medicinal use in vitro and in vivo conditions.

scholarly journals Design and In silico Studies of 2,5-Disubstituted 1,2,4-Triazole and 1,3,4-Thiadiazole Derivatives as Pteridine Reductase 1 Inhibitors

2021 ◽  
pp. 166-178
Author(s):  
Shraddha Phadke ◽  
Devender Pathak ◽  
Rakesh Somani
Keyword(s):  
In Silico ◽  
Therapeutic Potential ◽  
Structural Features ◽  
Lipinski’S Rule ◽  
Drug Mechanism ◽  
In Silico Studies ◽  
Lipinski’S Rule Of Five ◽  
Thiadiazole Derivatives

Aims: Design and in silico studies of 2,5-disubstituted triazole and thiadiazole derivatives as Pteridine Reductase 1 inhibitors. With a view to develop effective agents against Leishmaniasis, 2-substituted-5-[(1H-benzimidazol-2yl) methyl] azole derivatives (A1-A12) were designed against the target enzyme Pteridine reductase 1. Methodology: The series was designed by targeting Pteridine reductase 1 which is an enzyme responsible for folate and pterin metabolism. Based on thorough study of the enzyme structure and structural features of ligands required for optimum interaction with the enzyme, a series of 12 compounds consisting of 2,5-disubstituted 1,2,4-triazole and 1,3,4-thiadiazole derivatives was designed. In silico studies were carried out which included docking studies (using V Life software) to understand binding of the compounds with enzyme PTR1, ADMET studies, drug likeness studies for physicochemical properties and bioactivity studies to understand the possible mechanism of action of the compounds. These studies were undertaken using online softwares, molinspiration and admetSAR web servers. Results: Compounds A10 and A12 gave the best docking scores of -59.9765 and -60.4373 respectively that were close to dihydrobiopterin (original substrate). All the compounds complied with Lipinski’s rule of five. Most of the compounds displayed favorable ADMET properties. Conclusion: The 2,5-disubstituted 1,2,4-triazole and 1,3,4-thiadiazole derivatives exhibited good binding affinity for PTR1 enzyme (PDB code: 1E92). The docking scores indicated that enzyme binding may be governed by the nature and size of the substituents on the azole ring. The compounds display well-defined drug-like and pharmacokinetic properties based on Lipinski’s rule of five with additional physicochemical and ADMET parameters. Bioactivity studies suggested the possible drug mechanism as enzyme inhibition. Hence, this study provides evidence for consideration of valuable ligands in 2,5-disubstituted 1,2,4-triazole and 1,3,4-thiadiazole derivatives as potential pteridine reductase 1 inhibitor and further in vitro and in vivo investigations may prove its therapeutic potential.

scholarly journals ANALISIS GC-MS (GAS CHROMATOGRAPHY - MASS SPECTROMETRY) EKSTRAK METANOL DARI UMBI RUMPUT TEKI (Cyperus rotundus L.)

PHARMACON ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 849
Author(s):  
Ellen Hotmian ◽  
Elly Suoth ◽  
Fatimawali Fatimawali ◽  
Trina Tallei
Keyword(s):  
Mass Spectrometry ◽  
Gas Chromatography ◽  
Bioactive Compounds ◽  
Cyperus Rotundus ◽  
Gas Chromatography Mass Spectrometry ◽  
The Public ◽  
Chromatography Mass Spectrometry ◽  
Ms Analysis

ABSTRACTThe Nut Grass Tuber (Cyperus rotundus L.) is a plant that is believed by the public to cure several diseases. According to a study conducted in vivo and in vitro, the extract the tuber root has many potentials such as anticancer, anti-inflammatory, antibacterial, etc. This study aims to determine the polar bioactive compounds contained in the bulb tubers. The method used was the extraction of nut tuber dry powder using methanol as a solvent by maceration process and then analyzed using gas chromatography - mass spectrometry (GC-MS) to obtain information on the content of the tubers The results of GC-MS analysis from this study indicate that there are 177 possible components of the compound extracted using methanol. The results also showed that there were three possible polar bioactive compounds at the highest peak of the GC-MS analysis, namely 7-Isopropenyl-1,4a-dimethyl-4,4a, 5,6, 7,8-hexahydro-3H-naphthalen-2-one, 1 (2H) -Naphthalenone, 3,4,4a, 5,6,7-hexahydro-4a, 5-dimethyl-3- (1-methylethenyl) -, [3S- (3a, 4aa, 5a)] -, and 2 (1H) Naphthalenone, 3,5,6,7,8,8a-hexahydro-4,8a-dimethyl-6- (1-methylethenyl) -.Keywords         : Methanolic extract, nut grass tuber, Cyperus rotundus L., GC-MS   ABSTRAKUmbi Rumput Teki (Cyperus rotundus L.) merupakan tumbuhan yang dipercayai masyarakat dapat menyembuhkan beberapa penyakit. Menurut sebuah penelitian yang dilakukan secara in vivo maupun in vitro, kandungan ekstrak umbi rumput teki memiliki banyak potensi seperti antikanker, antiinflamasi, antibakteri, dll. Penelitian ini bertujuan untuk mengetahui senyawa-senyawa bioaktif polar yang terkandung pada umbi rumput teki. Metode yang digunakan yaitu ekstraksi serbuk kering umbi rumput teki menggunakan pelarut metanol dengan proses maserasi kemudian dianalisis menggunakan kromatografi gas – spektrometri massa (GC-MS) untuk mendapatkan informasi kandungan dalam umbi rumput teki. Hasil analisis GC-MS dari penelitian ini menunjukkan bahwa terdapat 177 kemungkinan komponen senyawa yang diekstraksi menggunakan pelarut methanol. Hasil penelitian juga menunjukkan bahwa terdapat tiga kemungkinan senyawa bioaktif polar pada puncak tertinggi hasil analisis GC-MS, yaitu 7-Isopropenyl-1,4a-dimethyl-4,4a,5,6,7,8-hexahydro-3H-naphthalen-2-one, 1(2H)-Naphthalenone, 3,4,4a,5,6,7-hexahydro-4a,5-dimethyl-3-(1-methylethenyl)-, [3S-(3a,4aa,5a)]-, dan 2(1H)Naphthalenone, 3,5,6,7,8,8a-hexahydro-4,8a-dimethyl-6-(1-methylethenyl)-. Kata kunci      : Ekstrak metanol, umbi rumput teki, Cyperus rotundus L., GC-MS

scholarly journals Chemical Profiling, Pharmacological Insights and In Silico Studies of Methanol Seed Extract of Sterculia foetida

Plants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1135
Author(s):  
Najmul Alam ◽  
Naureen Banu ◽  
Md. Arfin Ibn Aziz ◽  
Niloy Barua ◽  
Umme Ruman ◽  
...  
Keyword(s):  
In Silico ◽  
Brine Shrimp ◽  
Docking Study ◽  
Clot Lysis ◽  
Phytochemical Analysis ◽  
Molecular Docking Study ◽  
Ms Analysis ◽  
In Silico Studies

Sterculia foetida, also known as jangli badam in Bangladesh, is a traditionally used plant that has pharmacological activities. A qualitative phytochemical analysis was performed to assess the metabolites in a methanolic extract of S. foetida seeds (MESF), and the cytotoxic, thrombolytic, anti-arthritics, analgesic, and antipyretic activities were examined using in vitro, in vivo, and in silico experiments. Quantitative studies were performed through gas chromatography-mass spectroscopy (GC-MS) analysis. The brine shrimp lethality bioassays and clot lysis were performed to investigate the cytotoxic and thrombolytic activities, respectively. The anti-arthritics activity was assessed using the albumin denaturation assay. Analgesic activity was determined using the acetic acid-induced writhing test and the formalin-induced paw-licking test. A molecular docking study was performed, and an online tool was used to perform ADME/T (absorption, distribution, metabolism, and excretion/toxicity) and PASS (Prediction of Activity Spectra for Substances). GC-MS analysis identified 29 compounds in MESF, consisting primarily of phenols, terpenoids, esters, and other organic compounds. MESF showed moderate cytotoxic activity against brine shrimp and significant thrombolytic and anti-arthritics activities compared with the relative standards. The extract also showed a dose-dependent and significant analgesic and antipyretic activities. Docking studies showed that 1-azuleneethanol, acetate returned the best scores for the tested enzymes. These findings suggested that MESF represents a potent source of thrombolytic, anti-arthritic, analgesic, antipyretic agents with moderate cytotoxic effects.

Anti-thrombotic Effect of a PAI-1 Inhibitor in Rats Given Endotoxin

1996 ◽  
Vol 75 (01) ◽  
pp. 118-126 ◽  
Author(s):  
T Abrahamsson ◽  
V Nerme ◽  
M Strömqvist ◽  
B Åkerblom ◽  
A Legnehed ◽  
...  
Keyword(s):  
Plasminogen Activator Inhibitor ◽  
Rat Plasma ◽  
Clot Lysis ◽  
Fibrin Deposition ◽  
Plasminogen Activator Inhibitor 1 ◽  
Fab Fragment ◽  
Dose Dependent Decrease ◽  
Pai 1

SummaryThe aim of this study was to investigate the anti-thrombotic effects of an inhibitor of the plasminogen activator inhibitor-1 (PAI-1) in rats given endotoxin. In studies in vitro, PRAP-1, a Fab-fragment of a polyclonal antibody against human PAI-1, was shown to inhibit PAI-1 activity in rat plasma as well as to stimulate clot-lysis of the euglobulin fraction derived from rat plasma. Endotoxin administered to anaesthetised rats produced a marked increase in plasma PAI-1 activity. To study fibrin formation and lysis in vivo after intravenous (i. v.) injection of the coagulant enzyme batroxobin, 125I-fibrinogen was administered to the animals. The thrombi formed by batroxobin were rapidly lysed in control animals, while the rate of lysis was markedly attenuated in rats given endotoxin. PRAP-1 was administered i.v. (bolus + infusion) to rats given endotoxin and batroxobin and the PAI-1 inhibitor caused a dose-dependent decrease in the 125I-fibrin deposition in the lungs. An immunohistochemical technique was used to confirm this decrease in density of fibrin clots in the tissue. Furthermore, PRAP-1 decreased plasma PAI-1 activity in the rats and this reduction was correlated to the decrease in lung 125I-fibrin deposition at the corresponding time point. It is concluded that in this experimental model the PAI-1 antibody PRAP-1 may indeed inhibit thrombosis in animals exposed to endotoxin.

The Roles of α2-Antiplasmin and Plasminogen Activator Inhibitor 1 (PAI-1) in the Inhibition of Clot Lysis

1993 ◽  
Vol 70 (02) ◽  
pp. 301-306 ◽  
Author(s):  
Linda A Robbie ◽  
Nuala A Booth ◽  
Alison M Croll ◽  
Bruce Bennett
Keyword(s):  
Plasminogen Activator ◽  
Plasminogen Activator Inhibitor ◽  
Fibrin Clot ◽  
Clot Lysis ◽  
Plasminogen Activator Inhibitor 1 ◽  
Dependent Inhibition ◽  
Activator Inhibitor ◽  
Pai 1

SummaryThe relative importance of the two major inhibitors of fibrinolysis, α2-antiplasmin (α2-AP) and plasminogen activator inhibitor (PAI-1), were investigated using a simple microtitre plate system to study fibrin clot lysis in vitro. Cross-linked fibrin clots contained plasminogen and tissue plasminogen activator (t-PA) at concentrations close to physiological. Purified α2-AP and PAI-1 caused dose-dependent inhibition. All the inhibition due to normal plasma, either platelet-rich or poor, was neutralised only by antibodies to α2-AP. Isolated platelets, at a final concentration similar to that in blood, 2.5 × 108/ml, markedly inhibited clot lysis. This inhibition was neutralised only by antibodies to PAI-1. At the normal circulating ratio of plasma to platelets, α2-AP was the dominant inhibitor. When the platelet:plasma ratio was raised some 20-fold, platelet PAI-1 provided a significant contribution. High local concentrations of PAI-1 do occur in thrombi in vivo, indicating a role for PAI-1, complementary to that of α2-AP, in such situations.

Effects of Ellagic Acid upon the Rabbit Fibrinolytic System

1972 ◽  
Vol 27 (01) ◽  
pp. 063-071
Author(s):  
S. G Iatridis ◽  
P. G Iatridis
Keyword(s):  
Continuous Infusion ◽  
Ellagic Acid ◽  
Animal Experimentation ◽  
Inhibitory Effect ◽  
In Vivo Studies ◽  
Clot Lysis ◽  
Hageman Factor ◽  
Lysis Activity ◽  
Site Of Action

SummaryThe present investigation deals with in vivo studies of possible relations of active Hageman factor (HFa) to the problems of thrombolysis. The study is based upon animal experimentation in which 40 normal, 5 dicumarolized and 5 heparinized rabbits each received ellagic acid (Elac 10-2 M) by intravenous continuous infusion at a rate of 1 ml/min for a period of 25 min. The data suggest that the Elac infusion induced in vivo activation of HF. Streptokinase (SK) injection 25 min from the start of Elac i. v. infusion failed to induce clot lysis in blood drawn one min after its injection. The phenomenon was more prominent with low (SK 250 U or 500 U) concentrations of SK. With higher concentrations, SK-induced clot lysis activity was not affected by Elac infusion.In dicumarolized and heparinized rabbits Elac infusion still counteracted the fibrinolysis activating effect of low concentration of SK. The possibility that the above described phenomenon was due to either hypercoagulability or to a non-specific inhibitory effect of Elac upon SK was explored and excluded.It is concluded that HFa and SK have the same site of action. Thus it seems that HFa may block the precursor upon which SK acts by forming a complex with it. It is stressed that activation of this precursor by HFa requires a suitable surface.

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