Investigation of Potential Antioxidant, Thrombolytic and Neuropharmacological Activities of Homalomena aromatica Leaves Using Experimental and In Silico Approaches

The leaves of Homalomena aromatica are traditionally used in Bangladesh for the treatment of different chronic ailments. The purpose of this study was to explore in vitro antioxidant, thrombolytic activities, and in vivo neuropharmacological effects of methanolic extract of Homalomena aromatica (MEHA) leaves. Antioxidant activity of MEHA was assessed by a DPPH free radical scavenging assay and total phenolics content, total flavonoids content were also measured. The thrombolytic activity was determined by percentage of clot lysis and neuropharmacological activities by hole board, tail suspension, forced swimming and elevated plus maze tests. The results showed that the IC50 value of the extract against DPPH was 199.51 μg/mL. Quantitative analysis displayed higher contents of phenolics and flavonoids (147.71 mg gallic acid equivalent/g & 66.65 mg quercetin equivalent/g dried extract, respectively). The extract also showed a significant clot lysis (33.31%) activity. In case of anxiolytic activity, the elevate plus maze (EPM) test demonstrated an increase in time spent in open arms, and in case of hole board test, the number of head dipping was also significantly increased (p < 0.05). All the test compared with control (1% Tween in water) and standard (diazepam 1 mg/kg), significant dose (200 & 400 mg/kg) dependent anxiolytic activity was found. In antidepressant activity, there was a significant decrease in period of immobility in both test models (tail suspension and forced swimming) (p < 0.05). Moreover, 13 compounds were identified as bioactive, showed good binding affinities to xanthine oxidoreductase, tissue plasminogen activator receptor, potassium channel receptor, human serotonin receptor targets in molecular docking experiments. Furthermore, ADME/T analysis revealed their drug-likeness, likely pharmacological actions and non-toxic upon consumption. Taken together, our finding support the traditional medicinal use of this plant, which may provide a potential source for future drug discovery.

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In vitro and in vivo evaluation of pharmacological potentials of Campsis radicans L

Clinical Phytoscience ◽

10.1186/s40816-019-0144-9 ◽

2019 ◽

Vol 5 (1) ◽

Cited By ~ 5

Author(s):

Mirazul Islam ◽

Tabassum Jannat ◽

Md. Ruhul Kuddus ◽

Mohammad Abdur Rashid ◽

Mohammad Rashedul Haque

Keyword(s):

Castor Oil ◽

Methanol Extract ◽

Radical Scavenging ◽

Free Radical Scavenging ◽

Clot Lysis ◽

Thrombolytic Activity ◽

Tail Immersion ◽

Soluble Fractions

Abstract Background Campsis radicans L. is a flowering plant in Bangladesh, traditionally used for the treatment of several human diseases. In this study, in vitro antioxidant, thrombolytic, membrane stabilizing and in vivo analgesic, hypoglycemic, anti-diarrheal and CNS antidepressant activities of organic soluble fractions of crude methanol extract of C. radicans leaf were investigated using appropriate experimental models. Methods The leaves of C. radicans were collected, authenticated, dried and extracted with methanol at room temperature for 30 days. The concentrated methanol extract was partitioned to petroleum-ether (PESF), dichloromethane (DMSF) and ethyl acetate (EASF) soluble fractions. The antioxidant activity of these fractions was determined by DPPH free radical scavenging method. Total phenolic content was determined by the Folin-Ciocalteau’s spectrophotometric method. The thrombolytic activity was assessed by measuring clot lysis ability whereas the membrane stabilizing activity was evaluated by heat- and hypotonic solution-induced hemolysis assay. Tail immersion procedure and acetic acid- induced writhing model were used to measure the analgesic activity of C. radicans. The hypoglycemic, anti-diarrheal and CNS antidepressant activities were determined by oral glucose tolerance test, castor oil-induced diarrheal model and thiopental-sodium induced sleeping time test in mice, respectively. Results All the organic soluble fractions of C. radicans contained phenolic compounds varying from 6.38 to 60.13 mg of GAE/gm of extractive, while in DPPH assay, EASF showed the highest free radical scavenging activity with IC50 is 4.69 μg/ml. The PESF exhibited highest thrombolytic activity (57.14% clot lysis) and the DMSF showed maximum 53.95% inhibition of heat-induced hemolysis of human RBCs. In both tail immersion and acetic acid induced writhing models, the PESF, DMSF, EASF at the doses of 200 and 400 mg/kg body weight, induced a significant (P < 0.001) decrease in the painful sensation in mice. Substantial (P < 0.05) anti-hyperglycemic activity of test samples was found in mice loaded with glucose at the same doses mentioned earlier. Castor oil induced diarrheal test of the plant extractives has shown significant effect in comparison to control group. In CNS antidepressant activity assay, the test samples were able to reduce the duration of sleep in mice caused by thiopental administration. Conclusion All these findings revealed that C. radicans possess significant antioxidant, thrombolytic, membrane stabilizing, analgesic, hypoglycemic, anti-diarrheal and CNS antidepressant activities.

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

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-020-00099-x ◽

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.

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SYNTHESIS OF BENTONITE NANOCLAY AND INCORPORATION OF CASSIA FISTULA LEAF EXTRACT TO FORM ORGANOBENTONITE: CHARACTERIZATION AND ITS BIOMEDICAL APPLICATIONS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i9.26717 ◽

2018 ◽

Vol 11 (9) ◽

pp. 381

Author(s):

Anand Raj Lfa ◽

Jeslin J

Keyword(s):

Biomedical Applications ◽

Leaf Extract ◽

Spherical Shape ◽

Xrd Analysis ◽

Antioxidant Property ◽

Clot Lysis ◽

Cassia Fistula ◽

Thrombolytic Activity ◽

Lysis Activity

Objective: In this work, methanolic leaf extract from Cassia fistula (known as aragvadha) was incorporated into bentonite nanoclay to form organobentonite. This organobentonite of nanosize was further used for its effective biomedical applications since medicinal clay finds its own advantage over decades.Methods: The bentonite nanoclay was produced by energetic stirring followed by centrifugation and was characterized using scanning electron microscopy (SEM), X-ray diffraction (XRD), and Fourier transform infrared (FTIR). The organobentonite was produced using freeze and thaw method. Antioxidant property was studied using Molyneux method, and thrombolytic activity was analyzed using in vitro clot lysis method.Results: The nanosize of bentonite nanoclay between 57 and 82 nm with irregular to spherical shape was confirmed using SEM analysis. The sharp diffraction peak in XRD analysis shows the crystalline nature of bentonite nanoclay, and FTIR results revealed the successful incorporation of the methanolic extract within the bentonite nanoclay. The organobentonite exhibits 84.5% antioxidant property as well as 31% clot lysis activity when compared to the extract and the bentonite nanoclay.Conclusion: Thus, the non-toxic and inexpensive bentonite nanoclay have a high aspect ratio with multifarious applications in medicine, food, cosmetics, and health products. Through this study, the bentonite nanoclay modified using plant alkaloid (organobentonite) is found to possess good biomedical property.

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In vitro Antioxidant, Membrane Stabilizing and Thrombolytic Activities of Glycosmis arborea

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v15i2.12579 ◽

2012 ◽

Vol 15 (2) ◽

pp. 141-143 ◽

Cited By ~ 1

Author(s):

Sayed Mamur Hossain ◽

Farhana Islam ◽

Tasnuva Sharmin ◽

Hasib Sheikh ◽

AM Rashedul Hasan ◽

...

Keyword(s):

Carbon Tetrachloride ◽

Methanol Extract ◽

Soluble Fraction ◽

Pharmaceutical Journal ◽

Clot Lysis ◽

Hypotonic Solution ◽

Rat Erythrocytes ◽

Thrombolytic Activity ◽

Negative Controls

The methanol extract of leaves and stems of Glycosmis arborea and their pet-ether, carbon tetrachloride, chloroform and aqueous soluble partitionates were subjected to assays for antioxidant activity by Folin-Ciocalteau reagent, membrane stabilizing and thrombolytic activities. The carbon tetrachloride soluble fraction of stems of G. arborea demonstrated the presence of significant amount of phenolic compounds (36.95 ± 0.54 mg of GAE/g of extract). The extractives inhibited heat as well as hypotonic solution-induced haemolysis of rat erythrocytes in vitro. The pet-ether soluble fraction of leaves and stems of G. arborea showed 20.46 and 38.24% and 22.50 and 48.25%. inhibition of hemolysis of RBC caused by heat and hypotonic solution, as compared to 30.55 and 72.91% inhibition of hemolysis of RBC caused by the standard Acetyl salicylic acid at 0.01 mg/ml concentration, respectively. Among the four fractions, the chloroform soluble materials of the stems of G. arborea revealed highest thrombolytic activity with clot lysis value of 36.50% while standard streptokinase and water used as positive and negative controls, showed 64.25±0.26 and 2.35±0.35 % lysis of clot respectively DOI: http://dx.doi.org/10.3329/bpj.v15i2.12579 Bangladesh Pharmaceutical Journal 15(2): 141-143, 2012

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Biological Activities of In-House Developed Haloxylon griffithii Plant Extract Formulations

Plants ◽

10.3390/plants10071427 ◽

2021 ◽

Vol 10 (7) ◽

pp. 1427

Author(s):

Shagufta Kamal ◽

Ismat Bibi ◽

Kanwal Rehman ◽

Ameer Fawad Zahoor ◽

Amna Kamal ◽

...

Keyword(s):

Gallic Acid ◽

High Performance ◽

Therapeutic Potential ◽

Biological Activities ◽

Radical Scavenging ◽

Viable Cell ◽

Clot Lysis ◽

Haemolytic Activity ◽

Thrombolytic Activity ◽

Microbial Species

The therapeutic potential of whitish glaucous sub-shrub Haloxylon griffithii (H. griffithii), abundantly present in southern regions of South Asia, has been neglected. The current study aimed to assess the phytochemicals and pharmacological potential of native and gemm forms of H. griffithii. Results of antimicrobial activity revealed that all tested bacteria were susceptible at concentrations ≤50 µg/mL, while tested fungal species were susceptible at ≤25 µg/mL. The values of minimum bactericidal concentrations (MBCs) ranged between 10.75 ± 0.20 to 44.25 ± 0.42 µg/mL, 8.25 ± 0.02 to 28.20 ± 0.80 µg/mL. The value of minimum inhibitory concentration (MIC) of all microbial species was ≤100 µg/mL and the antibiotic mechanism showed that both extracts were highly bactericidal and fungicidal. Results of average log reduction of viable cell count in time kill assay indicated that Pseudomonas aeruginosa (P. aeruginosa) NCTC 1662, Candida albicans (C. albicans) IBL-01, Candidakrusei (C. krusei) ATCC 6258, and Aspergillus flavus (A. flavus) QC 6158 were the most susceptible microbial species. High performance liquid chromatography (HPLC)-based quantification confirmed the presence of gallic acid p.coumeric acid catechin, vanillin, ellagic acid, and salicylic acid, while in native extract only gallic acid. Native and gemm extracts exhibited excellent radical scavenging potential measured by 1,1-diphenyl-2-picryl-hydrazyl radical scavenging assay. Significant thrombolytic activity was found in both extracts with negligible haemolytic activity. Highest percent (%) clot lysis was observed with gemm extracts (87.9 ± 0.85% clot lysis). In summary, we infer that valuable evidence congregated can be exploited for better understanding of gemm H. griffithii’s health benefits, further, to increase its utility with enriching dietary sources of health-promoting compounds.

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Phytochemical and Pharmacological Potential of Enhydra fluctuans Available in Bangladesh

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2019/v29i430243 ◽

2019 ◽

pp. 1-11

Author(s):

S. Kamal ◽

S. R. Rony ◽

S. Sharmin ◽

F. R. Laboni ◽

M. H. Sohrab

Keyword(s):

Cytotoxic Activity ◽

Radical Scavenging ◽

Diffusion Method ◽

Clot Lysis ◽

Cytotoxic Activities ◽

Hypotonic Solution ◽

Chemical Screening ◽

Soluble Fractions

Objectives: The possible phytochemical constituents, thrombolytic and membrane stabilizing activities of the crude ethanolic extract of Enhydra fluctuans (CE) were investigated along with the antimicrobial, antioxidant and cytotoxic potentials of its petroleum ether (PESF), carbon tetrachloride (CTCSF), chloroform (CSF) and aqueous (AQSF) soluble fractions. Materials & Methods: The coarse leaf powder was extracted at room temperature with ethanol. Solvent-solvent partitioning was done to obtain the four soluble fractions. Anticoagulant potential was determined by the in vitro thrombolytic model, membrane stabilization method was used to assess in vitro anti-inflammatory activity, the disc diffusion method was used for anti-microbial screening, antioxidant potential was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and brine shrimp lethality bioassay method was used for cytotoxic activity determination. Results: Chemical screening of the crude extract evidenced the presence of alkaloids, saponins, tannins, flavonoids, reducing sugars and gums. It showed significant clot lysis property of 46.91%. It also significantly inhibited heat and hypotonic solution induced lysis of the human red blood cell membrane with values of 71.80% and 47.60%, respectively. CTCSF and PESF showed mild antimicrobial activity. AQSF showed most prominent antioxidant activity with IC50 value of 12.27 µg/mL. CTCSF showed LC50 value of 0.84 µg/mL, with most potent cytotoxic activity. Conclusion: Significant thrombolytic, membrane stabilizing, antioxidant and in vitro cytotoxic activities of the ethanolic plant extract were observed in this study. In vivo activities and isolation of active compound(s) from this extract are yet to be investigated.

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Effect of Standard Heparin and a Low Molecular Weight Heparin on Thrombolytic and Fibrinolytic Activity of Single-Chain Urokinase Plasminogen Activator In Vitro

Thrombosis and Haemostasis ◽

10.1055/s-0038-1651029 ◽

1989 ◽

Vol 62 (03) ◽

pp. 923-926 ◽

Cited By ~ 9

Author(s):

D M Lourenço ◽

A M Dosne ◽

A Kher ◽

M Samama

Keyword(s):

Molecular Weight ◽

Low Molecular Weight Heparin ◽

Clot Lysis ◽

Low Molecular Weight ◽

Single Chain ◽

Plasma Clot ◽

Thrombolytic Activity ◽

Significant Difference ◽

Plasma Factor

SummaryThe effect of unfractioned heparin (UH) and low molecular weight heparin (LMWH) (Kabi 2165 - Fragmin®) on in vitro scu-PA thrombolytic and fibrinogenolytic activity was investigated. Thrombolytic activity was evaluated by following lysis of radiolabeled plasma clot immersed in plasma in presence of scu-PA alone or with either form of heparin. A 200 IU/ml scu-PA concentration produced clot lysis within 7 hr. UH or LMWH led to a slightly faster clot lysis which was statistically significant only at the 2nd and 3rd hour. No significant difference could be evidenced between UH and LMWH effect. During clot lysis, plasmin, generated within the clot led to a gradual transformation of scu-PA to tcu-PA, specially after a 4-hr incubation. Appearance of tcu-PA activity in the plasma surrounding the clot was significantly inhibited by either form of heparin. This finding contrasts with results observed in purified systems and suggests the presence of heparin-dependent plasma factor(s) inhibiting tcu-PA formation or its activity. Possible candidates might be anti-thrombin III and PAI-3.No fibrinogen breakdown was observed when plasma was incubated for 7 hr at 37° C in presence of scu-PA alone (200 IU/ ml) or with either form of heparin. However, in presence of a plasma clot, an important fibrinogen breakdown was observed during clot lysis reflecting the action of plasmin and/or tcu-PA generated within the clot, in the surrounding plasma. Fibrinogenolysis was less pronounced in the presence of both heparin preparations possibly as a consequence of the reduction in the tcu-PA level. These results underline the importance of plasma factors in the interaction of heparin with plasminogen activators such as scu-PA.

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Thrombolytic Activity of Methanolic Extracts of Desmodium paniculatum (L.) and Sarcochlamys pulcherrima (Roxb.)

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v17i1.22318 ◽

2015 ◽

Vol 17 (1) ◽

pp. 67-69 ◽

Cited By ~ 1

Author(s):

Mohammed Aktar Sayeed ◽

Humayun Kabir ◽

Mohammad Mamun Ur Rashid ◽

Md Farid Ahamad Bhuiyan ◽

Mohammad A Rashid

Keyword(s):

Pharmaceutical Journal ◽

Positive Control ◽

Negative Control ◽

Clot Lysis ◽

Herbal Extracts ◽

Thrombolytic Activity ◽

Methanolic Extracts ◽

Desmodium Paniculatum

An in vitro thrombolytic model was used to check the clot lysis effect of two herbal extracts viz., Desmodium paniculatum (L.) and Sarchochlamys pulcherrima (Roxb.) by using Streptokinase as positive control and water as negative control. D. paniculatum and S. pulcherrima showed 31.92 ± 8.09% and 36.12 ± 6.81% clot lysis, respectively. From our study we found that D. paniculatum and S. pulcherrima showed significant % of clot lysis effect with reference to Streptokinase (72.54 ± 6.03%). and water (3.48 ± 0.84%). DOI: http://dx.doi.org/10.3329/bpj.v17i1.22318 Bangladesh Pharmaceutical Journal 17(1): 67-69, 2014

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Deciphering the Pharmacological Properties of Methanol Extract of Psychotria calocarpa Leaves by In Vivo, In Vitro and In Silico Approaches

Pharmaceuticals ◽

10.3390/ph13080183 ◽

2020 ◽

Vol 13 (8) ◽

pp. 183 ◽

Cited By ~ 3

Author(s):

Tahmina Akter Bristy ◽

Niloy Barua ◽

Abu Montakim Tareq ◽

Shahenur Alam Sakib ◽

Saida Tasnim Etu ◽

...

Keyword(s):

Antioxidant Activity ◽

In Silico ◽

Methanol Extract ◽

Radical Scavenging ◽

Clot Lysis ◽

Total Phenol Content ◽

Molecular Docking Study ◽

Lysis Activity ◽

Dose Dependent

The present study explores the neuropharmacological, antinociceptive, antidiarrheal, antioxidant, thrombolytic and cytotoxic activity of methanol extract of Psychotria calocarpa leaves (MEPC). In anxiolytic activity testing of MEPC by elevated plus maze test, hole–board test and light–dark test, the extract exhibited a dose-dependent reduction of anxiety while the open field test observed a decreased locomotion. The administration of MEPC revealed a significant dose-dependent reduction of depressant behavior in forced swimming and tail suspension test. Additionally, the antinociceptive and antidiarrheal activity exposed a significant reduction of nociception and diarrheal behavior at the highest dose. In addition, a strong antioxidant activity was observed in DPPH-free radical-scavenging assay (IC50 = 461.05 μg/mL), total phenol content (118.31 ± 1.12 mg) and total flavonoid content (100.85 ± 0.97 mg). The significant clot–lysis activity was also observed with moderate toxicity (LC50 = 247.92 μg/mL) level in the lethality assay of brine shrimp. Moreover, in silico molecular docking study showed that the compound Psychotriasine could offer promising active site interactions for binding proteins. Furthermore, ADME/T and toxicological properties of the compound satisfied the Lipinski’s rule of five and Veber rules for drug-like potential and toxicity level. Overall, MEPC had a potential neuropharmacological, antinociceptive, antidiarrheal and antioxidant activity that warranted further investigation.

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In silico and antithrombotic studies of 1,3,4-oxadiazoles derived from benzimidazole

Bangladesh Journal of Pharmacology ◽

10.3329/bjp.v11i1.23981 ◽

2015 ◽

Vol 11 (1) ◽

pp. 67 ◽

Cited By ~ 2

Author(s):

B. Vishwanathan ◽

B. M. Gurupadayya ◽

K. Venkata Sairam

Keyword(s):

In Silico ◽

Factor Xa ◽

Docking Studies ◽

Negative Control ◽

Clot Lysis ◽

Drug Candidate ◽

Thrombolytic Activity ◽

Reference Drug ◽

Oxadiazole Derivatives

In the present study, a series of 1,3,4-oxadiazole derivatives (4a-4k) derived from benzimidazole were docked onto factor Xa (PDB: 1NFY) protein using SYBYLX 2.1. and also evaluated for in vitro clot lysis for thrombolytic activity. The synthesized molecules were also screened for in silico ADME studies. The molecular docking studies highlighted that the molecules showed high affinity towards 1NFY with higher docking score and the in silico ADME results were promising and indicated that the molecules holds great potential as a drug candidate. The thrombolytic evaluation was performed for decrease in solid clot weight by the clot lysis study at a concentration of 6.25, 12.5 and 25 µM strengths, respectively. The results of in vitro clot lysis for thrombolytic evaluation revealed that the tested compounds 4a-4k exhibited significant clot lysis with respect to negative control phosphate buffered saline and in comparison to the reference drug streptokinase (30,000 IU). Among all the tested compounds, compound 4j, 4d and 4g exhibited potent thrombolytic activity with EC50 value of 16.2, 18.1 and 23.7 µM, respectively. The thrombolytic efficacy investigation highlights that the synthesized compound 4j could be considered for further clinical studies to ascertain its possible hit as thrombolytic agents.

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