scholarly journals In Vivo antiplatelet activity aggregation assay of bromelain fractionate by ethanol from extract pineapple core (Ananas comosus[l.] merr.)

Author(s):  
F F Musfiroh ◽  
S Setiasih ◽  
S Handayani ◽  
S Hudiyono ◽  
N M Ilyas
Author(s):  
Mihir K Patel ◽  
Kiranj K. Chaudagar ◽  
Anita A. Mehta

Objective: Although recent advances in the treatment of congestive heart disease, mortality among patients’ remains a questionable remark. Therefore, we evaluated the role of capsaicin on in vitro and ex vivo platelet aggregation induced by Adenosine Di-Phosphate (ADP) as well as in in vivo thrombosis models and role of NO, KATP was also identified in the capsaicin-induced anti-platelet animal model as well as in vivo model of arterial thrombosis.Methods: According to body weight wistar rats were divided into five groups. Group I and Group II was treated with saline and capsaicin (3 mg/kg, i. v), while animals from Group III were treated with N(ω)-nitro-L-arginine methyl ester (L-NAME) (30 mg/kg, i. v) 30 min before administration of capsaicin (3 mg/kg, i. v). Group IV animals were treated with glibenclamide (10 mg/kg,i. v) 30 min before administration of capsaicin (3 mg/kg, i. v). Group V was considered as a positive control and administered clopidogrel (30 mg/kg, p. o). Animals were subjected for in vitro, ex-vivo platelet aggregation assay. ADP (30µM) was utilized as an aggregating agent in these experiments. After these assays; animals of each group were subjected for subaqueous tail bleeding time in a rat model and FeCl3-induced arterial thrombosis model in rats.Results: In ADP-induced in vitro platelet aggregation, a significant reduction in % platelet aggregation was observed at 50µM (64.35±4.641) and 100µM (52.72±4.192) concentration of capsaicin as compared to vehicle control (85.82±3.716). Capsaicin (3 mg/kg, i. v) also showed a significant reduction (49.53±4.075) in ex-vivo ADP-induced platelet aggregation as compared to vehicle control (89.38±2.057). In FeCl3 induced arterial thrombosis model, Capsaicin (3 mg/kg, i. v) exhibited an increase in time to occlusion in this rodent model and presence of the L-NAME and glibenclamide had inhibited the activity of capsaicin.Conclusion: In our study, capsaicin (50 µM, 100µM) exhibited potent anti-platelet activity in ADP-induced platelet aggregation, similarly capsaicin exhibited significant anti-platelet action in the ex-vivo study. Moreover, the presence of L-NAME and glibenclamide inhibited the anti-thrombotic and anti-platelet action of capsaicin. Therefore, it was concluded that NO and KATP may be involved in the anti-thrombotic action of capsaicin.


2019 ◽  
Vol 3 (7) ◽  
pp. 240-245
Author(s):  
Jude Okokon ◽  
◽  
Kenneth Opara ◽  
John Udobang ◽  
Hemant Bankehde ◽  
...  
Keyword(s):  

2014 ◽  
Vol 9 (1) ◽  
pp. 1934578X1400900
Author(s):  
Chia-Lin Lee ◽  
Ming-Hon Yen ◽  
Fang-Rong Chang ◽  
Chin-Chung Wu ◽  
Yang-Chang Wu

Three phenanthrenes (1–3), four indole alkaloids (4–7) and one steroid (8) were isolated from the leaves of Calanthe arisanensis for the first time. In the antiplatelet aggregation assay, phenanthrenes 1 and 2 showed potential antiplatelet activity. We have reported and discussed here the antiplatelet aggregation properties of the eleven naturally-occurring phenanthrenes (1–2 and 9–17) isolated from the underground part of the plant and eighteen chemically synthesized phenanthrenes (18–35). Overall, our data demonstrated that 1,4-phenanthrenequinones 20, 21 and 22 (collagen, IC50 0.2, 0.2, 0.1 μg/mL; thrombin, IC50 0.8, 1.0, 1.1 μg/mL, respectively) could be promising lead candidates for further cardiovascular disease studies.


2000 ◽  
Vol 349 (1) ◽  
pp. 159-167 ◽  
Author(s):  
Yutaka SHIMOYAMA ◽  
Gozoh TSUJIMOTO ◽  
Masaki KITAJIMA ◽  
Michiya NATORI

We identified three novel human type-II classic cadherins, cadherin-7, -9 and -10, by cDNA cloning and sequencing, and confirmed that they interact with catenins and function in cell-cell adhesion as do other classic cadherins. Cell-cell binding activities of the eight human type-II classic cadherins, including the three new molecules, were evaluated by long-term cell-aggregation experiments using mouse L fibroblast clones transfected with the individual cadherins. The experiments indicated that all the type-II cadherins appeared to possess similar binding strength, which was virtually equivalent to that of E-cadherin. We next examined the binding specificities of the type-II cadherins using the mixed cell-aggregation assay. Although all of the type-II cadherins exhibited binding specificities distinct from that of E-cadherin, heterophilic interactions ranging from incomplete to complete were frequently observed among them. The combinations of cadherin-6 and -9, cadherin-7 and -14, cadherin-8 and -11, and cadherin-9 and -10 interacted in a complete manner, and in particular cadherin-7 and -14, and cadherin-8 and -11 showed an indistinguishable binding specificity against other cadherin subclasses, at least in this assay system. Although these data were obtained from an in vitro study, they should be useful for understanding cadherin-mediated mechanisms of development, morphogenesis and cell-cell interactions in vivo.


2020 ◽  
Vol 11 (3) ◽  
pp. 4760-4766
Author(s):  
Hartati R ◽  
Suarantika F ◽  
Fidrianny I

Ananas comosus L. Merr, known as pineapple, belongs to the Bromeliaceae family. This plant has been used as traditional medicine and continues until now in conventional herbal medicine. The pineapple was distributed in some countries such as China, India, Indonesia, Malaysia, Thailand and originated from South America. This article delved the scientific work about Ananas comosus focussing their usage as traditional medicine, chemical compounds and biological activities. All of the pieces of information were obtained from the scientific literature such as Science Direct, Google Scholar, Scopus and PubMed. Based on the literature survey,different parts of pineapple (Ananas comosus) are used in traditional medicine, used asan anti-inflammatory agent,anti-oedema, digestive disorder, antimicrobial, vermicide, and purgative. Phytochemical compounds from A. comosus have been provided, including ascorbic acid, quercetin, flavones-3-ol, flavones, and ferulic acid. The crude extracts of A. comosus have many pharmacological activities such as anti-fungal, anti-inflammatory, antioxidant, antibacterial. This discovery becomes possible due to scientific isolation and in vivo or in vitro analysis of A.comosus.


2021 ◽  
Vol 9 (3) ◽  
pp. 222-234
Author(s):  
A. K. Brel ◽  
N. V. Atapina ◽  
Yu. N. Budaeva ◽  
S. V. Lisina ◽  
S. S. Tsaruk ◽  
...  

A high prevalence of thrombotic disorders, insufficient effectiveness or safety of antithrombotic therapy is an urgent problem of modern healthcare. The main means of preventing thrombosis is acetylsalicylic acid. Despite its long history, aspirin attracts researchers in the fields of medicinal chemistry, biology, and medicine. The development of new antiplatelet agents, including chemical modification of the acetylsalicylic acid molecule, remains relevant. Modification of the acetylsalicylic acid molecule using amino acids and obtaining their salt forms makes it possible to maintain antiplatelet or antithrombotic properties, as well as to impart additional pharmacodynamic effects. In modern science, a lot of attention is paid to the sulfur-containing amino acid taurine. An analysis of modern scientific literature revealed the protective effect of taurine in diabetes mellitus and cardiovascular diseases, liver dysfunction, gastrointestinal tract, and kidney diseases.The aim of the article is to study synthesis of new compounds, determination of their physical characteristics and assessment of their antiplatelet and antithrombotic activities in vitro and in vivo.Materials and methods. To confirm the structure of the synthesized new derivatives of hydroxybenzoic acids with a taurine fragment by the acelation method, thin layer chromatography and NMR spectra were used. In vitro studies were carried out on the model of ADP-induced platelet aggregation according to the Born G. methods modified by V.A. Gabbasov. In vivo, the studies were carried out on the model of arterial thrombosis induced by the application of iron chloride in the following groups of animals: intact, with experimental diabetes mellitus and three-year-olds; the rate of bleeding from the tail vein was also evaluated.Results. New compounds – derivatives of ortho-, meta- and para-hydroxybenzoic acids with a taurine residue – were synthesized. A procedure for the preparation of N-hydroxybenzoyl taurine compounds and their salt forms have been described; their spectral characteristics and melting points have been determined. The synthesized compounds are superior to acetylsalicylic acid in solubility and are not inferior to it in antiplatelet and antithrombotic activities. The results of the in vitro antiplatelet activity assessment in a wide concentration range from 10-4M to 10-8M, are presented. It has been revealed that the dipotassium salt of N-(2-hydroxybenzoyl)taurine exhibits a less antiplatelet activity than the dipotassium salt of N-(3-hydroxybenzoyl)taurine. The most pronounced antiplatelet activity is exhibited by the compound N-(4-hydroxybenzoyl)taurine. In in vivo experiments on the model of arterial thrombosis in 3-year-olds or animals with experimental diabetes mellitus, carotid artery thrombosis occurred faster than in young or intact animals. A single preliminary oral administration of the test compounds prolonged the time of the thrombus formation, which makes it possible to conclude that they have an antithrombotic effect. In this study, the dipotassium salt of N-(3-hydroxybenzoyl)taurine exhibits a more pronounced activity than that of acetylsalicylic acid.Conclusion. Against the background of the modeled pathologies, the studied drugs showed the expected antithrombotic activity, in terms of the severity not inferior to that found in acetylsalicylic acid.


2012 ◽  
Vol 87 (2) ◽  
pp. 174-179 ◽  
Author(s):  
M. Ahmed ◽  
M.D. Laing ◽  
I.V. Nsahlai

AbstractEthanol extracts of 25 plant species were screened for anthelmintic effects against Haemonchus contortus. Ethanol extracts of each plant were used at various concentrations (10, 20 and 30%) to treat 10-day faecal cultures, incubated at 27°C with control cultures which were treated with ethanol for 48 h. Five plants with high efficacies (Ananas comosus, Aloe ferox, Allium sativum, Lespedeza cuneata and Warburgia salutaris) were selected from the first screening for further investigation using ethanol, dichloromethane and water extracts at four concentrations (2.5, 5, 10 and 20%). Ethanol was the most effective solvent. Larval counts decreased with increasing extract concentrations, of which 10 and 20% had similar effects. Lespedeza cuneata caused more than 70% mortality at all concentrations. However, there remains a need to assess in vivo efficacy of these plants.


2019 ◽  
Vol 18 (3) ◽  
pp. 574-576
Author(s):  
VV Bykov ◽  
V Yu Serebrov ◽  
VV Udut ◽  
EV Udut ◽  
VP Fisenko

Objective. Specific activity of an antiplatelet drug of indolinone series (codenamed DI) was studied in vitro in a model of ADP-induced platelet aggregation in vitro and in vivo in a model of streptozotocininduced diabetes mellitus in rats. Material and Methods. Acetylsalicylic acid and dipyridamole were used as reference drugs. In vitro tests have demonstrated that DI exhibits antiplatelet activity in a wide range of concentrations (0,75×10-6 – 1.5×10-5 М, р<0,05), being comparable to acetylsalicylic acid and dipyridamole. In vivo tests have demonstrated dose-dependent antiplatelet activity of DI in doses of 2,5 – 20 mg/kg (21-14 %). Results and Discussion.Increasing the dose of DI above 10 mg/kg doesn’t increase its antiplatelet activity. After multiple oral administration to rats with streptozotocin-induced diabetes mellitus in 10 mg/kg dose, DI has exhibited antiplatelet activity, reducing the platelet aggregation rate to that of the control group (р<0,05). Conclusion. Thus, DI isapromisingcompound for furtherdevelopmentof an antiplatelet drug with new mechanism of action Bangladesh Journal of Medical Science Vol.18(3) 2019 p.574-576


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