scholarly journals Inhibitory Effects of Two Ferulates from Angelica Sinensis on Platelet Aggregation and Oxytocin-induced Uterine Contraction

2009 ◽  
Vol 2 (1) ◽  
pp. 43-46 ◽  
Author(s):  
Y. Yu ◽  
B. Q. Lin ◽  
L. Yu ◽  
Y. Q. Hua ◽  
J. A. Duan ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Uterine Contraction ◽  
Adenosine Diphosphate ◽  
Inhibitory Effect ◽  
Biologically Active ◽  
Angelica Sinensis ◽  
Hydrophobic Property ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity

Ferulic acid (FA) is widely considered as a biologically active component in Angelica sinensis, and used as one of the marker compounds for the quality control of Angelica sinensis. However, in A. sinensis, FA mainly exists as its ester, coniferyl ferulate (CF). CF is unstable and readily hydrolyzed into FA during conventional extraction. Herein, their antiplatelet aggregation activities and relaxant effects on oxytocin-induced mouse uterine muscle contraction were investigated and compared. The results showed that FA inhibited arachidonic acid (AA), adenosine diphosphate (ADP) and thrombin (THR)-induced platelet aggregation with IC50 values of 974.8 ± 97.5, 737.9 ± 40.2 and 244.6 ± 25.6 μg/ml, respectively. The potency of CF is much higher than that of FA, and the IC50 values for AA, ADP and THR were 7.1 ± 0.3, 276.4 ± 53.4 and 77.5 ± 23.1 μg/ml, respectively. IC50 of FA was 23.8 ± 6.2 μg/ml for oxytocin-induced uterine contraction in vitro. CF could only be tested at low concentration and its IC50 could not be calculated thereafter because of its strong hydrophobic property. So CF has more potent antiplatelet aggregation activity, while FA has stronger inhibitory effect on oxytocin-induced uterine contraction in vitro

Triterpenoids with Antiplatelet Aggregation Activity from the Roots of Ilex pubescens

Planta Medica ◽  
2016 ◽  
Vol 83 (09) ◽  
pp. 797-804 ◽  
Author(s):  
Qinglong Tan ◽  
Maosong Qiu ◽  
Di Cao ◽  
Tianqin Xiong ◽  
Lei Zhang ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Adenosine Diphosphate ◽  
Significant Inhibition ◽  
Triterpene Saponins ◽  
Rabbit Plasma ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity ◽  
Ilex Pubescens ◽  
New Compounds

AbstractTwo new triterpenes and five new triterpene saponins, named ilexpusons A–G (1–7), as well as eight known compounds were isolated from Ilex pubescens. The structures of the new compounds were established by a combination of chemical and spectroscopic methods, including HRESIMS, 1H-NMR, 13C-NMR, 1H-1H COSY, HSQC, HMBC, and NOESY. Additionally, the biological activity of compounds 1 – 15 against adenosine diphosphate-induced platelet aggregation in rabbit plasma was determined. Among the tested compounds, 1, 2, 5, 6, 8, 13, 14, and 15 exhibited significant inhibition of platelet aggregation in vitro.

scholarly journals TO STUDY THE IN VITRO INHIBITION OF BLOOD PLATELET AGGREGATION BY ISOLATED COMPOUNDS FROM CLAUSENA DENTATA (WILLD.) ROEM.

2019 ◽  
pp. 128-133
Author(s):  
ANNAMALAI MADURAM ◽  
RAJU KAMARAJ
Keyword(s):  
Platelet Aggregation ◽  
Tamil Nadu ◽  
Adenosine Diphosphate ◽  
Blood Platelet ◽  
Stem Bark ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity ◽  
Treatment Of Wounds ◽  
Trees And Shrubs

Objectives: The objectives of the study were to study the antiplatelet aggregation activity of compounds isolated from extracts of Clausena dentata. Clausena (Rutaceae) is a genus of about 23 species of unarmed trees and shrubs. The stem bark of C. dentata is used in veterinary medicine for the treatment of wounds and sprains. Even though C. dentata has a lot of potential medical uses, the study of pharmacological properties is very scarce. Methods: The plant C. dentata was collected from Kadagaman, near Tiruvannamalai, Tamil Nadu, India, and authenticated by Centre for Advanced Study in Botany, University of Madras, Chennai. The dry powder of stem bark was extracted with hexane, chloroform, and methanol. The extracts were subjected to qualitative phytochemical screening and column chromatography. Four compounds were isolated. All the isolated compounds were subjected to adenosine diphosphate (ADP)-induced platelet aggregation and compared with aspirin. Results: The isolated compounds from C. dentata and standard aspirin showed significant antiplatelet activity against ADP-induced platelet aggregation. Conclusion: The compounds, 3-(1,1-dimethylallyl)xanthyletin, dentatin, nordentatin, and carbazole showed significant antiplatelet aggregation activity. Among the compounds, nordentatin showed more activity of antiplatelet aggregation.

The Inhibition of Platelet Aggregation by an Aorta Intima Extract

1974 ◽  
Vol 32 (02/03) ◽  
pp. 417-431 ◽  
Author(s):  
A. du P Heyns ◽  
D. J van den Berg ◽  
G. M Potgieter ◽  
F. P Retief
Keyword(s):  
Platelet Aggregation ◽  
Degradation Products ◽  
Adenosine Diphosphate ◽  
Inhibitory Effect ◽  
Protective Role ◽  
Vascular Trauma ◽  
Wear And Tear ◽  
Sequential Addition ◽  
Aggregation Activity

SummaryThe platelet aggregating activity of extracts of different layers of the arterial wall was compared to that of Achilles tendon. Arterial media and tendon extracts, adjusted to equivalent protein content as an index of concentration, aggregated platelets to the same extent but an arterial intima extract did not aggregate platelets. Platelet aggregation induced by collagen could be inhibited by mixing with intima extract, but only to a maximum of about 80%. Pre-mixing adenosine diphosphate (ADP) with intima extracts diminished the platelet aggregation activity of the ADP. Depending on the relationship between ADP and intima extract concentrations aggregating activity could either be completely inhibited or inhibition abolished. Incubation of ADP with intima extract and subsequent separation of degradation products by paper chromatography, demonstrated a time-dependent breakdown of ADP with AMP, adenosine, inosine and hypoxanthine as metabolic products; ADP removal was complete. Collagen, thrombin and adrenaline aggregate platelets mainly by endogenous ADP of the release reaction. Results of experiments comparing inhibition of aggregation caused by premixing aggregating agent with intima extract, before exposure to platelets, and the sequential addition of first the intima extract and then aggregating agent to platelets, suggest that the inhibitory effect of intima extract results from ADP breakdown. It is suggested that this ADP degradation by intima extract may play a protective role in vivo by limiting the size of platelet aggregates forming at the site of minimal “wear and tear” vascular trauma.

Inhibition of Platelet Function by Antiarrhythmic Drugs, Verapamil and Disopyramide

1982 ◽  
Vol 47 (02) ◽  
pp. 150-153 ◽  
Author(s):  
P Han ◽  
C Boatwright ◽  
N G Ardlie
Keyword(s):  
Platelet Aggregation ◽  
Platelet Function ◽  
Antiarrhythmic Drugs ◽  
Adenosine Diphosphate ◽  
Inhibitory Effect ◽  
Second Phase ◽  
Ionophore A23187 ◽  
High Concentrations ◽  
Artery Disease

SummaryVarious cardiovascular drugs such as nitrates and propranolol, used in the treatment of coronary artery disease have been shown to have an antiplatelet effect. We have studied the in vitro effects of two antiarrhythmic drugs, verapamil and disopyramide, and have shown their inhibitory effect on platelet function. Verapamil, a calcium channel blocker, inhibited the second phase of platelet aggregation induced by adenosine diphosphate (ADP) and inhibited aggregation induced by collagen. Disopyramide similarly inhibited the second phase of platelet aggregation caused by ADP and aggregation induced by collagen. Either drug in synergism with propranolol inhibited ADP or collagen-induced platelet aggregation. Disopyramide at high concentrations inhibited arachidonic add whereas verapamil was without effect. Verapamil, but not disopyramide, inhibited aggregation induced by the ionophore A23187.

Ticlopidine Selectively Inhibits Human Platelet Responses to Adenosine Diphosphate

1991 ◽  
Vol 66 (06) ◽  
pp. 694-699 ◽  
Author(s):  
Marco Cattaneo ◽  
Benjaporn Akkawat ◽  
Anna Lecchi ◽  
Claudio Cimminiello ◽  
Anna M Capitanio ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Adenosine Diphosphate ◽  
Inhibitory Effect ◽  
Clot Retraction ◽  
Fibrinogen Binding ◽  
Low Concentrations ◽  
Binding Inhibition ◽  
High Concentrations ◽  
Formalin Fixed

SummaryPlatelet aggregation and fibrinogen binding were studied in 15 individuals before and 7 days after the oral administration of ticlopidine (250 mg b.i.d.). Ticlopidine significantly inhibited platelet aggregation induced by adenosine diphosphate (ADP), the endoperoxide analogue U46619, collagen or low concentrations of thrombin, but did not inhibit platelet aggregation induced by epinephrine or high concentrations of thrombin. Ticlopidine inhibited 125I-fibrinogen binding induced by ADP, U46619 or thrombin (1 U/ml). The ADP scavengers apyrase or CP/CPK, added in vitro to platelet suspensions obtained before ticlopidine, caused the same pattern of aggregation and 125I-fibrihogen binding inhibition as did ticlopidine. Ticlopidine did not inhibit further platelet aggregation and 125I-fibrinogen binding induced in the presence of ADP scavengers. After ticlopidine administration, thrombin or U46619, but not ADP, increased the binding rate of the anti-GPIIb/IIIa monoclonal antibody 7E3 to platelets. Ticlopidine inhibited clot retraction induced by reptilase plus ADP, but not that induced by thrombin or by reptilase plus epinephrine, and prevented the inhibitory effect of ADP, but not that of epinephrine, on the PGE1-induced increase in platelet cyclic AMP. The number of high- and low-affinity binding sites for 3H-ADP on formalin-fixed platelets and their K d were not modified by ticlopidine. These findings indicate that ticlopidine selectively inhibits platelet responses to ADP.

scholarly journals Synthesis of 3,15-Disuccinate-12-Coumarin Substituted Andrographolide Derivatives and Their Antiplatelet Aggregation Activities In Vitro

2020 ◽  
Vol 15 (5) ◽  
pp. 1934578X2091086
Author(s):  
Xue Li ◽  
Jiang-Wei Wang ◽  
Bin Huang ◽  
Zhi-Xiang Peng ◽  
Yuan-Yuan Zhang ◽  
...  
Keyword(s):  
Adenosine Diphosphate ◽  
Biological Evaluation ◽  
Significant Inhibition ◽  
Inhibition Activity ◽  
Antiplatelet Aggregation ◽  
Candidate Structure ◽  
Dependent Behavior ◽  
Aggregation Activity ◽  
Dose Dependent

In order to develop a series of novel compounds with antiplatelet aggregation activities, 3,15-disuccinate-12-coumarin substituted derivatives were designed and synthesized based on the natural product andrographolide. In vitro antiplatelet aggregation activities were evaluated by the turbidimetric method with thrombin, adenosine diphosphate (ADP), arachidonic acid (AA), and collagen as inducers. The biological evaluation revealed that compound 11k showed significant inhibition activity for thrombin, AA, and collagen-induced platelet aggregation at the same time and exhibited a dose-dependent behavior. Compound 11c showed the highest antiplatelet aggregation activity induced by ADP. Most of the derivatives had no significant cytotoxicity. Therefore, our work proved that 3,15-disuccinate-12-coumarin substituted andrographolide derivatives had the potential to become a novel candidate structure for antiplatelet aggregation and deserved further study.

Inhibitory effects of antibiotics on platelet aggregation in vitro

1997 ◽  
Vol 16 (11) ◽  
pp. 662-666 ◽  
Author(s):  
Hiroko Kariyazono ◽  
Kazuo Nakamura ◽  
Terutoshi Shinkawa ◽  
Yukinori Moriyama ◽  
Hitoshi Toyohira ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Blood Concentration ◽  
Chemical Structure ◽  
Inhibitory Action ◽  
Adenosine Diphosphate ◽  
Inhibitory Effect ◽  
Carboxyl Group ◽  
Inhibitory Effects ◽  
Induced Aggregation

1 We evaluated in vitro inhibitory effects of six types of antibiotic, aztreonam (AZT), cefamandole (CMD), cefmetazole (CMZ), cefotiam (CTM), flomoxef (FMOX) and latamoxef (LMOX), on platelet aggregation, using healthy volunteers' blood. Four types-FMOX, LMOX, CTM and CMD-inhibited, in concentration of 2500 ?g/ml, the secondary aggregation induced by 3.0 ?M adenosine diphosphate (ADP), and also inhibited the aggregation induced by 0.5 ?g/ml collagen. AZT in the same concentration, did not inhibit the aggregation induced by collagen, and it inhibited only ADP induced aggregation. CMZ, in the same concentration, inhibited neither of the two aggregations. 2 The inhibitory effects of the antibiotics on collagen- induced aggregation were dependent on the concen tration of respective antibiotics. When classified by the strength of inhibitory action, LMOX and FMOX were strong, followed by CTM and CMD. The action of AZT and CMZ was weak. In particular, LMOX showed a 32% inhibitory effect at concentration of 50 ?g/ml, a level near the blood concentration obtained with clinical usual dose. 3 No relationship was observed between inhibitory effects of antibiotics on ADP- or collagen-induced aggregation and the presence or absence of carboxyl group and/or N-methyltetrazolethiol group in the chemical structure.

scholarly journals Phenolic Chemical Composition of Petroselinum Crispum Extract and Its Effect on Haemostasis

2011 ◽  
Vol 6 (7) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Douglas S. A. Chaves ◽  
Flávia S. Frattani ◽  
Mariane Assafim ◽  
Ana Paula de Almeida ◽  
Russolina B. Zingali ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Chemical Composition ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
The Other ◽  
Petroselinum Crispum ◽  
In Vitro Activity ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity

From the aqueous extract (Pc) of Petroselinum crispum (Mill) flat leaves specimens were isolated and identified the flavonoids apigenin (1), apigenin-7- O-glucoside or cosmosiin (2), apigenin-7- O-apiosyl-(1→2)- O-glucoside or apiin (3) and the coumarin 2″,3″-dihydroxy-furanocoumarin or oxypeucedanin hydrate (4). The inhibitory activity toward clotting formation and platelet aggregation was assessed for Pc flavonoids (1) and (2), and the coumarin (4). Pc showed no inhibition on clotting activity when compared with the control. On the other hand, a strong antiplatelet aggregation activity was observed for Pc (IC50 = 1.81 mg/mL), apigenin (IC50 = 0.036 mg/mL) and cosmosiin (IC50 = 0.18 mg/mL). In all cases ADP was used as inductor of platelet aggregation. Our results showed that Pc, apigenin and cosmosiin interfere on haemostasis inhibiting platelet aggregation. To the best of our knowledge this is the first report for the cosmosiin antiplatelet aggregation in vitro activity.

scholarly journals Inhibitory Effect of Propolis on Platelet Aggregation In Vitro

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Yun-Xiang Zhang ◽  
Ting-Ting Yang ◽  
Liu Xia ◽  
Wei-Fen Zhang ◽  
Jia-Fu Wang ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Platelet Rich Plasma ◽  
Water Extract ◽  
Adenosine Diphosphate ◽  
Caffeic Acid Phenethyl Ester ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Receptor Activator ◽  
Dose Dependent

Platelet hyperactivity plays an important role in arterial thrombosis and atherosclerosis. The present study was aimed to investigate the effects of different extracts of propolis and components of flavonoids on platelet aggregation. Platelet-rich plasma was prepared and incubated in vitro with different concentrations of the tested extracts and components of flavonoids. Platelets aggregation was induced by different agonists including adenosine diphosphate (ADP, 10 μM), thrombin receptor activator peptide (TRAP, 50 μM), and collagen (5 μg/mL). At 25 mg/L to 300 mg/mL, the water extract propolis (WEP) inhibited three agonists-induced platelet aggregations in a dose-dependent manner. The flavonoids isolated from the propolis also showed markedly inhibited platelet aggregation induced by collagen, ADP, and TRAP, respectively. The components including caffeic acid phenethyl ester (CAPE), galangin, apigenin, quercetin, kaempferol, ferulic acid, rutin, chrysin, pinostrobin, and pinocembrin and their abilities of inhibiting platelet aggregation were studied. It was concluded that propolis had an antiplatelet action in which flavonoids were mainly implicated.

Effect of Dipyridamole on Spontaneous Platelet Aggregation in Whole Blood Decreases with the Time After Venepuncture: Evidence for the Role of ADP

1987 ◽  
Vol 58 (02) ◽  
pp. 744-748 ◽  
Author(s):  
A R Saniabadi ◽  
G D O Lowe ◽  
J C Barbenel ◽  
C D Forbes
Keyword(s):  
Platelet Aggregation ◽  
Correlation Coefficient ◽  
Whole Blood ◽  
Blood Platelet ◽  
Inhibitory Effect ◽  
Time Interval ◽  
Adp Receptor ◽  
Spontaneous Platelet Aggregation

SummarySpontaneous platelet aggregation (SPA) was studied in human whole blood at 3, 5, 10, 20, 30, 40 and 60 minutes after venepuncture. Using a whole blood platelet counter, SPA was quantified by measuring the fall in single platelet count upon rollermixing aliquots of citrated blood at 37° C. The extent of SPA increased with the time after venepuncture, with a correlation coefficient of 0.819. The inhibitory effect of dipyridamole (Dipy) on SPA was studied: (a) 10 μM at each time interval; (b) 0.5-100 μM at 3 and 30 minutes and (c) 15 μM in combination with 100 μM adenosine, 8 μM 2-chloroadenosine (2ClAd, an ADP receptor blocker) and 50 μM aspirin. There was a rapid decrease in the inhibitory effect of Dipy with the time after venepuncture; the correlation coefficient was -0.533. At all the concentrations studied, Dipy was more effective at 3 minutes than at 30 minutes after venepuncture. A combination of Dipy with adenosine, 2ClAd or aspirin was a more effective inhibitor of SPA than either drug alone. However, when 15 μM Dipy and 10 μM Ad were added together, the inhibitory effect of Dipy was not increased significantly, suggesting that Dipy inhibits platelet aggregation independent of Ad. The increase in SPA with the time after venepuncture was abolished when blood was taken directly into the anticoagulant containing 5 μM 2ClAd. It is suggested that ADP released from the red blood cells is responsible for the increased platelet aggregability with the time after venepuncture and makes a serious contribution to the artifacts of in vitro platelet function studies.

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