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 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.

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

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.

scholarly journals Design, Synthesis, andIn VitroAntiplatelet Aggregation Activities of Ferulic Acid Derivatives

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Peng-Xuan Zhang ◽  
Hang Lin ◽  
Cheng Qu ◽  
Yu-Ping Tang ◽  
Nian-Guang Li ◽  
...  
Keyword(s):  
Ferulic Acid ◽  
Target Compound ◽  
Design Synthesis ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity ◽  
New Compounds

In order to discover new compounds with antiplatelet aggregation activities, some ferulic acid (FA) derivatives were designed and synthesized. Thein vitroantiplatelet aggregation activities of these compounds were assessed by turbidimetric test. The results showed that the target compound7fhad potent antiplatelet aggregation activity with its IC5027.6 μmol/L, and7fcan be regarded as a novel potent antiplatelet aggregation candidate.

Binding of (14C) Dipyradamole (RA 8) to Platelets and Inhibition of ADP Induced Platelet Aggregation

1975 ◽  
Author(s):  
K. Subbarao ◽  
B. Rucinski ◽  
S. Niewiarowski
Keyword(s):  
Platelet Aggregation ◽  
Human Plasma ◽  
Platelet Rich Plasma ◽  
Total Radioactivity ◽  
Plasma Medium ◽  
Rabbit Plasma ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity ◽  
Induced Aggregation

RA 8 (cone. 10-5-10-6 M) strongly inhibits ADP induced aggregation of washed platelets but has no similar effect if platelets are suspended in the plasma medium, α, Acid glyco protein (GP) of human plasma has been found to complex PA 8 and to block its antiplatelet aggregation activity (Mewiarowski, S. et al. J. Lab. Clin. Med. 1975, in press). Incubation of washed platelets of human or rabbit with (14C) RA 8 (cone. 10-6 M) resulted in a binding of 20-30% radioactivity to platelets reaching a maximum within 1 minute incubation at 37° C and remaining constant for the length of time. Addition of human or rabbit plasma and oc, GP inhibited binding of RA 8 whereas other fractions such as fibrinogen, Cohn fraction II, IV and albumin did not show any effect. The binding of RA 8 to platelets correlated with the inhibition of ADP induced aggregation. The binding was independent of temperature at the range of 4-50° C and of pH at the range of 6.0-8.0. Intravenous injection of (14C) dipyradamole to rabbits at a dose of 25 mg/kg and 10 mg/kg weight resulted in a 32.6% and 6.0% (respectively) inhibition of ADP induced aggregation in platelet rich plasma (PRP). In both instances 3.0% of the total radioactivity recovered in PRP was associated with platelets. It can be suggested that α, GP present in blood may also inhibit binding of drug to platelets in vivo and interfere with its antiplatelet aggregation activity. Large doses of RA 8 are needed to overcome this effect.

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.

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.

Platelet Aggregation Induced in Vitro by Therapeutic Ultrasound

1977 ◽  
Vol 38 (03) ◽  
pp. 0640-0651 ◽  
Author(s):  
B. V Chater ◽  
A. R Williams
Keyword(s):  
Platelet Aggregation ◽  
Direct Action ◽  
Adenosine Diphosphate ◽  
Ultrasonic Cavitation ◽  
Related Phenomenon ◽  
Release Reaction ◽  
Physical Conditions ◽  
Platelet Aggregates ◽  
Active Substances

SummaryPlatelets were found to aggregate spontaneously when exposed to ultrasound generated by a commercial therapeutic device. At a given frequency, aggregation was found to be a dose-related phenomenon, increasing intensities of ultrasound inducing more extensive and more rapid aggregation. At any single intensity, the extent aggregation was increased as the frequency of the applied ultrasound was decreased (from 3.0 to 0.75 MHz).Ultrasound-induced platelet aggregation was found to be related to overall platelet sensitivity to adenosine diphosphate. More sensitive platelets were found to aggregate spontaneously at lower intensities of sound, and also the maximum extent of aggregation was found to be greater. Examination of ultrasound-induced platelet aggregates by electron microscopy demonstrated that the platelets had undergone the release reaction.The observation that haemoglobin was released from erythrocytes in whole blood irradiated under identical physical conditions suggests that the platelets are being distrupted by ultrasonic cavitation (violent gas/bubble oscillation).It is postulated that overall platelet aggregation is the result of two distinct effects. Firstly, the direct action of ultrasonic cavitation disrupts a small proportion of the platelet population, resulting in the liberation of active substances. These substances produce aggregation, both directly and indirectly by inducing the physiological release reaction in adjacent undamaged platelets.

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.

Dipyridamole Inhibits Platelet Aggregation in Whole Blood

1983 ◽  
Vol 50 (04) ◽  
pp. 852-856 ◽  
Author(s):  
P Gresele ◽  
C Zoja ◽  
H Deckmyn ◽  
J Arnout ◽  
J Vermylen ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Whole Blood ◽  
Ex Vivo ◽  
Platelet Rich Plasma ◽  
Significant Negative Correlation ◽  
Significant Inhibition ◽  
Oral Drug ◽  
Human Blood Samples ◽  
Induced Aggregation

SummaryDipyridamole possesses antithrombotic properties in the animal and in man but it does not inhibit platelet aggregation in plasma. We evaluated the effect of dipyridamole ex vivo and in vitro on platelet aggregation induced by collagen and adenosine- 5’-diphosphate (ADP) in human whole blood with an impedance aggregometer. Two hundred mg dipyridamole induced a significant inhibition of both ADP- and collagen-induced aggregation in human blood samples taken 2 hr after oral drug intake. Administration of the drug for four days, 400 mg/day, further increased the antiplatelet effect. A significant negative correlation was found between collagen-induced platelet aggregation in whole blood and dipyridamole levels in plasma (p <0.001). A statistically significant inhibition of both collagen (p <0.0025) and ADP-induced (p <0.005) platelet aggregation was also obtained by incubating whole blood in vitro for 2 min at 37° C with dipyridamole (3.9 μM). No such effects were seen in platelet-rich plasma, even after enrichment with leukocytes. Low-dose adenosine enhanced in vitro inhibition in whole blood.Our results demonstrate that dipyridamole impedes platelet aggregation in whole blood by an interaction with red blood cells, probably involving adenosine.

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