scholarly journals Design, Synthesis and Anti-Platelet Aggregation Activity Study of Ginkgolide-1,2,3-triazole Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2156 ◽  
Author(s):  
Jian Cui ◽  
Le’An Hu ◽  
Wei Shi ◽  
Guozhen Cui ◽  
Xumu Zhang ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Functional Groups ◽  
Ginkgo Biloba ◽  
Active Component ◽  
Platelet Activating Factor ◽  
Cycloaddition Reaction ◽  
Design Synthesis ◽  
Antiplatelet Aggregation ◽  
Ic50 Values ◽  
Aggregation Activity

Ginkgolides are the major active component of Ginkgo biloba for inhibition of platelet activating factor receptor. An azide-alkyne Huisgen cycloaddition reaction was used to introduce a triazole nucleus into the target ginkgolide molecules. A series of ginkgolide-1,2,3-triazole conjugates with varied functional groups including benzyl, phenyl and heterocycle moieties was thus synthesized. Many of the designed derivatives showed potent antiplatelet aggregation activities with IC50 values of 5~21 nM.

scholarly journals Chemical Constituents from the Whole Plant of Cuscuta reflexa

2020 ◽  
Vol 10 (5) ◽  
pp. 337-344
Author(s):  
Tin Thu Thu Aung ◽  
Meng-Yuan Xia ◽  
Pyae Phyo Hein ◽  
Rong Tang ◽  
Dong-Dong Zhang ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Platelet Activating Factor ◽  
Rabbit Platelet ◽  
Cuscuta Reflexa ◽  
Chemical Structures ◽  
Antiplatelet Aggregation ◽  
Whole Plant ◽  
Aggregation Activity

Abstract Two new 2H-pyran-2-one glucosides, cuscutarosides A (1) and B (2), and one new steroidal glucoside, 7β-methoxy-β-sitosterol 3-O-β-glucopyranoside (3), together with 12 known compounds (4–15) were isolated from the whole plant of Cuscuta reflexa (Convolvulaceae) collected from Myanmar. The chemical structures of these new compounds were elucidated based on extensive spectroscopic analysis. The antiobesity activity of these isolates was evaluated using porcine pancreatic lipase (PPL), and the antiplatelet aggregation activity was screened using rabbit platelets induced by thrombin, platelet-activating factor (PAF), arachidonate (AA), or collagen. 7β-Methoxy-β-sitosterol 3-O-β-glucopyranoside (3) showed weak PPL inhibitory activity. Cuscutaroside A (1), its acetylated derivative (1a), and scrophenoside B (8) showed weak inhibitory activity against rabbit platelet aggregation induced by collagen. Compound 1a also showed inhibitory activity against rabbit platelet aggregation induced by AA. Graphic Abstract

Inhibition by Glaucocalyxin A of Aggregation of Rabbit Platelets Induced by ADP, Arachidonic Acid and Platelet-Activating Factor, and Inhibition of [3H]-PAF Binding

1992 ◽  
Vol 67 (04) ◽  
pp. 458-460 ◽  
Author(s):  
Zhang Bin ◽  
Long Kun
Keyword(s):  
Arachidonic Acid ◽  
Platelet Aggregation ◽  
Platelet Activating Factor ◽  
Northeastern China ◽  
Ethereal Extract ◽  
Ic50 Value ◽  
Rabbit Platelets ◽  
Ic50 Values ◽  
Induced Aggregation

SummaryGlaucocalyxin A is a new diterpenoid isolated from the ethereal extract of the leaves of Rabdosia japonica (Burm f) Hara var glaucocalyx (Maxim) Hara (Labiatae) collected in the northeastern China. When it was incubated with washed rabbit platelets, glaucocalyxin A inhibited ADP- or arachidonic acid-induced platelet aggregation with IC50 values of 4.4 μmol/1, 14.1 μmol/1 respectively. Glaucocalyxin A also inhibited PAF-induced aggregation of rabbit platelets which were refractory to ADP and arachidonic acid with an IC50 value of 13.7 μmol/1. Analysis of [3H]-PAF binding showed that glaucocalyxin A prevented [3H]-PAF binding to intact washed rabbit platelets with an IC50 value of 8.16 μmol/1, which was consistent with its inhibition of PAF-induced platelet 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.

N, N’-disubstitutedphenyl-4-ethoxyl benzene-1, 3-disulfonamides: design, synthesis, and evaluation of anti-platelet aggregation activity

2019 ◽  
Vol 28 (9) ◽  
pp. 1388-1401
Author(s):  
Xin Chen ◽  
Xiujie Liu ◽  
kai Qiu ◽  
Xiang Xu ◽  
Caiwen Li ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Design Synthesis ◽  
Aggregation Activity

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.

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 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 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.

Design, Synthesis and Anticancer Activity of New Thiazole-Tetrazole or Triazole Hybrid Glycosides Targeting CDK-2 via Structure-Based Virtual Screening

2019 ◽  
Vol 19 (11) ◽  
pp. 933-948 ◽  
Author(s):  
Asmaa F. Kassem ◽  
Eman M. H. Abbas ◽  
Dina S. El-Kady ◽  
Hanem M. Awad ◽  
Wael A. El-Sayed
Keyword(s):  
Anticancer Activity ◽  
Cycloaddition Reaction ◽  
Molecular Surface ◽  
Dipolar Cycloaddition ◽  
Breast Adenocarcinoma ◽  
Cyclin Dependent Kinase ◽  
Design Synthesis ◽  
Adenocarcinoma Cells ◽  
Ic50 Values ◽  
Epithelium Cells

Background & Objective: The target tetrazole glycosides were synthesized by construction of ring system by cycloaddition reaction of benzothiazole-linked nitrile derivative and sodium azide followed by N-glycosylation process and deprotection. Methods: The triazole glycosides were prepared by applying click approach involving dipolar cycloaddition of benzothiazole possessing alkyne functionality and different glycosyl azides. The products incorporating acyclic analogs of sugar moieties were synthesized through alkylation using acyclic oxygenated halides. Results: The anticancer activity was studied against human breast adenocarcinoma cells (MCF-7) and human normal Retina pigmented epithelium cells (RPE-1). High activities were revealed by three compounds with IC50 values 11.9-16.5 µM compared to doxorubicin (18.6 µM) in addition to other four derivatives with good inhibition activities. Conclusion: Enzyme docking investigation was performed into cyclin-dependent kinase 2 (CDK2); a potential target for cancer medication. Compounds which have possessed highest activities revealed good fitting inside the binding site of the protein molecular surface and showed minimum binding energy.

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