A Naphthalenic Derivative ND-1 Inhibits Thrombus Formation by Interfering the Binding of Fibrinogen to Integrin <i>α</i>IIb<i>β</i>3

Ding, Xue; Liu, Tongdan; Xie, Zhouling; Zhao, Qing; Yuan, Chengfu; Liu, Xiaodong; Wang, Caihui; Gamariel, Rwibasira Rudinga; Xin, Ming; Li, Zhiyu; Kong, Yi

doi:10.1155/2016/8587164

Cited by 4 publications

(5 citation statements)

References 33 publications

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“…Washed platelets were prepared as described previously . Briefly, whole blood withdrawn from the abdominal aorta of rats after anesthesia was collected into tubes containing acid-citrate–dextrose (1:6).…”

Section: Methodsmentioning

confidence: 99%

Secondary Metabolites from the Leather Coral-Derived Fungal Strain Xylaria sp. FM1005 and Their Glycoprotein IIb/IIIa Inhibitory Activity

et al. 2021

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Five new tyrosine derivatives (1−5), one new phenylacetic acid derivative (6), two new quinazolinone analogues (7 and 8), one new naphthalenedicarboxylic acid (9), and one new 3,4-dihydroisocoumarin derivative (10), together with seven known compounds, were isolated from the fungus Xylaria sp. FM1005, which was isolated from Sinularia densa (leather coral) collected in the offshore region of the Big Island, Hawaii. The structures of compounds 1−10 were elucidated by extensive analysis of NMR spectroscopy, HRESIMS, and ECD data. Due to their structure similarity to the antiplatelet drug tirofiban, compounds 1−5 together with 6 were investigated for their antithrombotic activities. Compounds 1 and 2 strongly inhibited the binding of fibrinogen to purified integrin IIIb/IIa in a dose-dependent manner with the IC 50 values of 0.89 and 0.61 μM, respectively, and compounds 1 and 2 did not show any cytotoxicity against A2780 and HEK 293 at 40 μM.

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Section: Methodsmentioning

confidence: 99%

Secondary Metabolites from the Leather Coral-Derived Fungal Strain Xylaria sp. FM1005 and Their Glycoprotein IIb/IIIa Inhibitory Activity

et al. 2021

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“…The analysis of interaction assays between ANTP266 and α IIb β 3 was similar to the previous study with some modifications [4,17]. The 96-well microplate coated with fibrinogen was blocked with 1% albumin bovine serum (BSA) in TACTS for 1 h at 37 °C and then washed with TACTS.…”

Section: Methodsmentioning

confidence: 99%

“…A rat arterio-venous shunt thrombosis model was used to determine the antithrombotic activity of ANTP266 in vivo as described previously with a minor modification [ 4 , 8 ]. Sprague-Dawley rats were randomized into five groups and injected 1 mg/kg of tirofiban, ANTP266 (1, 5, 10 mg/kg), and the vehicle by group.…”

Section: Methodsmentioning

confidence: 99%

“…Platelets are small cells circulating in blood vessels that can be activated when the vessel is injured and then aggregated to form a platelet plug to avoid bleeding. However pathological conditions can also trigger platelet activation, lead to platelet aggregation, and then incur cardiovascular disorders [ 3 , 4 ]. An amount of evidence has confirmed the pivotal role of platelet aggregation in pathological thrombus formation, which hints that inhibition of platelet aggregation is a good strategy in the treatment of CVDs [ 2 ].…”

Section: Introductionmentioning

confidence: 99%

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A Short Half-Life αIIbβ3 Antagonist ANTP266 Reduces Thrombus Formation

Liu

Ren

Ding

et al. 2018

IJMS

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Integrin αIIbβ3 plays a pivotal role in platelet aggregation. Three αIIbβ3 antagonists have been approved by the Food and Drug Administration (FDA) for the treatment of cardiovascular diseases. Unfortunately, all of these three drugs can cause the side effect of severe bleeding. Therefore, developing a new αIIbβ3 antagonist with low bleeding was needed. In the present study, we screened compounds by using a fibrinogen/integrin αIIbβ3 enzyme-linked immunosorbent assay (ELISA), and a novel αIIbβ3 antagonist ANTP266 was attained. The antithrombotic effects of ANTP266 were estimated by using two animal models, the bleeding risk was estimated by using a mice tail cutting assay, and the plasma half-life time was tested by LC-MS/MS. The results showed that ANTP266 potently decreased thrombosis formation, while not prolonging bleeding time at its effective dosage. The bleeding of ANTP266 reduced rapidly as time went on from 5 to 60 min, but tirofiban produced high bleeding continuously. The plasma half-life of ANTP266 in rats was 10.8 min. Taken together, ANTP266 is an effective antithrombotic agent with a low bleeding risk. The shorter bleeding time benefits from its short plasma half-life. ANTP266 could be a candidate for developing the αIIbβ3 antagonist of rapid elimination for a patient undergoing percutaneous coronary intervention.

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“…Human platelet-rich plasma (PRP) was obtained by purchasing apheresis platelets from Jiangsu Province Blood Center (Nanjing, PR China). Washed platelets were prepared as described previously [12].…”

Section: Human Blood Samples and Washed Platelet Preparationmentioning

confidence: 99%

Design, Synthesis and Evaluation of 1,4-benzodioxine Derivatives as Novel Platelet Aggregation Inhibitors

et al. 2018

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A Naphthalenic Derivative ND-1 Inhibits Thrombus Formation by Interfering the Binding of Fibrinogen to Integrin αIIbβ3

Cited by 4 publications

References 33 publications

Secondary Metabolites from the Leather Coral-Derived Fungal Strain Xylaria sp. FM1005 and Their Glycoprotein IIb/IIIa Inhibitory Activity

Secondary Metabolites from the Leather Coral-Derived Fungal Strain Xylaria sp. FM1005 and Their Glycoprotein IIb/IIIa Inhibitory Activity

A Short Half-Life αIIbβ3 Antagonist ANTP266 Reduces Thrombus Formation

Design, Synthesis and Evaluation of 1,4-benzodioxine Derivatives as Novel Platelet Aggregation Inhibitors

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