Key result
Compound 3o inhibits platelet aggregation and thrombosis better than NBP, protecting against ischemic brain injury.
Why the study?
The study was conducted to design and synthesize novel compounds to discover effective antiplatelet agglutination drugs for cerebrovascular diseases caused by thrombosis.
Does compound 3o inhibit platelet aggregation and thrombosis better than 3-n-butylphthalide in preclinical models?
Does compound 3o inhibit platelet aggregation and thrombosis better than 3-n-butylphthalide in preclinical models?
Compound 3o is a novel butylphthalide-hydroxycinnamic acid hybrid derivative that demonstrates promising antiplatelet, antithrombotic, and neuroprotective activities in preclinical models.
Should not change antithrombotic practice; hypothesis-generating for compound 3o in ischemic stroke.
Thirty‐eight novel butylphthalide‐hydroxycinnamic acid hybrid derivatives were designed and synthesized to discover effective antiplatelet agglutination drugs. Among these compounds, 3 o gave the optimal inhibitory activity against AA‐induced platelet aggregation in vitro and also exhibited better inhibition than the precursor 3‐n‐butylphthalide (NBP) against thrombin‐induced platelet contraction, carrageenan‐induced tail thrombosis, and FeCl3‐induced common carotid artery thrombosis. Further investigations on the anti‐ischemic stroke activity revealed that compound 3 o exhibited a remarkable protective effect against ischemic/reperfusion brain injury. The PAMPA‐BBB permeability and liver microsomal stability tests indicated that compound 3 o could traverse the blood‐brain barrier and possessed favorable metabolic stability. This research provides a new candidate compound for treating and preventing cerebrovascular diseases caused by thrombosis.
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Yang et al. (2024) studied Cerebrovascular diseases caused by thrombosis. Compound 3 o (butylphthalide-hydroxycinnamic acid hybrid derivative) vs. 3-n-butylphthalide (NBP) was evaluated on Inhibitory activity against platelet aggregation and thrombosis. Compound 3 o exhibited optimal inhibitory activity against platelet aggregation and thrombosis compared to 3-n-butylphthalide, and showed a protective effect against ischemic brain injury.
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