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Heparin-like anticoagulant polypeptides with tunable activity: Synthesis, characterization, anticoagulative properties and clot solubilities in vitro
Biomaterials Advances ( IF 7.9 ) Pub Date : 2021-09-01 , DOI: 10.1016/j.msec.2021.112405
Dedai Lu 1 , Yuanyuan Jin 1 , Xiangya Wang 1 , Liyuan Xie 1 , Qianqian Liu 1 , Yamin Chen 1 , Hui Wang 1 , Ziqiang Lei 1
Affiliation  

Due to the uncontrollable anticoagulant activity and limited source, Heparin, which is commonly used in clinical anticoagulation therapies, faces the risk of spontaneous bleeding and thrombocytopenia. Herein, a series of anionic poly(amino acid) s poly (l-Serine-ran-L-Glutamic acid-ran-L-Cysteine-SO3) (PSEC-SO3) were prepared by the controlled Ring Opening Polymerization (ROP) of N-Carboxyanhydrides (NCAs). The anticoagulant activities of PSEC-SO3 can be regulated by simply adjusting the feeding ratio of monomers. In vitro tests show that these polypeptides can effectively prolong the Activated Partical Thromboplastin Time (APTT) and inhibit Factor IIa and Factor Xa, but has no significant effect on Prothrombin Time (PT) and Thrombin Time (TT), which indicates that PSEC-SO3 mainly act on the intrinsic pathway. In summary, the activity-tunable heparin-like polypeptides are expected to have good application prospects in the anticoagulant field.



中文翻译:

具有可调活性的肝素样抗凝多肽:体外合成、表征、抗凝特性和凝块溶解度

由于抗凝活性不可控且来源有限,临床抗凝治疗中常用的肝素面临着自发性出血和血小板减少的风险。在此,一连串的阴离子聚(氨基酸)的聚(-Serine--L-谷氨酸酸-L-半胱氨酸-SO 3)(PSEC-SO 3)通过受控开环聚合来制备(ROP ) 的 N-羧酸酐 (NCA)。PSEC-SO 3的抗凝活性只需调节单体的进料比例即可调节。体外试验表明,这些多肽能有效延长活化部分凝血活酶时间(APTT)并抑制因子IIa和因子Xa,但对凝血酶原时间(PT)和凝血酶时间(TT)无显着影响,表明PSEC-SO 3主要作用于内在途径。综上所述,活性可调的类肝素多肽有望在抗凝领域具有良好的应用前景。

更新日期:2021-09-04
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