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Discovery of a Novel Cysteine Framework XXIV Conotoxin from Conus striatus , S24a, with Potential Analgesic Activity
International Journal of Peptide Research and Therapeutics ( IF 2.0 ) Pub Date : 2020-09-07 , DOI: 10.1007/s10989-020-10109-4
Yuanyuan Qiang , Jianguo Niu , Yun Wu , Zhao Di , Feng Wang , Lianxiang Zhang , Kunmei Liu , Boyao Zhao , Lei Wang

A novel conotoxin, S24a, containing 26 amino acid residues was first derived from the cDNA library of Conus striatus. This conotoxin has the same conserved signal peptide as A-superfamily conotoxins and some unconserved residues in the pro-region. According to the mature peptide sequence of this conotoxin, S24a was prepared by the Escherichia coli expression system and purified by affinity chromatography, Sephadex gel filtration and reversed-phase high-performance liquid chromatography (RP-HPLC). The molecular weight of S24a was identified by MALDI-TOF-MS. Biological function experiments showed that S24a could inhibit frog sciatic nerve muscle contraction. Moreover, a high dose of S24a (100 μg/kg) had more potent and longer lasting analgesic activity compared with lidocaine and pethidine in the hotplate pain model and the formalin pain model in mice, which indicated that S24a can be further developed as a potential analgesic drug lead.



中文翻译:

从潜在的镇痛活性的圆锥形线虫S24a中发现一种新型的半胱氨酸骨架XXIV芋螺毒素

一种新颖的芋螺毒素,S24a中,含有26个氨基酸残基首先从cDNA文库衍生的细线芋螺。该芋螺毒素具有与A超家族芋螺毒素相同的保守信号肽,并且在前区具有一些非保守残基。根据该芋螺毒素的成熟肽序列,由大肠杆菌制备S24a表达系统,并通过亲和色谱,Sephadex凝胶过滤和反相高效液相色谱(RP-HPLC)进行纯化。通过MALDI-TOF-MS鉴定S24a的分子量。生物学功能实验表明,S24a可以抑制青蛙坐骨神经肌肉的收缩。此外,在小鼠的热板痛模型和福尔马林痛模型中,与利多卡因和哌替啶相比,高剂量的S24a(100μg/ kg)具有更强的持久镇痛作用,这表明S24a可以进一步发展为潜在的镇痛药铅。

更新日期:2020-09-08
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