| 王磊,吴赟,任政华,等.T-超家族芋螺毒素S10a的制备及功能研究[J].中国海洋药物,2017,36(3):89-93. |
| T-超家族芋螺毒素S10a的制备及功能研究 |
| Production and functional analysis of T-superfamily conotoxin S10a |
| 投稿时间：2016-12-09 修订日期：2017-01-04 |
| DOI： |
| 中文关键词: T-超家族，芋螺毒素，固相化学合成，镇痛 |
| English Keywords:T-superfamily, Contoxin, Solid-phase polypeptide synthesis, Analgesic |
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| 中文摘要: |
| 目的 对从线纹芋螺中发现的T-超家族毒素S10a进行制备，并对其毒性和活性进行初步评价。方法 利用固相化学合成的方法进行S10a的制备，并利用RP-HPLC方法进行分离纯化，制备的样品采用MALDI-TOF-TOF的方法进行鉴定。利用斑马鱼、小鼠、细胞株对毒素的毒性进行评价，利用小鼠热板模型，分析了其镇痛活性。结果 利用固相化学合成进行毒素的制备，结果显示合成多肽的纯度高，分子量与预测结果相一致。S10a对斑马鱼、小鼠及四种细胞细胞株表现出了不同水平的毒性。S10a在小鼠热板镇痛模型上表现出了良好的镇痛活性，与阳性对照药哌替啶相比，S10a的高剂量组（0.7mg/kg）的镇痛作用时间更长。 |
| English Summary: |
| Objective To produce enough T-superfamily contoxin S10a and investigate the bioactivities. Methods Conotoxin S10a was synthesized by solid-phase polypeptide synthesis according to the amino acid sequences. The synthesized S10a was purified by HPLC and identified by MALDI-TOF-TOF. The toxicity of S10a was measured using zebrafish, mice and cell lines. The hotplate pain model was used to investigate the analgesics activity of S10a. Results Conotoxin S10a was successfully synthesized with corrected molecular weight. S10a appear potent and longer-lasting analgesics in the hotplate pain model mice when compared to pathidine. Additionally, S10a show toxicity to zebrafish, mice in different degree. |
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