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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MALDITOF-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4种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。
OBJECTIVE To prepare the T-superfamily toxin S10a from Taro, and to evaluate its toxicity and activity. Methods The preparation of S10a was carried out by solid-phase chemical synthesis and purified by RP-HPLC. The samples were identified by MALDITOF-TOF. Toxicity of the zebrafish, mouse and cell lines to toxins was evaluated, and the analgesic activity was analyzed using a mouse hot plate model. Results The preparation of toxins by solid-phase chemical synthesis showed that the purity of the synthesized peptides was high and the molecular weight was consistent with the predicted results. S10a showed different levels of toxicity to zebrafish, mouse and four cell lines. S10a showed good analgesic activity on a mouse hot plate analgesic model, and the higher dose of S10a (0.7 mg / kg) had longer analgesic effects than the positive control, pethidine.