【摘要】：設(shè)計、合成了一類新型谷胱甘肽(glutathione,GSH)和凋亡酶-3(Caspase-3)響應的環(huán)肽分子熒光探針.該類探針主要由能量共振轉(zhuǎn)移(FRET)分子熒光對、Caspase-3特異性識別多肽序列和GSH響應雙硫鍵組成,分為不含穿膜肽序列(CP)和包含穿膜肽序列(cp CP)的兩種不同環(huán)肽分子熒光探針.2種環(huán)肽分子熒光探針均能實現(xiàn)在GSH和Caspase-3同時存在情況下的精確成像,同時具有良好的響應性、特異性和高信噪比.該類環(huán)肽分子熒光探針在細胞培養(yǎng)環(huán)境中具有良好的穩(wěn)定性和生物相容性.利用該探針,可以實現(xiàn)對星形孢菌素(STS)誘發(fā)的細胞凋亡進行實時、原位的成像監(jiān)測,并對抗腫瘤藥物阿霉素(DOX)和順鉑(cisplatin)誘導的細胞凋亡進行成像.這種具有多重響應并能用于精確成像的分子熒光探針將極大地促進疾病的精確診斷.
[Abstract]:A new type of glutathione (glutathione)-3 (Caspase-3)-responsive cyclopeptide fluorescent probe was designed and synthesized. This kind of probe is mainly composed of energy resonance transfer (FRET) molecule fluorescence specific recognition polypeptide sequence of Caspase-3 and GSH responsive disulfide bond. Two kinds of cyclopeptide molecular fluorescence probes, including (CP) without transmembrane peptide sequence and (cp CP) with transmembrane peptide sequence, can achieve accurate imaging in the presence of both GSH and Caspase-3, and have good responsiveness. Specificity and high signal-to-noise ratio. This kind of cyclic peptide molecular fluorescence probe has good stability and biocompatibility in cell culture environment. The probe can be used to monitor the apoptosis induced by astrocystin (STS) in situ and to image the apoptosis induced by adriamycin (DOX) and cisplatin (cisplatin). This molecular fluorescence probe, which has multiple responses and can be used for accurate imaging, will greatly facilitate the accurate diagnosis of disease.
【作者單位】： 生物醫(yī)用高分子材料教育部重點實驗室武漢大學化學與分子科學學院;
【基金】：國家自然科學基金(基金號51690152,51233003)資助項目
【分類號】：O657.3

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