一种新型设计肽作为药物载体的潜在应用研究

Application research of a novel peptide designed as a potential carrier

目前有大量关于全程电荷匹配设计肽的应用的研究,但是关于半程电荷匹配设计肽作为药物的应用研究却未见报道.本文对新型设计的半程电荷匹配肽P9(AC-Pro-Ser-Phe-Asn-Phe-Lys-Phe-Glu-Pro-NH2)的研究发现,P9可以成功地将作为疏水药物模型的芘稳定悬浮于水溶液中.大豆卵磷脂微囊被用以模拟细胞膜.荧光数据显示芘可以借助P9的包埋作用以晶体状态存在于水溶液中.并且当包埋体加入到脂质体微囊体系中时,芘可以从P9的包埋体系中以分子形态释放到膜的脂质层内.实验发现当包埋于芘上的P9较多,包埋壁较厚,芘的释放速度相对变缓.我们可以利用这一特性,通过调节加入的P9的浓度来控制包埋于芘上P9的厚度,从而控制芘的释放速率.研究表明,具有半程电荷匹配性质的P9肽可以作为运载疏水药物的载体.

While a great deal of research has focused on the application of full-sequence ionic complementary peptide, detection of the capability of half-sequence ionic complementary peptide such as drug carriers, is rarely reported. This paper presents that the half-sequence ionic complementary peptide P9 （AC-Pro- Ser-Phe-Asn-Phe- Lys-Phe-Glu-Pro-NH2） can successfully stabilize a model hydrophobic drug pyrene in the aqueous solution. Soybean lecithin vesicles were used to mimic plasma membranes. Fluorescence data show that the pyrene is presented in the crystalline form when stabilized by P9 solution, and molecularly migrated from its peptide encapsulations into the membrane bilayers when the suspension is mixed with lipidosome vesicles. Slower release was observed when thicker coating was applied onto pyrene, which could be to control the wall thickness coating the cargo, and consequently the release rate. The result indicated that P9, with half-sequence ionic complement, may serve as a hydrophobic compounds carrier.