陰離子細胞貫穿胜肽及其用於胞內遞送的用途ANIONIC CELL PENETRATING PEPTIDE AND ITS USE FOR INTRACELLULAR DELIVERY

專利類型

發明

專利國別 (專利申請國家)

美國

專利申請案號

13/557,994

專利證號

US 8,614,194 B1

專利獲證名稱

陰離子細胞貫穿胜肽及其用於胞內遞送的用途ANIONIC CELL PENETRATING PEPTIDE AND ITS USE FOR INTRACELLULAR DELIVERY

專利所屬機關 (申請機關)

高雄醫學大學

獲證日期

2013/12/24

技術說明

自然界的細胞穿膜肽(CPP)為陽離子或兩性的短胜肽，具有穿越細胞膜及運送結合的裝載物進入細胞之能力。此發明中，陰離子性聚天門冬酸 類胜肽被證實可為CPP之一新分類。如參考胜肽 (Acp-R7)之表現，在37 和 4 oC 下，聚天門冬酸均呈現良好的細胞穿透效率及細胞吞食證據，當與螢光劑和藥物為裝載物鍵結所得的含聚天門冬酸之複合物可以顯著地被運送入細胞。並且，親脂性較親水性的聚天門冬酸具有較高的穿膜能力。 聚天門冬酸對Hela癌細胞株和人類脂肪幹細胞(ADSC)均顯示無毒性，並且其中一種聚天門冬酸在10 μΜ濃度下對Hela 之穿膜能力較Acp-R7優異。目前研究顯示，聚天門冬酸這類陰離子性CPP 乃透過macropinocytosis行為進入到細胞中。 Cell-penetrating peptides (CPPs) are cationic or amphiphilic in nature, they are short peptides capable of translocating across the plasma membrane of live cells and transporting conjugated cargos into cells. In this invention, an anionic peptide, polyaspartate, being a kind of CPP is reported. As well as the reference, hepta-arginine (Acp-R7), did, the polyaspartates perform good penetrating efficiency and cellular uptake evidence both at 37 and 4 oC. Linking with fluorescence and drug as cargos, the polyaspartate containing complex can be translocated into cells significantly. Moreover, lipophilic polyaspartate demonstrates higher penetrating abilities than hydrophilic one does. The polyaspartate presents less toxicity to HeLa cell and human adipose-derived stem cells (ADSC), moreover, one of polyaspartate possesses better transduction capacity than Acp-R7 in HeLa at 10 μΜ. The cellular uptake of polyaspartate, this anionic CPP, is happen through macropinocytosis.

備註

本部(發文號1100044017)同意貴校110年1月28日高醫產學字第1101100305號函申請終止維護專利。(高醫)

連絡單位 (專責單位/部門名稱)

智財保護與科技管理組

連絡電話

07-3138030

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