本研究以 Polyglycerol dendrimer (PGD) 代數二 (G2) 和代數三 (G3) 作為起始劑，
與 Z-L-Lysine (ZLL) NCAs 進行開環聚合反應，在去除保護基後，成功合成十二枝
化、二十四枝化的星狀聚賴胺酸 (Poly(L-lysine), PLL)，進一步在側鏈接枝肉桂醛、
香蘭醛和茴香醛三種天然醛類疏水性官能基，鑑定分析聚胺酸之平均聚合度、接枝
比和分子量，設計一系列不同特性的陽離子型星狀聚胺酸，應用於基因之傳遞載體
和抗癌藥物。由體外細胞實驗中，可以知道雖然接枝疏水基團能增加細胞對載體的
攝取率，卻也發現其導致的溶血率和細胞毒性相對較高。基因傳遞載體的應用中，
將帶正電的星狀聚胺酸與帶負電的環狀的去氧核醣核酸，經由靜電作用力進行穩定
複合，同時還分析複合物的粒徑大小和形態，並透過載體將環狀的去氧核醣核酸送
入細胞內進行表達，得知星狀聚賴胺酸在接枝醛基後能顯著的提升轉染效率，尤其
於接枝香蘭醛中的轉染效率為最高。其次，在陽離子型星狀聚胺酸作為抗癌藥物的
應用中，研究透過傷口癒合性試驗分析星狀聚胺酸對癌細胞的遷移率，篩選出星狀
聚賴胺酸接枝香蘭醛可對癌細胞的遷移具有最高的抑制效果，進一步由光學影像觀
察癌細胞凋亡時的外觀變化，發現聚胺酸上之陽離子可選擇性的破壞癌細胞膜，使
癌細胞通透性增加，造成細胞腫脹，同時也利用螢光染色的方式分析癌細胞凋亡時
出現的細胞膜不連續、碎裂與染色質凝聚，當癌細胞在星狀聚賴胺酸接枝香蘭醛中
作用一小時，即可誘導胱天蛋白酶-3、-9 活化，引發癌細胞凋亡。綜上所述，星狀
聚賴胺酸在接枝香蘭醛後，期望可以作為潛在的新型合成性基因載體，或作為單一
的抗癌性藥物，運用於未來生物醫學領域中。

Polyglycerol dendrimer generation two and generation three (PGD G2 and PGD G3) were used to serve as initiators to synthesize 12-armed and 24-armed star-shaped poly(L-lysine) (G2-PLL and G3-PLL) via ring opening polymerization (ROP). Three different natural aldehydes which were cinnamaldehyde (CA), vanillin (VA) and 4-methoxybezaldehyde (MA) respectively were grafted on PLL. Average polymerization and grafted efficiency of polypeptides were identified and calculated by nuclear magnetic resonance spectroscopy (NMR) and gel permeation chromatography (GPC). A series cationic star-shaped polypeptides were successfully designed to evaluate the gene delivery vectors and anticancer agent application. As we know, hydrophobic group can promote cellular uptake, however, it will cause hemolysis and cytotoxicity in vitro. Cationic polypeptides served as gene delivery vectors were able to form stable complexes with deoxyribonucleic acid plasmids (pDNA). Delivery of pDNA into cells through a vector significantly elevated transfection efficiency when PLL grafted with aldehyde group, especially in G3-PLL9-g-VA0.25. Polypeptides serve as anticancer agents to inhibit migration of cancer cells, and it was found that G3-PLL9-gVA0.25 have the highest efficiency. Cationic polypeptides have ability to increase the permeability of the cancer cells and cause the cells swelling. G3-PLL9-g-VA0.25 caused cancer cell membrane discontinuity and fragmentation, besides, it also led to chromatin condensation, and induce apoptosis by activating caspase-3 and caspase-9. Above all, G3-PLL9-g-VA0.25 can be a potential gene vectors and anticancer agents applied in biomedical field in the future.

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