Department of Chemistry and Center of Excellence for Innovation in Chemistry (PERCH-CIC), Faculty of Science, Ramkhamhaeng University, Bangkapi, Bangkok, 10240 Thailand.
Bodindecha (Sing Singhaseni) School, 40 Ramkhamhaeng 43/1, Plabpla Wangthonglang, Bangkok, 10310 Thailand.
Org Biomol Chem. 2023 Mar 1;21(9):1967-1979. doi: 10.1039/d2ob02129c.
T-shaped spermine-based cationic lipids with identical and nonidentical hydrophobic tails having variable carbon lengths (from C10 to C18) were designed and synthesized. These lipids were characterized, and their structure-activity relationships were determined for DNA binding and transfection ability of these compounds when formulated as cationic liposomes. These liposomes were then applied as non-viral vectors to transfect HEK293T, HeLa, PC3, H460, HepG2, and Calu'3 cell lines with plasmid DNA encoding the green fluorescent protein. ST9, ST12 and ST13 with nonidentical tails could deliver DNA into HEK293T cells up to 60% under serum-free conditions. The lipid ST15 bearing nonidentical tails was found to be a potent gene transfer agent under 40% serum conditions in HEK293T and HeLa cells. Besides their low cytotoxicity, these lipoplexes also exhibited greater transfection efficiency than the commercially available transfection agent, Lipofectamine 3000.
设计并合成了具有相同和不同疏水尾部且碳链长度（从 C10 到 C18）可变的 T 形 spermine 阳离子脂质。对这些脂质进行了表征，并确定了它们作为阳离子脂质体的 DNA 结合和转染能力的结构-活性关系。然后，将这些脂质体用作非病毒载体，用编码绿色荧光蛋白的质粒 DNA 转染 HEK293T、HeLa、PC3、H460、HepG2 和 Calu'3 细胞系。带有不同尾部的 ST9、ST12 和 ST13 在无血清条件下可将 DNA 递送至 HEK293T 细胞中达 60%。在 HEK293T 和 HeLa 细胞中，带有不同尾部的脂质 ST15 在 40%血清条件下是一种有效的基因转移剂。除了低细胞毒性外，这些脂质体与市售转染试剂 Lipofectamine 3000 相比，还表现出更高的转染效率。
