Rahmani Danial, Taheri Ramezan Ali, Moosazadeh Moghaddam Mehrdad
Tissue Engineering and Regenerative Medicine Research Center, Baqiyatallah University of Medical Sciences, Tehran, Iran.
Nanobiotechnology Research Center, Baqiyatallah University of Medical Sciences, Tehran, Iran.
Amino Acids. 2025 Jan 25;57(1):12. doi: 10.1007/s00726-024-03438-x.
In recent years, the use of cationic peptides as alternative drugs with anticancer activity has received attention. In this study, the targeted release of curcumin (Cur) and CM11 peptide alone and together against hepatocellular carcinoma (HCC) was evaluated using chitosan nanoparticles (CS NPs) coated with Pres1 that target the SB3 antigen of HCC cells (PreS1-Cur-CM11-CS NPs). SB3 protein is the specific antigen of HCC and the PreS1 peptide is a part of the hepatitis B antigen, which can specifically bind to the SB3 protein. Chitosan was used to prepare NPs. To Cur and CM11 loading, drugs were added to the CS solution in appropriate concentrations. Pres1 was coupled to the surface of the NPs using EDC catalyst to target NPs against HepG2 cells. SEM and DLS analysis confirmed that the PreS1-Cur-CM11-CS NPs had a size of about 132 nm, the ideal size for penetrating the cell membrane. The loading of Cur and CM11 was equal to 87% and 65%, respectively, which had a sustained and better release in the acidic environment than in the physiological environment. The MTT assay showed that PreS1-Cur-CM11-CS NPs act in a targeted and specific manner with the highest toxicity on the HepG2 cells compared to the control by a decrease in viability of about 26% after 48 h based on cell apoptosis. The results showed that PreS1-Cur-CM11-CS NPs are capable of targeted and specific drug release against HepG2 cancer cells and have significant potential to fight this cancer.
近年来,阳离子肽作为具有抗癌活性的替代药物受到关注。在本研究中,使用包被有靶向肝癌细胞(HCC)SB3抗原的前S1蛋白(PreS1-Cur-CM11-CS NPs)的壳聚糖纳米粒(CS NPs)评估了姜黄素(Cur)和CM11肽单独及联合对肝癌的靶向释放。SB3蛋白是肝癌的特异性抗原,前S1肽是乙肝抗原的一部分,可特异性结合SB3蛋白。用壳聚糖制备纳米粒。为了负载Cur和CM11,将药物以适当浓度加入CS溶液中。使用EDC催化剂将前S1蛋白偶联到纳米粒表面,使纳米粒靶向HepG2细胞。扫描电子显微镜(SEM)和动态光散射(DLS)分析证实,PreS1-Cur-CM11-CS NPs的尺寸约为132nm,这是穿透细胞膜的理想尺寸。Cur和CM11的负载量分别为87%和65%,在酸性环境中比在生理环境中具有持续且更好的释放效果。MTT试验表明,PreS1-Cur-CM11-CS NPs以靶向和特异性方式发挥作用,与对照组相比,对HepG2细胞的毒性最高,基于细胞凋亡,48小时后细胞活力降低约26%。结果表明,PreS1-Cur-CM11-CS NPs能够对HepG2癌细胞进行靶向和特异性药物释放,具有对抗这种癌症的巨大潜力。