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MA Kailun¹,GU Jiwei²,YAN Chengyun¹

(1. College of Pharmaty, Guilin Medical University, Guilin 541199, China; 2. The First Affiliated Hospital ofJiamusi University, Jiamusi 154000,China)

AbstractObjective To construct a nucleus-targeted nanocarrier ( NLS-KALA-SA, NKSN ) consisting of fusionpeplide KALA, nuclear localization signal( NLS) and stearie acid( SA ). Methods The polypeptide nanocarrier NS.KAL.A-SA was synthesized by Fmoc solid phase synthesis method. Results The NlS-KALA-SA nanoparticles werespherical shaped with an average size of (76.4+7.6) mm and a Zeta potential of ( 43.7+5.8 ) mV. The diameter ofnanoparticles follows a normal distribution, with a narrow particle size distribution and a polydispersity index ( Pl )(Pl<0.3 ). The results of cellular uptake study showed that NLS-KALA-SA nanoparticle loaded with coumarin-6(C6) ( C6/NKSN ) was predominantly aecumulated in the nucleus of A549 cells. The results of cellular toxicityexperiments showed that NLS-KALA-SA was almost no cytotoxic to A549 cells at all tested concentrations range of 0.01-1 000 mg/ml. Conclusion 'The results demonstrate that the NLS-KALA-SA is safe and non-toxic nanocarrierwith transmembrane transport and nuclear localization functions, which is expected to become a promising peptidenanocarrier for caneer treatment.

Keywords: nuclear localization signal; KALA peptide; nanoparticles; nucleus-targeted; lung cancer

DOI:10.19296/j.cnki.1008-2409.2024-02-009

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