Targeted delivery of melittin to cancer cells by AS1411 anti-nucleolin aptamer |
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| Authors: | Seyed Hossein Rajabnejad Ahad Mokhtarzadeh Khalil Abnous Seyed Mohammad Taghdisi Mohammad Ramezani |
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| Affiliation: | 1. Pharmaceutical Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran;2. Research Institute of Food Science and Technology, Mashhad, Iran;3. Immunology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran;4. Department of Biotechnology, Higher Education Institute of Rab-Rashid, Tabriz, Iran;5. Targeted Drug Delivery Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran |
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| Abstract: | Melittin, a small water-soluble cationic amphipathic α-helical linear peptide, consisted of 26 amino acids, is the honeybee venom major constituent. Several reports have proved the lytic and apoptotic effects of melittin in several cancerous cell lines. In this study, we aimed to fabricate an AS1411 aptamer–melittin to specifically deliver melittin to nucleolin positive cells (A549). Melittin was covalently attached to antinucleolin aptamer (AS1411) and its toxicity in A549 (nucleolin positive) and L929 (nucleolin negative) was studied using MTT and Annexin V flow cytometry methods. Aptamer–melittin conjugate formation was confirmed by gel electrophoresis. Hemolytic effect of aptamer–melittin conjugate was compared to melittin alone. The aptamer–melittin conjugate showed efficient cell uptake and was more cytotoxic in A549 cells than melittin (p?in vitro. This system can reduce the cytotoxic effects of melittin on cells with no nucleolin receptor overexpression which comprise most of normal cells such as L929 cells. |
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| Keywords: | Cancer aptamer targeted delivery system melittin |
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