Highly in vitro anti-cancer activity of melittin-loaded niosomes on non-small cell lung cancer cells

• Published in: Toxicon (Oxford) Vol. 241; p. 107673
• Main Authors: Honari, Pooyan, Shahbazzadeh, Delavar, Behdani, Mahdi, Pooshang Bagheri, Kamran
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.04.2024
• Subjects: Anticancer peptides; Apoptosis; bcl-2-Associated X Protein - genetics; Carcinoma, Non-Small-Cell Lung - drug therapy; Caspase 3; Humans; Liposomes; Lung Neoplasms - drug therapy; Melitten - pharmacology; Melittin; Niosomes; Non-small cell lung cancer; Venom; Anticancer peptides; Melittin; Venom; Non-small cell lung cancer; Niosomes; Apoptosis
• DOI: 10.1016/j.toxicon.2024.107673
• ISSN: 0041-0101

Development of promising medicines from natural sources, specially venom, is of highly necessitated to combat against life-threatening cancers. Non-small cell lung cancer (NSCLC) has a significant percentage of mortalities. Melittin, from bee venom, is a potent anticancer peptide but its toxicity has limited its therapeutic applications. Accordingly, this study aims to synthesize niosomes with suitable stability and capacity for carrying melittin as a drug. Additionally, it seeks to evaluate the anti-cancer activity of melittin-loaded niosomes on non-small cell lung cancer. The niosome was prepared by thin film hydration method. Cytotoxicity and apoptosis were assessed on A549, Calu-3, and MRC5 cells. Real-time PCR was used to determine expression of apoptotic and pro-apoptotic Bax, Bcl2, and Casp3 genes. Immunocytochemistry (ICC) was also used to confirm expression of the abovementioned genes. Furthermore, wound healing assay was performed to compare inhibition effects of melittin-loaded niosomes with free melittin on migration of cancer cells. IC50 values of melittin-loaded niosomes for A549, Calu-3, and MRC5 cells were respectively 0.69 μg/mL, 1.02 μg/mL, and 2.56 μg/mL after 72 h. Expression level of Bax and Casp3 increased ‘10 and 8’ and ‘9 and 10.5’ fold in A549 and Calu-3, whereas Bcl2 gene expression decreased 0.19 and 0.18 fold in the mentioned cell lines. The cell migration inhibited by melittin-loaded niosomes. Melittin-loaded niosomes had more anti-cancer effects and less toxicity on normal cells than free melittin. Furthermore, it induced apoptosis and inhibited cancer cells migration. Our results showed that melittin-loaded niosomes may be a drug lead and it has the potential to be future developed for lung cancer treatment. [Display omitted] •This tudy aimed at evaluation of anti-cancer activity of melittin-loaded niosomes on non-small cell lung cancer.•The action mechanisms of melittin-loaded niosomes were apoptosis and cell migration inhibition.•Melittin-loaded niosomes may be a drug lead and it has the potential to be future developed for lung cancer treatment.•Melittin-loaded niosomes had more anti-cancer effects and less toxicity on normal cells than free melittin.