Exploring Tryptophan-based Short Peptides: Promising Candidate for Anticancer and Antimicrobial Therapies

Area of Science:

• Medicinal Chemistry
• Peptide Synthesis
• Anticancer Drug Discovery

Background:

• Ultra-short peptides offer high selectivity and low toxicity, making them valuable therapeutic agents.
• Dipeptides, tripeptides, and tetrapeptides are recognized for their anticancer potential.
• This study focuses on novel tryptophan-based peptides for cancer treatment.

Purpose of the Study:

• To synthesize and evaluate the anticancer and antibacterial properties of novel ultra-short peptides.
• To assess the efficacy of tryptophan-based peptides against cancer cell lines.
• To compare the activity of synthesized peptides with doxorubicin.

Main Methods:

• Microwave-assisted solid-phase peptide synthesis was employed to create 10 ultra-short peptides.
• In vitro antibacterial activity was screened using the agar dilution method.
• Anticancer efficacy was evaluated against HeLa and MCF-7 cell lines using HPLC, LC-MS, and NMR spectroscopy for characterization.

Main Results:

• Two synthesized peptides exhibited potent anticancer activity with IC50 values of 3.9±0.13 μM and 1.8±0.09 μM.
• These peptides demonstrated superior efficacy compared to the reference drug doxorubicin.
• Peptides 3b and 4b showed enhanced antibacterial activity, while peptides 3a, 4c, and 4d exhibited antifungal activity.

Conclusions:

• Novel tryptophan-based peptides show promising anticancer and antimicrobial activities.
• Peptides 3e and 4e were identified as highly potent anticancer agents against tested cell lines.
• The study highlights the potential of ultra-short peptides as next-generation therapeutics.