Development of a Novel Peptide with RGD Tumor Homing Motif: Evaluation of its Anticancer Potential in Hepatocellular Carcinoma and Colon Cancer Cells

Theodor Bilharz Research Institute

Bibliographic Information

Authors: Mohamed R.A.; Marie O.M.; Badran D.I.; Hammam O.A.; Ahmed H.O.

Journal: Recent Patents on Biotechnology

Publisher: Bentham Science Publishers

Publication Date: January 2025

Volume / Issue: Volume 19 / Issue 2

Pages: 128–141

ISSN: 18722083

DOI: 10.2174/0118722083300452240315035722

Scopus: View on Scopus

PubMed: 39916422

Document Type: Article

Authors and Affiliations

Mohamed R.A., Department of Chemistry, Faculty of Science, Suez Canal University, Ismailia, Egypt; Marie O.M., Department of Chemistry, Faculty of Science, Suez Canal University, Ismailia, Egypt; Badran D.I., Department of Medical Biochemistry, Faculty of Medicine, Suez Canal University, Ismailia, Egypt; Hammam O.A., Department of Pathology, Theodor Bilharz Research Institute, Giza, Egypt; Ahmed H.O., Department of Biochemistry and Molecular Biology, Theodor Bilharz Research Institute, Giza, Egypt

Abstract

Background: Peptide-based therapy has emerged as a promising avenue for treating various disorders, and recent research has highlighted the potential of anti-cancer peptides (ACPs) in cancer treatment. In this context, this study aimed to design a novel peptide incorporating a tumor-homing peptide (RGD) and C-amidation to enhance its anticancer activity, particularly against liver (HepG2) and colon (HCT-116) cancer cell lines. Objectives: The primary objective was to design a peptide with improved anticancer properties by leveraging the tumor-homing capabilities of RGD and enhancing its activity through C-amidation. The study sought to evaluate the cytotoxicity of the designed peptide against red blood cells (RBCs) and normal Vero cells. Furthermore, the anticancer efficacy of the peptide was assessed in hepatocellular carcinoma (HepG2) and colon cancer (HCT-116) cell lines. The specific objectives included examining the apoptot-ic induction and morphological changes in treated cells compared to untreated cells. Methods: The peptide was designed using the ACPred-FL bioinformatics tool, and its cytotoxicity was assessed through hemolysis assays against RBCs and normal Vero cells. Anticancer activity was evaluated against HepG2 and HCT-116 cell lines. The analysis of apoptotic induction involved measuring the relative gene expression of oncogenic marker BCL2 and apoptotic markers (BAX, BID, CAS-8). Additionally, Cytopathologi-cal examination and Western Blot analysis were employed to study morphological changes and confirm the quantification of relevant markers. Results: The designed peptide, consisting of twelve amino acids with a molecular mass of 1230.6233 Da and an isoelectric point of 9.81, exhibited low erythrocyte lysis and minimal toxicity to normal cells. The IC50 values demonstrated significant anticancer activity against both HepG2 (36.49±2.6 µg/mL) and HCT-116 (11.03±2.5 µg/mL) cell lines. Treated cells exhibited a significant decrease in the oncogenic marker BCL2 and an upregulation of apoptotic markers (BAX, BID, CAS-8). Western Blot analysis confirmed these results in addition to cytopathological examination that scattered apoptotic and de-generative changes. Conclusion: The designed peptide is considered a patent product that displayed remarkable anticancer activity against hepatocellular carcinoma and colon cancer cell lines, effectively modulating apoptotic and oncogenic markers. These findings highlight the potential of the peptide as a therapeutic agent for cancer treatment, emphasizing its clinical significance in combating liver and colon cancers. Nonetheless, further research and development are war-ranted to explore the translational potential of this peptide in clinical studies. © 2025 Bentham Science Publishers.

Keywords

ACPs; apoptosis; colon cancer; hepatocellular carcinoma; Peptide; tumor homing peptide; Animals; Antineoplastic Agents; Carcinoma, Hepatocellular; Chlorocebus aethiops; Colonic Neoplasms; HCT116 Cells; Hemolysis; Hep G2 Cells; Humans; Liver Neoplasms; Oligopeptides; Patents as Topic; Vero Cells; Amino acids; Cell culture; Cell death; Oncology; Peptides; antineoplastic agent; caspase 8; cisplatin; doxorubicin; glyceraldehyde 3 phosphate dehydrogenase; protein Bax; protein bcl 2; protein Bid; unclassified drug; arginyl-glycyl-aspartic acid; oligopeptide; Anti-cancer peptide; Anticancer activities; Apoptotic; Cell lines; Homing peptide; Novel peptides; Oncogenics; amidation; amino acid sequence; animal cell; antineoplastic activity; Article; bioinformatics; cell viability; controlled study; cytopathology; cytotoxicity; gene expression; gene expression level; HCT 116 cell line; Hep-G2 cell line; human; human cell; IC50; liver cell carcinoma; nonhuman; polyacrylamide gel electrophoresis; real time polymerase chain reaction; RNA extraction; spectrophotometry; Vero cell line; Western blotting; animal; chemistry; colon tumor; drug effect; drug therapy; liver tumor; metabolism; patent; pathology

Citation Information

Scopus Citations: 3

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