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Published on: December 1, 2020
Identification of Novel Anti- non-small cell lung cancer (NSCLC) Peptide in toad Skin（Chan Pi） Extract through
Xiaoxin Tu1, Jia Wu2, Ying Dong3
1The Second Clinical College of Guangzhou University of Chinese Medicine, Guangzhou 510120, China.
Abstract:
Toad skin (Bufo bufo gargarizans Cantor), known as Chan Pi in traditional Chinese medicine, has long been recognized for its therapeutic potential, particularly in cancer treatment. While the pharmacological activities of small molecules in toad skin such as bufadienolides have been extensively studied, peptides-another class of bioactive molecules-remain largely unexplored. In this study, we employed a peptidomics-based approach combined with in silico screening and experimental validation to identify novel bioactive peptides with potential anticancer properties from toad skin extracts. Approximately 2500 distinct peptides were identified using both database searching and de novo sequencing. Computational screening with two predictive models identified 26 candidate peptides with bioactivity scores exceeding 0.75. Among them, three peptides with potential anti-lung cancer activity were synthesized for in vitro evaluation against NSCLC cell lines, A549 and H1975. Peptide STPECLLGMWK exerts selective anti-proliferative effects on TKI resistant H1975 lung cancer cells in a dose-dependent manner. These findings provide new insights into the peptide composition of toad skin extracts and highlight their potential as a source of novel anticancer agents, laying the groundwork for future cancer therapeutics development.
Insights
Researchers explored toad skin peptides for cancer treatment. One peptide, STPECLLGMWK, showed selective anti-lung cancer effects on resistant cells, offering potential for new cancer therapeutics.
Area of Science:
- Biochemistry
- Pharmacology
- Traditional Chinese Medicine
Background:
- Toad skin (Chan Pi) is recognized in traditional Chinese medicine for cancer treatment.
- Bioactive small molecules like bufadienolides are studied, but peptides from toad skin are largely unexplored.
- Peptides represent a promising, understudied class of bioactive molecules in toad skin.
Purpose of the Study:
- To identify novel bioactive peptides with anticancer properties from toad skin extracts.
- To investigate the potential of these peptides as new anticancer agents.
- To explore the therapeutic value of peptides in traditional Chinese medicine.
Main Methods:
- Employed a peptidomics approach combined with in silico screening and experimental validation.
- Identified approximately 2500 distinct peptides using database searching and de novo sequencing.
- Synthesized three candidate peptides for in vitro evaluation against non-small cell lung cancer (NSCLC) cell lines.
Main Results:
- Identified 26 candidate peptides with high bioactivity scores (>0.75) via computational screening.
- Peptide STPECLLGMWK demonstrated selective anti-proliferative effects on TKI-resistant H1975 lung cancer cells.
- Showed dose-dependent activity, highlighting specific therapeutic potential.
Conclusions:
- Toad skin is a valuable source of novel bioactive peptides with anticancer potential.
- Peptide STPECLLGMWK shows promise for targeting resistant lung cancer.
- Findings lay the groundwork for developing new peptide-based cancer therapeutics.
