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[Inhibition of angiogenesis by antitumor antibiotic C1027 and its effect on tumor metastasis]
1Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Beijing.
Objective:
To investigate the effect of C1027, an enediyne antitumor antibiotic, on angiogenesis and its anti-metastatic activity.
Methods:
Chick embryo chorioallantoic membrane assay was used for anti-angiogenesis activity and bFGF receptor binding assay was used for the elucidation of the possible mechanism. Spontaneous pulmonary metastasis of Lewis carcinoma in mice was employed to evaluate the anti-metastatic effect.
Results:
C1027 was highly potent in suppressing angiogenesis with a minimum effective dose of 0.01 microgram/egg. Enediyne chromophore moiety of the C1027 molecule was essential to anti-angiogenesis activity. Receptor binding assay showed that C1027 blocked bFGF binding to its receptor with an IC50 value of 2.3 x 10(-6) micrograms/ml. C1027 markedly inhibited pulmonary metastasis of Lewis carcinoma in mice. Compared at equitoxic dosage level (1/4 LD50), C1027 (0.01 mg/kg, i.v., x 2) was more effective than mitomycin (1.25 mg/kg, i.v., x 2) and the percent inhibition of metastatic foci in the lung was 98% and 78%, respectively.
Conclusions:
C1027 is a new potent anti-angiogenesis agent with markedly anti-metastatic activity. The mechanism of C1027 suppressing angiogenesis may be related to its blocking effect on bFGF binding to its receptor.
Insights
C1027, an enediyne antitumor antibiotic, effectively inhibits angiogenesis and metastasis. It blocks basic fibroblast growth factor (bFGF) binding to its receptor, showing potent anti-cancer properties.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Context:
- Tumor growth and metastasis rely on angiogenesis.
- Enediyne antitumor antibiotics represent a class of potent anti-cancer agents.
- Understanding the mechanisms of anti-angiogenesis and anti-metastasis is crucial for developing novel cancer therapies.
Purpose:
- To evaluate the anti-angiogenic and anti-metastatic potential of the enediyne antitumor antibiotic C1027.
- To elucidate the mechanism underlying C1027's anti-angiogenic activity, specifically its interaction with basic fibroblast growth factor (bFGF) signaling.
- To assess the efficacy of C1027 in inhibiting spontaneous pulmonary metastasis in a preclinical mouse model.
Summary:
- C1027 demonstrated significant anti-angiogenic activity in the chick embryo chorioallantoic membrane assay, with a minimum effective dose of 0.01 microgram/egg.
- The enediyne chromophore moiety of C1027 was identified as essential for its anti-angiogenic effects.
- Receptor binding assays revealed that C1027 inhibits bFGF binding to its receptor (IC50 = 2.3 x 10^-6 micrograms/ml).
- In vivo studies showed that C1027 markedly inhibited pulmonary metastasis of Lewis carcinoma in mice, achieving 98% inhibition at equitoxic doses, outperforming mitomycin.
Impact:
- C1027 emerges as a potent anti-angiogenesis agent with significant anti-metastatic capabilities.
- The findings suggest that C1027's mechanism involves blocking bFGF receptor binding, offering a novel therapeutic strategy.
- This research provides a strong foundation for the further development of C1027 as a targeted anti-cancer therapy.
