Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
体外研究
High TOP1 enzymatic activity MCF7 (Luminal subtype) and HCC1419 (HER2 subtype) show high sensitivity toward Camptothecin (0.1 μM to 5 μM; 72 hours) treatment, exhibiting the IC50 values of 0.089 μM and 0.067 μM, respectively.
Camptothecin (0.5 μM; 6 and 24 hours) reduces desferrioxamine-activated VEGF expression.
Camptothecin (0.5 μM; 8 to 24 hours) strongly prevents the desferrioxamine-dependent HIF-1a accumulation.
Cell Viability Assay
Cell Line:
MCF7 (Luminal subtype) and HCC1419 (HER2 subtype)
Concentration:
0.1 μM to 5 μM
Incubation Time:
72 hours
Result:
High TOP1 enzymatic activity MCF7 (Luminal subtype) and HCC1419 (HER2 subtype) show high sensitivity toward CPT (0.1 μM to 5 μM; 72 hours) treatment, exhibiting the IC50 values of 0.089 μM and 0.067 μM, respectively.
RT-PCR
Cell Line:
HeLa and HEK293 cell lines
Concentration:
0.5 μmol/L
Incubation Time:
6 and 24 hours
Result:
Reduces desferrioxamine-activated VEGF expression in both cell lines after 6 and 24 hours of treatment, whereas in normoxic condition camptothecin does not affect the VEGF mRNA level.
Western Blot Analysis
Cell Line:
HeLa and HEK293 cell lines
Concentration:
0.5 μmol/L
Incubation Time:
8 to 24 hours
Result:
Strongly prevents the desferrioxamine-dependent HIF-1a accumulation after 8 to 24 hours, whereas it does not affect HIF-1b levels.
体内研究
Camptothecin (2 mg/kg every other day) treats mice, has developed numerous pulmonary metastases.
Treatment with both kinase inhibitor of nuclear factor-kappaB-1 (KINK-1) and Camptothecin led to a statistically significant reduction in the number of pulmonary metastases.
Animal Model:
C57BL6 mice (injected with B16F10 melanoma cells)
Dosage:
2 mg/kg
Administration:
every other day, after 19 days
Result:
Has developed numerous pulmonary metastases.
分子式
C20H16N2O4
分子量
348.35
CAS号
7689-03-4
中文名称
喜树碱
运输条件
Room temperature in continental US; may vary elsewhere.