Camptothecin (CPT) 是一种生物碱，作为 DNA 拓扑异构酶 I (Topo I) 抑制剂，IC50 为 679 nM。它对结直肠癌、乳腺癌、肺癌和卵巢癌表现出强效的抗肿瘤活性，并通过改变人类癌细胞中的微小 RNA (miRNA) 表达模式来调节缺氧诱导因子 1α (HIF-1α) 活性。
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Camptothecin (CPT), an alkaloid, acts as an inhibitor for DNA topoisomerase I (Topo I) with an IC50 value of 679 nM[1]. Demonstrating significant antitumor effects on colorectal, breast, lung, and ovarian cancers, CPT also affects the activity of hypoxia-inducible factor-1α (HIF-1α) by altering the patterns of microRNAs (miRNA) expression in human cancer cells[2].[3].
体内研究
Administering Camptothecin (2 mg/kg every other day) to mice presenting extensive pulmonary metastases resulted in a significant reduction of these metastases when combined with the kinase inhibitor of nuclear factor-kappaB-1 (KINK-1)[5].
体外研究
MCF7 (Luminal subtype) and HCC1419 (HER2 subtype) cells, characterized by elevated TOP1 enzyme activity, are particularly susceptible to Camptothecin treatment (ranging from 0.1 μM to 5 μM over 72 hours), showing IC50 values of 0.089 μM and 0.067 μM, respectively[4].
A dosage of Camptothecin at 0.5 μM for 6 and 24 hours notably decreases the expression of VEGF activated by desferrioxamine. Furthermore, Camptothecin administration (0.5 μM; 8 to 24 hours) effectively inhibits the accumulation of HIF-1α induced by desferrioxamine[2].
Camptothecin/喜树碱 细胞实验
Cell Line
Concentration
Treated Time
Description
References
CCRF-CEM SLFN11-del and parental cells
100 nM
4 hours
Short treatments with CPT (4 hours) induced potent inhibition of DNA replication regardless of SLFN11
Mol Cell. 2018 Feb 1;69(3):371-384.e6.
K562
100 nM
24 hours
Evaluate cytotoxicity of CPT on K562 cells
Proc Natl Acad Sci U S A. 2021 Feb 9;118(6):e2015654118.
HEK293
100 nM
24 hours
Evaluate cytotoxicity of CPT on HEK293 cells
Proc Natl Acad Sci U S A. 2021 Feb 9;118(6):e2015654118.
DMS114
100 nM
24 hours
Evaluate cytotoxicity of CPT on DMS114 cells
Proc Natl Acad Sci U S A. 2021 Feb 9;118(6):e2015654118.
CCRF-CEM
100 nM
24 hours
Evaluate cytotoxicity of CPT on CCRF-CEM cells
Proc Natl Acad Sci U S A. 2021 Feb 9;118(6):e2015654118.
DU145 SLFN11 KO
100 nM
24 hours
Evaluate cytotoxicity of CPT on SLFN11 KO cells
Proc Natl Acad Sci U S A. 2021 Feb 9;118(6):e2015654118.
Mouse embryonic fibroblasts (MEFs)
1 μM
1 hour
Used to study CPT-induced DNA double-strand breaks (DSBs) repair. Results showed that Exo1−/− and Exo1DA/DA MEFs had significantly reduced co-localization of activated pRPA-S4/S8 and γH2AX, indicating the critical role of EXO1 nuclease activity in DSB repair.
Nucleic Acids Res. 2022 Aug 12;50(14):8093-8106
HEK293 cells
50 nM
1 h
To analyze the direct effects of PrimPolS538A at the replication fork, a DNA fiber assay was used to assess ongoing replication after UV damage. Despite increased UV-C sensitivity, both PrimPolS538A and PrimPolS538E had minimal effect on fork stalling, suggesting that the genotoxic effects of PrimPolS538A may be initiated outside of S phase replication.
Sci Adv. 2021 Dec 3;7(49):eabh1004.
U2OS cells
1 µM
1 h
To assess the impact of USP21 knockdown on BRCA2 protein levels, results showed that USP21 knockdown led to a significant reduction in BRCA2 protein levels
Nat Commun. 2017 Jul 26;8(1):137.
MEFs
30 nM
24 h
To evaluate the effect of Camptothecin-induced single-strand breaks converted into double-strand breaks during DNA replication and observe RAD51 foci formation. Results showed that 30 nM Camptothecin treatment for 24 h resulted in RAD51 foci formation in Brca2LP/LP and Brca2LP/KO MEFs, indicating that BRCA2-DSS1 interaction is dispensable for RAD51 loading when homologous DNA is close during DNA replication.
Nat Commun. 2022 Apr 1;13(1):1751.
A431 cells
10 μM
6 h
Induced apoptosis and enhanced ectodomain shedding of Dsg2, resulting in accumulation of the 95 kDa fragment.
Oncogene. 2012 Mar 29;31(13):1636-48.
A549 cells
5 µM
24 h
To evaluate the apoptosis induced by Camptothecin, the results showed that Camptothecin significantly induced apoptosis but did not lead to the degradation of the telomeric G-overhang.
Nucleic Acids Res. 2005 Apr 14;33(7):2192-203.
HT1080 cells
2.5-50 nM
24 h
To evaluate the potentiation of cytotoxicity of DNA damaging agents by CRT0044876. Results showed that CRT0044876 did not potentiate the cytotoxicity of Camptothecin.
Nucleic Acids Res. 2005 Aug 19;33(15):4711-24.
Jurkat cells
2 μM and 20 μM
0, 1, 2, 3, 4, 5 h
Comparing the efficacy of ApoqPCR with other apoptosis quantifiers, the results showed that ApoqPCR was more sensitive in detecting and distinguishing low levels of apoptosis, and could more clearly resolve values at higher levels of apoptosis.
Nucleic Acids Res. 2012 Aug;40(15):e113.
PBMC
0 to 0.2 μM, in 0.02 μM increments
3.5 h
Evaluating the sensitivity of ApoqPCR in low-level apoptosis changes, the results showed that ApoqPCR has an advantage in detecting low-level apoptosis changes.
Nucleic Acids Res. 2012 Aug;40(15):e113.
Camptothecin/喜树碱 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c mice
4T1.2 breast cancer model
Intravenous injection
5 mg/kg
Evaluate the distribution and antitumor efficacy of PEG 5K-Fmoc-VE 2/CPT-S-S-VE in tumor tissues
Biomaterials. 2015 Sep;62:176-87
CD-1 mice
Oral administration model
Oral
5 mg/kg
Single dose, lasting 8 hours
To evaluate the enhancement effect of PAMAM dendrimers on the oral absorption of Camptothecin, results showed that both PAMAM G4.0 and G3.5 increased the oral absorption of Camptothecin, enhancing its concentration in blood and liver.
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