β-Lapachone functions as a topoisomerase I inhibitor. At a concentration of 25 μM, β-Lapachone inhibits camptothecin-induced DNA cleavage [1]. Lapachone (at concentrations ranging from 10 to 40 μM) significantly diminishes the colony-forming ability of CHO cells and demonstrates cytotoxicity during the S phase. Additionally, β-Lapachone induces substantial DNA strand breaks in CHO cells at concentrations exceeding 10 μM [2]. β-Lapachone (10 μM) inhibits JCPyV replication in IMR-32 cells. β-Lapachone at 1.0 μM significantly impacts JCPyV propagation in JCI cells. Moreover, β-Lapachone at concentrations ranging from 0.01 to 0.1 μM inhibits VP1 production in JCI cells [4].
体内研究
β-Lapachone (0.066%) mitigates cisplatin-induced renal injury, and its combination with cisplatin enhances this effect in mice. Additionally, β-Lapachone increases the expression of the Mre11-Rad50-Nbs1 (MRN) complex in mice [3].
体外研究
β-Lapachone functions as a topoisomerase I inhibitor. At a concentration of 25 μM, β-Lapachone inhibits camptothecin-induced DNA cleavage [1].
Lapachone (at concentrations ranging from 10 to 40 μM) significantly diminishes the colony-forming ability of CHO cells and demonstrates cytotoxicity during the S phase. Additionally, β-Lapachone induces substantial DNA strand breaks in CHO cells at concentrations exceeding 10 μM [2].
β-Lapachone (10 μM) inhibits JCPyV replication in IMR-32 cells. β-Lapachone at 1.0 μM significantly impacts JCPyV propagation in JCI cells. Moreover, β-Lapachone at concentrations ranging from 0.01 to 0.1 μM inhibits VP1 production in JCI cells [4].
β-Lapachone/β-拉帕醌 细胞实验
Cell Line
Concentration
Treated Time
Description
References
BT549
0.5 μM
48 h
β-lapachone significantly enhanced the sensitivity of BT549 cells to phenformin, reducing tumor cell proliferation.
Nat Commun. 2021 Jun 3;12(1):3299.
BT474
1.0 μM
48 h
β-lapachone significantly enhanced the sensitivity of BT474 cells to phenformin, reducing tumor cell proliferation.
Nat Commun. 2021 Jun 3;12(1):3299.
MDA-MB-231
0.5 μM
48 h
β-lapachone significantly enhanced the sensitivity of MDA-MB-231 cells to phenformin, reducing tumor cell proliferation.
Induced apoptosis, observed 180-200 bp oligonucleosome DNA laddering and apoptotic cells via flow cytometry
Cancer Res. 1995 Sep 1;55(17):3706-11.
MDA-MB-231 cells
10 μM
2 h
To evaluate the effect of β-Lapachone on PP-InsP levels in NQO1-deficient cells, the results showed that β-Lapachone did not affect 5-PP-InsP5 levels but significantly reduced ATP levels.
Proc Natl Acad Sci U S A. 2023 Aug 22;120(34):e2306868120.
HCT116 cells
2.5 μM, 5 μM, or 10 μM
2 h
To evaluate the effect of β-Lapachone on PP-InsP levels, the results showed that β-Lapachone dose-dependently decreased PP-InsP levels, while InsP6 levels remained stable.
Proc Natl Acad Sci U S A. 2023 Aug 22;120(34):e2306868120.
MDA-MB-231 cells
10 μM
2 h
In MDA-MB-231 cells, which lack NQO1, β-lapachone did not reduce PP-InsP levels, but ATP levels dropped significantly.
Proc Natl Acad Sci U S A. 2023 Aug 22;120(34):e2306868120.
MDA-MB-231 breast cancer cells
6 μM
2 h
To evaluate the cytotoxicity of β-Lapachone micelles on NQO1-overexpressing cells, results showed more than 50% cell death in NQO1+ cells at a 6 μM dose.
J Control Release. 2007 Oct 8;122(3):365-74.
DU-145 prostate cancer cells
6 μM
2 h
To evaluate the cytotoxicity of β-Lapachone micelles on NQO1-overexpressing cells, results showed more than 50% cell death in NQO1+ cells at a 6 μM dose.
J Control Release. 2007 Oct 8;122(3):365-74.
H596 non-small cell lung cancer cells
5 μM, 10 μM
2 h
To evaluate the cytotoxicity of β-Lapachone micelles on NQO1-overexpressing cells, results showed 26% and 85% cell death in NQO1+ cells at 5 μM and 10 μM doses, respectively.
J Control Release. 2007 Oct 8;122(3):365-74.
shNQO1 A549 cells
10 μM
4 h
In shNQO1 A549 cells, β-lap had a weaker inhibitory effect on NF-κB, indicating that NQO1 plays a crucial role in β-lap-mediated suppression of NF-κB activation.
Exp Mol Med. 2010 May 31;42(5):327-34.
A549 human lung cancer cells
10 μM
4 h
Suppressed radiation-induced NF-κB activation, almost completely abrogated NF-κB DNA binding activity, and inhibited the transcription of NF-κB target genes.
Exp Mol Med. 2010 May 31;42(5):327-34.
IMR-90 fibroblasts
>40 µM
IMR-90 fibroblasts were resistant to the cytotoxic effects of β-Lapachone.
Proc Natl Acad Sci U S A. 2007 Jul 10;104(28):11832-7.
A549 NSCLC cells
2.5 µM
2 h
β-Lapachone killed A549 cells in an NQO1-dependent manner, inducing ROS formation, DNA damage, PARP-1 hyperactivation, NAD+/ATP depletion, and apoptosis.
Proc Natl Acad Sci U S A. 2007 Jul 10;104(28):11832-7.
H596 NSCLC cells
4 µM
2 h
β-Lapachone killed NSCLC cells in an NQO1-dependent manner, inducing ROS formation, DNA damage, PARP-1 hyperactivation, NAD+/ATP depletion, and apoptosis.
Proc Natl Acad Sci U S A. 2007 Jul 10;104(28):11832-7.
CHEF/18A cells
4 μM
5 h
β-Lapachone inhibited potentially lethal DNA damage repair (PLDR) processes, thereby reducing x-ray-induced cell transformation. At equivalent survival levels, β-Lapachone treatment resulted in an 8-fold decrease in transformation frequency.
Proc Natl Acad Sci U S A. 1989 Jul;86(13):4963-7.
β-Lapachone/β-拉帕醌 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
MDA-MB-231 mammary tumor model
Intraperitoneal injection
25 mg/kg
Β-lapachone every 2 days, phenformin daily, continuous treatment
Combined β-lapachone and phenformin treatment significantly inhibited MDA-MB-231 mammary tumor growth and increased oxidative damage in mammary tumors.
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