Pixantrone dimaleate induces cell death in various cancer cell lines regardless of cell cycle perturbation, with IC50 values of 37.3 nM, 126 nM, and 136 nM for T47D, MCF-10A, and OVCAR5 cells, respectively, after treatment with concentrations ranging from 0 to 10 μM for 72 hours [1]. Pixantrone dimaleate induces DNA damage at a high concentration of 500 nM after treatment for 24 hours, leading to severe chromosomal aberrations and mitotic catastrophe in PANC1 cells [1]. Pixantrone dimaleate at a concentration of 100 nM for 24 hours may interfere with chromosome segregation by generating merotelic kinetochore attachments, leading to chromosome non-disjunction [1]. Pixantrone dimaleate exhibits potent growth inhibition of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK, and ABCB1-transfected MDCK/MDR cells, with IC50 values of 0.10 μM, 0.56 μM, 0.058 μM, and 4.5 μM, respectively, after treatment with concentrations ranging from 0 to 100 μM for 72 hours [2]. Pixantrone dimaleate (0.01-0.2 μM) induces the concentration-dependent formation of linear DNA by targeting topoisomerase IIα and generates semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, possibly due to low cellular uptake [2]. Pixantrone dimaleate (0.01-10 μM) exhibits strong inhibitory effects on rat 97-116 peptide-specific T cell proliferation [4].
体内研究
Pixantrone dimaleate administered intravenously at a dose of 27 mg/kg, given every 7 days for three cycles, does not exacerbate pre-existing moderate degenerative cardiomyopathy in mice. Furthermore, it induces minimal cardiotoxicity upon repeated treatment cycles and leads to lower mortality rates compared to Mitoxantrone in mice pre-treated with Doxorubicin [3].
Pixantrone dimaleate administered intravenously at a dose of 16.25 mg/kg, given weekly for three cycles, alters the responses of lymph node cells (LNC) and affects T cell subpopulations in TAChR-immunized Lewis rats. Additionally, it demonstrates both preventive and therapeutic effects in experimental autoimmune myasthenia gravis (EAMG) rats [4].
体外研究
Pixantrone dimaleate induces cell death in various cancer cell lines regardless of cell cycle perturbation, with IC50 values of 37.3 nM, 126 nM, and 136 nM for T47D, MCF-10A, and OVCAR5 cells, respectively, after treatment with concentrations ranging from 0 to 10 μM for 72 hours [1].
Pixantrone dimaleate induces DNA damage at a high concentration of 500 nM after treatment for 24 hours, leading to severe chromosomal aberrations and mitotic catastrophe in PANC1 cells [1].
Pixantrone dimaleate at a concentration of 100 nM for 24 hours may interfere with chromosome segregation by generating merotelic kinetochore attachments, leading to chromosome non-disjunction [1].
Pixantrone dimaleate exhibits potent growth inhibition of human leukemia K562 cells, etoposide-resistant K/VP.5 cells, MDCK, and ABCB1-transfected MDCK/MDR cells, with IC50 values of 0.10 μM, 0.56 μM, 0.058 μM, and 4.5 μM, respectively, after treatment with concentrations ranging from 0 to 100 μM for 72 hours [2].
Pixantrone dimaleate (0.01-0.2 μM) induces the concentration-dependent formation of linear DNA by targeting topoisomerase IIα and generates semiquinone free radicals in an enzymatic reducing system, although not in a cellular system, possibly due to low cellular uptake [2].
Pixantrone dimaleate (0.01-10 μM) exhibits strong inhibitory effects on rat 97-116 peptide-specific T cell proliferation [4].
Pixantrone/马来酸匹衫琼 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Escherichia coli ATCC 25922
32 µg/mL
16-24 hours
Evaluate the synergistic antimicrobial activity between Pixantrone and rifampin, results showed Pixantrone significantly enhanced the antimicrobial effect of rifampin
Microbiol Spectr. 2022 Dec 21;10(6):e0211422.
Pseudomonas aeruginosa PAO1
32 µg/mL
16-24 hours
Evaluate the synergistic antimicrobial activity between Pixantrone and rifampin, results showed Pixantrone significantly enhanced the antimicrobial effect of rifampin
Microbiol Spectr. 2022 Dec 21;10(6):e0211422.
Klebsiella pneumoniae ATCC 700603
32 µg/mL
16-24 hours
Evaluate the synergistic antimicrobial activity between Pixantrone and rifampin, results showed Pixantrone significantly enhanced the antimicrobial effect of rifampin
Microbiol Spectr. 2022 Dec 21;10(6):e0211422.
Acinetobacter baumannii ATCC 19606
32 µg/mL
16-24 hours
Evaluate the synergistic antimicrobial activity between Pixantrone and rifampin, results showed Pixantrone significantly enhanced the antimicrobial effect of rifampin
Microbiol Spectr. 2022 Dec 21;10(6):e0211422.
Huh-7 cells
5 µM
36 hours
Screening for compounds inhibiting LASV genome replication, Pixantrone maleate inhibited LASV MG activity by over 90%
Viruses. 2022 Dec 30;15(1):105.
A549 cells
5 µM
48 hours
Evaluating the inhibitory effect of Pixantrone maleate on JUNV replication, IC50 value of 3.66 µM
Viruses. 2022 Dec 30;15(1):105.
Pixantrone/马来酸匹衫琼 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nu/nu mice
A549 tumor model
Tail vein injection
10 mg/kg
Injected on days 14, 17, 20, 23, and 26, continued until day 32
To evaluate the anti-tumor effect of Pix-PSL in the A549 tumor model, results showed that the Pix-PSL group had significantly better tumor growth inhibition compared to other Pix formulation groups.
Drug Deliv. 2018 Nov;25(1):1200-1212
ICR mice
Peritonitis-sepsis model and subcutaneous abscess model
Intraperitoneal injection
30 mg/kg
Single dose, observed for 7 days
Evaluate the in vivo antimicrobial efficacy of combination therapy, results showed the combination significantly improved survival rates and reduced abscess area and bacterial load
United States, Arizona
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Arizona Clinical Research Center
Tucson, Arizona, United States, 85712
United States, Arkansas
Highlands Oncology Group
Springdale, Arkansas, United States, 72764
United States, California
USC/Norris Comprehensive Cancer Center and Hospital
Los Angeles, California, United States, 90033-0800
United States, Maryland
Marlene and Stewart Greenebaum Cancer Center, University of Maryland
Baltimore, Maryland, United States, 21201
United States, Ohio
Ireland Cancer Center
Cleveland, Ohio, United States, 44106-5055
United States, Tennessee
Boston Baskin Cancer Group, University Tennessee
Memphis, Tennessee, United States, 38104
United States, Texas
University of Texas - MD Anderson Cancer Center
Houston, Texas, United States, 77030 收起 <<
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