5,6-Dichlorobenzimidazole riboside (DRB) is a nucleoside analog that inhibits various carboxyl-terminal domain kinases, including casein kinase II and cell cycle-dependent kinases (CDK), and exhibits antitumor activity. It can also trigger apoptosis[1][2][3][4][5][6][7].
体内研究
5,6-Dichlorobenzimidazole riboside, administered intraperitoneally at doses of 2.0-3.0 mg/0.25 mL water twice daily for five days, does not affect the replication of the PR8 strain of influenza virus in mice[7].
体外研究
5,6-Dichlorobenzimidazole riboside, at concentrations of 10-80 µg/mL over 72 hours, induces p53-dependent apoptosis in human colon cancer cells by inhibiting RNA synthesis[5].
5,6-Dichlorobenzimidazole riboside, at 10-100 µM for 72 hours, prompts apoptosis in human MCF-7 breast cancer cells by modulating Mcl-1 and BclxL levels and activating caspase family members in both a time- and dose-dependent manner[6].
DRB 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HeLa cells
5-60 μM
15 min
DRB significantly inhibits RNA synthesis and has a stronger inhibitory effect on uridine uptake in HeLa cells compared to L cells.
J Cell Biol. 1976 May;69(2):229-40
HeLa cell extract
2-6 μM
60 minutes
To determine the inhibitory effect of DRB on RNA polymerase II-mediated transcription in vitro, results showed that DRB significantly inhibited transcription at 2-6 μM concentration.
Proc Natl Acad Sci U S A. 1982 May;79(10):3167-70
HeLa cells
4-6 μM
15-60 minutes
To determine the inhibitory effect of DRB on RNA transcription, results showed that DRB significantly inhibited RNA synthesis at 4-6 μM concentration.
Proc Natl Acad Sci U S A. 1982 May;79(10):3167-70
mouse embryos
80 μM
4 to 20 hours
To study the effect of DRB on early mouse embryo development, found that inhibition of minor ZGA resulted in embryo arrest at the two-cell stage
Proc Natl Acad Sci U S A. 2018 Jul 17;115(29):E6780-E6788
T-47D cells
75 μM
72 hours
DRB inhibited T-47D cell proliferation, but no cleavage of PARP was observed.
Sci Rep. 2023 Aug 3;13(1):12621
MCF-7 cells
75 μM
72 hours
DRB inhibited MCF-7 cell proliferation and induced apoptosis, as evidenced by increased Annexin V-positive cells, DNA fragmentation, and activation of caspase-7, caspase-9, and PARP.
Sci Rep. 2023 Aug 3;13(1):12621
HeLa cells
70 μM
1 hour
To study the effect of DRB on adenovirus transcription, it was found that DRB inhibits transcription from the major late promoter, but the synthesis of polypeptide IX mRNA is resistant to DRB.
Nucleic Acids Res. 1979 Nov 24;7(6):1405-18
Friend cells
125 μM
30 minutes
To investigate the effect of DRB on β-globin mRNA, results showed that DRB inhibited the appearance of β-globin mRNA in the cytoplasm by greater than 87%.
Nucleic Acids Res. 1981 Jul 24;9(14):3307-19
Chorioallantoic membrane cells
0.38 × 10⁻⁴ M
36 hours
To study the inhibitory effect of DRB on Lee virus replication, results showed that DRB at 0.38 × 10⁻⁴ M concentration could inhibit 75% of virus replication.
J Exp Med. 1954 Mar;99(3):227-50
DRB 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Chicken embryos and mice
Embryonated chicken eggs and mice models
Allantoic injection for chicken embryos; intraperitoneal injection for mice
Chicken embryos: 4 mg; Mice: 4 mg/day
Chicken embryos: single injection; Mice: twice daily for 48 hours
To study the inhibitory effect of DRB on Lee virus replication in vivo, results showed that DRB significantly inhibited virus replication in both chicken embryos and mice without observable toxicity.
J Exp Med. 1954 Mar;99(3):227-50
Mouse
Mouse embryos
In vitro culture
80 μM
4 to 20 hours
To study the effect of DRB on early mouse embryo development, found that inhibition of minor ZGA resulted in embryo arrest at the two-cell stage
Proc Natl Acad Sci U S A. 2018 Jul 17;115(29):E6780-E6788
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