Medicinal applications and molecular targets of dequalinium chloride.
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Bailly C
Medicinal applications and molecular targets of dequalinium chloride.
Biochem Pharmacol. 2021 Apr;186:114467. doi: 10.1016/j.bcp.2021.114467. Epub 2021 Feb 10.
- PubMed ID
- 33577890 [ View in PubMed]
- Abstract
For more than 60 years dequalinium chloride (DQ) has been used as anti-infective drug, mainly to treat local infections. It is a standard drug to treat bacterial vaginosis and an active ingredient of sore-throat lozenges. As a lipophilic bis-quaternary ammonium molecule, the drug displays membrane effects and selectively targets mitochondria to deplete DNA and to block energy production in cells. But beyond its mitochondriotropic property, DQ can interfere with the correct functioning of diverse proteins. A dozen of DQ protein targets have been identified and their implication in the antibacterial, antiviral, antifungal, antiparasitic and anticancer properties of the drug is discussed here. The anticancer effects of DQ combine a mitochondrial action, a selective inhibition of kinases (PKC-alpha/beta, Cdc7/Dbf4), and a modulation of Ca(2+)-activated K(+) channels. At the bacterial level, DQ interacts with different multidrug transporters (QacR, AcrB, EmrE) and with the transcriptional regulator RamR. Other proteins implicated in the antiviral (MPER domain of gp41 HIV-1) and antiparasitic (chitinase A from Vibrio harveyi) activities have been identified. DQ also targets alpha -synuclein oligomers to restrict protofibrils formation implicated in some neurodegenerative disorders. In addition, DQ is a typical bolaamphiphile molecule, well suited to form liposomes and nanoparticules useful for drug entrapment and delivery (DQAsomes and others). Altogether, the review highlights the many pharmacological properties and therapeutic benefits of this old 'multi-talented' drug, which may be exploited further. Its multiple sites of actions in cells should be kept in mind when using DQ in experimental research.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Dequalinium Alpha-synuclein Protein Humans UnknownModulatorDetails Dequalinium Calmodulin Protein Humans UnknownAntagonistDetails Dequalinium Protein kinase C (Protein Group) Protein group Humans UnknownInhibitorDetails Dequalinium Response regulator RamR Protein Streptomyces coelicolor (strain ATCC BAA-471 / A3(2) / M145) UnknownRegulatorDetails Dequalinium Small conductance calcium-activated potassium channel protein 3 Protein Humans UnknownBlockerDetails - Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Dequalinium Acriflavine resistance protein B Protein Escherichia coli (strain K12) UnknownSubstrateDetails