Medicinal applications and molecular targets of dequalinium chloride.

Article Details

Citation

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
DrugTargetKindOrganismPharmacological ActionActions
DequaliniumAlpha-synucleinProteinHumans
Unknown
Modulator
Details
DequaliniumCalmodulinProteinHumans
Unknown
Antagonist
Details
DequaliniumProtein kinase C (Protein Group)Protein groupHumans
Unknown
Inhibitor
Details
DequaliniumResponse regulator RamRProteinStreptomyces coelicolor (strain ATCC BAA-471 / A3(2) / M145)
Unknown
Regulator
Details
DequaliniumSmall conductance calcium-activated potassium channel protein 3ProteinHumans
Unknown
Blocker
Details
Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
DequaliniumAcriflavine resistance protein BProteinEscherichia coli (strain K12)
Unknown
Substrate
Details