Abstract
Quinacrine (QC), a synthetic drug belonging to the 9-aminoacridine family, has been used extensively to treat malaria and multiple ailments over the past several decades. Following its discovery in the 1920s and extensive use for the treatment of malaria for nearly two decades, numerous studies have explored its antineoplastic potential in both preclinical and clinical settings. Multiple studies spanning over seven decades have examined a wide range of QC anticancer activities across various types of cancers, along with the underlying mechanisms. Many of these mechanisms, including activation of the p53 signaling cascade and simultaneous NF-κB signaling inhibition, have been reported in various studies, bringing QC to a unique polypharmacological category drug possessing the potential to treat a wide variety of diseases, including cancer. This article summarizes most of the research conducted over several decades to uncover new molecular mechanisms activated or inactivated and directly correlate with antineoplastic activity QC.
Highlights
Quinacrine (IUPAC name: 4-N-(6-chloro-2-methoxyacridin-9-yl)-1-N,1-N-diethylpentane1,4-diamine) is a synthetic drug belonging to the family of acridine-based synthetic compounds and the 9-aminoacridine subfamily
The chemical structure of QC is composed of three heterocyclics with acridine, which was designed and produced by the pharmaceutical organization Bayer in 1928 during the post-World War I period and was actively used for four years during World War II to treat soldiers infected with malaria [1]
A few studies have presented evidence suggesting that quinacrine inhibits ribosome biogenesis (RBG) by suppressing the activity of the RPA194 catalytic subunit of RNA polymerase-I and nucleolar RBG nucleostemin (NS/GNL3), inducing nucleolar stress, which leads to a reduction in RAD51 recruitment to the DNA damage site and eventually causes disruption of the homologous recombination repair mechanism [49,51]
Summary
Quinacrine (IUPAC name: 4-N-(6-chloro-2-methoxyacridin-9-yl)-1-N,1-N-diethylpentane1,4-diamine) is a synthetic drug belonging to the family of acridine-based synthetic compounds and the 9-aminoacridine subfamily. Low concentrations of QC have been shown to induce redistribution of Ca2+ ions, leading to disruption of IP3 dependent Ca2+ oscillation, hampering the growth of Plasmodium falciparum, as they exhibit stage-specific Ca2+ oscillations in the ring form during the trophozoite stage, which is a key requirement for the maturation of the parasite inside erythrocytes. Owing to its fluorescent and DNA-binding properties, QC is routinely used in laboratories to stain chromosomes and study their patterns. This technique is explicitly called “Q-banding” [9,10,11]. QC was extensively utilized as a sterilizing agent in the 1980s [12,13]
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