Antimicrobial activity of 9-oxo and 9-thio acridines: Correlation with intercalation into DNA and effects on macromolecular biosynthesis

Efflux pumps of Gram-negative bacteria: what they do, how they do it, with what and how to deal with them

“…Because a heavy inoculum is introduced directly into the neutrophil-rich peritoneum, it is opined that the protection from infection results from the highly concentrated level of TZ within the lysosomes of the neutrophil (Daniel and Wójcikowski, 1999a,b) that eventually would fuse with the phagosome that contains the phagocytosed organism. The high concentration of TZ within the phagolysosome may exceed the in vitro MIC of TZ and because TZ can readily penetrate the cell envelope of the bacterium (Motohashi et al, 2003), it can easily reach sensitive TZ targets such as DNA where it readily intercalates between nucleic bases of DNA (Crémieux et al, 1995). The fact that TZ also enhances killing of intracellular bacteria (Crémieux et al, 1995; Ordway et al, 2003; Martins et al, 2004, 2009c; Amaral et al, 2007), suggests that the protection by TZ from a virulent infection takes place via many mechanisms of action.…”

“…The high concentration of TZ within the phagolysosome may exceed the in vitro MIC of TZ and because TZ can readily penetrate the cell envelope of the bacterium (Motohashi et al, 2003), it can easily reach sensitive TZ targets such as DNA where it readily intercalates between nucleic bases of DNA (Crémieux et al, 1995). The fact that TZ also enhances killing of intracellular bacteria (Crémieux et al, 1995; Ordway et al, 2003; Martins et al, 2004, 2009c; Amaral et al, 2007), suggests that the protection by TZ from a virulent infection takes place via many mechanisms of action.…”

Cytotoxic activity of acridin-3,6-diyl dithiourea hydrochlorides in human leukemia line HL-60 and resistant subline HL-60/ADR

“…Acridines have been used as antimicrobial [7,8], antiparasitic [9] and anticancer agents for many years and binding to DNA considered to be a principal mode of their bioactivity [10]. The best known acridine drug amsacrine [N-(4-(acridin-9-ylamino)-3-methoxyphenyl) methanesulfonamide] is routinely employed for systemic treatment of human cancers [11].…”

Assessment of Anti-Quorum Sensing Activity for Some Ornamental and Medicinal Plants Native to Egypt

“…Antimicrobial agents exhibit their activity through different mechanisms such as disrupting cell wall function or disrupting protein and DNA synthesis [1–3]. As a result, multidrug resistance spreads rapidly, and development of new antimicrobial or antipathogenic agents that act upon new microbial targets becomes a very pressing priority [4].…”