Disease relevance of Aminoacridine

• Membrane preparations isolated from the photosynthetic lamellae of the cyanobacterium Plectonema boryanum generate upon illumination a transmembrane pH gradient of approximately 2 to 3 pH units (acid inside), as determined from the distribution of either fluorescent or radioactive amines (9 aminoacridine and [14C]methylamine, respectively) [1].
• Both the electronic and steric properties of the side chain are shown to be important in determining the hypoxia selectivity of the compounds, by controlling the degree of aminoacridine/iminoacridan tautomerism [2].
• The main disadvantages of the cholinesterase inhibitors used in clinical trials are the short duration of action in the case of physostigmine and the potential for liver toxicity seen with the aminoacridine derivatives [3].
• Could an aminoacridine interfere with the cellular mechanisms involved in the process of human immunodeficiency virus infection [4]?
• The response to nitracrine, 1-nitro-9-[3'(N,N-dimethyl)aminopropyl] aminoacridine, an anticancer agent, was examined in two strains of murine lymphoma L5178Y inversely cross-sensitive to X-rays and UV light [5].

High impact information on Aminoacridine

• For 13 aminoquinoline and aminoacridine compounds, relative drug resistance was negatively correlated with lipid solubility at physiological pH (r2 = 0.90, p < 0.0001) [6].
• Loss of the transmembrane pH gradient in the anterior portion of the sperm head, monitored by the fluorescent pH probe 9-N-dodecyl aminoacridine, follows the B to S transition in sperm incubated with ZP from unfertilized eggs, but no loss is observed when the B to S transition is induced using ZP from TPA-treated eggs [7].
• When the pH is increased to 7-8 to form the free bases of the nitroacridine chromophores, the 2- and 3-nitro isomers retain the aminoacridine configuration, but the 1- and 4-nitro isomers convert to the iminoacridan configuration [8].
• Evidence for plasma membrane impermeability to small ions in acrosome-intact mouse spermatozoa bound to mouse zonae pellucidae, using an aminoacridine fluorescent pH probe: time course of the zona-induced acrosome reaction monitored by both chlortetracycline and pH probe fluorescence [9].
• CI-921, an aminoacridine derivative, diminished lipid peroxidation by 65% at 15 microM [10].

Biological context of Aminoacridine

• Results from these studies indicate that oxidative stress and GSH depletion may enhance Alzheimer patients' susceptibility to the hepatotoxic potential of aminoacridine drugs [11].

Anatomical context of Aminoacridine

• A novel method for quantitating secretion is described based on measurements of the cellular uptake of the fluorescent aminoacridine dye quinacrine into low-pH secretory granules [12].
• A pharmacological decrease of the potassium permeability in islet cells (by tetraethylammonium or 9 aminoacridine) potentiates (and to some extent even mimicks) the insulin-releasing property of glucose [13].
• Lysosomes of peritoneal macrophages, selectively pinpointed by aminoacridine-induced fluorescence, do not fuse with vacuoles containing viable Toxoplasma gondii RH strain [14].

Associations of Aminoacridine with other chemical compounds

• The probes used were a membrane-bound fluorescent aminoacridine, which monitors surface charge-density changes, the native carotenoids and added oxonol VI for monitoring electrical potential in the membrane and the pH indicators neutral red and cresol red [15].

Gene context of Aminoacridine

• Inhibition of the U1A-RNA complex by an aminoacridine derivative [16].
• The addition of the aminoacridine derivative to stem loop 2 RNA increases the susceptibility of other portions of the loop to digestion by RNase A, which implies that binding of the ligand changes the conformation or dynamics of the stem loop target site [16].

Analytical, diagnostic and therapeutic context of Aminoacridine

• Single cell uptake and metabolism of DACA and the related but more basic aminoacridine 9-[3-(dimethylamino)propylamino]acridine (DAPA), and penetration through V79 and EMT6 MCL, were investigated by high-performance liquid chromatography [17].

References