Disease relevance of Digitoxigenin

• Kinetics of digitoxin and the bis- and monodigitoxosides of digitoxigenin in renal insufficiency [1].
• Altered distribution and toxicity of digitoxigenin in fasted mice [2].
• Digitoxin and digitoxigenin produced their maximum inotropic responses, without induction of arrhythmias, at about 30 min [3].

Psychiatry related information on Digitoxigenin

• The relationship between magnitude of electroshock stimulation and the effects of digitoxigenin, pentylenetetrazol and brain monoamine reduction on electroshock convulsive thresholds [4].

High impact information on Digitoxigenin

• Human liver alcohol dehydrogenase (alcohol: NAD" oxidoreductase, EC 1.1.1.1) catalyzes the oxidation of the 3 beta-OH group of digitoxigenin, digoxigenin, and gitoxigenin to their 3-keto derivatives, which have been characterized by high performance liquid chromatography and mass spectrometry [5].
• We now report that digitoxigenin monodigitoxoside UDP-glucuronosyltransferase (DIG UDP-glucuronosyltransferase), a liver microsomal enzyme activity induced by PCN in rats, is also inducible, as is P-450p, in primary monolayer cultures of adult rat hepatocytes [6].
• Induction of digitoxigenin monodigitoxoside UDP-glucuronosyltransferase activity by glucocorticoids and other inducers of cytochrome P-450p in primary monolayer cultures of adult rat hepatocytes and in human liver [6].
• The target size for the ATPase activity was reduced to approximately 320,000 daltons if the cells were pretreated with digitoxigenin [7].
• Kinetics of digitoxin and the bis- and monodigitoxosides of digitoxigenin in normal subjects [8].

Biological context of Digitoxigenin

• The syntheses of the title compounds were accomplished by Koenig-Knorr condensation of acylated furanoses with digitoxigenin followed by basic hydrolysis of protecting groups [9].
• A single component with low affinity to digitoxigenin (IC50 = 110 +/- 10 nM) characterized the alpha 1 kidney form [10].
• A Stereoselective Synthesis of Digitoxin and Digitoxigen Mono- and Bisdigitoxoside from Digitoxigenin via a Palladium-Catalyzed Glycosylation [11].
• The addition of an aminosugar group to digitoxigenin or an amine group to galactose-digitoxigenin results in an agent with greater ability to reduce heart rate and to increase cardiac contractility and cardiac index without affecting the tension-time index [12].
• On the substrate specificity of the digitoxigenin monodigitoxoside conjugating UDP-glucuronyltransferase in rat liver [13].

Anatomical context of Digitoxigenin

• Expression of the alpha 3-subunit isoform in dog heart membranes was consistent with a high affinity digitoxigenin-sensitive class of Na,K-ATPase (IC50 = 7 +/- 2 nM) [10].
• By in vitro assays with detergent activated liver microsomes it was found that (1) digitoxigenin monodigitoxoside is by far the best substrate of all cardenolides and cardenolide digitoxosides tested [13].
• Digitoxigenin, in addition to its direct contractile force effect on the myocardium, modulates contractile force through adrenergic mechanisms [14].
• The deaminated metabolite of ASI-222 appeared both in the urine and the feces together with the genin, digitoxigenin and the parent drug which constituted the majority of the radioactivity excreted [15].
• Treatment of K562 cells with other cardiotonic steroids, such as cinobufagin, ouabain and digitoxigenin, at the concentration of 10 nM for four days resulted in weak or no effect on the cells [16].

Associations of Digitoxigenin with other chemical compounds

• The most active compounds showed Na(+),K(+)-ATPase inhibitory potencies (IC(50)) 17-25 times higher than the standards digitoxigenin and digoxin and 3-11 times higher inotropic potencies (EC(50)) in isolated guinea pig left atria [17].
• Other cardiotonic steroids including ouabain, digitoxigenin and cinobufagin did not enhance VDR activation [18].
• Additionally, structure-activity relationships among four cardiotonic steroids were determined by comparing the contractile force effects of bolus i.v. injections of digitoxigenin (the genin), digitoxigenin-galactose (genin-neutral sugar combination), digitoxigenin-aminogalactose (ASI-222, genin-aminosugar combination) and digoxin [14].
• A weak reactivity component was similar to the one of the corresponding glycosides (IC50 of about 10(-6) M) and a high reactivity component exhibited IC50 values varying from 0.1 to 0.5 X 10(-6) M for digitoxigenin and ouabagenin respectively [19].
• Intravenous administration of digitoxigenin (DTXGN) evokes seizure episodes in mice which may be dependent on brain biogenic amines such as serotonin (5-HT) [2].

Gene context of Digitoxigenin

• It was proven that digitoxigenin (dt-0) is by far the best substrate for the cytosolic sulfotransferases (ST) [20].

Analytical, diagnostic and therapeutic context of Digitoxigenin

• EEG was recorded from several brain regions during the i.v. infusion of digitoxigenin to conscious, freely-moving rats [21].
• At a dosage of 20 mg/kg in the intact rat, it elicited ECG changes similar to those seen with a 10-mg/kg dose of digitoxigenin [22].

References