The indolequinone compound EO9 has good pharmacodynamic properties in terms of bioreductive activation and selectivity for either NAD(P)H:quinone oxidoreductase-1 (NQO1)-rich aerobic or NQO1-deficient hypoxic cells. However, its pharmacokinetic properties are poor and this fact is believed to be...
The solubility of sodium 1-naphthalenesulfonate and sodium 2-naphthalenesulfonate in pure organic solvents of acetone, 1,4-dioxane, cyclohexanone, ethanol, ethyl acetate and isopropanol were measured by using the isothermal saturation method at temperature ranging from (278.15 to 323.15) K under...
In this work, solid–liquid equilibria (SLE) data for ternary sodium 1-naphthalenesulfonate+sodium 2-naphthalenesulfonate+water system was measured at (283.15, 303.15 and 323.15)K respectively. The diagrams for solid liquid phase of the ternary system were well-established by the measured solubi...
Seeds of Crotalaria scassellatii (Fabaceae) store pyrrolizidine alkaloids as tertiary amines. During the beginning of seed germination the tertiary alkaloids are rapidly converted into the respective alkaloid N-oxides which are the ultimate forms of alkaloid transport, metabolism and storage in ...
Tussilago farfara (Kuan Donghua) is an important Chinese herbal medicine which has been shown to contain many bioactive compounds and widely used to relieve cough and resolve phlegm. However, besides therapeutic bioactive compounds, this herb has been found to contain toxic pyrrolizidine alkaloi...
Tussilago farfara L. (family Asteraceae) is a valuable medicinal plant that has been used as a cough suppressant and as an antibacterial and anti-inflammatory drug. Mucopolysac charides, flavonoids, sterols, phenolic acids and pyrrolizidine alkaloids (PAs) are the main active compounds of coltsf...
Pyrrolizidine alkaloids (PAs) are considered to be one of the most hepatotoxic groups of compounds of plant origin and are present in about 3% of the world’s flowering plants. Most PAs represent a considerable health hazard to both livestock and humans through the consumption of plants and PA-c...
A rapid, selective and sensitive ultra-performance liquid chromatography–electrospray ionization mass spectrometry (UPLC–ESIMS) method was firstly developed and validated for the simultaneous determination of two hepatotoxic pyrrolizidine alkaloids (HPAs), senecionine (SEN), adonifoline (ADO),...
. Laboratory and field tracer experiments with 14C-labelled senecionine Noxide (SO) and distant biosynthetic precursors such as [14C]putrescine revealed that pyrrolizidine alkaloid N-oxides (PAs) in Senecio vernalis Waldstr. Kit. (Asteraceae) show no significant turnover over periods of up to 29...
The roles of cytochrome CYP3A and CYP2B isozymes in the bioactivation and detoxification of the pyrrolizidine alkaloid (PA) senecionine (SN) have been investigatedin vitrowith sheep and hamster hepatic microsomes. Our results show that the rate of SN activation measured by (±)-6,7-dihydro-7-hyd...
The distribution and acid-base behaviour of the four solutes harmine, chromotropic acid (4,5-dihydroxynaphthalene-2,7-disulfonate, disodium salt), 2-naphthol and 5,10,15,20-tetrakis [4-trimethylammonium)phenyl]-21H,23H-porphine tetra-p-tosylate (TTMP) have been studied in water-in-oil (w/o) micr...
A new inorgano-organic ion exchanger has been prepared by anchoring chromotropic acid (4,5-dihydroxynapthalene-3,7-disulphonic acid, disodium salt) onto zirconium molybdate (ZM). The inorgano-organic ion exchanger has been termed ZMCA. ZM and ZMCA have been characterised for elemental, spectral ...
A simple and efficient synthesis of the opioid analgesic agent (R)-phenampromide with high enantiopurity (>99% ee) via the formation of an aziridinium ion as a key step using commercially available starting material is described.
The Auger electron emitter 123I was examined in the form of 4-[123I]iodoantipyrine and as [123I]NaI for its effectiveness in killing cells of different sensitivity to photon irradiation. Micronucleus assays showed that 4-[123I]iodoantipyrine is 23 times more effective in cell inactivation than [...
Radioiodinated 4-[*I]iodoantipyrine labeled with radioiodine (i.e., 123I or 125I or 131I) has been used for modeling radiation damage on cell nuclei of tumor cells where the characteristic high linear energy transfer (high-LET) of the Auger electron could be demonstrated. Also, the compound is c...
A dilemma in behavioral brain mapping is that conventional techniques immobilize the subject, extinguishing all but the simplest behaviors. This is avoided if brain activation is imaged after completion of the behavior and tissue capture of the tracer. A single-pass flow tracer proposed for posi...
We evaluated acute alterations of local cerebral perfusion following 30 min of transient right proximal middle cerebral artery (MCA) clip-occlusion in the rat and following two intervals of postischemic reperfusion. Local cerebral blood flow (lCBF) was assessed by [ 1 4 C]iodoantipy...
Protein kinase C (PKC) activity was measured in rat brain with 2 h of middle cerebral artery (MCA) and common carotid artery (CCA) occlusion, using dual autoradiography of [ 1 4 C]iodoantipyrine (IAP) and [ 3 H]phorbol-12,13-dibutyrate (PDBu). In the ischemic brain, it requir...
Background Central pain syndrome is characterized by a combination of abnormal pain sensations, and pain medications often provide little or no relief. Accumulating animal and clinical studies have shown that impairments of the spinothalamic tract (STT) and thalamocingulate pathway ca...
Deux phases polymorphes, α et β, pour le complexe à transfert de charge (TTF) 3 (TNF) 2 , où TTF=tétrathiofulvalène et TNF=2,4,7-trinitro-9-fluorénone, ont été caractérisées par diffraction des rayons X et spectroscopie infrarouge. Un changement structural de la TNF co...
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